Article · Wikipedia archive · Last revised Jun 23, 2026

Zamicastat

Zamicastat is a peripherally selective dopamine β-hydroxylase (DBH) inhibitor which is under development for the treatment of pulmonary arterial hypertension (PAH) and heart failure. It is structurally related to etamicastat and is said to be an improved version of this drug. 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.

Last revised
Jun 23, 2026
Read time
≈ 1 min
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154 w
Citations
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Source
Wikipedia ↗
Zamicastat
Clinical data
Other namesBIA-5-1058; BIA 5-1058
Drug classDopamine β-hydroxylase inhibitor
Identifiers
  • 4-[2-(benzylamino)ethyl]-3-[(3R)-6,8-difluoro-3,4-dihydro-2H-chromen-3-yl]-1H-imidazole-2-thione
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC21H21F2N3OS
Molar mass401.48 g·mol−1
3D model (JSmol)
  • C1[C@H](COC2=C1C=C(C=C2F)F)N3C(=CNC3=S)CCNCC4=CC=CC=C4
  • InChI=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
  • Key:ZSSLCFLHEFXANG-GOSISDBHSA-N

Zamicastat (INNTooltip International Nonproprietary Name; 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.12 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.1 However, no recent development has been reported for heart failure.1

See also

See also

References

References

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