Zamicastat Explained

Class:Dopamine β-hydroxylase inhibitor
Cas Number:1080028-80-3
Pubchem:25052630
Drugbank:DB12389
Chemspiderid:32701723
Unii:YLU32D0DNV
Chembl:4594440
Synonyms:BIA-5-1058; BIA 5-1058
Iupac Name:4-[2-(benzylamino)ethyl]-3-[(3''R'')-6,8-difluoro-3,4-dihydro-2''H''-chromen-3-yl]-1H-imidazole-2-thione
C:21
H:21
F:2
N:3
O:1
S:1
Smiles:C1[C@H](COC2=C1C=C(C=C2F)F)N3C(=CNC3=S)CCNCC4=CC=CC=C4
Stdinchi:1S/C21H21F2N3OS/c22-16-8-15-9-18(13-27-20(15)19(23)10-16)26-17(12-25-21(26)28)6-7-24-11-14-4-2-1-3-5-14/h1-5,8,10,12,18,24H,6-7,9,11,13H2,(H,25,28)/t18-/m1/s1
Stdinchikey:ZSSLCFLHEFXANG-GOSISDBHSA-N

Zamicastat (; developmental code name BIA-5-1058) is a peripherally selective dopamine β-hydroxylase (DBH) inhibitor which is under development for the treatment of pulmonary arterial hypertension (PAH) and heart failure.[1] It is structurally related to etamicastat and is said to be an improved version of this drug.[2] As of July 2022, zamicastat is in phase 2 clinical trials for PAH and phase 1 clinical trials for heart failure. However, no recent development has been reported for heart failure.

See also

Notes and References

  1. Web site: Zamicastat . AdisInsight . 28 July 2022 . 21 October 2024.
  2. Dey SK, Saini M, Prabhakar P, Kundu S . Dopamine β hydroxylase as a potential drug target to combat hypertension . Expert Opin Investig Drugs . 29 . 9 . 1043–1057 . September 2020 . 32658551 . 10.1080/13543784.2020.1795830 .