{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,8]],"date-time":"2026-09-08T17:18:09Z","timestamp":1788887889431,"version":"build-2803163510"},"reference-count":169,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2023,8,1]],"date-time":"2023-08-01T00:00:00Z","timestamp":1690848000000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2023,8,1]],"date-time":"2023-08-01T00:00:00Z","timestamp":1690848000000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2023,7,3]],"date-time":"2023-07-03T00:00:00Z","timestamp":1688342400000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by-nc-nd\/4.0\/"}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["Pharmacological Research"],"published-print":{"date-parts":[[2023,8]]},"DOI":"10.1016\/j.phrs.2023.106847","type":"journal-article","created":{"date-parts":[[2023,7,14]],"date-time":"2023-07-14T21:24:07Z","timestamp":1689369847000},"page":"106847","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":25,"special_numbering":"C","title":["Small molecule protein kinase inhibitors approved by regulatory agencies outside of the United States"],"prefix":"10.1016","volume":"194","author":[{"given":"Robert","family":"Roskoski Jr.","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"key":"10.1016\/j.phrs.2023.106847_bib1","doi-asserted-by":"crossref","first-page":"309","DOI":"10.1038\/nrd773","article-title":"Protein kinases \u2013 the major drug targets of the twenty-first century?","volume":"1","author":"Cohen","year":"2002","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.phrs.2023.106847_bib2","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1016\/j.phrs.2015.07.010","article-title":"A historical overview of protein kinases and their targeted small molecule inhibitors","volume":"100","author":"Roskoski","year":"2015","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib3","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2022.106552","article-title":"Properties of FDA-approved small molecule protein kinase inhibitors: a 2023 update","volume":"187","author":"Roskoski","year":"2023","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib4","doi-asserted-by":"crossref","first-page":"190","DOI":"10.1016\/j.tips.2022.12.007","article-title":"Futibatinib (Lytgobi) for cholangiocarcinoma","volume":"44","author":"Roskoski","year":"2023","journal-title":"Trends Pharm. Sci."},{"key":"10.1016\/j.phrs.2023.106847_bib5","doi-asserted-by":"crossref","first-page":"551","DOI":"10.1038\/s41573-021-00195-4","article-title":"Kinase drug discovery 20 years after imatinib: progress and future directions","volume":"20","author":"Cohen","year":"2021","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.phrs.2023.106847_bib6","doi-asserted-by":"crossref","first-page":"798","DOI":"10.1038\/s41573-021-00303-4","article-title":"Trends in kinase drug discovery: targets, indications and inhibitor design","volume":"20","author":"Attwood","year":"2021","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.phrs.2023.106847_bib7","doi-asserted-by":"crossref","first-page":"818","DOI":"10.1016\/j.tips.2019.09.002","article-title":"The landscape of atypical and eukaryotic protein kinases","volume":"40","author":"Kanev","year":"2019","journal-title":"Trends Pharm. Sci."},{"key":"10.1016\/j.phrs.2023.106847_bib8","doi-asserted-by":"crossref","first-page":"201","DOI":"10.1007\/978-3-7091-6232-3_42","article-title":"Effect of Fasudil HCl, a protein kinase inhibitor, on cerebral vasospasm","volume":"77","author":"Shibuya","year":"2001","journal-title":"Acta Neurochir. Suppl."},{"key":"10.1016\/j.phrs.2023.106847_bib9","doi-asserted-by":"crossref","first-page":"53","DOI":"10.1007\/BF01541267","article-title":"The effects of an intracellular calcium antagonist HA 1077 on delayed cerebral vasospasm in dogs","volume":"90","author":"Shibuya","year":"1988","journal-title":"Acta Neurochir. (Wien. )"},{"key":"10.1016\/j.phrs.2023.106847_bib10","doi-asserted-by":"crossref","first-page":"123","DOI":"10.1016\/S0163-7258(98)00070-9","article-title":"H-series protein kinase inhibitors and potential clinical applications","volume":"82","author":"Ono-Saito","year":"1999","journal-title":"Pharm. Ther."},{"key":"10.1016\/j.phrs.2023.106847_bib11","doi-asserted-by":"crossref","first-page":"pii: E908","DOI":"10.3390\/molecules23040908","article-title":"PKIDB: a curated, annotated and updated database of protein kinase inhibitors in clinical trials","volume":"23","author":"Carles","year":"2018","journal-title":"Molecules"},{"key":"10.1016\/j.phrs.2023.106847_bib12","doi-asserted-by":"crossref","first-page":"1047","DOI":"10.1021\/acs.jmedchem.1c00963","article-title":"Small molecule kinase inhibitor drugs (1995-2021): medical indication, pharmacology, and synthesis","volume":"65","author":"Ayala-Aguilera","year":"2022","journal-title":"J. Med Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib13","doi-asserted-by":"crossref","first-page":"1912","DOI":"10.1126\/science.1075762","article-title":"The protein kinase complement of the human genome","volume":"298","author":"Manning","year":"2002","journal-title":"Science"},{"key":"10.1016\/j.phrs.2023.106847_bib14","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2021.105579","article-title":"Properties of FDA-approved small molecule phosphatidylinositol 3-kinase inhibitors prescribed for the treatment of malignancies","volume":"168","author":"Roskoski","year":"2021","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib15","doi-asserted-by":"crossref","first-page":"1115","DOI":"10.1016\/j.chembiol.2014.08.013","article-title":"Oral druggable space beyond the rule of 5: insights from drugs and clinical candidates","volume":"21","author":"Doak","year":"2014","journal-title":"Chem. Biol."