Mibefradil

CARDIOVASCULAR SYSTEM

Also known as: mibefradil dihydrochloride, posicor, Ro 40-5967

FDA approvedATC C08CX01

Data last refreshed: 2026-11-10 (DrugCentral release 2024-11-01)

Open interactive profile (3D, safety, PGx)

Key facts

Mibefradil is a drug catalogued in DrugCentral. It was first approved by the FDA in 1997. DrugCentral lists 21 molecular targets, including CACNA1I, KCNH2 and CACNA1G. Recorded indications include Angina pectoris and Hypertensive disorder.

Molecular targets: CACNA1I, KCNH2, CACNA1G and CACNA1H (21 listed in DrugCentral).
Indications: Angina pectoris and Hypertensive disorder.
ATC code: C08CX01 (Other selective calcium channel blockers with mainly vascular effects).
Molecular formula: C29H38FN3O3; molecular weight 495.64 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

Angina pectoris
Hypertensive disorder

Contraindications (4)

Atrioventricular Conduction Defect
Complete atrioventricular block
Disease of liver
Sick sinus syndrome

Mechanism & targets

Molecular targets (21)

Target	Gene	Action	Activity
Voltage-dependent T-type calcium channel subunit alpha-1I	CACNA1I	unknown	IC50 6.90
Potassium voltage-gated channel subfamily H member 2	KCNH2	unknown	Ki 6.72
Voltage-dependent T-type calcium channel subunit alpha-1G	CACNA1G	unknown	IC50 6.70
Voltage-dependent T-type calcium channel subunit alpha-1H	CACNA1H	blocker	IC50 6.60
Voltage-dependent P/Q-type calcium channel subunit alpha-1A	Cacna1a	other	IC50 6.50
Voltage-dependent R-type calcium channel subunit alpha-1E	Cacna1e	other	IC50 6.40
Sodium channel protein type 9 subunit alpha	SCN9A	unknown	IC50 6.30
Sodium channel protein type 2 subunit alpha	Scn2a	unknown	IC50 6.30
Sodium channel protein type 4 subunit alpha	Scn4a	unknown	IC50 6.30
Sodium channel protein type 5 subunit alpha	SCN5A	unknown	IC50 6.30
Cytochrome P450 3A4	CYP3A4	unknown	Ki 6.22
Cytochrome P450 2D6	CYP2D6	unknown	IC50 6.14
Voltage-dependent N-type calcium channel subunit alpha-1B	CACNA1B	unknown	IC50 5.87
Multidrug resistance protein 1	ABCB1	unknown	IC50 5.80
Voltage-dependent L-type calcium channel subunit alpha-1C	CACNA1C	blocker	IC50 4.90
Potassium channel subfamily K member 9	KCNK9	unknown	IC50 4.61
Cation channel sperm-associated protein 3	CATSPER3	blocker	IC50 4.50
Cation channel sperm-associated protein 1	CATSPER1	blocker	IC50 4.50
Cation channel sperm-associated protein 2	CATSPER2	blocker	IC50 4.50
Cation channel sperm-associated protein 4	CATSPER4	blocker	IC50 4.50

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1997-08-01	FDA	—	—

ATC classification

ATC code	Therapeutic hierarchy
`C08CX01`	CARDIOVASCULAR SYSTEM › CALCIUM CHANNEL BLOCKERS › SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS › Other selective calcium channel blockers with mainly vascular effects

Chemical structure

Molecular formula	C₂₉H₃₈FN₃O₃
Molecular weight	495.64 g/mol
CAS number	116644-53-2
InChIKey	HBNPJJILLOYFJU-VMPREFPWSA-N
PubChem CID	60663

COCC(=O)O[C@]1(CCN(C)CCCC2=NC3=C(N2)C=CC=C3)CCC2=CC(F)=CC=C2[C@@H]1C(C)C

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Mibefradil used for?

DrugCentral lists the following indications for Mibefradil: Angina pectoris and Hypertensive disorder.

How does Mibefradil work?

Its molecular targets in DrugCentral include CACNA1I, KCNH2, CACNA1G and CACNA1H (blocker).

When was Mibefradil first approved?

Mibefradil was first approved by the FDA in 1997.

What is the chemical formula of Mibefradil?

Mibefradil has the molecular formula C29H38FN3O3 and a molecular weight of 495.64 g/mol.

Browse: all drugs starting with M · drug guides by category · protein targets A–Z.

Sources

DrugCentral drug card 1797 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
ChEMBL CHEMBL1534525 — compound record and bioactivity
PubChem CID 60663 — chemical identifiers
DrugBank DB01388 — drug record
FDA UNII 27B90X776A — substance identity
DailyMed: FDA labels for Mibefradil — current prescribing information (label search)
UniProt Q9P0X4 (CACNA1I) — target protein
UniProt Q12809 (KCNH2) — target protein
UniProt O43497 (CACNA1G) — target protein
UniProt O95180 (CACNA1H) — target protein
UniProt Q15858 (SCN9A) — target protein
UniProt Q14524 (SCN5A) — target protein

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