bepridil
Trade name: vascor
Approved
Dec 28, 1990
Bepridil is a calcium channel blocker that has well characterized anti-anginal properties and known but poorly characterized type 1 anti-arrhythmic and anti-hypertensive properties. It has inhibitory effects on both the slow calcium and fast sodium inward currents in myocardial and vascular smooth muscle, interferes with calcium binding to calmodulin, and blocks both voltage and receptor operated calcium channels. It is used to treat hypertension (high blood pressure), angina (chest pain), sustained atrial fibrillation and tachyarrhythmia. The most common side effects were upper gastrointestinal complaints (nausea, dyspepsia or GI distress), diarrhea, dizziness, asthenia and nervousness. Certain drugs could increase the likelihood of potentially serious adverse effects with bepridil hydrochloride. In general, these are drugs that have one or more pharmacologic activities similar to bepridil hydrochloride, including anti-arrhythmic agents such as quinidine and procainamide, cardiac glycosides and tricyclic anti-depressants. Anti-arrhythmics and tricyclic anti-depressants could exaggerate the prolongation of the QT interval observed with bepridil hydrochloride. Cardiac glycosides could exaggerate the depression of AV nodal conduction observed with bepridil hydrochloride. — NCATS
Clinical trial activity
0 trials · 0 clinical orgs · 3 marketing orgs
Timeline
1990s
- Dec 28, 1990
Carter-Wallace — Earliest FDA Approval
- Dec 28, 1990
Johnson and Johnson — NDA Secondary Org
- Dec 28, 1990
Medpointe — NDA Secondary Org
- Dec 28, 1990
Carter-Wallace — NDA Organization
Indications
Mechanism of action
Voltage-gated calcium channel blocker
- Voltage-dependent T-type calcium channel subunit alpha-1H (CACNA1H) ↗
- Voltage-dependent calcium channel subunit alpha-2/delta-1 (CACNA2D1) ↗
- Voltage-dependent L-type calcium channel subunit alpha-1C (CACNA1C) ↗
- Voltage-dependent calcium channel subunit alpha-2/delta-3 (CACNA2D3) ↗
- Voltage-dependent L-type calcium channel subunit alpha-1S (CACNA1S) ↗
- Voltage-dependent calcium channel subunit alpha-2/delta-2 (CACNA2D2) ↗
- Voltage-dependent L-type calcium channel subunit alpha-1D (CACNA1D) ↗
- Voltage-dependent P/Q-type calcium channel subunit alpha-1A (CACNA1A) ↗
- Voltage-dependent N-type calcium channel subunit alpha-1B (CACNA1B) ↗
- Voltage-dependent T-type calcium channel subunit alpha-1G (CACNA1G) ↗
- Voltage-dependent calcium channel subunit alpha-2/delta-4 (CACNA2D4) ↗
- Voltage-dependent T-type calcium channel subunit alpha-1I (CACNA1I) ↗
- Voltage-dependent L-type calcium channel subunit alpha-1F (CACNA1F) ↗
- Voltage-dependent R-type calcium channel subunit alpha-1E (CACNA1E) ↗
- Voltage-dependent L-type calcium channel subunit beta-3 (CACNB3) ↗
- Voltage-dependent calcium channel gamma-7 subunit (CACNG7) ↗
- Voltage-dependent calcium channel gamma-5 subunit (CACNG5) ↗
- Voltage-dependent calcium channel gamma-2 subunit (CACNG2) ↗
- Voltage-dependent L-type calcium channel subunit beta-4 (CACNB4) ↗
- Voltage-dependent L-type calcium channel subunit beta-2 (CACNB2) ↗
- Voltage-dependent L-type calcium channel subunit beta-1 (CACNB1) ↗
- Voltage-dependent calcium channel gamma-4 subunit (CACNG4) ↗
- Voltage-dependent calcium channel gamma-8 subunit (CACNG8) ↗
- Voltage-dependent calcium channel gamma-3 subunit (CACNG3) ↗
- Voltage-dependent calcium channel gamma-6 subunit (CACNG6) ↗
- Voltage-dependent calcium channel gamma-1 subunit (CACNG1) ↗
- Voltage-gated T-type calcium channel alpha-1H subunit
- Voltage-gated calcium channel alpha2/delta subunit 1
- Voltage-gated L-type calcium channel alpha-1C subunit
- Voltage-gated N-type calcium channel alpha-1B subunit
- Voltage-gated L-type calcium channel alpha-1S subunit
- Voltage-gated L-type calcium channel alpha-1D subunit
- Voltage-gated calcium channel alpha2/delta subunit 2
- Voltage-gated P/Q-type calcium channel alpha-1A subunit
- Voltage-gated T-type calcium channel alpha-1G subunit
- Voltage-gated T-type calcium channel alpha-1I subunit
- Voltage-dependent R-type calcium channel subunit alpha-1E
- Voltage-gated L-type calcium channel
- Voltage-gated T-type calcium channel
- Voltage-dependent L-type calcium channel subunit beta-2
- Voltage-dependent N-type calcium channel subunit alpha-1B/Voltage-dependent calcium channel subunit alpha-2/delta-1/Voltage-dependent L-type calcium channel subunit beta-3
- Voltage-dependent L-type calcium channel alpha1C/alpha2delta/beta1b
- Voltage-dependent P/Q-type calcium channel alpha1A/alpha2delta/beta1b
- N-type calcium channel alpha-1b/alpha2delta-1/beta-1b
- L-type calcium channel alpha-1c/beta-2/alpha2delta-1
- Voltage-dependent L-type calcium channel subunit beta-3
- Voltage-dependent L-type calcium channel subunit alpha-1C/L-type calcium channel subunit beta-3/calcium channel subunit alpha-2/delta-1
Approval history
- approvedDec 28, 1990
Chemistry & pharmacology
SMILES
O.Cl.CC(C)COCC(CN(CC1=CC=CC=C1)C2=CC=CC=C2)N3CCCC3- Mol. weight
- 421.016 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Discontinued
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaBepridil ↗
- NCATS4W2P15D93M ↗
- ChEMBLCHEMBL81 ↗
- ChEMBLCHEMBL1200382 ↗
- ChEMBLCHEMBL1116 ↗
- ChEMBLCHEMBL1008 ↗
Also known as
- bepadin
- bepadin
- bepadin
- bepadin
- bepricol
- bepridil
- bepridil
- bepridil
- bepridil
- bepridil
- bepridil
- bepridil
- bepridil
- bepridil
- bepridil
- (+/-)-bepridil
- bepridil hcl
- bepridil hcl
- bepridil hcl
- bepridil hydrochloride
- bepridil hydrochloride
- bepridil hydrochloride
- bepridil hydrochloride
- bepridil hydrochloride hydrate
- bepridil hydrochloride hydrate
- bepridil hydrochloride hydrate
- bepridil hydrochloride hydrate
- bepridil hydrochloride hydrate
- bepridil hydrochloride hydrate
- bepridil monohydrochloride
- bepridil monohydrochloride monohydrate
- cerm-1978
- cerm-1978
- cordium
- dl-bepridil
- org 5730
- vascor
- vascor
Organizations
Marketing (3)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Carter-Wallace | For profit | NDA | Dec 28, 1990 |
| Johnson and Johnson | For profit | NDA2 | Dec 28, 1990 |
| Medpointe | For profit | NDA2 | Dec 28, 1990 |