},{"key":"10.1016\/j.phrs.2023.106847_bib16","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2021.105422","article-title":"Orally effective FDA-approved protein kinase targeted covalent inhibitors (TCIs)","volume":"165","author":"Roskoski","year":"2021","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib17","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2022.106642","article-title":"Deucravacitinib is an allosteric TYK2 protein kinase inhibitor FDA-approved for the treatment of psoriasis","volume":"189","author":"Roskoski","year":"2023","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib18","doi-asserted-by":"crossref","first-page":"19","DOI":"10.1016\/j.phrs.2019.03.006","article-title":"Properties of FDA-approved small molecule protein kinase inhibitors","volume":"144","author":"Roskoski","year":"2019","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib19","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2019.104609","article-title":"Properties of FDA-approved small molecule protein kinase inhibitors: a 2020 update","volume":"152","author":"Roskoski","year":"2020","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib20","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2021.105463","article-title":"Properties of FDA-approved small molecule protein kinase inhibitors: a 2021 update","volume":"165","author":"Roskoski","year":"2021","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib21","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2021.106037","article-title":"Properties of FDA-approved small molecule protein kinase inhibitors: A 2022 update","volume":"175","author":"Roskoski","year":"2022","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib22","doi-asserted-by":"crossref","first-page":"407","DOI":"10.1126\/science.1862342","article-title":"Crystal structure of the catalytic subunit of cyclic adenosine monophosphate-dependent protein kinase","volume":"253","author":"Knighton","year":"1991","journal-title":"Science"},{"key":"10.1016\/j.phrs.2023.106847_bib23","doi-asserted-by":"crossref","first-page":"628","DOI":"10.1016\/j.tibs.2015.09.002","article-title":"Dynamics-driven allostery in protein kinases","volume":"40","author":"Kornev","year":"2015","journal-title":"Trends Biochem Sci."},{"key":"10.1016\/j.phrs.2023.106847_bib24","doi-asserted-by":"crossref","DOI":"10.1016\/j.jbc.2021.100746","article-title":"From structure to the dynamic regulation of a molecular switch: a journey over 3 decades","volume":"296","author":"Taylor","year":"2021","journal-title":"J. Biol. Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib25","doi-asserted-by":"crossref","first-page":"471","DOI":"10.1016\/j.phrs.2018.11.035","article-title":"Cyclin-dependent protein serine\/threonine kinase inhibitors as anticancer drugs","volume":"139","author":"Roskoski","year":"2019","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib26","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2021.105660","article-title":"Hydrophobic and polar interactions of FDA-approved small molecule protein kinase inhibitors with their target enzymes","volume":"169","author":"Roskoski","year":"2021","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib27","doi-asserted-by":"crossref","first-page":"576","DOI":"10.1096\/fasebj.9.8.7768349","article-title":"Protein kinases 6. The eukaryotic protein kinase superfamily: kinase (catalytic) domain structure and classification","volume":"9","author":"Hanks","year":"1995","journal-title":"FASEB J."},{"key":"10.1016\/j.phrs.2023.106847_bib28","doi-asserted-by":"crossref","first-page":"176","DOI":"10.1002\/pro.5560030203","article-title":"cAMP-dependent protein kinase: crystallographic insights into substrate recognition and phosphotransfer","volume":"3","author":"Madhusudan","year":"1994","journal-title":"Protein Sci."},{"key":"10.1016\/j.phrs.2023.106847_bib29","doi-asserted-by":"crossref","first-page":"15733","DOI":"10.1021\/bi971438n","article-title":"Participation of ADP dissociation in the rate-determining step in cAMP-dependent protein kinase","volume":"36","author":"Zhou","year":"1997","journal-title":"Biochemistry"},{"key":"10.1016\/j.phrs.2023.106847_bib30","doi-asserted-by":"crossref","first-page":"192","DOI":"10.1016\/j.bioorg.2011.07.004","article-title":"Protein kinase biochemistry and drug discovery","volume":"39","author":"Schwartz","year":"2011","journal-title":"Bioorg. Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib31","doi-asserted-by":"crossref","first-page":"440","DOI":"10.1016\/j.bbapap.2009.10.017","article-title":"Defining the conserved internal architecture of a protein kinase","volume":"1804","author":"Kornev","year":"2010","journal-title":"Biochim Biophys. Acta"},{"key":"10.1016\/j.phrs.2023.106847_bib32","doi-asserted-by":"crossref","first-page":"6818","DOI":"10.1073\/pnas.1814279116","article-title":"Defining a new nomenclature for the structures of active and inactive kinases","volume":"116","author":"Modi","year":"2019","journal-title":"Proc. Natl. Acad. Sci. USA"},{"issue":"D1","key":"10.1016\/j.phrs.2023.106847_bib33","doi-asserted-by":"crossref","first-page":"D654","DOI":"10.1093\/nar\/gkab920","article-title":"Kincore: a web resource for structural classification of protein kinases and their inhibitors","volume":"50","author":"Modi","year":"2022","journal-title":"Nucleic Acids Res"},{"key":"10.1016\/j.phrs.2023.106847_bib34","doi-asserted-by":"crossref","first-page":"17783","DOI":"10.1073\/pnas.0607656103","article-title":"Surface comparison of active and inactive protein kinases identifies a conserved activation mechanism","volume":"103","author":"Kornev","year":"2006","journal-title":"Proc. Natl. Acad. Sci. USA"},{"key":"10.1016\/j.phrs.2023.106847_bib35","doi-asserted-by":"crossref","first-page":"14377","DOI":"10.1073\/pnas.0807988105","article-title":"A helix scaffold for the assembly of active protein kinases","volume":"105","author":"Kornev","year":"2008","journal-title":"Proc. Natl. Acad. Sci. USA"},{"key":"10.1016\/j.phrs.2023.106847_bib36","doi-asserted-by":"crossref","DOI":"10.1371\/journal.pbio.1001680","article-title":"Deciphering the structural basis of eukaryotic protein kinase regulation","volume":"11","author":"Meharena","year":"2013","journal-title":"PLoS Biol."},{"key":"10.1016\/j.phrs.2023.106847_bib37","doi-asserted-by":"crossref","first-page":"1219","DOI":"10.1016\/S0968-0896(98)00099-6","article-title":"A molecular gate which controls unnatural ATP analogue recognition by the tyrosine kinase v-Src","volume":"6","author":"Liu","year":"1998","journal-title":"Bioorg. Med Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib38","doi-asserted-by":"crossref","first-page":"769","DOI":"10.1146\/annurev-biochem-090308-173656","article-title":"The evolution of protein kinase inhibitors from antagonists to agonists of cellular signaling","volume":"80","author":"Dar","year":"2011","journal-title":"Annu Rev. Biochem"},{"key":"10.1016\/j.phrs.2023.106847_bib39","doi-asserted-by":"crossref","first-page":"916","DOI":"10.1016\/j.chembiol.2018.05.002","article-title":"Redefining the protein kinase conformational space with machine learning","volume":"25","author":"Ung","year":"2018","journal-title":"Cell Chem. Biol."