{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,20]],"date-time":"2026-10-20T18:41:07Z","timestamp":1792521667589,"version":"4.5.0"},"reference-count":186,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2021,4,1]],"date-time":"2021-04-01T00:00:00Z","timestamp":1617235200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2021,4,1]],"date-time":"2021-04-01T00:00:00Z","timestamp":1617235200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2021,4,1]],"date-time":"2021-04-01T00:00:00Z","timestamp":1617235200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-017"},{"start":{"date-parts":[[2021,4,1]],"date-time":"2021-04-01T00:00:00Z","timestamp":1617235200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-037"},{"start":{"date-parts":[[2021,4,1]],"date-time":"2021-04-01T00:00:00Z","timestamp":1617235200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-012"},{"start":{"date-parts":[[2021,4,1]],"date-time":"2021-04-01T00:00:00Z","timestamp":1617235200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-029"},{"start":{"date-parts":[[2021,4,1]],"date-time":"2021-04-01T00:00:00Z","timestamp":1617235200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-004"}],"funder":[{"DOI":"10.13039\/501100018551","name":"Science and Technology Innovation Talents in Universities of Henan Province","doi-asserted-by":"publisher","award":["21HASTIT045"],"award-info":[{"award-number":["21HASTIT045"]}],"id":[{"id":"10.13039\/501100018551","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100000138","name":"U.S. Department of Education","doi-asserted-by":"publisher","award":["19IRTSTHN001"],"award-info":[{"award-number":["19IRTSTHN001"]}],"id":[{"id":"10.13039\/100000138","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["81973177"],"award-info":[{"award-number":["81973177"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["81703326"],"award-info":[{"award-number":["81703326"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["European Journal of Medicinal Chemistry"],"published-print":{"date-parts":[[2021,4]]},"DOI":"10.1016\/j.ejmech.2021.113284","type":"journal-article","created":{"date-parts":[[2021,2,15]],"date-time":"2021-02-15T03:45:47Z","timestamp":1613360747000},"page":"113284","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":60,"special_numbering":"C","title":["New drug approvals for 2020: Synthesis and clinical applications"],"prefix":"10.1016","volume":"215","author":[{"given":"Shuo","family":"Yuan","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yong-Qiang","family":"Luo","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jia-Hui","family":"Zuo","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hui","family":"Liu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Fang","family":"Li","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7207-643X","authenticated-orcid":false,"given":"Bin","family":"Yu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"key":"10.1016\/j.ejmech.2021.113284_bib1","doi-asserted-by":"crossref","first-page":"299","DOI":"10.1038\/d41573-020-00074-4","article-title":"FDA new drug approvals in Q1 2020","volume":"19","author":"Urquhart","year":"2020","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2021.113284_bib2","doi-asserted-by":"crossref","first-page":"503","DOI":"10.1038\/d41573-020-00129-6","article-title":"FDA new drug approvals in Q2 2020","volume":"19","author":"Urquhart","year":"2020","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2021.113284_bib3","doi-asserted-by":"crossref","first-page":"746","DOI":"10.1038\/d41573-020-00182-1","article-title":"FDA new drug approvals in Q3 2020","volume":"19","author":"Urquhart","year":"2020","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2021.113284_bib4","article-title":"FDA drug approvals","author":"Mullard","year":"2021","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2021.113284_bib5","doi-asserted-by":"crossref","first-page":"85","DOI":"10.1038\/d41573-019-00014-x","article-title":"FDA drug approvals","volume":"18","author":"Mullard","year":"2019","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2021.113284_bib6","doi-asserted-by":"crossref","first-page":"79","DOI":"10.1038\/d41573-020-00001-7","article-title":"FDA drug approvals","volume":"19","author":"Mullard","year":"2020","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2021.113284_bib7","doi-asserted-by":"crossref","first-page":"509","DOI":"10.1007\/s40265-020-01287-y","article-title":"Teprotumumab: first approval","volume":"80","author":"Markham","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib8","doi-asserted-by":"crossref","first-page":"1355","DOI":"10.1007\/s40265-020-01378-w","article-title":"Remdesivir: first approval","volume":"80","author":"Lamb","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib9","doi-asserted-by":"crossref","first-page":"331","DOI":"10.1080\/17512433.2020.1750366","article-title":"A\u00a0pharmacological profile of intravenous amisulpride for the treatment of postoperative nausea and vomiting","volume":"13","author":"Fox","year":"2020","journal-title":"Expet Rev. Clin. Pharmacol."},{"key":"10.1016\/j.ejmech.2021.113284_bib10","doi-asserted-by":"crossref","first-page":"733","DOI":"10.1007\/s40265-020-01300-4","article-title":"Eptinezumab: first approval","volume":"80","author":"Dhillon","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib11","article-title":"Oral once-daily berotralstat for the prevention of hereditary angioedema attacks: a randomized, double-blind, placebo-controlled phase 3 trial","author":"Zuraw","year":"2020","journal-title":"J.\u00a0Allergy Clin. Immunol."},{"key":"10.1016\/j.ejmech.2021.113284_bib12","doi-asserted-by":"crossref","first-page":"495","DOI":"10.1007\/s40265-020-01277-0","article-title":"Osilodrostat: first approval","volume":"80","author":"Duggan","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib13","doi-asserted-by":"crossref","first-page":"1595","DOI":"10.1007\/s40265-020-01399-5","article-title":"Triheptanoin: first approval","volume":"80","author":"Shirley","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib14","doi-asserted-by":"crossref","first-page":"1027","DOI":"10.1007\/s40265-020-01339-3","article-title":"Viltolarsen: first approval","volume":"80","author":"Dhillon","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib15","doi-asserted-by":"crossref","first-page":"1019","DOI":"10.1007\/s40265-020-01337-5","article-title":"Sacituzumab govitecan: first approval","volume":"80","author":"Syed","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib16","doi-asserted-by":"crossref","first-page":"1607","DOI":"10.1007\/s40265-020-01404-x","article-title":"Belantamab mafodotin: first approval","volume":"80","author":"Markham","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib17","doi-asserted-by":"crossref","first-page":"3551","DOI":"10.1021\/acs.jmedchem.7b01890","article-title":"The