Rencofilstat

Rencofilstat
Clinical data
Other names	CRV431
Identifiers
	IUPAC name N-[(7R,8R)-8-[(2S,5S,8R,11S,14S,17S,20S,23R,26S,29S,32S)-5-ethyl-1,7,8,10,16,20,23,25,28,31-decamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacont-2-yl]-8-hydroxy-7-methyloctyl]acetamide;
CAS Number	1383420-08-3;
PubChem CID	134812041;
ChemSpider	81368207;
UNII	M3H4D91AY5;
ChEMBL	ChEMBL4297487;
Chemical and physical data
Formula	C67H122N12O13
Molar mass	1303.784 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC[C@H]1C(=O)N([C@@H](C(=O)N([C@H](C(=O)N[C@H](C(=O)N([C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N1)[C@@H]([C@H](C)CCCCCCNC(=O)C)O)C)C(C)C)C)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)CC(C)C)C)C)C;
	InChI InChI=1S/C67H122N12O13/c1-26-48-63(88)73(19)46(17)62(87)74(20)50(34-38(4)5)59(84)72-53(41(10)11)66(91)75(21)49(33-37(2)3)58(83)69-44(15)57(82)70-45(16)61(86)76(22)51(35-39(6)7)64(89)77(23)52(36-40(8)9)65(90)78(24)54(42(12)13)67(92)79(25)55(60(85)71-48)56(81)43(14)31-29-27-28-30-32-68-47(18)80/h37-46,48-56,81H,26-36H2,1-25H3,(H,68,80)(H,69,83)(H,70,82)(H,71,85)(H,72,84)/t43-,44+,45-,46-,48+,49+,50+,51+,52+,53+,54+,55+,56-/m1/s1; Key:KBARHGHBFILILC-NGIJKBHDSA-N;

Rencofilstat (CRV431) is a pan-cyclophilin inhibitor and analog of cyclosporine A developed for nonalcoholic steatohepatitis^[1] and hepatocellular carcinoma.^[2]^[3]^[4]

References

↑ Harrison, Stephen A.; Mayo, Patrick R.; Hobbs, Todd M.; Canizares, Carlos; Foster, Erin P.; Zhao, Caroline; Ure, Daren R.; Trepanier, Daniel J.; Greytok, Jill A.; Foster, Robert T. (December 2022). "Rencofilstat, a cyclophilin inhibitor: A phase 2a, multicenter, single-blind, placebo-controlled study in F2/F3 NASH". Hepatology Communications. 6 (12): 3379–3392. doi:10.1002/hep4.2100. PMC 9701462. PMID 36271849.
↑ Stauffer, Winston; Bobardt, Michael; Ure, Daren; Foster, Robert; Gallay, Philippe (17 October 2023). "The Cyclophilin Inhibitor Rencofilstat Decreases HCV-Induced Hepatocellular Carcinoma Independently of Its Antiviral Activity". Viruses. 15 (10): 2099. doi:10.3390/v15102099. PMC 10612079. PMID 37896876.
↑ Remenchik, Ellen; Mayo, Patrick R.; Hobbs, Todd M.; Greytok, Jill A.; Foster, Erin P.; Zhao, Caroline; Ure, Daren; Trepanier, Daniel J.; Foster, Robert T. (March 2023). "Effect of a High-Fat Meal on Single-Dose Rencofilstat (CRV431) Oral Bioavailability in Healthy Human Subjects". Clinical Pharmacology in Drug Development. 12 (3): 287–293. doi:10.1002/cpdd.1179. PMID 36251165. S2CID 252915396.
↑ Ure, Daren; Leslie, Jack; Haddon, Lacey; Fu, Claude; Mann, Jelena; Mann, Derek (4 April 2023). "Abstract 4125: Rencofilstat exerts a dominant role in synergistic anti-PD1-combination effects in a fatty liver model of hepatocellular carcinoma". Cancer Research. 83 (7_Supplement): 4125. doi:10.1158/1538-7445.AM2023-4125. S2CID 258002007.