},{"issue":"D1","key":"10.1016\/j.phrs.2023.106847_bib40","doi-asserted-by":"crossref","first-page":"D552","DOI":"10.1093\/nar\/gkaa945","article-title":"KinaseMD: kinase mutations and drug response database","volume":"49","author":"Hu","year":"2021","journal-title":"Nucleic Acids Res"},{"key":"10.1016\/j.phrs.2023.106847_bib41","doi-asserted-by":"crossref","first-page":"2691","DOI":"10.1021\/jm901443h","article-title":"Through the \"gatekeeper door\": exploiting the active kinase conformation","volume":"53","author":"Zuccotto","year":"2010","journal-title":"J. Med Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib42","doi-asserted-by":"crossref","first-page":"2936","DOI":"10.2174\/138161212800672813","article-title":"New directions in targeting protein kinases: focusing upon true allosteric and bivalent inhibitors","volume":"18","author":"Lamba","year":"2012","journal-title":"Curr. Pharm. Des."},{"key":"10.1016\/j.phrs.2023.106847_bib43","doi-asserted-by":"crossref","first-page":"409","DOI":"10.1021\/jm0608107","article-title":"Molecular recognition of protein kinase binding pockets for design of potent and selective kinase inhibitors","volume":"50","author":"Liao","year":"2007","journal-title":"J. Med Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib44","doi-asserted-by":"crossref","first-page":"26","DOI":"10.1016\/j.phrs.2015.10.021","article-title":"Classification of small molecule protein kinase inhibitors based upon the structures of their drug-enzyme complexes","volume":"103","author":"Roskoski","year":"2016","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib45","doi-asserted-by":"crossref","first-page":"249","DOI":"10.1021\/jm400378w","article-title":"KLIFS: a knowledge-based structural database to navigate kinase-ligand interaction space","volume":"57","author":"van Linden","year":"2014","journal-title":"J. Med Chem."},{"issue":"D1","key":"10.1016\/j.phrs.2023.106847_bib46","doi-asserted-by":"crossref","first-page":"D365","DOI":"10.1093\/nar\/gkv1082","article-title":"KLIFS: a structural kinase-ligand interaction database","volume":"44","author":"Kooistra","year":"2016","journal-title":"Nucleic Acids Res"},{"key":"10.1016\/j.phrs.2023.106847_bib47","first-page":"gkaa895","article-title":"KLIFS: an overhaul after the first 5 years of supporting kinase research","author":"Kanev","year":"2020","journal-title":"Nucleic Acids Res"},{"key":"10.1016\/j.phrs.2023.106847_bib48","doi-asserted-by":"crossref","first-page":"2235","DOI":"10.2174\/1568026617666170224121313","article-title":"Structure-based virtual screening approaches in kinase-directed drug discovery","volume":"17","author":"Bajusz","year":"2017","journal-title":"Curr. Top. Med Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib49","doi-asserted-by":"crossref","first-page":"990","DOI":"10.1038\/40187","article-title":"Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension","volume":"389","author":"Uehata","year":"1997","journal-title":"Nature"},{"key":"10.1016\/j.phrs.2023.106847_bib50","doi-asserted-by":"crossref","first-page":"276","DOI":"10.3389\/fphar.2015.00276","article-title":"The function of Rho-associated kinases ROCK1 and ROCK2 in the pathogenesis of cardiovascular disease","volume":"6","author":"Hartmann","year":"2015","journal-title":"Front Pharm."},{"key":"10.1016\/j.phrs.2023.106847_bib51","doi-asserted-by":"crossref","first-page":"15","DOI":"10.1016\/j.imlet.2019.12.012","article-title":"Targeting ROCK signaling in health, malignant and non-malignant diseases","volume":"219","author":"Shahbazi","year":"2020","journal-title":"Immunol. Lett."},{"key":"10.1016\/j.phrs.2023.106847_bib52","doi-asserted-by":"crossref","first-page":"2269","DOI":"10.1021\/acs.jmedchem.5b00683","article-title":"Rho kinase (ROCK) inhibitors and their therapeutic potential","volume":"59","author":"Feng","year":"2016","journal-title":"J. Med Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib53","doi-asserted-by":"crossref","first-page":"4342","DOI":"10.1021\/acs.jmedchem.2c01753","article-title":"Application and study of ROCK inhibitors in pulmonary fibrosis: recent developments and future Perspectives","volume":"66","author":"Xie","year":"2023","journal-title":"J. Med Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib54","doi-asserted-by":"crossref","first-page":"260","DOI":"10.1074\/jbc.M508847200","article-title":"The structure of dimeric ROCK I reveals the mechanism for ligand selectivity","volume":"281","author":"Jacobs","year":"2006","journal-title":"J. Biol. Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib55","doi-asserted-by":"crossref","first-page":"717","DOI":"10.1517\/14656566.2014.890183","article-title":"Icotinib: activity and clinical application in Chinese patients with lung cancer","volume":"15","author":"Guan","year":"2014","journal-title":"Expert Opin. Pharm."},{"key":"10.1016\/j.phrs.2023.106847_bib56","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1016\/j.bbrc.2004.04.150","article-title":"The ErbB\/HER receptor protein-tyrosine kinases and cancer","volume":"319","author":"Roskoski","year":"2004","journal-title":"Biochem Biophys. Res Commun."},{"key":"10.1016\/j.phrs.2023.106847_bib57","doi-asserted-by":"crossref","first-page":"34","DOI":"10.1016\/j.phrs.2013.11.002","article-title":"The ErbB\/HER family of protein-tyrosine kinases and cancer","volume":"79","author":"Roskoski","year":"2014","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib58","doi-asserted-by":"crossref","first-page":"42","DOI":"10.1016\/j.phrs.2014.06.001","article-title":"ErbB\/HER protein-tyrosine kinases: Structure and small molecule inhibitors","volume":"87","author":"Roskoski","year":"2014","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib59","doi-asserted-by":"crossref","first-page":"395","DOI":"10.1016\/j.phrs.2018.11.014","article-title":"Small molecule inhibitors targeting the EGFR\/ErbB family of protein-tyrosine kinases in human cancers","volume":"139","author":"Roskoski","year":"2019","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib60","first-page":"209","article-title":"Global cancer statistics 2020: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries","volume":"71","author":"Sung","year":"2021","journal-title":"CA Cancer J. Clin."},{"key":"10.1016\/j.phrs.2023.106847_bib61","doi-asserted-by":"crossref","first-page":"177","DOI":"10.1016\/j.lungcan.2011.10.023","article-title":"Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies","volume":"76","author":"Tan","year":"2012","journal-title":"Lung Cancer"},{"key":"10.1016\/j.phrs.2023.106847_bib62","doi-asserted-by":"crossref","first-page":"195","DOI":"10.1016\/j.lungcan.2010.11.007","article-title":"Phase I study of icotinib hydrochloride (BPI-2009H), an oral EGFR tyrosine kinase inhibitor, in patients with advanced NSCLC and other solid tumors","volume":"73","author":"Zhao","year":"2011","journal-title":"Lung Cancer"},{"key":"10.1016\/j.phrs.2023.106847_bib63","doi-asserted-by":"crossref","first-page":"953","DOI":"10.1016\/S1470-2045(13)70355-3","article-title":"Icotinib versus gefitinib in previously treated advanced non-small-cell lung cancer (ICOGEN): a randomised, double-blind phase 3 non-inferiority trial","volume":"14","author":"Shi","year":"2013","journal-title":"Lancet Oncol."