{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,27]],"date-time":"2026-10-27T15:53:33Z","timestamp":1793116413924,"version":"4.5.0"},"reference-count":93,"publisher":"Elsevier BV","issue":"3","license":[{"start":{"date-parts":[[2025,3,1]],"date-time":"2025-03-01T00:00:00Z","timestamp":1740787200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2025,3,1]],"date-time":"2025-03-01T00:00:00Z","timestamp":1740787200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2025,3,1]],"date-time":"2025-03-01T00:00:00Z","timestamp":1740787200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-017"},{"start":{"date-parts":[[2025,3,1]],"date-time":"2025-03-01T00:00:00Z","timestamp":1740787200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-037"},{"start":{"date-parts":[[2025,3,1]],"date-time":"2025-03-01T00:00:00Z","timestamp":1740787200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-012"},{"start":{"date-parts":[[2025,3,1]],"date-time":"2025-03-01T00:00:00Z","timestamp":1740787200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-029"},{"start":{"date-parts":[[2025,3,1]],"date-time":"2025-03-01T00:00:00Z","timestamp":1740787200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-004"}],"funder":[{"DOI":"10.13039\/501100017668","name":"Anhui Provincial Key Research and Development Plan","doi-asserted-by":"publisher","award":["2022i01020004"],"award-info":[{"award-number":["2022i01020004"]}],"id":[{"id":"10.13039\/501100017668","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100003995","name":"Natural Science Foundation of Anhui Province","doi-asserted-by":"publisher","award":["2308085MH310"],"award-info":[{"award-number":["2308085MH310"]}],"id":[{"id":"10.13039\/501100003995","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100003995","name":"Natural Science Foundation of Anhui Province","doi-asserted-by":"publisher","award":["2408085MH192"],"award-info":[{"award-number":["2408085MH192"]}],"id":[{"id":"10.13039\/501100003995","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["bmn.com","elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["Drug Discovery Today"],"published-print":{"date-parts":[[2025,3]]},"DOI":"10.1016\/j.drudis.2025.104318","type":"journal-article","created":{"date-parts":[[2025,2,20]],"date-time":"2025-02-20T18:36:41Z","timestamp":1740076601000},"page":"104318","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":24,"title":["Drugs targeting peroxisome proliferator-activated receptors"],"prefix":"10.1016","volume":"30","author":[{"given":"Zhouling","family":"Xie","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jiwei","family":"Xin","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chuping","family":"Huang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7080-1768","authenticated-orcid":false,"given":"Chenzhong","family":"Liao","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"key":"10.1016\/j.drudis.2025.104318_b0005","doi-asserted-by":"crossref","first-page":"1143","DOI":"10.1007\/s40265-024-02075-8","article-title":"Elafibranor: first approval","volume":"84","author":"Blair","year":"2024","journal-title":"Drugs"},{"key":"10.1016\/j.drudis.2025.104318_b0010","doi-asserted-by":"crossref","first-page":"1487","DOI":"10.1007\/s40265-024-02114-4","article-title":"Seladelpar: first approval","volume":"84","author":"Hoy","year":"2024","journal-title":"Drugs"},{"key":"10.1016\/j.drudis.2025.104318_b0015","doi-asserted-by":"crossref","first-page":"4027","DOI":"10.1021\/jm101360s","article-title":"Targeting peroxisome proliferator-activated receptors (PPARs): development of modulators","volume":"55","author":"Pirat","year":"2012","journal-title":"J Med Chem"},{"key":"10.1016\/j.drudis.2025.104318_b0020","doi-asserted-by":"crossref","DOI":"10.1155\/2013\/549627","article-title":"Peroxisome proliferator-activated receptor targets for the treatment of metabolic diseases","volume":"2013","author":"Monsalve","year":"2013","journal-title":"Mediators Inflamm"},{"key":"10.1016\/j.drudis.2025.104318_b0025","doi-asserted-by":"crossref","first-page":"83","DOI":"10.1080\/13543776.2024.2332661","article-title":"Peroxisome proliferator-activated receptor agonists and