Mibefradil
This unique calcium channel blocker selectively blocks T-type calcium channels (in addition to L-type channels), which had potential advantages in treating heart disease and hypertension. It was withdrawn from the market shortly after approval because it caused dangerous interactions with many commonly used medications by inhibiting liver enzymes that metabolize drugs.
Molecular Weight
495.6000 g/mol
LogP
5.80
TPSA
67.50 Ų
Lipinski RO5
Pass
Therapeutic Areas
Mechanism of Action
Blocks L-type voltage-gated calcium channels in vascular smooth muscle and cardiac myocytes, reducing calcium influx during depolarization. This produces vasodilation, decreased myocardial contractility, and reduced heart rate.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Blocks L-type voltage-gated calcium channels in vascular smooth muscle and cardiac myocytes, reducing calcium influx during depolarization. This produces vasodilation, decreased myocardial contractility, and reduced heart rate.
2D Structure
Cite this structure
Embed this structure
SMILES
COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C
InChI
InChI=1S/C29H38FN3O3/c1-20(2)28-23-12-11-22(30)18-21(23)13-14-29(28,36-27(34)19-35-4)15-17-33(3)16-7-10-26-31-24-8-5-6-9-25(24)32-26/h5-6,8-9,11-12,18,20,28H,7,10,13-17,19H2,1-4H3,(H,31,32)/t28-,29-/m0/s1
Molecular Formula
C29H38FN3O3
HBD / HBA
1 / 6
Rotatable Bonds
12
Heavy Atoms
36
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
Frequently Asked Questions
This unique calcium channel blocker selectively blocks T-type calcium channels (in addition to L-type channels), which had potential advantages in treating heart disease and hypertension. It was withdrawn from the market shortly after approval because it caused dangerous interactions with many commonly used medications by inhibiting liver enzymes that metabolize drugs.
Blocks L-type voltage-gated calcium channels in vascular smooth muscle and cardiac myocytes, reducing calcium influx during depolarization. This produces vasodilation, decreased myocardial contractility, and reduced heart rate.
Yes, Mibefradil is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL45816. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 60663. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.
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