},{"key":"10.1016\/j.phrs.2023.106847_bib64","doi-asserted-by":"crossref","first-page":"2211","DOI":"10.1007\/s40265-014-0333-2","article-title":"Ripasudil: first global approval","volume":"74","author":"Garnock-Jones","year":"2014","journal-title":"Drugs"},{"key":"10.1016\/j.phrs.2023.106847_bib65","doi-asserted-by":"crossref","DOI":"10.1038\/srep19640","article-title":"Effects of K-115 (Ripasudil), a novel ROCK inhibitor, on trabecular meshwork and Schlemm's canal endothelial cells","volume":"6","author":"Kaneko","year":"2016","journal-title":"Sci. Rep."},{"key":"10.1016\/j.phrs.2023.106847_bib66","doi-asserted-by":"crossref","first-page":"e254","DOI":"10.1111\/aos.12599","article-title":"Intra-ocular pressure-lowering effects of a Rho kinase inhibitor, ripasudil (K-115), over 24\u2009h in primary open-angle glaucoma and ocular hypertension: a randomized, open-label, crossover study","volume":"93","author":"Tanihara","year":"2015","journal-title":"Acta Ophthalmol."},{"key":"10.1016\/j.phrs.2023.106847_bib67","doi-asserted-by":"crossref","first-page":"1288","DOI":"10.1001\/jamaophthalmol.2013.323","article-title":"Phase 1 clinical trials of a selective Rho kinase inhibitor, K-115","volume":"131","author":"Tanihara","year":"2013","journal-title":"JAMA Ophthalmol."},{"key":"10.1016\/j.phrs.2023.106847_bib68","doi-asserted-by":"crossref","first-page":"179","DOI":"10.1016\/j.critrevonc.2007.01.006","article-title":"Vascular endothelial growth factor (VEGF) signaling in tumor progression","volume":"62","author":"Roskoski","year":"2007","journal-title":"Crit. Rev. Oncol. Hematol."},{"key":"10.1016\/j.phrs.2023.106847_bib69","doi-asserted-by":"crossref","first-page":"287","DOI":"10.1016\/j.bbrc.2008.07.121","article-title":"VEGF receptor protein-tyrosine kinases: structure and regulation","volume":"375","author":"Roskoski","year":"2008","journal-title":"Biochem Biophys. Res Commun."},{"key":"10.1016\/j.phrs.2023.106847_bib70","doi-asserted-by":"crossref","first-page":"116","DOI":"10.1016\/j.phrs.2017.03.010","article-title":"Vascular endothelial growth factor (VEGF) and VEGF receptor inhibitors in the treatment of renal cell carcinomas","volume":"120","author":"Roskoski","year":"2017","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib71","doi-asserted-by":"crossref","DOI":"10.3389\/fonc.2021.749083","article-title":"Efficacy and response biomarkers of apatinib in the treatment of malignancies in China: a review","volume":"11","author":"Tian","year":"2021","journal-title":"Front Oncol."},{"key":"10.1016\/j.phrs.2023.106847_bib72","doi-asserted-by":"crossref","first-page":"7981","DOI":"10.1158\/0008-5472.CAN-10-0111","article-title":"Apatinib (YN968D1) reverses multidrug resistance by inhibiting the efflux function of multiple ATP-binding cassette transporters","volume":"70","author":"Mi","year":"2010","journal-title":"Cancer Res"},{"key":"10.1016\/j.phrs.2023.106847_bib73","doi-asserted-by":"crossref","first-page":"1374","DOI":"10.1111\/j.1349-7006.2011.01939.x","article-title":"YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo","volume":"102","author":"Tian","year":"2011","journal-title":"Cancer Sci."},{"key":"10.1016\/j.phrs.2023.106847_bib74","doi-asserted-by":"crossref","first-page":"1961","DOI":"10.1002\/ijc.28829","article-title":"Multicenter phase ii study of apatinib, a novel VEGFR inhibitor in heavily pretreated patients with metastatic triple-negative breast cancer","volume":"135","author":"Hu","year":"2014","journal-title":"Int. J. Cancer"},{"key":"10.1016\/j.phrs.2023.106847_bib75","doi-asserted-by":"crossref","first-page":"709","DOI":"10.1016\/j.bbrc.2003.08.055","article-title":"STI-571: an anticancer protein-tyrosine kinase inhibitor","volume":"309","author":"Roskoski","year":"2003","journal-title":"Biochem Biophys. Res Commun."},{"key":"10.1016\/j.phrs.2023.106847_bib76","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2022.106156","article-title":"Targeting BCR-Abl in the treatment of Philadelphia-chromosome positive chronic myelogenous leukemia","volume":"178","author":"Roskoski","year":"2022","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib77","doi-asserted-by":"crossref","first-page":"1191","DOI":"10.3324\/haematol.2013.096776","article-title":"Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitors","volume":"99","author":"Kim","year":"2014","journal-title":"Haematologica"},{"key":"10.1016\/j.phrs.2023.106847_bib78","doi-asserted-by":"crossref","first-page":"1939","DOI":"10.1038\/leu.2015.42","article-title":"Radotinib is an effective inhibitor of native and kinase domain-mutant BCR-ABL1","volume":"29","author":"Zabriskie","year":"2015","journal-title":"Leukemia"},{"key":"10.1016\/j.phrs.2023.106847_bib79","doi-asserted-by":"crossref","first-page":"237","DOI":"10.1177\/2040620717719851","article-title":"Radotinib and its clinical potential in chronic-phase chronic myeloid leukemia patients: an update","volume":"8","author":"Eskazan","year":"2017","journal-title":"Ther. Adv. Hematol."},{"key":"10.1016\/j.phrs.2023.106847_bib80","doi-asserted-by":"crossref","first-page":"7180","DOI":"10.1158\/1078-0432.CCR-17-0957","article-title":"Phase III clinical trial (rerise study) results of efficacy and safety of radotinib compared with imatinib in newly diagnosed chronic phase chronic myeloid leukemia","volume":"23","author":"Kwak","year":"2017","journal-title":"Clin. Cancer Res"},{"key":"10.1016\/j.phrs.2023.106847_bib81","doi-asserted-by":"crossref","first-page":"1153","DOI":"10.1007\/s40265-016-0606-z","article-title":"Olmutinib: first global approval","volume":"76","author":"Kim","year":"2016","journal-title":"Drugs"},{"key":"10.1016\/j.phrs.2023.106847_bib82","doi-asserted-by":"crossref","first-page":"689","DOI":"10.1158\/0008-5472.CAN-18-1281","article-title":"Novel third-generation EGFR tyrosine kinase inhibitors and strategies to overcome therapeutic resistance in lung cancer","volume":"79","author":"Murtuza","year":"2019","journal-title":"Cancer Res"},{"key":"10.1016\/j.phrs.2023.106847_bib83","doi-asserted-by":"crossref","first-page":"1407","DOI":"10.1002\/cncr.33385","article-title":"Olmutinib in T790M-positive non-small cell lung cancer after failure of first-line epidermal growth factor receptor-tyrosine kinase inhibitor therapy: A global, phase 2 study","volume":"127","author":"Park","year":"2021","journal-title":"Cancer"},{"key":"10.1016\/j.phrs.2023.106847_bib84","doi-asserted-by":"crossref","DOI":"10.2147\/CMAR.S189626","article-title":"Safety, tolerability, and pharmacokinetics of simotinib, a novel specific EGFR tyrosine kinase inhibitor, in patients with advanced non-small cell lung cancer: results of a phase Ib trial","volume":"11","author":"Hu","year":"2019","journal-title":"Cancer Manag Res"},{"key":"10.1016\/j.phrs.2023.106847_bib85","doi-asserted-by":"crossref","first-page":"1057","DOI":"10.1007\/s40265-018-0939-x","article-title":"Anlotinib: first global approval","volume":"78","author":"Syed","year":"2018","journal-title":"Drugs"},{"key":"10.1016\/j.phrs.2023.106847_bib86","doi-asserted-by":"crossref","first-page":"1207","DOI":"10.1111\/cas.13536","article-title":"Preclinical characterization of anlotinib, a highly potent and selective vascular endothelial growth factor receptor-2 inhibitor","volume":"109","author":"Xie","year":"2018","journal-title":"Cancer Sci."