antagonists: an updated patent review (2020-2023)","volume":"34","author":"De Filippis","year":"2024","journal-title":"Expert Opin Ther Pat"},{"key":"10.1016\/j.drudis.2025.104318_b0030","doi-asserted-by":"crossref","first-page":"947","DOI":"10.1111\/cbdd.14020","article-title":"A new insight into the treatment of diabetes by means of pan PPAR agonists","volume":"100","author":"Chandra","year":"2022","journal-title":"Chem Biol Drug Des"},{"key":"10.1016\/j.drudis.2025.104318_b0035","doi-asserted-by":"crossref","first-page":"14","DOI":"10.1186\/1475-2840-4-14","article-title":"Dual and pan-peroxisome proliferator-activated receptors (PPAR) co-agonism: the bezafibrate lessons","volume":"4","author":"Tenenbaum","year":"2005","journal-title":"Cardiovasc Diabetol"},{"key":"10.1016\/j.drudis.2025.104318_b0040","doi-asserted-by":"crossref","first-page":"809","DOI":"10.1038\/s41569-021-00569-6","article-title":"PPAR control of metabolism and cardiovascular functions","volume":"18","author":"Montaigne","year":"2021","journal-title":"Nat Rev Cardiol"},{"key":"10.1016\/j.drudis.2025.104318_b0045","doi-asserted-by":"crossref","first-page":"39","DOI":"10.1007\/978-3-030-11488-6_3","article-title":"Understanding peroxisome proliferator-activated receptors: from the structure to the regulatory actions on metabolism","volume":"1127","author":"Lamas Bervejillo","year":"2019","journal-title":"Adv Exp Med Biol"},{"key":"10.1016\/j.drudis.2025.104318_b0050","doi-asserted-by":"crossref","first-page":"2367","DOI":"10.3390\/cells9112367","article-title":"The role of PPARs in disease","volume":"9","author":"Wagner","year":"2020","journal-title":"Cells"},{"key":"10.1016\/j.drudis.2025.104318_b0055","doi-asserted-by":"crossref","first-page":"1572","DOI":"10.3390\/cells12121572","article-title":"Recent insights into the role of PPARs in disease","volume":"12","author":"Wagner","year":"2023","journal-title":"Cells"},{"key":"10.1016\/j.drudis.2025.104318_b0060","doi-asserted-by":"crossref","first-page":"5055","DOI":"10.3390\/ijms20205055","article-title":"Exploration and development of PPAR modulators in health and disease: an update of clinical evidence","volume":"20","author":"Cheng","year":"2019","journal-title":"Int J Mol Sci"},{"key":"10.1016\/j.drudis.2025.104318_b0065","doi-asserted-by":"crossref","first-page":"409","DOI":"10.1146\/annurev.med.53.082901.104018","article-title":"The mechanisms of action of PPARs","volume":"53","author":"Berger","year":"2002","journal-title":"Annu Rev Med"},{"key":"10.1016\/j.drudis.2025.104318_b0070","doi-asserted-by":"crossref","first-page":"571","DOI":"10.1172\/JCI27989","article-title":"Sorting out the roles of PPAR\u03b1 in energy metabolism and vascular homeostasis","volume":"116","author":"Lefebvre","year":"2006","journal-title":"J Clin Invest"},{"key":"10.1016\/j.drudis.2025.104318_b0075","doi-asserted-by":"crossref","first-page":"2046","DOI":"10.1111\/brv.12320","article-title":"PPARs in the central nervous system: roles in neurodegeneration and neuroinflammation","volume":"92","author":"Zolezzi","year":"2017","journal-title":"Biol Rev Camb Philos Soc"},{"key":"10.1016\/j.drudis.2025.104318_b0080","doi-asserted-by":"crossref","DOI":"10.3389\/fendo.2022.1074911","article-title":"PPAR\u03b1: an emerging target of metabolic syndrome, neurodegenerative and cardiovascular diseases","volume":"13","author":"Lin","year":"2022","journal-title":"Front Endocrinol (Lausanne)"},{"key":"10.1016\/j.drudis.2025.104318_b0085","doi-asserted-by":"crossref","first-page":"75","DOI":"10.1016\/j.biochi.2016.12.019","article-title":"The role and regulation of the peroxisome proliferator activated receptor \u03b1 in human liver","volume":"136","author":"Kersten","year":"2017","journal-title":"Biochimie"},{"key":"10.1016\/j.drudis.2025.104318_b0090","doi-asserted-by":"crossref","first-page":"542","DOI":"10.1038\/ncpcardio1278","article-title":"Fibrates and future PPAR\u03b1 agonists in the treatment of cardiovascular disease","volume":"5","author":"Staels","year":"2008","journal-title":"Nat Clin Pract Cardiovasc Med"},{"key":"10.1016\/j.drudis.2025.104318_b0095","doi-asserted-by":"crossref","first-page":"855","DOI":"10.1056\/NEJMe2313802","article-title":"PPAR