Seladelpar

Seladelpar
Clinical data
Other names	MBX-8025; RWJ-800025
ATC code	None;
Legal status
Legal 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 data
Formula	C21H23F3O5S
Molar mass	444.47 g·mol−1
3D 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[edit]

^ "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.

External links[edit]

Seladelpar - AdisInsight

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[AdisInsight-1] "Seladelpar - CymaBay Therapeutics". AdisInsight. Springer Nature Switzerland AG.

[pmid18808307-2] 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.

[pmid21752880-3] 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.

[Metabolex2006-4] "Targeting Mixed Dyslipidemia and Metabolic Syndrome". Metabolex, Inc. 2005. Archived from the original on 2006-10-17.

[5] 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.

[6] 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.

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v t e PPARTooltip Peroxisome proliferator-activated receptor modulators
PPARαTooltip Peroxisome proliferator-activated receptor alpha	Agonists: 15-HETE 15-HpETE Aleglitazar Aluminium clofibrate Arachidonic acid Bezafibrate Chiglitazar Clofibrate CP-775146 Daidzein DHEA (prasterone) (in rodents) Elafibranor Etomoxir Fenofibrate Genistein Gemfibrozil GW-7647 Lanifibranor Leukotriene B₄ LG-101506 LG-100754 Lobeglitazone Muraglitazar Oleylethanolamide Palmitoylethanolamide Pemafibrate Perfluorononanoic acid Perfluorooctanoic acid Pioglitazone Saroglitazar Sodelglitazar Tesaglitazar Tetradecylthioacetic acid Troglitazone WY-14643 Antagonists: GW-6471 MK-886
PPARδTooltip Peroxisome proliferator-activated receptor delta	Agonists: 15-HETE 15-HpETE Arachidonic acid Bezafibrate Daidzein Elafibranor Fonadelpar Genistein GW-0742 GW-501516 L-165,041 Lanifibranor LG-101506 Seladelpar Sodelglitazar Tetradecylthioacetic acid Antagonists: FH-535 GSK-0660 GSK-3787
PPARγTooltip Peroxisome proliferator-activated receptor gamma	Agonists: 5-Oxo-ETE 5-Oxo-15-hydroxy-ETE 15-Deoxy-Δ^12,14-prostaglandin J₂ 15-HETE 15-HpETE Aleglitazar Arachidonic acid Balaglitazone Berberine Bezafibrate Cannabidiol Cevoglitazar Chiglitazar Ciglitazone Daidzein Darglitazone Edaglitazone Efatutazone Englitazone Etalocib Farglitazar Genistein GW-1929 Ibuprofen Imiglitazar Indeglitazar Lanifibranor LG-100268 LG-100754 LG-101506 Lobeglitazone Muraglitazar (muroglitazar) nTZDpa Naveglitazar Netoglitazone Oxeglitazar Peliglitazar Pemaglitazar Perfluorononanoic acid Pioglitazone Prostaglandin J₂ Ragaglitazar Reglitazar Rivoglitazone Rosiglitazone RS5444 Saroglitazar Sipoglitazar Sodelglitazar Telmisartan Tesaglitazar Troglitazone SPPARMsTooltip Selective PPARγ modulator: BADGE EPI-001 INT-131 MK-0533 S26948 Antagonists: FH-535 GW-9662 SR-202 T-0070907 Unknown: SR-1664
Non-selective	Agonists: Ciprofibrate Clinofibrate Clofibride Englitazone Etofibrate Farglitazar Netoglitazone Ronifibrate Rivoglitazone Simfibrate
See also Receptor/signaling modulators

See also[edit]

References[edit]

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