},{"key":"10.1016\/j.phrs.2023.106847_bib87","first-page":"36","article-title":"China National Medical Products Administration approval summary: anlotinib for the treatment of advanced non-small cell lung cancer after two lines of chemotherapy","volume":"39","author":"Zhou","year":"2019","journal-title":"Cancer Commun. (Lond. )"},{"key":"10.1016\/j.phrs.2023.106847_bib88","doi-asserted-by":"crossref","first-page":"1001","DOI":"10.3892\/ol.2020.11685","article-title":"Anlotinib as a molecular targeted therapy for tumors","volume":"20","author":"Gao","year":"2020","journal-title":"Oncol. Lett."},{"issue":"16","key":"10.1016\/j.phrs.2023.106847_bib89","doi-asserted-by":"crossref","first-page":"1757","DOI":"10.1007\/s40265-018-0998-z","article-title":"Fruquintinib: first global approval","volume":"78","author":"Shirley","year":"2018","journal-title":"Drugs"},{"key":"10.1016\/j.phrs.2023.106847_bib90","doi-asserted-by":"crossref","first-page":"5840","DOI":"10.3390\/ijms24065840","article-title":"Evaluation of fruquintinib in the continuum of care of patients with colorectal cancer","volume":"24","author":"Lavacchi","year":"2023","journal-title":"Int J. Mol. Sci."},{"key":"10.1016\/j.phrs.2023.106847_bib91","doi-asserted-by":"crossref","first-page":"461","DOI":"10.5582\/bst.2019.01243","article-title":"Rapid advances in research on and development of anticancer drugs in China","volume":"13","author":"Yao","year":"2019","journal-title":"Biosci. Trends"},{"key":"10.1016\/j.phrs.2023.106847_bib92","doi-asserted-by":"crossref","first-page":"117","DOI":"10.1111\/cas.12320","article-title":"Flumatinib, a selective inhibitor of BCR-ABL\/PDGFR\/KIT, effectively overcomes drug resistance of certain KIT mutants","volume":"105","author":"Zhao","year":"2014","journal-title":"Cancer Sci."},{"key":"10.1016\/j.phrs.2023.106847_bib93","doi-asserted-by":"crossref","first-page":"70","DOI":"10.1158\/1078-0432.CCR-20-1600","article-title":"Flumatinib versus imatinib for newly diagnosed chronic phase chronic myeloid leukemia: a phase iii, randomized, open-label, multi-center FESTnd study","volume":"27","author":"Zhang","year":"2021","journal-title":"Clin. Cancer Res"},{"key":"10.1016\/j.phrs.2023.106847_bib94","doi-asserted-by":"crossref","first-page":"1987","DOI":"10.1007\/s40265-020-01439-0","article-title":"Filgotinib: first approval","volume":"80","author":"Dhillon","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.phrs.2023.106847_bib95","doi-asserted-by":"crossref","first-page":"784","DOI":"10.1016\/j.phrs.2016.07.038","article-title":"Janus kinase (JAK) inhibitors in the treatment of inflammatory and neoplastic diseases","volume":"111","author":"Roskoski","year":"2016","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib96","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2022.106362","article-title":"Janus kinase (JAK) inhibitors in the treatment of neoplastic and inflammatory disorders","volume":"183","author":"Roskoski","year":"2022","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib97","doi-asserted-by":"crossref","first-page":"9323","DOI":"10.1021\/jm501262q","article-title":"Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634","volume":"57","author":"Menet","year":"2014","journal-title":"J. Med Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib98","doi-asserted-by":"crossref","first-page":"740","DOI":"10.1016\/j.jtho.2020.11.028","article-title":"Beyond Osimertinib: The development of third-generation EGFR tyrosine kinase inhibitors for advanced EGFR+ NSCLC","volume":"16","author":"Nagasaka","year":"2021","journal-title":"J. Thorac. Oncol."},{"key":"10.1016\/j.phrs.2023.106847_bib99","doi-asserted-by":"crossref","first-page":"590","DOI":"10.1080\/07357907.2022.2069254","article-title":"Three third-generation epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer: similarities and differences","volume":"40","author":"Chen","year":"2022","journal-title":"Cancer Invest"},{"key":"10.1016\/j.phrs.2023.106847_bib100","doi-asserted-by":"crossref","first-page":"835","DOI":"10.1007\/s40265-020-01318-8","article-title":"Tirabrutinib: first approval","volume":"80","author":"Dhillon","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.phrs.2023.106847_bib101","doi-asserted-by":"crossref","first-page":"277","DOI":"10.1358\/dot.2021.57.4.3264113","article-title":"Tirabrutinib hydrochloride for B-cell lymphomas","volume":"57","author":"Munakata","year":"2021","journal-title":"Drugs Today"},{"key":"10.1016\/j.phrs.2023.106847_bib102","doi-asserted-by":"crossref","DOI":"10.1186\/s13045-022-01353-w","article-title":"BTK inhibitors in the treatment of hematological malignancies and inflammatory diseases: mechanisms and clinical studies","volume":"15","author":"Alu","year":"2022","journal-title":"J. Hematol. Oncol."},{"key":"10.1016\/j.phrs.2023.106847_bib103","doi-asserted-by":"crossref","first-page":"395","DOI":"10.1016\/j.phrs.2016.09.011","article-title":"Ibrutinib inhibition of Bruton protein-tyrosine kinase (BTK) in the treatment of B cell neoplasms","volume":"113","author":"Roskoski","year":"2016","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib104","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2021.105806","article-title":"Blockade of mutant RAS oncogenic signaling with a special emphasis on KRAS","volume":"172","author":"Roskoski","year":"2021","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib105","doi-asserted-by":"crossref","first-page":"239","DOI":"10.1016\/j.phrs.2018.08.013","article-title":"Targeting oncogenic Raf protein-serine\/threonine kinases in human cancers","volume":"135","author":"Roskoski","year":"2018","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib106","doi-asserted-by":"crossref","first-page":"5","DOI":"10.1016\/j.bbrc.2011.11.145","article-title":"MEK1\/2 dual-specificity protein kinases: structure and regulation","volume":"417","author":"Roskoski","year":"2012","journal-title":"Biochem Biophys. Res Commun."