pharmacophore network: a computational method for exploring structure-activity relationships from a large chemical data set","volume":"61","author":"M\u00e9tivier","year":"2018","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib18","doi-asserted-by":"crossref","first-page":"10375","DOI":"10.1021\/acs.jmedchem.8b00407","article-title":"Lead-like drugs: a perspective","volume":"61","author":"Raymer","year":"2018","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib19","doi-asserted-by":"crossref","first-page":"660","DOI":"10.1038\/nrd1467","article-title":"Fragment-based lead discovery","volume":"3","author":"Rees","year":"2004","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2021.113284_bib20","doi-asserted-by":"crossref","first-page":"9375","DOI":"10.1021\/acs.jmedchem.9b00359","article-title":"Overview of recent strategic advances in medicinal chemistry","volume":"62","author":"Wu","year":"2019","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib21","doi-asserted-by":"crossref","first-page":"3463","DOI":"10.1021\/jm040031v","article-title":"Fragment-based drug discovery","volume":"47","author":"Erlanson","year":"2004","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib22","doi-asserted-by":"crossref","first-page":"112667","DOI":"10.1016\/j.ejmech.2020.112667","article-title":"New drug approvals for 2019: synthesis and clinical applications","volume":"205","author":"Yuan","year":"2020","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib23","doi-asserted-by":"crossref","first-page":"616","DOI":"10.1111\/pde.13612","article-title":"Clinical studies evaluating abametapir lotion, 0.74%, for the treatment of head louse infestation","volume":"35","author":"Bowles","year":"2018","journal-title":"Pediatr. Dermatol."},{"key":"10.1016\/j.ejmech.2021.113284_bib24","doi-asserted-by":"crossref","first-page":"167","DOI":"10.1093\/jme\/tjw132","article-title":"Ovicidal efficacy of abametapir against eggs of human head and body lice (anoplura: pediculidae)","volume":"54","author":"Bowles","year":"2017","journal-title":"J.\u00a0Med. Entomol."},{"key":"10.1016\/j.ejmech.2021.113284_bib25","first-page":"1","article-title":"Effect of a new head lice treatment, abametapir lotion, 0.74%, on louse eggs: a randomized, double-blind study","volume":"6","author":"Bowles","year":"2019","journal-title":"Glob. Pediatr. Health"},{"key":"10.1016\/j.ejmech.2021.113284_bib26","doi-asserted-by":"crossref","first-page":"777","DOI":"10.1021\/jo402084m","article-title":"Reductive couplings of 2-halopyridines without external ligand: phosphine-free nickel-catalyzed synthesis of symmetrical and unsymmetrical 2, 2\u2019-bipyridines","volume":"79","author":"Liao","year":"2014","journal-title":"J.\u00a0Org. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib27","doi-asserted-by":"crossref","first-page":"2749","DOI":"10.1007\/s00436-020-06786-1","article-title":"Enhancing the antimalarial activity of artesunate","volume":"119","author":"Adebayo","year":"2020","journal-title":"Parasitol. Res."},{"key":"10.1016\/j.ejmech.2021.113284_bib28","doi-asserted-by":"crossref","first-page":"238","DOI":"10.1016\/j.medmal.2018.01.004","article-title":"Use of artesunate in non-malarial indications","volume":"48","author":"Raffetin","year":"2018","journal-title":"Med. Maladies Infect."},{"key":"10.1016\/j.ejmech.2021.113284_bib29","doi-asserted-by":"crossref","first-page":"261","DOI":"10.1016\/j.ebiom.2019.06.026","article-title":"Pre-clinical study of iron oxide nanoparticles fortified artesunate for efficient targeting of malarial parasite","volume":"45","author":"Kannan","year":"2019","journal-title":"EBioMedicine"},{"key":"10.1016\/j.ejmech.2021.113284_bib30","doi-asserted-by":"crossref","first-page":"18134","DOI":"10.1038\/s41598-019-54639-4","article-title":"Determinants of post-malarial anemia in African children treated with parenteral artesunate","volume":"9","author":"Scheu","year":"2019","journal-title":"Sci. Rep."},{"key":"10.1016\/j.ejmech.2021.113284_bib31","series-title":"Simple Process for Preparing Artesunate by One-Pot Method by Taking Artemisinin as Raw Material","author":"Dong","year":"2011"},{"key":"10.1016\/j.ejmech.2021.113284_bib32","doi-asserted-by":"crossref","first-page":"1485","DOI":"10.1007\/s40265-020-01386-w","article-title":"Fostemsavir: first approval","volume":"80","author":"Markham","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib33","doi-asserted-by":"crossref","first-page":"62","DOI":"10.1021\/acs.jmedchem.7b01337","article-title":"Inhibitors of HIV-1 attachment: the discovery and development of temsavir and its prodrug fostemsavir","volume":"61","author":"Meanwell","year":"2018","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib34","doi-asserted-by":"crossref","first-page":"6308","DOI":"10.1021\/acs.jmedchem.8b00759","article-title":"Discovery of the human immunodeficiency virus type 1 (HIV-1) attachment inhibitor temsavir and its phosphonooxymethyl prodrug fostemsavir","volume":"61","author":"Wang","year":"2018","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib35","doi-asserted-by":"crossref","first-page":"1232","DOI":"10.1056\/NEJMoa1902493","article-title":"Fostemsavir in adults with multidrug resistant HIV-1 infection","volume":"382","author":"Kozal","year":"2020","journal-title":"N.\u00a0Engl. J. Med."},{"key":"10.1016\/j.ejmech.2021.113284_bib36","first-page":"433","article-title":"First-in-class HIV drug is approved","volume":"324","author":"Voelker","year":"2020","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2021.113284_bib37","doi-asserted-by":"crossref","first-page":"740","DOI":"10.1016\/S2352-3018(20)30240-X","article-title":"Safety and efficacy of the HIV-1 attachment inhibitor prodrug fostemsavir in heavily treatment-experienced individuals: week 96 results of the phase 3 BRIGHTE study","volume":"7","author":"Lataillade","year":"2020","journal-title":"Lancet HIV"},{"key":"10.1016\/j.ejmech.2021.113284_bib38","series-title":"Prodrugs of Piperazine and Substituted Piperidine Antiviral Agents","author":"Ueda","year":"2005"},{"key":"10.1016\/j.ejmech.2021.113284_bib39","doi-asserted-by":"crossref","first-page":"1341","DOI":"10.1016\/j.cmi.2018.06.006","article-title":"Toxicity of nifurtimox as second-line treatment after benznidazole intolerance in patients with chronic Chagas disease: when available options fail","volume":"24","author":"Crespillo-Andujar","year":"2018","journal-title":"Clin. Microbiol. Infect."},{"key":"10.1016\/j.ejmech.2021.113284_bib40","first-page":"1056","article-title":"Safety profile of nifurtimox for treatment of Chagas disease in the United States, Clin","volume":"63","author":"Forsyth","year":"2016","journal-title":"Inf. Disp."