agonists in primary biliary cholangitis","volume":"390","author":"Schnabl","year":"2024","journal-title":"N Engl J Med"},{"key":"10.1016\/j.drudis.2025.104318_b0100","doi-asserted-by":"crossref","first-page":"9","DOI":"10.1016\/j.tips.2023.11.004","article-title":"PPAR agonists for the treatment of neuroinflammatory diseases","volume":"45","author":"Titus","year":"2024","journal-title":"Trends Pharmacol Sci"},{"key":"10.1016\/j.drudis.2025.104318_b0105","doi-asserted-by":"crossref","first-page":"2086","DOI":"10.1002\/med.21970","article-title":"Molecular mechanisms and therapeutic perspectives of peroxisome proliferator-activated receptor \u03b1 agonists in cardiovascular health and disease","volume":"43","author":"Pu","year":"2023","journal-title":"Med Res Rev"},{"key":"10.1016\/j.drudis.2025.104318_b0110","unstructured":"Tempest Therapeutics. Pipeline | TPST-1120 | TPST-1495 | TREX\u20131 |. https:\/\/www.tempesttx.com\/pipeline. Accessed February 18, 2025."},{"key":"10.1016\/j.drudis.2025.104318_b0115","doi-asserted-by":"crossref","first-page":"37731","DOI":"10.1074\/jbc.R100034200","article-title":"PPAR\u03b3: a nuclear regulator of metabolism, differentiation, and cell growth","volume":"276","author":"Rosen","year":"2001","journal-title":"J Biol Chem"},{"key":"10.1016\/j.drudis.2025.104318_b0120","doi-asserted-by":"crossref","first-page":"557","DOI":"10.1038\/nm.3159","article-title":"PPAR\u03b3 signaling and metabolism: the good, the bad and the future","volume":"19","author":"Ahmadian","year":"2013","journal-title":"Nat Med"},{"key":"10.1016\/j.drudis.2025.104318_b0125","doi-asserted-by":"crossref","first-page":"391","DOI":"10.1038\/nature13887","article-title":"An ERK\/Cdk5 axis controls the diabetogenic actions of PPAR\u03b3","volume":"517","author":"Banks","year":"2015","journal-title":"Nature"},{"key":"10.1016\/j.drudis.2025.104318_b0130","doi-asserted-by":"crossref","first-page":"15","DOI":"10.1517\/14740330802597821","article-title":"How safe is the use of thiazolidinediones in clinical practice?","volume":"8","author":"Rizos","year":"2009","journal-title":"Expert Opin Drug Saf"},{"key":"10.1016\/j.drudis.2025.104318_b0135","doi-asserted-by":"crossref","first-page":"1272","DOI":"10.1038\/s41423-020-0394-y","article-title":"GED-0507 is a novel potential antifibrotic treatment option for pulmonary fibrosis","volume":"17","author":"Speca","year":"2020","journal-title":"Cell Mol Immunol"},{"key":"10.1016\/j.drudis.2025.104318_b0140","unstructured":"Medibiofarma. MBF 118. https:\/\/medibiofarma.com\/mbf-118. Accessed February 18, 2025."},{"key":"10.1016\/j.drudis.2025.104318_b0145","unstructured":"ClinicalTrials.gov. Study Details | Safety and Efficacy of MBF-118 in Patients with Crohn Disease. https:\/\/www.clinicaltrials.gov\/study\/NCT05940558. Accessed February 18, 2025."},{"key":"10.1016\/j.drudis.2025.104318_b0150","doi-asserted-by":"crossref","first-page":"3339","DOI":"10.3390\/ijms19113339","article-title":"The role of PPAR-\u03b4 in metabolism, inflammation, and cancer: many characters of a critical transcription Factor","volume":"19","author":"Liu","year":"2018","journal-title":"Int J Mol Sci"},{"key":"10.1016\/j.drudis.2025.104318_b0155","doi-asserted-by":"crossref","first-page":"451","DOI":"10.1016\/B978-0-12-800101-1.00014-4","article-title":"The role of PPAR\u03b4 signaling in the cardiovascular system","volume":"121","author":"Ding","year":"2014","journal-title":"Prog Mol Biol Transl Sci"},{"key":"10.1016\/j.drudis.2025.104318_b0160","doi-asserted-by":"crossref","DOI":"10.1016\/j.jtauto.2023.100188","article-title":"PPAR agonists for the treatment of primary biliary cholangitis: old and new tales","volume":"6","author":"Colapietro","year":"2023","journal-title":"J Transl Autoimmun"},{"key":"10.1016\/j.drudis.2025.104318_b0165","doi-asserted-by":"crossref","first-page":"10109","DOI":"10.1021\/acs.jmedchem.9b01882","article-title":"Targeting peroxisome proliferator-activated receptor delta (PPAR\u03b4): a medicinal chemistry perspective","volume":"63","author":"Kadayat","year":"2020","journal-title":"J Med