Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C37H48N4O8S2 |
Molecular Weight | 740.929 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCCC1(CCCC)CN(C2=CC=CC=C2)C3=CC(SC)=C(OCC(=O)N[C@@H](C(=O)N[C@@H](CC)C(O)=O)C4=CC=C(O)C=C4)C=C3S(=O)(=O)N1
InChI
InChIKey=XULSCZPZVQIMFM-IPZQJPLYSA-N
InChI=1S/C37H48N4O8S2/c1-5-8-19-37(20-9-6-2)24-41(26-13-11-10-12-14-26)29-21-31(50-4)30(22-32(29)51(47,48)40-37)49-23-33(43)39-34(25-15-17-27(42)18-16-25)35(44)38-28(7-3)36(45)46/h10-18,21-22,28,34,40,42H,5-9,19-20,23-24H2,1-4H3,(H,38,44)(H,39,43)(H,45,46)/t28-,34+/m0/s1
Molecular Formula | C37H48N4O8S2 |
Molecular Weight | 740.929 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
A-4250 (odevixibat) is a selective inhibitor of the ileal bile acid transporter (IBAT) that acts locally in the gut. Ileum absorbs glyco-and taurine-conjugated forms of the bile salts. IBAT is the first step in absorption at the brush-border membrane. A-4250 works by decreasing the re-absorption of bile acids from the small intestine to the liver, whichreduces the toxic levels of bile acids during the progression of the disease. It exhibits therapeutic intervention by checking the transport of bile acids. Studies show that A-4250 has the potential to decrease the damage in the liver cells and the development of fibrosis/cirrhosis of the liver known to occur in progressive familial intrahepatic cholestasis. A-4250 is a designated orphan drug in the USA for October 2012. A-4250 is a designated orphan drug in the EU for October 2016. A-4250 was awarded PRIME status for PFIC by EMA in October 2016. A-4250 is in phase II clinical trials by Albireo for the treatment of primary biliary cirrhosis (PBC) and cholestatic pruritus. In an open label Phase 2 study in children with cholestatic liver disease and pruritus, odevixibat showed reductions in serum bile acids and pruritus in most patients and exhibited a favorable overall tolerability profile.
Originator
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/29704003
The primary efficacy objective was to demonstrate the efficacy of once daily dosing of A-4250, 1.5–3 mg orally during a four-week treatment period to relieve patients with primary biliary cholangitis from cholestatic pruritus.
Route of Administration:
Oral
Substance Class |
Chemical
Created
by
admin
on
Edited
Sun Dec 18 20:31:38 UTC 2022
by
admin
on
Sun Dec 18 20:31:38 UTC 2022
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Record UNII |
2W150K0UUC
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Record Status |
Validated (UNII)
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Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
658118
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FDA ORPHAN DRUG |
370812
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FDA ORPHAN DRUG |
371012
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admin on Sun Dec 18 20:31:38 UTC 2022 , Edited by admin on Sun Dec 18 20:31:38 UTC 2022
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EU-Orphan Drug |
EU/3/18/2103
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admin on Sun Dec 18 20:31:38 UTC 2022 , Edited by admin on Sun Dec 18 20:31:38 UTC 2022
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FDA ORPHAN DRUG |
370912
Created by
admin on Sun Dec 18 20:31:38 UTC 2022 , Edited by admin on Sun Dec 18 20:31:38 UTC 2022
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2563966
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C166598
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SUB193727
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10153627
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10706
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2W150K0UUC
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501692-44-0
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2W150K0UUC
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GH-119
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Related Record | Type | Details | ||
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SOLVATE->ANHYDROUS | |||
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SALT/SOLVATE -> PARENT |
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TARGET -> INHIBITOR |
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ACTIVE MOIETY |
Originator: Albireo; Class: Antipruritic; Mechanism of Action: Sodium-bile acid cotransporter-inhibitor; Orphan Drug Status: Yes for Primary biliary cirrhosis, Intrahepatic cholestasis, Alagille syndrome; On Fast track: No; New Molecular Entity: Yes; Highest Development Phases: Phase II for Intrahepatic cholestasis, Primary biliary cirrhosis, Pruritus - Phase I for Alagille syndrome; Most Recent Events: 25 Jul 2016 Phase-II clinical trials in Intrahepatic cholestasis (PO) (Albireo pipeline, July 2016), 06 Nov 2015 Phase-II clinical trials in Pruritus (In adolescents, In children, In infants) in Germany (PO) (EudraCT2015-001157-32), 21 Aug 2015 Phase-II clinical trials in Pruritus (In children, In infants, In adolescents) in Denmark (PO) (EudraCT2015-001157-32)
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