},{"key":"10.1016\/j.ejmech.2021.113284_bib41","doi-asserted-by":"crossref","first-page":"5022","DOI":"10.1073\/pnas.0711014105","article-title":"A\u00a0mechanism for cross-resistance to nifurtimox and benznidazole in trypanosomes","volume":"105","author":"Wilkinson","year":"2008","journal-title":"Proc. Natl. Acad. Sci. U. S. A."},{"key":"10.1016\/j.ejmech.2021.113284_bib42","doi-asserted-by":"crossref","first-page":"69","DOI":"10.1086\/656917","article-title":"Tolerance and safety of nifurtimox in patients with chronic chagas disease","volume":"51","author":"Jackson","year":"2010","journal-title":"Clin. Infect. Dis."},{"key":"10.1016\/j.ejmech.2021.113284_bib43","series-title":"N-amino Tetrahydrothiazine Derivatives, Method of Manufacture and Use","author":"Brard","year":"2008"},{"key":"10.1016\/j.ejmech.2021.113284_bib44","doi-asserted-by":"crossref","first-page":"1813","DOI":"10.1056\/NEJMoa2007764","article-title":"Remdesivir for the treatment of COVID-19 - preliminary report","volume":"383","author":"Beigel","year":"2020","journal-title":"N.\u00a0Engl. J. Med."},{"key":"10.1016\/j.ejmech.2021.113284_bib45","first-page":"5752","article-title":"Remdesivir for adults with COVID-19 : a living systematic review for an American college of physicians practice points","volume":"20","author":"Wilt","year":"2020","journal-title":"Ann. Intern. Med."},{"key":"10.1016\/j.ejmech.2021.113284_bib46","doi-asserted-by":"crossref","first-page":"1610","DOI":"10.1136\/bmj.m1610","article-title":"Remdesivir in COVID-19","volume":"369","author":"Ferner","year":"2020","journal-title":"BMJ"},{"key":"10.1016\/j.ejmech.2021.113284_bib47","series-title":"Methods for Treating Filoviridae Virus Infections","author":"Chun","year":"2016"},{"key":"10.1016\/j.ejmech.2021.113284_bib48","series-title":"Methods for Treating Flaviviridae Virus Infections","author":"Clarke","year":"2017"},{"key":"10.1016\/j.ejmech.2021.113284_bib49","doi-asserted-by":"crossref","first-page":"517","DOI":"10.1080\/14656566.2020.1714029","article-title":"An overview of intravenous amisulpride as a new therapeutic option for the prophylaxis and treatment of postoperative nausea and vomiting","volume":"21","author":"Smyla","year":"2020","journal-title":"Expet Opin. Pharmacother."},{"key":"10.1016\/j.ejmech.2021.113284_bib50","doi-asserted-by":"crossref","first-page":"1099","DOI":"10.1097\/ALN.0000000000002133","article-title":"Amisulpride prevents postoperative nausea and vomiting in patients at high risk: a randomized, double-blind, placebo-controlled trial","volume":"128","author":"Kranke","year":"2018","journal-title":"Anesthesiology"},{"key":"10.1016\/j.ejmech.2021.113284_bib51","series-title":"Process for Preparation of Amisulpride","author":"Paghdar","year":"2011"},{"key":"10.1016\/j.ejmech.2021.113284_bib52","doi-asserted-by":"crossref","first-page":"1739","DOI":"10.1007\/s40265-020-01414-9","article-title":"Oliceridine: first approval","volume":"80","author":"Markham","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib53","doi-asserted-by":"crossref","first-page":"1414","DOI":"10.1213\/ANE.0000000000003662","article-title":"Pharmacological characters of oliceridine, a \u03bc-opioid receptor G-protein-biased ligand in mice","volume":"129","author":"Liang","year":"2019","journal-title":"Anesth. Analg."},{"key":"10.1016\/j.ejmech.2021.113284_bib54","doi-asserted-by":"crossref","first-page":"6456","DOI":"10.1021\/acs.biochem.6b00948","article-title":"How oliceridine (TRV-130) binds and stabilizes a \u03bc-opioid receptor conformational state that selectively triggers G protein signaling pathways","volume":"55","author":"Schneider","year":"2016","journal-title":"Biochemistry"},{"key":"10.1016\/j.ejmech.2021.113284_bib55","doi-asserted-by":"crossref","first-page":"8019","DOI":"10.1021\/jm4010829","article-title":"Structure-activity relationships and discovery of a G protein biased mu opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain","volume":"56","author":"Chen","year":"2013","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib56","series-title":"Opioid Receptor Ligands and Methods of Using and Making Same","author":"Yamashita","year":"2012"},{"key":"10.1016\/j.ejmech.2021.113284_bib57","doi-asserted-by":"crossref","first-page":"1293","DOI":"10.1007\/s40265-016-0623-y","article-title":"Opicapone: a review in Parkinson\u2019s disease","volume":"76","author":"Scott","year":"2016","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib58","doi-asserted-by":"crossref","first-page":"1528","DOI":"10.1002\/mds.27475","article-title":"Opicapone for the treatment of Parkinson\u2019s disease: a review of a new licensed medicine","volume":"33","author":"Fabbri","year":"2018","journal-title":"Mov. Disord."},{"key":"10.1016\/j.ejmech.2021.113284_bib59","doi-asserted-by":"crossref","first-page":"197","DOI":"10.1001\/jamaneurol.2016.4703","article-title":"Opicapone as adjunct to levodopa therapy in patients with Parkinson disease and motor fluctuations: a randomized clinical trial","volume":"74","author":"Lees","year":"2017","journal-title":"JAMA Neurol"},{"key":"10.1016\/j.ejmech.2021.113284_bib60","doi-asserted-by":"crossref","first-page":"154","DOI":"10.1016\/S1474-4422(15)00336-1","article-title":"Opicapone as an adjunct to levodopa in patients with Parkinson\u2019s disease and end-of-dose motor fluctuations: a randomised, double-blind, controlled trial","volume":"15","author":"Ferreira","year":"2016","journal-title":"Lancet Neurol."},{"key":"10.1016\/j.ejmech.2021.113284_bib61","series-title":"Process for the Preparation of Opicapone and Intermediates Thereof","author":"Sathe","year":"2019"},{"key":"10.1016\/j.ejmech.2021.113284_bib62","doi-asserted-by":"crossref","first-page":"841","DOI":"10.1007\/s40265-020-01319-7","article-title":"Ozanimod: first approval","volume":"80","author":"Lamb","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib63","doi-asserted-by":"crossref","first-page":"839","DOI":"10.1212\/NXI.0000000000000839","article-title":"Effect of the sphingosine-1-phosphate receptor modulator ozanimod on leukocyte subtypes in relapsing MS","volume":"7","author":"Harris","year":"2020","journal-title":"Neurol. Neuroimmunol."},{"key":"10.1016\/j.ejmech.2021.113284_bib64","doi-asserted-by":"crossref","first-page":"1021","DOI":"10.1016\/S1474-4422(19)30238-8","article-title":"Safety and efficacy of ozanimod versus interferon beta-1a in relapsing multiple sclerosis (RADIANCE): a multicentre, randomised, 24-month, phase 3 trial","volume":"18","author":"Cohen","year":"2019","journal-title":"Lancet Neurol."},{"key":"10.1016\/j.ejmech.2021.113284_bib65","series-title":"Selective Sphingosine 1 Phosphate Receptor Modulators and Combination Therapy Therewith","author":"Martinborough","year":"2015"},{"key":"10.1016\/j.ejmech.2021.113284_bib66","series-title":"Selective Sphingosine 1 Phosphate Receptor Modulators and Methods of Chiral Synthesis","author":"Martinborough","year":"2011"},{"key":"10.1016\/j.ejmech.2021.113284_bib67","doi-asserted-by":"crossref","first-page":"506","DOI":"10.1097\/ACO.0000000000000877","article-title":"Remimazolam for anaesthesia or sedation","volume":"33","author":"Sneyd","year":"2020","journal-title":"Curr. Opin. Anaesthesiol."