Chem"},{"key":"10.1016\/j.drudis.2025.104318_b0170","doi-asserted-by":"crossref","first-page":"514","DOI":"10.1097\/FJC.0000000000000891","article-title":"The glitazars paradox: cardiotoxicity of the metabolically beneficial dual PPAR\u03b1 and PPAR\u03b3 activation","volume":"76","author":"Kalliora","year":"2020","journal-title":"J Cardiovasc Pharmacol"},{"key":"10.1016\/j.drudis.2025.104318_b0175","doi-asserted-by":"crossref","first-page":"195","DOI":"10.2174\/1874467212666190111165015","article-title":"A contemporary overview of PPAR\u03b1\/\u03b3 dual agonists for the management of diabetic dyslipidemia","volume":"12","author":"Balakumar","year":"2019","journal-title":"Curr Mol Pharmacol"},{"key":"10.1016\/j.drudis.2025.104318_b0180","doi-asserted-by":"crossref","first-page":"7331","DOI":"10.1021\/acs.jmedchem.2c02123","article-title":"Discovery of the first subnanomolar PPAR\u03b1\/\u03b4 dual agonist for the treatment of cholestatic liver diseases","volume":"66","author":"Feng","year":"2023","journal-title":"J Med Chem"},{"key":"10.1016\/j.drudis.2025.104318_b0185","doi-asserted-by":"crossref","first-page":"2571","DOI":"10.1021\/acs.jmedchem.1c02002","article-title":"Design, synthesis, and biological evaluation of triazolone derivatives as potent PPAR\u03b1\/\u03b4 dual agonists for the treatment of nonalcoholic steatohepatitis","volume":"65","author":"Feng","year":"2022","journal-title":"J Med Chem"},{"key":"10.1016\/j.drudis.2025.104318_b0190","doi-asserted-by":"crossref","first-page":"873","DOI":"10.1016\/j.bmcl.2012.11.060","article-title":"Design, development and evaluation of novel dual PPAR\u03b4\/PPAR\u03b3 agonists","volume":"23","author":"Gathiaka","year":"2013","journal-title":"Bioorg Med Chem Lett"},{"key":"10.1016\/j.drudis.2025.104318_b0195","unstructured":"T3D Therapeutics. Lead Product Candidate T3D-959. www.t3dtherapeutics.com\/lead-product-candidate-t3d-959\/. Accessed February 18, 2025."},{"key":"10.1016\/j.drudis.2025.104318_b0200","doi-asserted-by":"crossref","DOI":"10.1016\/j.diabres.2024.111688","article-title":"MASLD\/MASH and type 2 diabetes: two sides of the same coin? From single PPAR to pan-PPAR agonists","volume":"212","author":"Cooreman","year":"2024","journal-title":"Diabetes Res Clin Pract"},{"key":"10.1016\/j.drudis.2025.104318_b0205","doi-asserted-by":"crossref","first-page":"2246","DOI":"10.1021\/acs.jmedchem.7b01285","article-title":"Design, synthesis, and evaluation of a novel series of indole sulfonamide peroxisome proliferator activated receptor (PPAR) \u03b1\/\u03b3\/\u03b4 triple activators: discovery of lanifibranor, a new antifibrotic clinical candidate","volume":"61","author":"Boubia","year":"2018","journal-title":"J Med Chem"},{"key":"10.1016\/j.drudis.2025.104318_b0210","doi-asserted-by":"crossref","first-page":"1547","DOI":"10.1056\/NEJMoa2036205","article-title":"A randomized, controlled trial of the pan-PPAR agonist lanifibranor in NASH","volume":"385","author":"Francque","year":"2021","journal-title":"N Engl J Med"},{"key":"10.1016\/j.drudis.2025.104318_b0215","doi-asserted-by":"crossref","first-page":"352","DOI":"10.3390\/cells9020352","article-title":"PPAR-mediated toxicology and applied pharmacology","volume":"9","author":"Xi","year":"2020","journal-title":"Cells"},{"key":"10.1016\/j.drudis.2025.104318_b0220","doi-asserted-by":"crossref","first-page":"2189","DOI":"10.3390\/ijms19082189","article-title":"The opportunities and challenges of peroxisome proliferator-activated receptors ligands in clinical drug discovery and development","volume":"19","author":"Hong","year":"2018","journal-title":"Int J Mol Sci"},{"key":"10.1016\/j.drudis.2025.104318_b0225","doi-asserted-by":"crossref","first-page":"357","DOI":"10.1016\/j.freeradbiomed.2015.11.033","article-title":"PPAR-pan activation induces hepatic oxidative stress and lipidomic remodelling","volume":"95","author":"Ament","year":"2016","journal-title":"Free Radic Biol Med"},{"key":"10.1016\/j.drudis.2025.104318_b0230","doi-asserted-by":"crossref","first-page":"125","DOI":"10.1186\/1475-2840-11-125","article-title":"Fibrates are an essential part of modern anti-dyslipidemic arsenal: spotlight on atherogenic dyslipidemia and residual risk