Bepridil

Bepridil (trade name Vascor) is an amine calcium channel blocker once used to treat angina. It is no longer sold in the United States.

Bepridil
Clinical data
Trade namesVascor
AHFS/Drugs.comMonograph
MedlinePlusa699051
Pregnancy
category
  • US: C (Risk not ruled out)
    Routes of
    administration
    Oral
    ATC code
    Pharmacokinetic data
    BioavailabilityWell absorbed
    Protein binding99%
    MetabolismHepatic, CYP3A4-mediated
    Elimination half-life42 hours
    ExcretionRenal
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    Chemical and physical data
    FormulaC24H34N2O
    Molar mass366.549 g·mol−1
    3D model (JSmol)
      (verify)

    It is nonselective.[1]

    It has been discussed as a possible option in the treatment of atrial fibrillation.[2]

    It has been implicated in causing ventricular arrhythmia (torsades de pointes).

    Ebola research

    In June 2015 a research paper [3] was published finding bepridil to result in a 100% survival rate for mice exposed to ebola during an experiment searching for potential pharmaceutical ebola treatments; indicating its potential use in future ebola research and therapy.[4]

    References

    1. Bezprozvanny I, Tsien RW (September 1995). "Voltage-dependent blockade of diverse types of voltage-gated Ca2+ channels expressed in Xenopus oocytes by the Ca2+ channel antagonist mibefradil (Ro 40-5967)". Mol. Pharmacol. 48 (3): 540–9. PMID 7565636.
    2. Imai S, Saito F, Takase H, et al. (May 2008). "Use of bepridil in combination with Ic antiarrhythmic agent in converting persistent atrial fibrillation to sinus rhythm". Circ. J. 72 (5): 709–15. doi:10.1253/circj.72.709. PMID 18441448.
    3. Johansen, Lisa M.; Dewald, Lisa Evans; Shoemaker, Charles J.; Hoffstrom, Benjamin G.; Lear-Rooney, Calli M.; Stossel, Andrea; Nelson, Elizabeth; Delos, Sue E.; Simmons, James A.; Grenier, Jill M.; Pierce, Laura T.; Pajouhesh, Hassan; Lehár, Joseph; Hensley, Lisa E.; Glass, Pamela J.; White, Judith M.; Olinger, Gene G. (2015). "A screen of approved drugs and molecular probes identifies therapeutics with anti–Ebola virus activity". Science Translational Medicine. 7 (290): 290ra89. doi:10.1126/scitranslmed.aaa5597. PMID 26041706.
    4. "Zoloft as Ebola cure? Antidepressant is one of a number of promising drugs being looked at by scientists".


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