},{"key":"10.1016\/j.ejmech.2021.113284_bib68","doi-asserted-by":"crossref","first-page":"625","DOI":"10.1007\/s40265-020-01299-8","article-title":"Remimazolam: first approval","volume":"80","author":"Keam","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib69","doi-asserted-by":"crossref","first-page":"1021","DOI":"10.1002\/phar.1806","article-title":"Remimazolam: pharmacologic considerations and clinical role in anesthesiology","volume":"36","author":"Wesolowski","year":"2016","journal-title":"Pharmacotherapy"},{"key":"10.1016\/j.ejmech.2021.113284_bib70","doi-asserted-by":"crossref","first-page":"427","DOI":"10.1016\/j.gie.2018.04.2351","article-title":"A\u00a0phase III study evaluating the efficacy and safety of remimazolam (CNS-7056) compared with placebo and midazolam in patients undergoing colonoscopy","volume":"88","author":"Rex","year":"2018","journal-title":"Gastrointest. Endosc."},{"key":"10.1016\/j.ejmech.2021.113284_bib71","series-title":"Short-Acting Benzodiazepines","author":"Feldman","year":"2000"},{"key":"10.1016\/j.ejmech.2021.113284_bib72","doi-asserted-by":"crossref","first-page":"741","DOI":"10.1007\/s40265-020-01301-3","article-title":"Rimegepant: first approval","volume":"80","author":"Scott","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib73","doi-asserted-by":"crossref","first-page":"711","DOI":"10.1016\/S0140-6736(19)31611-3","article-title":"Rimegepant oral disintegrating tablet for migraine","volume":"394","author":"Edvinsson","year":"2019","journal-title":"Lancet"},{"key":"10.1016\/j.ejmech.2021.113284_bib74","doi-asserted-by":"crossref","first-page":"1240","DOI":"10.3389\/fphar.2020.01240","article-title":"Antagonism of CGRP signaling by rimegepant at two receptors","volume":"11","author":"Pan","year":"2020","journal-title":"Front. Pharmacol."},{"key":"10.1016\/j.ejmech.2021.113284_bib75","doi-asserted-by":"crossref","first-page":"1230","DOI":"10.1111\/head.12179","article-title":"Calcitonin gene-related peptide (CGRP) and migraine current understanding and state of development","volume":"53","author":"Bigal","year":"2013","journal-title":"Headache"},{"key":"10.1016\/j.ejmech.2021.113284_bib76","doi-asserted-by":"crossref","first-page":"10644","DOI":"10.1021\/jm3013147","volume":"55","author":"Luo","year":"2012","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib77","doi-asserted-by":"crossref","first-page":"1133","DOI":"10.1007\/s40265-020-01348-2","article-title":"Ripretinib: first approval","volume":"80","author":"Dhillon","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib78","doi-asserted-by":"crossref","first-page":"738","DOI":"10.1016\/j.ccell.2019.04.006","article-title":"Ripretinib (DCC-2618) is a switch control kinase inhibitor of a broad spectrum of oncogenic and drug-resistant KIT and PDGFR\u03b1 variants","volume":"35","author":"Smith","year":"2019","journal-title":"Cancer Cell"},{"key":"10.1016\/j.ejmech.2021.113284_bib79","doi-asserted-by":"crossref","first-page":"499","DOI":"10.1038\/s41568-019-0167-z","article-title":"Ripretinib turns off the switch in GIST","volume":"19","author":"Villanueva","year":"2019","journal-title":"Nat. Rev. Cancer"},{"key":"10.1016\/j.ejmech.2021.113284_bib80","first-page":"1","article-title":"Ripretinib in gastrointestinal stromal tumor: the long-awaited step forward, Ther","volume":"13","author":"Lostes-Bardaji","year":"2021","journal-title":"Adv. Med. Oncol."},{"key":"10.1016\/j.ejmech.2021.113284_bib81","first-page":"2364","article-title":"Fourth-line treatment approved for gastrointestinal tumor","volume":"323","author":"Voelker","year":"2020","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2021.113284_bib82","series-title":"Dihydronaphthyridines and Related Compounds Useful as Kinase Inhibitors for the Treatment of Proliferative Diseases","author":"Flynn","year":"2013"},{"key":"10.1016\/j.ejmech.2021.113284_bib83","doi-asserted-by":"crossref","first-page":"1853","DOI":"10.1007\/s40265-020-01410-z","article-title":"Risdiplam: first approval","volume":"80","author":"Dhillon","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib84","doi-asserted-by":"crossref","first-page":"6501","DOI":"10.1021\/acs.jmedchem.8b00741","article-title":"Discovery of risdiplam, a selective survival of motor neuron-2 (SMN2) gene splicing modifier for the treatment of spinal muscular atrophy (SMA)","volume":"61","author":"Ratni","year":"2018","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib85","first-page":"1026","article-title":"Oral drug approved for spinal muscular atrophy","volume":"324","author":"Jaklevic","year":"2020","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2021.113284_bib86","series-title":"Compounds for Treating Spinal Muscular Atrophy","author":"Ratni","year":"2015"},{"key":"10.1016\/j.ejmech.2021.113284_bib87","doi-asserted-by":"crossref","first-page":"1745","DOI":"10.1007\/s40265-020-01417-6","article-title":"Clascoterone: first approval","volume":"80","author":"Dhillon","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib88","doi-asserted-by":"crossref","first-page":"477","DOI":"10.1016\/j.jaad.2020.04.087","article-title":"Open-label, long-term extension study to evaluate the safety of clascoterone (CB-03-01) cream, 1% twice daily, in patients with acne vulgaris","volume":"83","author":"Eichenfield","year":"2020","journal-title":"J.\u00a0Am. Acad. Dermatol."},{"key":"10.1016\/j.ejmech.2021.113284_bib89","doi-asserted-by":"crossref","first-page":"913","DOI":"10.1111\/ced.14292","article-title":"Clascoterone as a novel treatment for androgenetic alopecia","volume":"45","author":"Sun","year":"2020","journal-title":"Clin. Exp. Dermatol."},{"key":"10.1016\/j.ejmech.2021.113284_bib90","doi-asserted-by":"crossref","first-page":"621","DOI":"10.1001\/jamadermatol.2020.0465","article-title":"Efficacy and safety of topical clascoterone cream, 1%, for treatment in patients with facial acne: two Phase 3 randomized clinical trials","volume":"156","author":"Hebert","year":"2020","journal-title":"JAMA Dermatol."},{"key":"10.1016\/j.ejmech.2021.113284_bib91","series-title":"Enzymatic Process for Obtaining 17 Alpha-Monoesters of Cortexolone And\/or its 9,11-dehydroderivatives","author":"Ajani","year":"2009"},{"key":"10.1016\/j.ejmech.2021.113284_bib92","doi-asserted-by":"crossref","first-page":"18099","DOI":"10.1074\/jbc.RA119.010732","article-title":"Reversible binding of the anticancer drug KXO1 (tirbanibulin) to the colchicine-binding site of beta-tubulin explains KXO1\u2019s low clinical toxicity","volume":"294","author":"Niu","year":"2019","journal-title":"J.