reduction","volume":"11","author":"Tenenbaum","year":"2012","journal-title":"Cardiovasc Diabetol"},{"key":"10.1016\/j.drudis.2025.104318_b0235","doi-asserted-by":"crossref","first-page":"507","DOI":"10.1038\/nrendo.2009.151","article-title":"Myopathy with statin-fibrate combination therapy: clinical considerations","volume":"5","author":"Jacobson","year":"2009","journal-title":"Nat Rev Endocrinol"},{"key":"10.1016\/j.drudis.2025.104318_b0240","doi-asserted-by":"crossref","first-page":"82","DOI":"10.1186\/1475-2840-12-82","article-title":"Selective peroxisome proliferator-activated receptor \u03b1 modulators (SPPARM\u03b1): the next generation of peroxisome proliferator-activated receptor \u03b1-agonists","volume":"12","author":"Fruchart","year":"2013","journal-title":"Cardiovasc Diabetol"},{"key":"10.1016\/j.drudis.2025.104318_b0245","doi-asserted-by":"crossref","first-page":"1129","DOI":"10.1016\/S0140-6736(07)61514-1","article-title":"Congestive heart failure and cardiovascular death in patients with prediabetes and type 2 diabetes given thiazolidinediones: a meta-analysis of randomised clinical trials","volume":"370","author":"Lago","year":"2007","journal-title":"Lancet"},{"key":"10.1016\/j.drudis.2025.104318_b0250","unstructured":"ClinicalTrials.gov. Study Details | RECORD: Rosiglitazone Evaluated for Cardiac Outcomes and Regulation of Glycaemia in Diabetes. www.clinicaltrials.gov\/study\/NCT00379769. Accessed February 18, 2025."},{"key":"10.1016\/j.drudis.2025.104318_b0255","doi-asserted-by":"crossref","first-page":"194","DOI":"10.1210\/er.2012-1042","article-title":"The impact of diabetes and diabetes medications on bone health","volume":"36","author":"Gilbert","year":"2015","journal-title":"Endocr Rev"},{"key":"10.1016\/j.drudis.2025.104318_b0260","doi-asserted-by":"crossref","first-page":"162","DOI":"10.1016\/j.cbi.2018.09.019","article-title":"New insights into molecular mechanisms of rosiglitazone in monotherapy or combination therapy against cancers","volume":"296","author":"Dang","year":"2018","journal-title":"Chem Biol Interact"},{"key":"10.1016\/j.drudis.2025.104318_b0265","doi-asserted-by":"crossref","DOI":"10.1136\/bmjdrc-2016-000364","article-title":"Pioglitazone and risk of mortality in patients with type 2 diabetes: results from a European multidatabase cohort study","volume":"5","author":"Strongman","year":"2017","journal-title":"BMJ Open Diabetes Res Care"},{"key":"10.1016\/j.drudis.2025.104318_b0270","doi-asserted-by":"crossref","first-page":"705","DOI":"10.1007\/s13300-017-0273-4","article-title":"Pioglitazone and the risk of bladder cancer: a meta-analysis","volume":"8","author":"Filipova","year":"2017","journal-title":"Diabetes Ther"},{"key":"10.1016\/j.drudis.2025.104318_b0275","doi-asserted-by":"crossref","first-page":"1106","DOI":"10.1056\/NEJMra041001","article-title":"Thiazolidinediones","volume":"351","author":"Yki-J\u00e4rvinen","year":"2004","journal-title":"N Engl J Med"},{"key":"10.1016\/j.drudis.2025.104318_b0280","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1007\/s40265-023-01979-1","article-title":"New therapies on the horizon for primary biliary cholangitis","volume":"84","author":"Tanaka","year":"2024","journal-title":"Drugs"},{"key":"10.1016\/j.drudis.2025.104318_b0285","doi-asserted-by":"crossref","first-page":"1101","DOI":"10.1080\/13543784.2022.2130750","article-title":"Seladelpar: an investigational drug for the treatment of early-stage primary biliary cholangitis (PBC)","volume":"31","author":"Wetten","year":"2022","journal-title":"Expert Opin Investig Drugs"},{"key":"10.1016\/j.drudis.2025.104318_b0290","doi-asserted-by":"crossref","first-page":"783","DOI":"10.1056\/NEJMoa2312100","article-title":"A phase 3 trial of seladelpar in primary biliary cholangitis","volume":"390","author":"Hirschfield","year":"2024","journal-title":"N Engl J Med"},{"key":"10.1016\/j.drudis.2025.104318_b0295","doi-asserted-by":"crossref","first-page":"795","DOI":"10.1056\/NEJMoa2306185","article-title":"Efficacy and safety of elafibranor in primary biliary cholangitis","volume":"390","author":"Kowdley","year":"2024","journal-title":"N Engl J Med"},{"key":"10.1016\/j.drudis.2025.104318_b0300","unstructured":"ClinicalTrials.gov. Study Details | A Study to Assess Safety and Effectiveness of Elafibranor in Adult Participants With Primary Sclerosing Cholangitis. www.clinicaltrials.gov\/study\/NCT05627362. Accessed February 18, 2025."