},{"key":"10.1016\/j.phrs.2023.106847_bib107","doi-asserted-by":"crossref","first-page":"20","DOI":"10.1016\/j.phrs.2016.12.009","article-title":"Allosteric MEK1\/2 inhibitors including cobimetanib and trametinib in the treatment of cutaneous melanomas","volume":"117","author":"Roskoski","year":"2017","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib108","doi-asserted-by":"crossref","first-page":"105","DOI":"10.1016\/j.phrs.2012.04.005","article-title":"ERK1\/2 MAP kinases: structure, function, and regulation","volume":"66","author":"Roskoski","year":"2012","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib109","doi-asserted-by":"crossref","first-page":"151","DOI":"10.1016\/j.phrs.2019.01.039","article-title":"Targeting ERK1\/2 protein-serine\/threonine kinases in human cancers","volume":"142","author":"Roskoski","year":"2019","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib110","doi-asserted-by":"crossref","first-page":"208","DOI":"10.1124\/mol.116.107037","article-title":"Ability of Bruton's tyrosine kinase inhibitors to sequester y551 and prevent phosphorylation determines potency for inhibition of Fc receptor but not B-cell receptor signaling","volume":"91","author":"Bender","year":"2017","journal-title":"Mol. Pharm."},{"key":"10.1016\/j.phrs.2023.106847_bib111","doi-asserted-by":"crossref","first-page":"127","DOI":"10.3390\/cancers10040127","article-title":"Responses to the selective bruton's tyrosine kinase (BTK) inhibitor tirabrutinib (ONO\/GS-4059) in diffuse large B-cell lymphoma cell lines","volume":"10","author":"Kozaki","year":"2018","journal-title":"Cancers (Basel)"},{"issue":"4","key":"10.1016\/j.phrs.2023.106847_bib112","doi-asserted-by":"crossref","first-page":"7201","DOI":"10.18632\/oncotarget.12786","article-title":"Bruton tyrosine kinase inhibitor ONO\/GS-4059: from bench to bedside","volume":"8","author":"Wu","year":"2017","journal-title":"Oncotarget"},{"key":"10.1016\/j.phrs.2023.106847_bib113","doi-asserted-by":"crossref","first-page":"609","DOI":"10.1007\/s40265-020-01291-2","article-title":"Delgocitinib: first approval","volume":"80","author":"Dhillon","year":"2020","journal-title":"Drugs"},{"key":"10.1016\/j.phrs.2023.106847_bib114","doi-asserted-by":"crossref","first-page":"41","DOI":"10.1007\/s00011-014-0782-9","article-title":"Pharmacological properties of JTE-052: a novel potent JAK inhibitor that suppresses various inflammatory responses in vitro and in vivo","volume":"64","author":"Tanimoto","year":"2015","journal-title":"Inflamm. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib115","doi-asserted-by":"crossref","first-page":"7163","DOI":"10.1021\/acs.jmedchem.0c00450","article-title":"Discovery of a janus kinase inhibitor bearing a highly three-dimensional spiro scaffold: JTE-052 (delgocitinib) as a new dermatological agent to treat inflammatory skin disorders","volume":"63","author":"Noji","year":"2020","journal-title":"J. Med Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib116","doi-asserted-by":"crossref","first-page":"823","DOI":"10.1016\/j.jaad.2019.12.015","article-title":"Delgocitinib ointment, a topical Janus kinase inhibitor, in adult patients with moderate to severe atopic dermatitis: A phase 3, randomized, double-blind, vehicle-controlled study and an open-label, long-term extension study","volume":"82","author":"Nakagawa","year":"2020","journal-title":"J. Am. Acad. Dermatol."},{"key":"10.1016\/j.phrs.2023.106847_bib117","doi-asserted-by":"crossref","first-page":"1751","DOI":"10.1007\/s40265-018-0997-0","article-title":"Pyrotinib: first global approval","volume":"78","author":"Blair","year":"2018","journal-title":"Drugs"},{"key":"10.1016\/j.phrs.2023.106847_bib118","doi-asserted-by":"crossref","first-page":"351","DOI":"10.1016\/S1470-2045(20)30702-6","article-title":"Pyrotinib plus capecitabine versus lapatinib plus capecitabine for the treatment of HER2-positive metastatic breast cancer (PHOEBE): a multicentre, open-label, randomised, controlled, phase 3 trial","volume":"22","author":"Xu","year":"2021","journal-title":"Lancet Oncol."},{"key":"10.1016\/j.phrs.2023.106847_bib119","article-title":"Effectiveness and safety of pyrotinib, and association of biomarker with progression-free survival in patients with her2-positive metastatic breast cancer: a real-world, multicentre analysis","volume":"10","author":"Chen","year":"2020","journal-title":"Front Oncol."},{"key":"10.1016\/j.phrs.2023.106847_bib120","doi-asserted-by":"crossref","first-page":"247","DOI":"10.21037\/tcr-22-1746","article-title":"Pyrotinib for HER2-positive metastatic breast cancer: a systematic review and meta-analysis","volume":"12","author":"Hu","year":"2023","journal-title":"Transl. Cancer Res"},{"key":"10.1016\/j.phrs.2023.106847_bib121","article-title":"Prediction of pyrotinib exposure based on physiologically-based pharmacokinetic model and endogenous biomarker","volume":"13","author":"Zhang","year":"2022","journal-title":"Front Pharm."},{"key":"10.1016\/j.phrs.2023.106847_bib122","doi-asserted-by":"crossref","first-page":"503","DOI":"10.1007\/s40265-021-01482-5","article-title":"Orelabrutinib: first approval","volume":"81","author":"Dhillon","year":"2021","journal-title":"Drugs"},{"key":"10.1016\/j.phrs.2023.106847_bib123","doi-asserted-by":"crossref","first-page":"571","DOI":"10.1002\/ajh.26826","article-title":"Orelabrutinib in relapsed or refractory chronic lymphocytic leukemia\/small lymphocytic lymphoma patients: Multi-center, single-arm, open-label, phase 2 study","volume":"98","author":"Xu","year":"2023","journal-title":"Am. J. Hematol."},{"key":"10.1016\/j.phrs.2023.106847_bib124","doi-asserted-by":"crossref","first-page":"887","DOI":"10.1007\/s40265-019-01131-y","article-title":"Peficitinib: first global approval","volume":"79","author":"Markham","year":"2019","journal-title":"Drugs"},{"key":"10.1016\/j.phrs.2023.106847_bib125","doi-asserted-by":"crossref","first-page":"4971","DOI":"10.1016\/j.bmc.2018.08.005","article-title":"Discovery and structural characterization of peficitinib (ASP015K) as a novel and potent JAK inhibitor","volume":"26","author":"Hamaguchi","year":"2018","journal-title":"Bioorg. Med Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib126","doi-asserted-by":"crossref","first-page":"333","DOI":"10.1080\/13543784.2023.2199919","article-title":"JAK inhibitors for rheumatoid arthritis","volume":"32","author":"Kubo","year":"2023","journal-title":"Expert Opin. Invest. Drugs"},{"key":"10.1016\/j.phrs.2023.106847_bib127","doi-asserted-by":"crossref","first-page":"727","DOI":"10.1007\/s40265-021-01489-y","article-title":"Surufatinib: first approval","volume":"81","author":"Syed","year":"2021","journal-title":"Drugs"},{"key":"10.1016\/j.phrs.2023.106847_bib128","doi-asserted-by":"crossref","DOI":"10.1177\/17588359211042689","article-title":"Current treatments and future potential of surufatinib in neuroendocrine tumors (NETs)","volume":"13","author":"Xu","year":"2021","journal-title":"Ther. Adv. Med Oncol."