\u00a0Biol. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib93","doi-asserted-by":"crossref","first-page":"49","DOI":"10.1080\/14728214.2020.1730810","article-title":"Actinic keratosis: where do we stand and where is the future going to take us?","volume":"25","author":"Cramer","year":"2020","journal-title":"Expet Opin. Emerg. Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib94","series-title":"Composition and Methods for Modulating a Kinase Cascade","author":"Hangauer","year":"2010"},{"key":"10.1016\/j.ejmech.2021.113284_bib95","doi-asserted-by":"crossref","first-page":"747","DOI":"10.1007\/s40265-020-01308-w","article-title":"Bempedoic acid: first approval","volume":"80","author":"Markham","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib96","doi-asserted-by":"crossref","first-page":"1022","DOI":"10.1056\/NEJMoa1803917","article-title":"Safety and efficacy of bempedoic acid to reduce LDL cholesterol","volume":"380","author":"Ray","year":"2019","journal-title":"N.\u00a0Engl. J. Med."},{"key":"10.1016\/j.ejmech.2021.113284_bib97","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1097\/MOL.0000000000000565","article-title":"Bempedoic acid: effects on lipoprotein metabolism and atherosclerosis","volume":"30","author":"Burke","year":"2019","journal-title":"Curr. Opin. Lipidol."},{"key":"10.1016\/j.ejmech.2021.113284_bib98","doi-asserted-by":"crossref","first-page":"1713","DOI":"10.1056\/NEJMoa1615664","article-title":"Evolocumab and clinical outcomes in patients with cardiovascular disease","volume":"376","author":"Sabatine","year":"2017","journal-title":"N.\u00a0Engl. J. Med."},{"key":"10.1016\/j.ejmech.2021.113284_bib99","series-title":"Hydroxyl Compounds and Compositions for Cholesterol Management and Related Uses","author":"Dasseux","year":"2004"},{"key":"10.1016\/j.ejmech.2021.113284_bib100","doi-asserted-by":"crossref","first-page":"3437","DOI":"10.1210\/jc.2019-00217","article-title":"Osilodrostat is a potential novel steroidogenesis inhibitor for the treatment of Cushing syndrome: an in\u00a0vitro study","volume":"104","author":"Creemers","year":"2019","journal-title":"J.\u00a0Clin. Endocrinol. Metab."},{"key":"10.1016\/j.ejmech.2021.113284_bib101","first-page":"1436","article-title":"New therapy offers direct cortisol control for Cushing disease","volume":"323","author":"Voelker","year":"2020","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2021.113284_bib102","doi-asserted-by":"crossref","first-page":"748","DOI":"10.1016\/S2213-8587(20)30240-0","article-title":"Efficacy and safety of osilodrostat in patients with Cushing\u2019s disease (LINC 3): a multicentre phase III study with a double-blind, randomised withdrawal phase","volume":"8","author":"Pivonello","year":"2020","journal-title":"Lancet Diabetes Endocrinol."},{"key":"10.1016\/j.ejmech.2021.113284_bib103","doi-asserted-by":"crossref","first-page":"1203","DOI":"10.1021\/ml400324c","article-title":"Discovery and in\u00a0vivo evaluation of potent dual CYP11B2 (aldosterone synthase) and CYP11B1 inhibitors","volume":"4","author":"Meredith","year":"2013","journal-title":"ACS Med. Chem. Lett."},{"key":"10.1016\/j.ejmech.2021.113284_bib104","series-title":"3-Fluoro-benzonitrile Inhibitors of 11-Beta-Hydroxylase","author":"Zhang","year":"2016"},{"key":"10.1016\/j.ejmech.2021.113284_bib105","doi-asserted-by":"crossref","first-page":"2133","DOI":"10.1111\/dom.14133","article-title":"Effect of setmelanotide, a melanocortin-4 receptor agonist, on obesity in Bardet-Biedl syndrome","volume":"22","author":"Haws","year":"2020","journal-title":"Diabetes Obes. Metabol."},{"key":"10.1016\/j.ejmech.2021.113284_bib106","doi-asserted-by":"crossref","first-page":"1321","DOI":"10.1016\/j.molmet.2017.06.015","article-title":"Evaluation of a melanocortin-4 receptor (MC4R) agonist (setmelanotide) in MC4R deficiency","volume":"6","author":"Collet","year":"2017","journal-title":"Mol. Metab."},{"key":"10.1016\/j.ejmech.2021.113284_bib107","doi-asserted-by":"crossref","first-page":"2614","DOI":"10.1111\/bph.13540","article-title":"Magel2-null mice are hyper-responsive to setmelanotide, a melanocortin 4 receptor agonist","volume":"173","author":"Bischof","year":"2016","journal-title":"Br. J. Pharmacol."},{"key":"10.1016\/j.ejmech.2021.113284_bib108","series-title":"Process for the Synthesis of Ac-Arg-cyclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH2","author":"Zheng Xin","year":"2011"},{"key":"10.1016\/j.ejmech.2021.113284_bib109","doi-asserted-by":"crossref","first-page":"2236","DOI":"10.1002\/jnr.24111","article-title":"Triheptanoin for the treatment of brain energy deficit: a 14-year experience","volume":"95","author":"Mochel","year":"2017","journal-title":"J.\u00a0Neurosci. Res."},{"key":"10.1016\/j.ejmech.2021.113284_bib110","doi-asserted-by":"crossref","first-page":"444","DOI":"10.1136\/jnnp-2019-321694","article-title":"Transition from ketogenic diet to triheptanoin in patients with GLUT1 deficiency syndrome","volume":"91","author":"Hainque","year":"2020","journal-title":"J.\u00a0Neurol. Neurosurg. Psychiatry"},{"key":"10.1016\/j.ejmech.2021.113284_bib111","doi-asserted-by":"crossref","first-page":"889","DOI":"10.1002\/ejlt.201100425","article-title":"Synthesis of triheptanoin and formulation as a solid diet for rodents","volume":"114","author":"Semak","year":"2012","journal-title":"Eur. J. Lipid Sci. Technol."},{"key":"10.1016\/j.ejmech.2021.113284_bib112","doi-asserted-by":"crossref","first-page":"445","DOI":"10.1111\/1751-2980.12912","article-title":"Beneficial effects of lactitol on the composition of gut microbiota in constipated patients","volume":"21","author":"Li","year":"2020","journal-title":"J.\u00a0Dig. Dis."},{"key":"10.1016\/j.ejmech.2021.113284_bib113","doi-asserted-by":"crossref","first-page":"97","DOI":"10.1007\/BF00555516","article-title":"Lactitol: gastrointestinal absorption and effect on blood lactate in healthy volunteers and patients with cirrhosis","volume":"35","author":"Metzger","year":"1988","journal-title":"Eur. J. Clin. Pharmacol."},{"key":"10.1016\/j.ejmech.2021.113284_bib114","series-title":"Preparation of Lactitol","author":"Sun","year":"2008"},{"key":"10.1016\/j.ejmech.2021.113284_bib115","doi-asserted-by":"crossref","first-page":"1835","DOI":"10.1007\/s40265-018-1006-3","article-title":"Vibegron: first global approval","volume":"78","author":"Keam","year":"2018","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib116","doi-asserted-by":"crossref","first-page":"609","DOI":"10.1021\/acs.jmedchem.5b01372","article-title":"Discovery of vibegron: a potent and selective beta3 adrenergic receptor agonist for the treatment of overactive bladder","volume":"59","author":"Edmondson","year":"2016","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib117","doi-asserted-by":"crossref","first-page":"783","DOI":"10.1016\/j.eururo.2017.12.022","article-title":"Vibegron, a novel potent and selective beta3-adrenoreceptor agonist, for the treatment of patients with overactive bladder: a randomized, double-blind, placebo-controlled Phase 3 study","volume":"73","author":"Yoshida","year":"2018","journal-title":"Eur. Urol."