Zamicastat

Zamicastat
Clinical data
Other names	BIA-5-1058; BIA 5-1058
Drug class	Dopamine β-hydroxylase inhibitor
Identifiers
	IUPAC name 4-[2-(benzylamino)ethyl]-3-[(3R)-6,8-difluoro-3,4-dihydro-2H-chromen-3-yl]-1H-imidazole-2-thione;
CAS Number	1080028-80-3;
PubChem CID	25052630;
DrugBank	DB12389;
ChemSpider	32701723;
UNII	YLU32D0DNV;
ChEMBL	ChEMBL4863440;
CompTox Dashboard (EPA)	DTXSID80148358 ;
Chemical and physical data
Formula	C21H21F2N3OS
Molar mass	401.48 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1[C@H](COC2=C1C=C(C=C2F)F)N3C(=CNC3=S)CCNCC4=CC=CC=C4;
	InChI 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.^[1]^[2] 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]

References

^ ^a ^b ^c "Zamicastat". AdisInsight. 28 July 2022. Retrieved 21 October 2024.
^ ^a ^b 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.

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