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VERAPAMIL Drug Record

  • Summary
  • Interactions
  • Claims
  • VERAPAMIL chembl:CHEMBL6966 ApprovedAntineoplastic

    Alternate Names:

    VERAPAMIL
    VERELAN
    CP-165331
    NSC-272306NA
    CP-16533-1
    TARKA
    ISOPTIN
    D-365
    COVERA-HS
    IPROVERATRIL
    CALAN
    VERAPAMILO
    SECURON®
    CP-165331 / CP-16533-1
    ANSYR®
    VERAPAMILUM
    VÉRAPAMIL
    pubchem.compound:2520
    rxcui:11170
    drugbank:00661
    chemidplus:52-53-9
    chembl:CHEMBL6966

    Drug Info:

    Drug Class anti-arrhythmia agents
    Year of Approval 1981
    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications antihypertensive agent
    (3 More Sources)

    Publications:

    Tfelt-Hansen et al., 2009, Verapamil for cluster headache. Clinical pharmacology and possible mode of action., Headache
    Morel et al., 1998, The action of calcium channel blockers on recombinant L-type calcium channel alpha1-subunits., Br. J. Pharmacol.
    Dilmac et al., 2004, Molecular determinants of frequency dependence and Ca2+ potentiation of verapamil block in the pore region of Cav1.2., Mol. Pharmacol.
    Patel et al., 2005, Effect of serum withdrawal on the contribution of L-type calcium channels (CaV1.2) to intracellular Ca2+ responses and chemotaxis in cultured human vascular smooth muscle cells., Br. J. Pharmacol.
    Beitelshees AL et al., 2009, CACNA1C gene polymorphisms, cardiovascular disease outcomes, and treatment response., Circ Cardiovasc Genet
    Bacon et al., 1989, Potent and specific inhibition of IL-8-, IL-1 alpha- and IL-1 beta-induced in vitro human lymphocyte migration by calcium channel antagonists., Biochem. Biophys. Res. Commun.
    Xu et al., 2008, Effect of amiodarone on Kv1.4 channel C-type inactivation: comparison of its effects with those induced by propafenone and verapamil., Pharmazie
    van Noord C et al., 2009, Calcium channel blockers, NOS1AP, and heart-rate-corrected QT prolongation., Pharmacogenet Genomics
    Dahllöf et al., Characterization of multidrug resistance in SEWA mouse tumor cells: increased glutathione transferase activity and reversal of resistance with verapamil., Anticancer Res.
    Aguirre Ghiso et al., 1998, Secretion of urokinase and metalloproteinase-9 induced by staurosporine is dependent on a tyrosine kinase pathway in mammary tumor cells., Int. J. Cancer
    Freeze et al., 2006, State-dependent verapamil block of the cloned human Ca(v)3.1 T-type Ca(2+) channel., Mol. Pharmacol.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Bergson P et al., 2011, Verapamil block of T-type calcium channels., Mol Pharmacol
    Shchepotin et al., Apoptosis induced by hyperthermia and verapamil in vitro in a human colon cancer cell line., Int J Hyperthermia
    Gong Y et al., 2015, PTPRD gene associated with blood pressure response to atenolol and resistant hypertension., J Hypertens
    Jacob et al., 1996, Effects of trandolapril and verapamil on glucose transport in insulin-resistant rat skeletal muscle., Metab. Clin. Exp.
    Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev
    Li P et al., 2011, A refined cytochrome P540 IC₅₀ shift assay for reliably identifying CYP3A time-dependent inhibitors., Drug Metab Dispos
    Collett et al., 1999, Modulation of the permeability of H2 receptor antagonists cimetidine and ranitidine by P-glycoprotein in rat intestine and the human colonic cell line Caco-2., J. Pharmacol. Exp. Ther.
    Mickisch et al., 1991, Transgenic mice that express the human multidrug-resistance gene in bone marrow enable a rapid identification of agents that reverse drug resistance., Proc. Natl. Acad. Sci. U.S.A.
    Colabufo NA et al., 2008, Synthesis and biological evaluation of (hetero)arylmethyloxy- and arylmethylamine-phenyl derivatives as potent P-glycoprotein modulating agents., J Med Chem
    Nesi G et al., 2014, SAR study on arylmethyloxyphenyl scaffold: looking for a P-gp nanomolar affinity., Eur J Med Chem
    Perestelo NR et al., 2011, Overcoming human P-glycoprotein-dependent multidrug resistance with novel dihydro-β-agarofuran sesquiterpenes., Eur J Med Chem
    Chae SW et al., 2015, Xanthone analogues as potent modulators of intestinal P-glycoprotein., Eur J Med Chem
    Marks KM et al., 2011, The selectivity of austocystin D arises from cell-line-specific drug activation by cytochrome P450 enzymes., J Nat Prod
    Tang X et al., 2012, Synthesis and evaluation of nitric oxide-releasing DDB derivatives as potential Pgp-mediated MDR reversal agents in MCF-7/Adr cells., Bioorg Med Chem Lett
    Gu X et al., 2012, Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors., Eur J Med Chem
    Gu X et al., 2012, Synthesis and biological evaluation of bifendate-chalcone hybrids as a new class of potential P-glycoprotein inhibitors., Bioorg Med Chem
    Liu XL et al., 2008, Functionalized chalcones as selective inhibitors of P-glycoprotein and breast cancer resistance protein., Bioorg Med Chem
    Nievergelt A et al., 2010, Identification of serotonin 5-HT1A receptor partial agonists in ginger., Bioorg Med Chem
    Lou K et al., 2014, Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies., J Med Chem
    Liu J et al., 2013, 20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs., Bioorg Med Chem
    Silva GL et al., 2001, Modulation of the multidrug-resistance phenotype by new tropane alkaloid aromatic esters from Erythroxylum pervillei., J Nat Prod
    Walz et al., 1989, Similar effects of cyclosporine and verapamil on lymphokine, interleukin 2 receptor, and proto-oncogene expression., Transplantation
    Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
    Liu et al., 2003, Calmodulin is involved in heat shock signal transduction in wheat., Plant Physiol.
    Chang SW et al., 2018, Genome-wide association study identifies pharmacogenomic loci linked with specific antihypertensive drug treatment and new-onset diabetes., Pharmacogenomics J
    Vandell AG et al., 2012, G protein receptor kinase 4 polymorphisms: β-blocker pharmacogenetics and treatment-related outcomes in hypertension., Hypertension
    Nielsen T et al., 2008, The KCNMB1 Glu65Lys polymorphism associates with reduced systolic and diastolic blood pressure in the Inter99 study of 5729 Danes., J Hypertens
    Zhao Q et al., 2008, Interactions among genetic variants from contractile pathway of vascular smooth muscle cell in essential hypertension susceptibility of Chinese Han population., Pharmacogenet Genomics
    Beitelshees AL et al., 2007, KCNMB1 genotype influences response to verapamil SR and adverse outcomes in the INternational VErapamil SR/Trandolapril STudy (INVEST)., Pharmacogenet Genomics
    Wong IL et al., 2009, Modulation of multidrug resistance protein 1 (MRP1/ABCC1)-mediated multidrug resistance by bivalent apigenin homodimers and their derivatives., J Med Chem
    Perrotton T et al., 2007, (R)- and (S)-verapamil differentially modulate the multidrug-resistant protein MRP1., J Biol Chem
    Price ET et al., 2011, Liver X receptor α gene polymorphisms and variable cardiovascular outcomes in patients treated with antihypertensive therapy: results from the INVEST-GENES study., Pharmacogenet Genomics
    Block et al., 1993, Transcriptional activation of low density lipoprotein receptor gene by angiotensin-converting enzyme inhibitors and Ca(2+)-channel blockers involves protein kinase C isoforms., Proc. Natl. Acad. Sci. U.S.A.
    Takemura et al., 1992, Effect of verapamil on the class I major histocompatibility complex antigen expression in K562 chronic myelogenous leukemia cells treated with recombinant human interferon-gamma., Cancer Lett.
    Tsukamoto et al., 1987, Effect of calcium channel blockers and trifluoperazine on rat liver regeneration., Eur. J. Pharmacol.
  • VERAPAMIL   KCNMB1