},{"key":"10.1016\/j.drudis.2025.104318_b0305","unstructured":"ClinicalTrials.gov. Study Details | Phase 3 Study to Evaluate the Efficacy and Safety of Elafibranor Versus Placebo in Patients With Nonalcoholic Steatohepatitis (NASH). www.clinicaltrials.gov\/study\/NCT02704403. Accessed February 18, 2025."},{"key":"10.1016\/j.drudis.2025.104318_b0310","doi-asserted-by":"crossref","first-page":"890","DOI":"10.1007\/s11596-023-2760-3","article-title":"Advances in studies of chiglitazar sodium, a novel PPAR pan-agonist, for the treatment of type 2 diabetes mellitus","volume":"43","author":"Zhang","year":"2023","journal-title":"Curr Med Sci"},{"key":"10.1016\/j.drudis.2025.104318_b0315","doi-asserted-by":"crossref","first-page":"87","DOI":"10.1007\/s40265-021-01648-1","article-title":"Chiglitazar: first approval","volume":"82","author":"Deeks","year":"2022","journal-title":"Drugs"},{"key":"10.1016\/j.drudis.2025.104318_b0320","doi-asserted-by":"crossref","first-page":"1573","DOI":"10.4239\/wjd.v14.i10.1573","article-title":"Indirect comparison of efficacy and safety of chiglitazar and thiazolidinedione in patients with type 2 diabetes: a meta-analysis","volume":"14","author":"Lin","year":"2023","journal-title":"World J Diabetes"},{"key":"10.1016\/j.drudis.2025.104318_b0325","doi-asserted-by":"crossref","DOI":"10.1155\/2012\/546548","article-title":"In vitro and in vivo characterizations of chiglitazar, a newly identified PPAR pan-agonist","volume":"2012","author":"He","year":"2012","journal-title":"PPAR Res"},{"key":"10.1016\/j.drudis.2025.104318_b0330","doi-asserted-by":"crossref","DOI":"10.1155\/2017\/4313561","article-title":"Chiglitazar preferentially regulates gene expression via configuration-restricted binding and phosphorylation inhibition of PPAR\u03b3","volume":"2017","author":"Pan","year":"2017","journal-title":"PPAR Res"},{"key":"10.1016\/j.drudis.2025.104318_b0335","doi-asserted-by":"crossref","first-page":"1571","DOI":"10.1016\/j.scib.2021.03.019","article-title":"Efficacy and safety of chiglitazar, a novel peroxisome proliferator-activated receptor pan-agonist, in patients with type 2 diabetes: a randomized, double-blind, placebo-controlled, Phase III trial (CMAP)","volume":"66","author":"Ji","year":"2021","journal-title":"Sci Bull (Beijing)"},{"key":"10.1016\/j.drudis.2025.104318_b0340","doi-asserted-by":"crossref","first-page":"1581","DOI":"10.1016\/j.scib.2021.02.027","article-title":"Chiglitazar monotherapy with sitagliptin as an active comparator in patients with type 2 diabetes: a randomized, double-blind, Phase III trial (CMAS)","volume":"66","author":"Jia","year":"2021","journal-title":"Sci Bull (Beijing)"},{"key":"10.1016\/j.drudis.2025.104318_b0345","doi-asserted-by":"crossref","first-page":"626","DOI":"10.3390\/metabo13050626","article-title":"Novel selective PPAR\u03b1 modulator pemafibrate for dyslipidemia, nonalcoholic fatty liver disease (NAFLD), and atherosclerosis","volume":"13","author":"Yamashita","year":"2023","journal-title":"Metabolites"},{"key":"10.1016\/j.drudis.2025.104318_b0350","doi-asserted-by":"crossref","first-page":"1805","DOI":"10.1007\/s40265-017-0818-x","article-title":"Pemafibrate: first global approval","volume":"77","author":"Blair","year":"2017","journal-title":"Drugs"},{"key":"10.1016\/j.drudis.2025.104318_b0355","doi-asserted-by":"crossref","first-page":"5","DOI":"10.1007\/s11883-020-0823-5","article-title":"Pemafibrate, a new selective PPAR\u03b1 modulator: drug concept and its clinical applications for dyslipidemia and metabolic diseases","volume":"22","author":"Yamashita","year":"2020","journal-title":"Curr Atheroscler Rep"},{"key":"10.1016\/j.drudis.2025.104318_b0360","doi-asserted-by":"crossref","first-page":"389","DOI":"10.5551\/jat.48918","article-title":"Clinical applications of a novel selective PPAR\u03b1 modulator, pemafibrate, in dyslipidemia and metabolic diseases","volume":"26","author":"Yamashita","year":"2019","journal-title":"J Atheroscler