Seladelpar

Chemical compound

None

Legal statusLegal status

Investigational

Identifiers

IUPAC name

2-[4-[(2R)-2-ethoxy-3-[4-(trifluoromethyl)phenoxy]propyl]sulfanyl-2-methylphenoxy]acetic acid

CAS Number

851528-79-5

PubChem CID

11236126

DrugBank

DB12390

ChemSpider

9411171

UNII

7C00L34NB9

KEGG

D11256

ChEMBL

ChEMBL230158

Chemical and physical dataFormulaC₂₁H₂₃F₃O₅SMolar mass444.47 g·mol⁻¹3D model (JSmol)

Interactive image

SMILES

CCO[C@H](COC1=CC=C(C=C1)C(F)(F)F)CSC2=CC(=C(C=C2)OCC(=O)O)C

InChI

InChI=1S/C21H23F3O5S/c1-3-27-17(11-28-16-6-4-15(5-7-16)21(22,23)24)13-30-18-8-9-19(14(2)10-18)29-12-20(25)26/h4-10,17H,3,11-13H2,1-2H3,(H,25,26)/t17-/m1/s1
Key:JWHYSEDOYMYMNM-QGZVFWFLSA-N

Seladelpar (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name; developmental code names MBX-8025, RWJ-800025) is a PPARδ receptor agonist that is being investigated for drug use by Metabolex.^[1]^[2]^[3] According to a press release they are examining its potential use for the treatment of dyslipidemia, metabolic syndrome, type 2 diabetes, and non-alcoholic steatohepatitis (NASH). The compound was licensed from Janssen Pharmaceutica NV.^[4] The drug completed a phase II trial for primary biliary cholangitis. "Seladelpar demonstrated robust, dose-dependent, clinically significant, and durable improvements in biochemical markers of cholestasis and inflammation in patients with PBC at risk of disease progression. Seladelpar appeared safe and well tolerated and was not associated with any increase in pruritus."^[5] A phase III trial in patients with PBC also found reduced pruritus and improved liver biochemistry, despite being terminated early.^[6]

References

^ "Seladelpar - CymaBay Therapeutics". AdisInsight. Springer Nature Switzerland AG.
^ Billin AN (October 2008). "PPAR-beta/delta agonists for Type 2 diabetes and dyslipidemia: an adopted orphan still looking for a home". Expert Opinion on Investigational Drugs. 17 (10): 1465–1471. doi:10.1517/13543784.17.10.1465. PMID 18808307. S2CID 86564263.
^ Bays HE, Schwartz S, Littlejohn T, Kerzner B, Krauss RM, Karpf DB, et al. (September 2011). "MBX-8025, a novel peroxisome proliferator receptor-delta agonist: lipid and other metabolic effects in dyslipidemic overweight patients treated with and without atorvastatin". The Journal of Clinical Endocrinology and Metabolism. 96 (9): 2889–2897. doi:10.1210/jc.2011-1061. PMID 21752880.
^ "Targeting Mixed Dyslipidemia and Metabolic Syndrome". Metabolex, Inc. 2005. Archived from the original on 2006-10-17.
^ Bowlus CL, Galambos MR, Aspinall RJ, Hirschfield GM, Jones DE, Dörffel Y, et al. (August 2022). "A phase II, randomized, open-label, 52-week study of seladelpar in patients with primary biliary cholangitis". Journal of Hepatology. 77 (2): 353–364. doi:10.1016/j.jhep.2022.02.033. hdl:10026.1/19044. PMID 35367282. S2CID 247890468.
^ Hirschfield GM, Shiffman ML, Gulamhusein A, Kowdley KV, Vierling JM, Levy C, et al. (August 2023). "Seladelpar efficacy and safety at 3 months in patients with primary biliary cholangitis: ENHANCE, a phase 3, randomized, placebo-controlled study". Hepatology. 78 (2): 397–415. doi:10.1097/HEP.0000000000000395. PMC 10344437. PMID 37386786.