},{"key":"10.1016\/j.phrs.2023.106847_bib129","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2019.104567","article-title":"The role of fibroblast growth factor receptor (FGFR) protein-tyrosine kinase inhibitors in the treatment of cancers including those of the urinary bladder","volume":"151","author":"Roskoski","year":"2020","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib130","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2022.106566","article-title":"Targeting CSF-1R represents an effective strategy in modulating inflammatory diseases","volume":"187","author":"Xiang","year":"2023","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib131","doi-asserted-by":"crossref","DOI":"10.3892\/ol.2023.13859","article-title":"Efficacy and safety of surufatinib in the treatment of advanced solid tumors: a systematic evaluation and meta\u2011analysis","volume":"25","author":"Cai","year":"2023","journal-title":"Oncol. Lett."},{"key":"10.1016\/j.phrs.2023.106847_bib132","doi-asserted-by":"crossref","DOI":"10.1111\/jne.13149","article-title":"Efficacy and toxicity of surufatinib in neuroendocrine tumors: A systematic review and meta-analysis","volume":"34","author":"Ali","year":"2022","journal-title":"J. Neuroendocr."},{"key":"10.1016\/j.phrs.2023.106847_bib133","doi-asserted-by":"crossref","first-page":"1665","DOI":"10.1007\/s40265-021-01584-0","article-title":"Savolitinib: first approval","volume":"81","author":"Markham","year":"2021","journal-title":"Drugs"},{"key":"10.1016\/j.phrs.2023.106847_bib134","doi-asserted-by":"crossref","first-page":"254","DOI":"10.1016\/j.lungcan.2023.02.018","article-title":"MET alterations in advanced non-small cell lung cancer","volume":"178","author":"Sakamoto","year":"2023","journal-title":"Lung Cancer"},{"issue":"4","key":"10.1016\/j.phrs.2023.106847_bib135","doi-asserted-by":"crossref","DOI":"10.1200\/PO.19.00386","article-title":"Mechanisms of acquired resistance to savolitinib, a selective MET inhibitor in MET-amplified gastric cancer","author":"Frigault","year":"2020","journal-title":"JCO Precis Oncol."},{"key":"10.1016\/j.phrs.2023.106847_bib136","doi-asserted-by":"crossref","first-page":"17","DOI":"10.1358\/dot.2023.59.1.3425324","article-title":"Savolitinib for non-small cell lung cancer","volume":"59","author":"Zaborowska-Szmi","year":"2023","journal-title":"Drugs Today"},{"key":"10.1016\/j.phrs.2023.106847_bib137","doi-asserted-by":"crossref","first-page":"6122","DOI":"10.3390\/cancers14246122","article-title":"Landscape of savolitinib development for the treatment of non-small cell lung cancer with MET alteration-a narrative review","volume":"14","author":"Zhu","year":"2022","journal-title":"Cancers (Basel)"},{"issue":"9","key":"10.1016\/j.phrs.2023.106847_bib138","doi-asserted-by":"crossref","first-page":"1107","DOI":"10.1007\/s40265-021-01533-x","article-title":"Lazertinib: first approval","volume":"81","author":"Dhillon","year":"2021","journal-title":"Drugs"},{"key":"10.1016\/j.phrs.2023.106847_bib139","doi-asserted-by":"crossref","first-page":"2575","DOI":"10.1158\/1078-0432.CCR-18-2906","article-title":"YH25448, an irreversible EGFR-TKI with potent intracranial activity in EGFR mutant non-small cell lung cancer","volume":"25","author":"Yun","year":"2019","journal-title":"Clin. Cancer Res"},{"key":"10.1016\/j.phrs.2023.106847_bib140","doi-asserted-by":"crossref","first-page":"1775","DOI":"10.1007\/s40265-021-01588-w","article-title":"Furmonertinib: first approval","volume":"81","author":"Deeks","year":"2021","journal-title":"Drugs"},{"key":"10.1016\/j.phrs.2023.106847_bib141","doi-asserted-by":"crossref","first-page":"1144","DOI":"10.1016\/j.jtho.2022.08.016","article-title":"And still they come over troubled waters: Can Asia's third-generation EGFR tyrosine kinase inhibitors (furmonertinib, aumolertinib, rezivertinib, limertinib, befotertinib, sh-1028, and lazertinib) affect global treatment of EGFR+ NSCLC","volume":"17","author":"Lau","year":"2022","journal-title":"J. Thorac. Oncol."},{"key":"10.1016\/j.phrs.2023.106847_bib142","doi-asserted-by":"crossref","first-page":"3","DOI":"10.1016\/S0169-409X(00)00129-0","article-title":"Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings","volume":"46","author":"Lipinski","year":"2001","journal-title":"Adv. Drug Deliv. Rev."},{"key":"10.1016\/j.phrs.2023.106847_bib143","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2023.106774","article-title":"Rule of five violations among the FDA-approved small molecule protein kinase inhibitors","volume":"191","author":"Roskoski","year":"2023","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib144","doi-asserted-by":"crossref","first-page":"430","DOI":"10.1016\/S1359-6446(04)03069-7","article-title":"Ligand efficiency: a useful metric for lead selection","volume":"9","author":"Hopkins","year":"2004","journal-title":"Drug Discov. Today"},{"key":"10.1016\/j.phrs.2023.106847_bib145","doi-asserted-by":"crossref","first-page":"881","DOI":"10.1038\/nrd2445","article-title":"The influence of drug-like concepts on decision-making in medicinal chemistry","volume":"6","author":"Leeson","year":"2007","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.phrs.2023.106847_bib146","doi-asserted-by":"crossref","first-page":"194","DOI":"10.1007\/s11095-015-1779-y","article-title":"Thermodynamic proxies to compensate for biases in drug discovery methods","volume":"33","author":"Ekins","year":"2016","journal-title":"Pharm. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib147","doi-asserted-by":"crossref","first-page":"105","DOI":"10.1038\/nrd4163","article-title":"The role of ligand efficiency metrics in drug discovery","volume":"13","author":"Hopkins","year":"2014","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.phrs.2023.106847_bib148","doi-asserted-by":"crossref","first-page":"22","DOI":"10.1016\/j.addr.2016.01.018","article-title":"Molecular inflation, attrition, and the rule of five.","volume":"101","author":"Leeson","year":"2016","journal-title":"Adv. Drug Deliv. Rev."},{"key":"10.1016\/j.phrs.2023.106847_bib149","doi-asserted-by":"crossref","first-page":"2615","DOI":"10.1021\/jm020017n","article-title":"Molecular properties that influence the oral bioavailability of drug candidates","volume":"45","author":"Veber","year":"2002","journal-title":"J. Med Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib150","doi-asserted-by":"crossref","first-page":"251","DOI":"10.1023\/A:1008130001697","article-title":"Property distribution of drug-related chemical databases","volume":"14","author":"Oprea","year":"2000","journal-title":"J. Comput. Aided Mol. Des."