    Interaction Score: 7.27

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18854753 18496125 17700361


    Sources:
    PharmGKB

  • VERAPAMIL   KCNIP1

    Interaction Score: 7.27

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18854753 18496125 17700361


    Sources:
    PharmGKB

  • VERAPAMIL   PLEKHH2

    Interaction Score: 1.82

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27670767


    Sources:
    PharmGKB

  • VERAPAMIL   GRK4

    Interaction Score: 1.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22949529


    Sources:
    PharmGKB

  • VERAPAMIL   PTPRD

    Interaction Score: 0.73

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26425837


    Sources:
    PharmGKB

  • VERAPAMIL   NOS1AP

    Interaction Score: 0.73

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19247217


    Sources:
    PharmGKB

  • VERAPAMIL   KCNA4

    Interaction Score: 0.73

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18604993


    Sources:
    NCI

  • VERAPAMIL   CACNA1G

    Interaction Score: 0.64

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    16699084 19125880 11752352 21149638


    Sources:
    TEND TTD

  • VERAPAMIL   CACNB1

    Interaction Score: 0.61

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Verapamil,Calan, Covera-HS
    Novel drug target Established target

    PMIDs:
    19125880


    Sources:
    TdgClinicalTrial TEND

  • VERAPAMIL   CACNB3

    Interaction Score: 0.61

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Verapamil,Calan, Covera-HS
    Novel drug target Established target

    PMIDs:
    19125880


    Sources:
    TdgClinicalTrial TEND

  • VERAPAMIL   CACNB4

    Interaction Score: 0.61

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Verapamil,Calan, Covera-HS
    Novel drug target Established target

    PMIDs:
    19125880


    Sources:
    TdgClinicalTrial TEND

  • VERAPAMIL   CACNB2

    Interaction Score: 0.55

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name Verapamil,Calan, Covera-HS

