Article · Wikipedia archive · Last revised Jul 4, 2026

Etamicastat

Etamicastat is a peripherally selective dopamine β-hydroxylase (DBH) inhibitor which was under development for the treatment of hypertension and heart failure but was never marketed. The peripheral selectivity of etamicastat is in contrast to the earlier DBH inhibitor nepicastat, which is centrally active and produced associated side effects. Etamicastat was found to reduce blood pressure but not affect heart rate in clinical trials. The development of etamicastat was discontinued by August 2016.

Last revised
Jul 4, 2026
Read time
≈ 1 min
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159 w
Citations
5
Source
Wikipedia ↗
Etamicastat
Clinical data
Other namesBIA 5-453; BIA-5-453
Drug classDopamine β-hydroxylase inhibitor
Identifiers
  • 4-(2-aminoethyl)-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
FormulaC14H15F2N3OS
Molar mass311.35 g·mol−1
3D model (JSmol)
  • C1[C@H](COC2=C1C=C(C=C2F)F)N3C(=CNC3=S)CCN
  • InChI=1S/C14H15F2N3OS/c15-9-3-8-4-11(7-20-13(8)12(16)5-9)19-10(1-2-17)6-18-14(19)21/h3,5-6,11H,1-2,4,7,17H2,(H,18,21)/t11-/m1/s1
  • Key:CWWWTTYMUOYSQA-LLVKDONJSA-N

Etamicastat (INNTooltip International Nonproprietary Name; developmental code name BIA 5-453) is a peripherally selective dopamine β-hydroxylase (DBH) inhibitor which was under development for the treatment of hypertension (high blood pressure) and heart failure but was never marketed.12 The peripheral selectivity of etamicastat is in contrast to the earlier DBH inhibitor nepicastat, which is centrally active and produced associated side effects.2 Etamicastat was found to reduce blood pressure but not affect heart rate in clinical trials.2 The development of etamicastat was discontinued by August 2016.1

See also

See also

References

References

  1. "Etamicastat". AdisInsight. 27 December 2019. 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.