},{"key":"10.1016\/j.phrs.2023.106847_bib151","doi-asserted-by":"crossref","first-page":"7210","DOI":"10.1021\/acs.jmedchem.1c00416","article-title":"Target-based evaluation of \"drug-like\" properties and ligand efficiencies","volume":"64","author":"Leeson","year":"2021","journal-title":"J. Med Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib152","doi-asserted-by":"crossref","first-page":"6401","DOI":"10.1021\/acs.jmedchem.8b00077","article-title":"Lipophilic efficiency as an important metric in drug design","volume":"61","author":"Johnson","year":"2018","journal-title":"J. Med Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib153","doi-asserted-by":"crossref","first-page":"7206","DOI":"10.1021\/jm500515d","article-title":"Physicochemical descriptors of aromatic character and their use in drug discovery","volume":"57","author":"Ritchie","year":"2014","journal-title":"J. Med Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib154","first-page":"3559","article-title":"The first general index of molecular complexity","volume":"1103","author":"Bertz","year":"1981","journal-title":"J. Am. Chem. Soc."},{"key":"10.1016\/j.phrs.2023.106847_bib155","doi-asserted-by":"crossref","first-page":"63","DOI":"10.1021\/ci00054a004","article-title":"Molecular complexity: a simplified formula adapted to individual atoms","volume":"27","author":"Hendrickson","year":"1987","journal-title":"J. Chem. Inf. Compout Sci."},{"key":"10.1016\/j.phrs.2023.106847_bib156","doi-asserted-by":"crossref","first-page":"6752","DOI":"10.1021\/jm901241e","article-title":"Escape from flatland: increasing saturation as an approach to improving clinical success","volume":"52","author":"Lovering","year":"2009","journal-title":"J. Med Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib157","doi-asserted-by":"crossref","first-page":"2312","DOI":"10.1021\/acs.jmedchem.5b01286","article-title":"How beyond rule of 5 drugs and clinical candidates bind to their targets","volume":"59","author":"Doak","year":"2016","journal-title":"J. Med Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib158","doi-asserted-by":"crossref","DOI":"10.1186\/s13045-020-00977-0","article-title":"Tyrosine kinase inhibitors for solid tumors in the past 20 years (2001-2020)","volume":"13","author":"Huang","year":"2020","journal-title":"J. Hematol. Oncol."},{"key":"10.1016\/j.phrs.2023.106847_bib159","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2019.104392","article-title":"The new entries in the therapeutic armamentarium: The small molecule JAK inhibitors","volume":"147","author":"Bechman","year":"2019","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib160","unstructured":"Bechman K., Galloway G.B., Winthrop K.L. Small-molecule protein kinase inhibitors and the risk of fungal infections. Curr Fungal Infect Rep. 10.1007\/s12281\u2013019-00350-w."},{"key":"10.1016\/j.phrs.2023.106847_bib161","doi-asserted-by":"crossref","first-page":"566","DOI":"10.3390\/ijms22020566","article-title":"The kinase chemogenomic set (KCGS): an open science resource for kinase vulnerability identification","volume":"22","author":"Wells","year":"2021","journal-title":"Int J. Mol. Sci."},{"key":"10.1016\/j.phrs.2023.106847_bib162","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2020.105412","article-title":"Posttranslational modifications as therapeutic targets for intestinal disorders","author":"Choo","year":"2021","journal-title":"Pharmacol. Res"},{"key":"10.1016\/j.phrs.2023.106847_bib163","doi-asserted-by":"crossref","first-page":"1283","DOI":"10.1021\/acs.jmedchem.0c01511","article-title":"Small-molecule kinase inhibitors for the treatment of nononcologic diseases","volume":"64","author":"Xie","year":"2021","journal-title":"J. Med Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib164","doi-asserted-by":"crossref","DOI":"10.1038\/s41467-021-23165-1","article-title":"Crowdsourced mapping of unexplored target space of kinase inhibitors","volume":"12","author":"Cicho\u0144ska","year":"2021","journal-title":"Nat. Commun."},{"key":"10.1016\/j.phrs.2023.106847_bib165","doi-asserted-by":"crossref","first-page":"13764","DOI":"10.1002\/anie.201914525","article-title":"New promise and opportunities for allosteric kinase inhibitors","volume":"59","author":"Lu","year":"2020","journal-title":"Angew. Chem. Int Ed. Engl."},{"key":"10.1016\/j.phrs.2023.106847_bib166","doi-asserted-by":"crossref","first-page":"1615","DOI":"10.1021\/acs.jctc.2c01171","article-title":"Strategy toward kinase-selective drug discovery","volume":"19","author":"Zhang","year":"2023","journal-title":"J. Chem. Theory Comput."},{"key":"10.1016\/j.phrs.2023.106847_bib167","doi-asserted-by":"crossref","first-page":"188","DOI":"10.1038\/nrd3368","article-title":"Impact of high-throughput screening in biomedical research","volume":"10","author":"Macarron","year":"2011","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.phrs.2023.106847_bib168","doi-asserted-by":"crossref","DOI":"10.1038\/s41570-022-00451-0","article-title":"Rules were made to be broken","author":"Hartung","year":"2023","journal-title":"Nat. Rev. Chem."},{"key":"10.1016\/j.phrs.2023.106847_bib169","doi-asserted-by":"crossref","first-page":"240","DOI":"10.1016\/j.phrs.2017.02.005","article-title":"Guidelines for preparing color figures for everyone including the colorblind","volume":"119","author":"Roskoski","year":"2017","journal-title":"Pharmacol. Res"}],"container-title":["Pharmacological Research"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S1043661823002037?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S1043661823002037?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2025,10,19]],"date-time":"2025-10-19T22:47:21Z","timestamp":1760914041000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S1043661823002037"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2023,8]]},"references-count":169,"alternative-id":["S1043661823002037"],"URL":"https:\/\/doi.org\/10.1016\/j.phrs.2023.106847","relation":{},"ISSN":["1043-6618"],"issn-type":[{"value":"1043-6618","type":"print"}],"subject":[],"published":{"date-parts":[[2023,8]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Small molecule protein kinase inhibitors approved by regulatory agencies outside of the United States","name":"articletitle","label":"Article Title"},{"value":"Pharmacological Research","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.phrs.2023.106847","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2023 The Author. Published by Elsevier Ltd.","name":"copyright","label":"Copyright"}],"article-number":"106847"}}