    PMIDs:
    19125880


    Sources:
    TdgClinicalTrial TEND

  • VERAPAMIL   CACNA1C

    Interaction Score: 0.47

    Interaction Types & Directionality:
    blocker (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Verapamil,Calan, Covera-HS
    Novel drug target Established target

    PMIDs:
    19125880 9846638 15286207 15880143 20031608


    Sources:
    TdgClinicalTrial TEND PharmGKB

  • VERAPAMIL   CACNA1I

    Interaction Score: 0.34

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    17016423 17139284


    Sources:
    TEND

  • VERAPAMIL   CACNA1F

    Interaction Score: 0.24

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Verapamil,Calan, Covera-HS
    Novel drug target Established target

    PMIDs:
    19125880


    Sources:
    TdgClinicalTrial TEND

  • VERAPAMIL   CACNA1D

    Interaction Score: 0.23

    Interaction Types & Directionality:
    blocker (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name Verapamil,Calan, Covera-HS

    PMIDs:
    19125880


    Sources:
    TdgClinicalTrial TEND

  • VERAPAMIL   NR1H3

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21562465


    Sources:
    PharmGKB

  • VERAPAMIL   CACNA1S

    Interaction Score: 0.18

    Interaction Types & Directionality:
    blocker (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Verapamil,Calan, Covera-HS
    Novel drug target Established target

    PMIDs:
    19125880


    Sources:
    TdgClinicalTrial TEND

  • VERAPAMIL   LDLR

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    7683421


    Sources:
    NCI

  • VERAPAMIL   CACNG1

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TEND

  • VERAPAMIL   PLAU

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9579573


    Sources:
    NCI

  • VERAPAMIL   ABCB1

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9862768 1671173 18257545 24607999 21856049 25686592 21348461 22209486 22405646 22429509 17964170 20363635 24992153 23683834 11754602


    Sources:
    DTC NCI

  • VERAPAMIL   IL2RA

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    2645720


    Sources:
    NCI

  • VERAPAMIL   HSPA4

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12857801


    Sources:
    NCI

  • VERAPAMIL   ABCC1

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19725578 17646169


    Sources:
    DTC

  • VERAPAMIL   TYMS

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    3436366


    Sources:
    NCI

  • VERAPAMIL   IL1B

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    2686646


    Sources:
    NCI

  • VERAPAMIL   MYC

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    1511424


    Sources:
    NCI

  • VERAPAMIL   SLC2A4

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8622594


    Sources:
    NCI

  • VERAPAMIL   BAX

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9354939


    Sources:
    NCI

  • VERAPAMIL   GSTP1

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    3566185


    Sources:
    NCI

  • VERAPAMIL   CXCL8

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    2686646


    Sources:
    NCI

  • VERAPAMIL   TGFB1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    NCI

  • VERAPAMIL   CYP3A4

    Interaction Score: 0.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    9187528 21393461


    Sources:
    DTC PharmGKB

  • TdgClinicalTrial: VERAPAMIL

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications antihypertensive agent
    Drug Class Small Molecule
    FDA Approval approved

    Publications:

  • TEND: VERAPAMIL

    • Version: 01-August-2011

    Alternate Names:

    Drug Info:
    Year of Approval 1981
    Drug Class anti-arrhythmia agents

    Publications:

  • DTC: VERAPAMIL

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL6966 ChEMBL Drug ID

    Drug Info:

    Publications:
    Nesi G et al., 2014, SAR study on arylmethyloxyphenyl scaffold: looking for a P-gp nanomolar affinity., Eur J Med Chem
    Gu X et al., 2012, Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors., Eur J Med Chem
    Marks KM et al., 2011, The selectivity of austocystin D arises from cell-line-specific drug activation by cytochrome P450 enzymes., J Nat Prod

  • NCI: VERAPAMIL

    • Version: 14-September-2017

    Alternate Names:
    C928 NCI drug code

    Drug Info:

    Publications:
    Bacon et al., 1989, Potent and specific inhibition of IL-8-, IL-1 alpha- and IL-1 beta-induced in vitro human lymphocyte migration by calcium channel antagonists., Biochem. Biophys. Res. Commun.
    Liu et al., 2003, Calmodulin is involved in heat shock signal transduction in wheat., Plant Physiol.
    Collett et al., 1999, Modulation of the permeability of H2 receptor antagonists cimetidine and ranitidine by P-glycoprotein in rat intestine and the human colonic cell line Caco-2., J. Pharmacol. Exp. Ther.

  • PharmGKB: verapamil

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Chang SW et al., 2018, Genome-wide association study identifies pharmacogenomic loci linked with specific antihypertensive drug treatment and new-onset diabetes., Pharmacogenomics J
    Zhao Q et al., 2008, Interactions among genetic variants from contractile pathway of vascular smooth muscle cell in essential hypertension susceptibility of Chinese Han population., Pharmacogenet Genomics
    Beitelshees AL et al., 2007, KCNMB1 genotype influences response to verapamil SR and adverse outcomes in the INternational VErapamil SR/Trandolapril STudy (INVEST)., Pharmacogenet Genomics

  • TTD: Verapamil

    • Version: 2020.06.01

    Alternate Names:
    D0R0FE TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL6966

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21