},{"key":"10.1016\/j.ejmech.2021.113284_bib118","doi-asserted-by":"crossref","first-page":"1437","DOI":"10.1021\/jm4017224","article-title":"Design, synthesis, and evaluation of conformationally restricted acetanilides as potent and selective beta3 adrenergic receptor agonists for the treatment of overactive bladder","volume":"57","author":"Moyes","year":"2014","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib119","doi-asserted-by":"crossref","first-page":"1809","DOI":"10.1093\/ajhp\/zxaa276","article-title":"Decitabine and cedazuridine","volume":"77","author":"Traynor","year":"2020","journal-title":"Am. J. Health Syst. Pharm."},{"key":"10.1016\/j.ejmech.2021.113284_bib120","doi-asserted-by":"crossref","first-page":"1373","DOI":"10.1007\/s40265-020-01389-7","article-title":"Decitabine\/cedazuridine: first approval","volume":"80","author":"Dhillon","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib121","doi-asserted-by":"crossref","first-page":"674","DOI":"10.1182\/blood.2019004143","article-title":"Oral cedazuridine\/decitabine for MDS and CMML: a phase 2 pharmacokinetic\/pharmacodynamic randomized crossover study","volume":"136","author":"Garcia-Manero","year":"2020","journal-title":"Blood"},{"key":"10.1016\/j.ejmech.2021.113284_bib122","doi-asserted-by":"crossref","first-page":"194","DOI":"10.1016\/S2352-3026(19)30030-4","article-title":"An oral fixed-dose combination of decitabine and cedazuridine in myelodysplastic syndromes: a multicentre, open-label, dose-escalation, phase 1 study","volume":"6","author":"Savona","year":"2019","journal-title":"Lancet Haematol."},{"key":"10.1016\/j.ejmech.2021.113284_bib123","first-page":"622","article-title":"Outpatient treatment option for patients with blood cancer","volume":"324","author":"Jaklevic","year":"2020","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2021.113284_bib124","doi-asserted-by":"crossref","first-page":"2582","DOI":"10.1021\/jm401856k","article-title":"Design, synthesis, and pharmacological evaluation of fluorinated tetrahydrouridine derivatives as inhibitors of cytidine deaminase","volume":"57","author":"Ferraris","year":"2014","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib125","doi-asserted-by":"crossref","DOI":"10.1111\/all.14670","article-title":"Oral berotralstat for the prophylaxis of hereditary angioedema attacks in patients in Japan: a phase 3 randomized trial","author":"Ohsawa","year":"2021","journal-title":"Allergy"},{"key":"10.1016\/j.ejmech.2021.113284_bib126","series-title":"Crystalline Salts of a Plasma Kallikrein Inhibitor","author":"El-Kattan","year":"2020"},{"key":"10.1016\/j.ejmech.2021.113284_bib127","doi-asserted-by":"crossref","first-page":"1043","DOI":"10.1517\/13543784.2012.688950","article-title":"Lonafarnib for cancer and progeria","volume":"21","author":"Wong","year":"2012","journal-title":"Expet Opin. Invest. Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib128","doi-asserted-by":"crossref","first-page":"427","DOI":"10.1212\/WNL.0b013e31829d85c0","article-title":"Neurologic features of hutchinson-gilford progeria syndrome after lonafarnib treatment","volume":"81","author":"Ullrich","year":"2013","journal-title":"Neurology"},{"key":"10.1016\/j.ejmech.2021.113284_bib129","doi-asserted-by":"crossref","first-page":"114","DOI":"10.1161\/CIRCULATIONAHA.116.022188","article-title":"Clinical trial of the protein farnesylation inhibitors lonafarnib, pravastatin, and zoledronic acid in children with hutchinson-gilford progeria syndrome","volume":"134","author":"Gordon","year":"2016","journal-title":"Circulation"},{"key":"10.1016\/j.ejmech.2021.113284_bib130","doi-asserted-by":"crossref","first-page":"1687","DOI":"10.1001\/jama.2018.3264","article-title":"Association of lonafarnib treatment vs no treatment with mortality rate in patients with hutchinson-gilford progeria syndrome","volume":"319","author":"Gordon","year":"2018","journal-title":"J.\u00a0Am. Med. Assoc."},{"key":"10.1016\/j.ejmech.2021.113284_bib131","doi-asserted-by":"crossref","first-page":"4290","DOI":"10.1021\/jm970464g","volume":"40","author":"Njoroge","year":"1997","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib132","doi-asserted-by":"crossref","first-page":"4890","DOI":"10.1021\/jm980462b","article-title":"(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]-pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamide (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent","volume":"41","author":"Njoroge","year":"1998","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib133","doi-asserted-by":"crossref","first-page":"433","DOI":"10.1007\/s40265-020-01275-2","article-title":"Avapritinib: first approval","volume":"80","author":"Dhillon","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib134","doi-asserted-by":"crossref","first-page":"561","DOI":"10.1358\/dot.2020.56.9.3170808","article-title":"Avapritinib for metastatic or unresectable gastrointestinal stromal tumors","volume":"56","author":"Alzofon","year":"2020","journal-title":"Drugs Today"},{"key":"10.1016\/j.ejmech.2021.113284_bib135","doi-asserted-by":"crossref","first-page":"609","DOI":"10.1158\/1078-0432.CCR-18-1858","article-title":"Robust activity of avapritinib, potent and highly selective inhibitor of mutated KIT, in patient-derived xenograft models of gastrointestinal stromal tumors","volume":"25","author":"Gebreyohannes","year":"2019","journal-title":"Clin. Cancer Res."},{"key":"10.1016\/j.ejmech.2021.113284_bib136","doi-asserted-by":"crossref","first-page":"108","DOI":"10.1158\/2159-8290.CD-20-0487","article-title":"Resistance to avapritinib in PDGFR\u03b1-driven GIST is caused by secondary mutations in the PDGFR\u03b1 kinase domain","volume":"11","author":"Grunewald","year":"2021","journal-title":"Cancer Discov."},{"key":"10.1016\/j.ejmech.2021.113284_bib137","series-title":"Compositions Useful for Treating Disorders Related to KIT","author":"Zhang","year":"2015"},{"key":"10.1016\/j.ejmech.2021.113284_bib138","doi-asserted-by":"crossref","first-page":"1125","DOI":"10.1007\/s40265-020-01347-3","article-title":"Capmatinib: first approval","volume":"80","author":"Dhillon","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib139","doi-asserted-by":"crossref","first-page":"517","DOI":"10.1016\/S1470-2045(18)30678-8","article-title":"Preliminary activity of capmatinib with gefitinib in NSCLC","volume":"19","author":"Burki","year":"2018","journal-title":"Lancet Oncol."