Thromb"},{"key":"10.1016\/j.drudis.2025.104318_b0365","doi-asserted-by":"crossref","first-page":"173","DOI":"10.1016\/j.jacl.2017.10.006","article-title":"Efficacy and safety of pemafibrate (K-877), a selective peroxisome proliferator-activated receptor \u03b1 modulator, in patients with dyslipidemia: results from a 24-week, randomized, double blind, active-controlled, phase III trial","volume":"12","author":"Ishibashi","year":"2018","journal-title":"J Clin Lipidol"},{"key":"10.1016\/j.drudis.2025.104318_b0370","doi-asserted-by":"crossref","first-page":"144","DOI":"10.1016\/j.atherosclerosis.2017.03.032","article-title":"Efficacy and safety of K-877, a novel selective peroxisome proliferator-activated receptor \u03b1 modulator (SPPARM\u03b1), in combination with statin treatment: two randomised, double-blind, placebo-controlled clinical trials in patients with dyslipidaemia","volume":"261","author":"Arai","year":"2017","journal-title":"Atherosclerosis"},{"key":"10.1016\/j.drudis.2025.104318_b0375","doi-asserted-by":"crossref","first-page":"80","DOI":"10.1016\/j.ahj.2018.09.011","article-title":"Rationale and design of the Pemafibrate to Reduce Cardiovascular Outcomes by Reducing Triglycerides in Patients with Diabetes (PROMINENT) study","volume":"206","author":"Pradhan","year":"2018","journal-title":"Am Heart J"},{"key":"10.1016\/j.drudis.2025.104318_b0380","doi-asserted-by":"crossref","first-page":"1923","DOI":"10.1056\/NEJMoa2210645","article-title":"Triglyceride lowering with pemafibrate to reduce cardiovascular risk","volume":"387","author":"Das Pradhan","year":"2022","journal-title":"N Engl J Med"},{"key":"10.1016\/j.drudis.2025.104318_b0385","unstructured":"ClinicalTrials.gov. Study Details | PROMINENT-Eye Ancillary Study (Protocol AD). www.clinicaltrials.gov\/study\/NCT03345901. Accessed February 18, 2025."},{"key":"10.1016\/j.drudis.2025.104318_b0390","doi-asserted-by":"crossref","DOI":"10.1002\/prp2.136","article-title":"Saroglitazar, a novel PPAR\u03b1\/\u03b3 agonist with predominant PPAR\u03b1 activity, shows lipid-lowering and insulin-sensitizing effects in preclinical models","volume":"3","author":"Jain","year":"2015","journal-title":"Pharmacol Res Perspect"},{"key":"10.1016\/j.drudis.2025.104318_b0395","doi-asserted-by":"crossref","DOI":"10.1016\/j.metabol.2024.155912","article-title":"Deciphering the molecular pathways of saroglitazar: a dual PPAR \u03b1\/\u03b3 agonist for managing metabolic NAFLD","volume":"155","author":"Ezhilarasan","year":"2024","journal-title":"Metabolism"},{"key":"10.1016\/j.drudis.2025.104318_b0400","doi-asserted-by":"crossref","first-page":"7706","DOI":"10.1038\/srep07706","article-title":"Observational study of effects of saroglitazar on glycaemic and lipid parameters on Indian patients with type 2 diabetes","volume":"5","author":"Chatterjee","year":"2015","journal-title":"Sci Rep"},{"key":"10.1016\/j.drudis.2025.104318_b0405","doi-asserted-by":"crossref","first-page":"80","DOI":"10.1186\/s12933-019-0884-3","article-title":"New dual peroxisome proliferator activated receptor agonist-saroglitazar in diabetic dyslipidemia and non-alcoholic fatty liver disease: integrated analysis of the real world evidence","volume":"18","author":"Kaul","year":"2019","journal-title":"Cardiovasc Diabetol"},{"key":"10.1016\/j.drudis.2025.104318_b0410","doi-asserted-by":"crossref","first-page":"132","DOI":"10.1177\/1932296813518680","article-title":"A multicenter, prospective, randomized, double-blind study to evaluate the safety and efficacy of saroglitazar 2 and 4 mg compared to pioglitazone 45 mg in diabetic dyslipidemia (PRESS V)","volume":"8","author":"Pai","year":"2014","journal-title":"J Diabetes Sci Technol"},{"key":"10.1016\/j.drudis.2025.104318_b0415","doi-asserted-by":"crossref","first-page":"63","DOI":"10.1089\/dia.2013.0253","volume":"16","author":"Jani","year":"2014","journal-title":"Diabetes Technol Ther"},{"key":"10.1016\/j.drudis.2025.104318_b0420","doi-asserted-by":"crossref","first-page":"2670","DOI":"10.1016\/j.cgh.2020.10.051","article-title":"A Phase 2 double blinded, randomized controlled trial of saroglitazar in patients with nonalcoholic steatohepatitis","volume":"19","author":"Gawrieh","year":"2021","journal-title":"Clin