},{"key":"10.1016\/j.ejmech.2021.113284_bib140","doi-asserted-by":"crossref","first-page":"659","DOI":"10.1080\/14737140.2019.1643239","article-title":"Capmatinib for the treatment of non-small cell lung cancer","volume":"19","author":"Vansteenkiste","year":"2019","journal-title":"Expert Rev. Anticancer Ther."},{"key":"10.1016\/j.ejmech.2021.113284_bib141","series-title":"Salts of 2-Fluoro-N-Methyl-4-[7-(quinolin-6-Yl-Methyl)- Imidazo[1,2-B][1,2,4]triazin-2-Yl]benzamide and Processes Related to Preparing the Same","author":"Weng","year":"2017"},{"key":"10.1016\/j.ejmech.2021.113284_bib142","doi-asserted-by":"crossref","first-page":"1345","DOI":"10.1007\/s40265-020-01374-0","article-title":"Lurbinectedin: first approval","volume":"80","author":"Markham","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib143","doi-asserted-by":"crossref","first-page":"1656502","DOI":"10.1080\/2162402X.2019.1656502","article-title":"Lurbinectedin synergizes with immune checkpoint blockade to generate anticancer immunity","volume":"8","author":"Xie","year":"2019","journal-title":"OncoImmunology"},{"key":"10.1016\/j.ejmech.2021.113284_bib144","doi-asserted-by":"crossref","first-page":"1470","DOI":"10.1016\/S1470-2045(18)30737-X","article-title":"Lurbinectedin for BRCA-mutated advanced breast cancer","volume":"19","author":"Gourd","year":"2018","journal-title":"Lancet Oncol."},{"key":"10.1016\/j.ejmech.2021.113284_bib145","doi-asserted-by":"crossref","first-page":"3972","DOI":"10.1002\/anie.201900035","article-title":"A\u00a0scalable total synthesis of the antitumor agents Et-743 and lurbinectedin","volume":"58","author":"He","year":"2019","journal-title":"Angew. Chem. Int., Ed. Engl."},{"key":"10.1016\/j.ejmech.2021.113284_bib146","doi-asserted-by":"crossref","first-page":"923","DOI":"10.1007\/s40265-020-01330-y","article-title":"Pemigatinib: first approval","volume":"80","author":"Hoy","year":"2020","journal-title":"Drugs"},{"issue":"4","key":"10.1016\/j.ejmech.2021.113284_bib147","doi-asserted-by":"crossref","first-page":"389","DOI":"10.2217\/fon-2020-0726","article-title":"Pemigatinib, a potent inhibitor of FGFRs for the treatment of cholangiocarcinoma","volume":"17","author":"Merz","year":"2020","journal-title":"Future Oncol."},{"key":"10.1016\/j.ejmech.2021.113284_bib148","doi-asserted-by":"crossref","first-page":"671","DOI":"10.1016\/S1470-2045(20)30109-1","article-title":"Pemigatinib for previously treated, locally advanced or metastatic cholangiocarcinoma: a multicentre, open-label, phase 2 study","volume":"21","author":"Abou-Alfa","year":"2020","journal-title":"Lancet Oncol."},{"key":"10.1016\/j.ejmech.2021.113284_bib149","doi-asserted-by":"crossref","first-page":"337","DOI":"10.1038\/s41571-020-0369-z","article-title":"Benefit from pemigatinib in cholangiocarcinoma","volume":"17","author":"Romero","year":"2020","journal-title":"Nat. Rev. Clin. Oncol."},{"key":"10.1016\/j.ejmech.2021.113284_bib150","series-title":"Substituted Tricyclic Compounds as FGFR Inhibitors","author":"Wu","year":"2013"},{"key":"10.1016\/j.ejmech.2021.113284_bib151","doi-asserted-by":"crossref","first-page":"1865","DOI":"10.1007\/s40265-020-01427-4","article-title":"Pralsetinib: first approval","volume":"80","author":"Markham","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib152","doi-asserted-by":"crossref","first-page":"261","DOI":"10.1016\/j.annonc.2020.10.599","article-title":"Structural basis of acquired resistance to selpercatinib and pralsetinib mediated by non-gatekeeper RET mutations","volume":"32","author":"Subbiah","year":"2021","journal-title":"Ann. Oncol."},{"key":"10.1016\/j.ejmech.2021.113284_bib153","first-page":"406","article-title":"FDA approves pralsetinib for treatment of adults with metastatic RET fusion-positive NSCLC","volume":"34","author":"Wright","year":"2020","journal-title":"Oncology"},{"key":"10.1016\/j.ejmech.2021.113284_bib154","series-title":"Inhibitors of RET","author":"Brubaker","year":"2017"},{"key":"10.1016\/j.ejmech.2021.113284_bib155","doi-asserted-by":"crossref","first-page":"675","DOI":"10.1007\/s40265-019-01105-0","article-title":"Relugolix: first global approval","volume":"79","author":"Markham","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib156","doi-asserted-by":"crossref","first-page":"193","DOI":"10.1016\/j.eururo.2020.03.053","article-title":"Relugolix: early promise for a novel oral androgen deprivation therapy with radiation therapy for prostate cancer","volume":"78","author":"Sachdev","year":"2020","journal-title":"Eur. Urol."},{"key":"10.1016\/j.ejmech.2021.113284_bib157","doi-asserted-by":"crossref","DOI":"10.1200\/JCO.2020.38.15_suppl.5602","article-title":"HERO phase III trial: results comparing relugolix, an oral GnRH receptor antagonist, versus leuprolide acetate for advanced prostate cancer","volume":"38","author":"Shore","year":"2020","journal-title":"J.\u00a0Clin. Oncol."},{"key":"10.1016\/j.ejmech.2021.113284_bib158","series-title":"Thienopyrimidine Compounds, Their Production and Use","author":"Furuya","year":"2000"},{"key":"10.1016\/j.ejmech.2021.113284_bib159","doi-asserted-by":"crossref","first-page":"1119","DOI":"10.1007\/s40265-020-01343-7","article-title":"Selpercatinib: first approval","volume":"80","author":"Markham","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib160","doi-asserted-by":"crossref","first-page":"34","DOI":"10.1158\/1078-0432.CCR-20-2278","article-title":"Overcoming MET-dependent resistance to selective RET inhibition in patients with RET fusion-positive lung cancer by combining selpercatinib with crizotinib","volume":"27","author":"Rosen","year":"2021","journal-title":"Clin. Cancer Res."},{"key":"10.1016\/j.ejmech.2021.113284_bib161","doi-asserted-by":"crossref","first-page":"813","DOI":"10.1056\/NEJMoa2005653","article-title":"Efficacy of selpercatinib in RET fusion-positive non-small-cell lung cancer","volume":"383","author":"Drilon","year":"2020","journal-title":"N.\u00a0Engl. J. Med."},{"key":"10.1016\/j.ejmech.2021.113284_bib162","article-title":"Selpercatinib (LOXO-292) in patients with RET-mutant medullary thyroid cancer","volume":"38","author":"Shah","year":"2020","journal-title":"J.\u00a0Clin. Oncol."},{"key":"10.1016\/j.ejmech.2021.113284_bib163","series-title":"Substituted Pyrazolo[1,5-A]pyridine Compounds as Ret Kinase Inhibitors","author":"Andrews","year":"2018"},{"key":"10.1016\/j.ejmech.2021.113284_bib164","doi-asserted-by":"crossref","first-page":"931","DOI":"10.1007\/s40265-020-01331-x","article-title":"Selumetinib: first approval","volume":"80","author":"Markham","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib165","doi-asserted-by":"crossref","first-page":"1430","DOI":"10.1056\/NEJMoa1912735","article-title":"Selumetinib in children with inoperable plexiform neurofibromas","volume":"382","author":"Gross","year":"2020","journal-title":"N.\u00a0Engl. J. Med."