Gastroenterol Hepatol"},{"key":"10.1016\/j.drudis.2025.104318_b0425","article-title":"Saroglitazar in non-alcoholic fatty liver disease from bench to bedside: a comprehensive review and sub-group meta-analysis","volume":"15","author":"Roy","year":"2023","journal-title":"Cureus"},{"key":"10.1016\/j.drudis.2025.104318_b0430","doi-asserted-by":"crossref","DOI":"10.1016\/j.clinre.2023.102174","article-title":"Effects of saroglitazar in the treatment of non-alcoholic fatty liver disease or non-alcoholic steatohepatitis: a systematic review and meta-analysis","volume":"47","author":"Bandyopadhyay","year":"2023","journal-title":"Clin Res Hepatol Gastroenterol"},{"key":"10.1016\/j.drudis.2025.104318_b0435","doi-asserted-by":"crossref","first-page":"1411","DOI":"10.1093\/jnci\/djs328","article-title":"Association between longer therapy with thiazolidinediones and risk of bladder cancer: a cohort study","volume":"104","author":"Mamtani","year":"2012","journal-title":"J Natl Cancer Inst"},{"key":"10.1016\/j.drudis.2025.104318_b0440","doi-asserted-by":"crossref","first-page":"31","DOI":"10.1038\/s41598-017-18274-1","article-title":"Structural basis for the enhanced anti\u2013diabetic efficacy of lobeglitazone on PPAR\u03b3","volume":"8","author":"Jang","year":"2018","journal-title":"Sci Rep"},{"key":"10.1016\/j.drudis.2025.104318_b0445","doi-asserted-by":"crossref","first-page":"326","DOI":"10.4093\/dmj.2020.0272","article-title":"Lobeglitazone: a novel thiazolidinedione for the management of type 2 diabetes mellitus","volume":"45","author":"Bae","year":"2021","journal-title":"Diabetes Metab J"},{"key":"10.1016\/j.drudis.2025.104318_b0450","article-title":"Efficacy and safety of lobeglitazone monotherapy in patients with type 2 diabetes mellitus over 24-weeks: a multicenter, randomized, double-blind, parallel-group, placebo controlled trial","volume":"9","author":"Kim","year":"2014","journal-title":"PLoS One"},{"key":"10.1016\/j.drudis.2025.104318_b0455","doi-asserted-by":"crossref","first-page":"16837","DOI":"10.1038\/s41598-017-17082-x","article-title":"Structures of PPAR\u03b3 complexed with lobeglitazone and pioglitazone reveal key determinants for the recognition of antidiabetic drugs","volume":"7","author":"Lee","year":"2017","journal-title":"Sci Rep"},{"key":"10.1016\/j.drudis.2025.104318_b0460","article-title":"Efficacy and safety of novel thiazolidinedione lobeglitazone for managing type-2 diabetes a meta-analysis","volume":"17","author":"Dutta","year":"2023","journal-title":"Diabetes Metab Syndr"},{"key":"10.1016\/j.drudis.2025.104318_b0465","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2023.106786","article-title":"Roles of the peroxisome proliferator-activated receptors (PPARs) in the pathogenesis of nonalcoholic fatty liver disease (NAFLD)","volume":"192","author":"Qiu","year":"2023","journal-title":"Pharmacol Res"}],"container-title":["Drug Discovery Today"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S1359644625000315?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S1359644625000315?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2025,4,11]],"date-time":"2025-04-11T23:13:49Z","timestamp":1744413229000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S1359644625000315"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2025,3]]},"references-count":93,"journal-issue":{"issue":"3","published-print":{"date-parts":[[2025,3]]}},"alternative-id":["S1359644625000315"],"URL":"https:\/\/doi.org\/10.1016\/j.drudis.2025.104318","relation":{},"ISSN":["1359-6446"],"issn-type":[{"value":"1359-6446","type":"print"}],"subject":[],"published":{"date-parts":[[2025,3]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Drugs targeting peroxisome proliferator-activated receptors","name":"articletitle","label":"Article Title"},{"value":"Drug Discovery Today","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.drudis.2025.104318","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2025 Elsevier Ltd. All rights are reserved, including those for text and data mining, AI training, and similar technologies.","name":"copyright","label":"Copyright"}],"article-number":"104318"}}