},{"key":"10.1016\/j.ejmech.2021.113284_bib166","doi-asserted-by":"crossref","first-page":"611","DOI":"10.1016\/j.ejmech.2016.06.043","article-title":"Autophagy regulates Selumetinib (AZD6244) induced-apoptosis in colorectal cancer cells","volume":"122","author":"Grasso","year":"2016","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib167","doi-asserted-by":"crossref","first-page":"2550","DOI":"10.1056\/NEJMoa1605943","article-title":"Activity of selumetinib in neurofibromatosis type 1-related plexiform neurofibromas","volume":"375","author":"Dombi","year":"2016","journal-title":"N.\u00a0Engl. J. Med."},{"key":"10.1016\/j.ejmech.2021.113284_bib168","series-title":"N3 Alkylated Benzimidazole Derivatives as Mek Inhibitors","author":"Wallace","year":"2003"},{"key":"10.1016\/j.ejmech.2021.113284_bib169","doi-asserted-by":"crossref","first-page":"1556","DOI":"10.1021\/acs.jmedchem.5b01501","article-title":"The importance of being Me: magic methyls, methyltransferase inhibitors, and the discovery of tazemetostat","volume":"59","author":"Kuntz","year":"2016","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib170","doi-asserted-by":"crossref","first-page":"513","DOI":"10.1007\/s40265-020-01288-x","article-title":"Tazemetostat: first approval","volume":"80","author":"Hoy","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib171","doi-asserted-by":"crossref","first-page":"1423","DOI":"10.1016\/S1470-2045(20)30451-4","article-title":"Tazemetostat in advanced epithelioid sarcoma with loss of INI1\/SMARCB1: an international, open-label, phase 2 basket study","volume":"21","author":"Gounder","year":"2020","journal-title":"Lancet Oncol."},{"key":"10.1016\/j.ejmech.2021.113284_bib172","doi-asserted-by":"crossref","first-page":"25967","DOI":"10.1039\/C5RA02365C","article-title":"Design, synthesis and biological evaluation of novel 1-methyl-3-oxo-2,3,5,6,7,8-hexahydroisoquinolins as potential EZH2 inhibitors","volume":"5","author":"Zhang","year":"2015","journal-title":"RSC Adv."},{"key":"10.1016\/j.ejmech.2021.113284_bib173","series-title":"Aryl-or Heteroaryl-Substituted Benzene Compounds","author":"Kuntz","year":"2012"},{"key":"10.1016\/j.ejmech.2021.113284_bib174","first-page":"2113","article-title":"Research teams unite to develop an early detection test for ovarian cancer","volume":"126","author":"Printz","year":"2020","journal-title":"Cancer"},{"key":"10.1016\/j.ejmech.2021.113284_bib175","doi-asserted-by":"crossref","first-page":"1033","DOI":"10.1007\/s40265-020-01340-w","article-title":"Tucatinib: first approval","volume":"80","author":"Lee","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.ejmech.2021.113284_bib176","doi-asserted-by":"crossref","first-page":"1336","DOI":"10.3389\/fonc.2020.01336","article-title":"Cost-effectiveness of tucatinib in human epidermal growth factor receptor 2-positive metastatic breast cancer from the US and Chinese perspectives","volume":"10","author":"Wu","year":"2020","journal-title":"Front. Oncol."},{"key":"10.1016\/j.ejmech.2021.113284_bib177","doi-asserted-by":"crossref","first-page":"1231","DOI":"10.1016\/j.annonc.2020.05.014","article-title":"Phase I dose-escalation trial of tucatinib in combination with trastuzumab in patients with HER2-positive breast cancer brain metastases","volume":"31","author":"Metzger Filho","year":"2020","journal-title":"Ann. Oncol."},{"key":"10.1016\/j.ejmech.2021.113284_bib178","series-title":"N4-phenyl-quinazoline-4 -amine Derivatives and Related Compounds as Erbb Type I Receptor Tyrosine Kinase Inhibitors for the Treatment of Hyperproliferative Diseases","author":"Lyssikatos","year":"2007"},{"key":"10.1016\/j.ejmech.2021.113284_bib179","doi-asserted-by":"crossref","first-page":"1191","DOI":"10.1007\/s11427-018-9342-2","article-title":"Artificial intelligence in drug design","volume":"61","author":"Zhong","year":"2018","journal-title":"Sci. China Life Sci."},{"key":"10.1016\/j.ejmech.2021.113284_bib180","doi-asserted-by":"crossref","first-page":"915","DOI":"10.1080\/17460441.2019.1626821","article-title":"Contemporary medicinal-chemistry strategies for discovery of blood coagulation factor Xa inhibitors","volume":"14","author":"Hao","year":"2019","journal-title":"Expet Opin. Drug Discov."},{"key":"10.1016\/j.ejmech.2021.113284_bib181","doi-asserted-by":"crossref","first-page":"9375","DOI":"10.1021\/acs.jmedchem.9b00359","article-title":"Overview of recent strategic advances in medicinal chemistry","volume":"62","author":"Wu","year":"2019","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib182","doi-asserted-by":"crossref","first-page":"375","DOI":"10.4155\/fmc-2018-0397","article-title":"Discovery of novel anti-influenza agents via contemporary medicinal chemistry strategies (2014-2018 update)","volume":"11","author":"Jia","year":"2019","journal-title":"Future Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib183","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2020.112374","article-title":"Medicinal chemistry insights into novel CDC25 inhibitors","volume":"201","author":"Tao","year":"2020","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113284_bib184","article-title":"Natural products as LSD1 inhibitors for cancer therapy","author":"Fang","year":"2020","journal-title":"Acta Pharm. Sin. B"},{"key":"10.1016\/j.ejmech.2021.113284_bib185","first-page":"481","article-title":"Identification of anti-cancer compounds from natural products","volume":"18","author":"Lu","year":"2020","journal-title":"Chin. J. Nat. Med."},{"key":"10.1016\/j.ejmech.2021.113284_bib186","doi-asserted-by":"crossref","first-page":"1695","DOI":"10.1016\/j.cclet.2020.03.028","article-title":"New techniques and strategies in drug discovery","volume":"31","author":"Du","year":"2020","journal-title":"Chin. Chem. Lett."}],"container-title":["European Journal of Medicinal Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0223523421001331?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0223523421001331?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2026,5,13]],"date-time":"2026-05-13T12:51:56Z","timestamp":1778676716000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0223523421001331"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2021,4]]},"references-count":186,"alternative-id":["S0223523421001331"],"URL":"https:\/\/doi.org\/10.1016\/j.ejmech.2021.113284","relation":{},"ISSN":["0223-5234"],"issn-type":[{"value":"0223-5234","type":"print"}],"subject":[],"published":{"date-parts":[[2021,4]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"New drug approvals for 2020: Synthesis and clinical applications","name":"articletitle","label":"Article Title"},{"value":"European Journal of Medicinal Chemistry","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.ejmech.2021.113284","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2021 Elsevier Masson SAS. All rights reserved.","name":"copyright","label":"Copyright"}],"article-number":"113284"}}