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ROFECOXIB Drug Record

  • Summary
  • Interactions
  • Claims
  • ROFECOXIB chembl:CHEMBL122

    Alternate Names:

    ROFECOXIB
    M01AH02
    MK-966
    MK-0966
    VIOXX
    MK0966
    4-[4-(METHYLSULFONYL)PHENYL]-3-PHENYL-2(5H)-FURANONE
    CEOXX®
    VIOXX®
    3-PHENYL-4-[4-(METHYLSULFONYL)PHENYL]-2(5H)-FURANONE
    CEOXX
    MK 966
    4-[4-(METHYLSULFONYL)PHENYL]-3-PHENYLFURAN-2(5H)-ONE
    chembl:CHEMBL122
    pubchem.compound:5090
    drugbank:00533
    chemidplus:162011-90-7
    rxcui:232158

    Drug Info:

    FDA Approval withdrawn
    Drug Class small molecule
    Drug Indications NSAID
    Drug Groups approved
    Drug Categories agents causing hyperkalemia
    Drug Categories agents that produce hypertension
    Drug Categories cox-2 inhibitors
    Drug Categories cytochrome p-450 cyp1a2 inhibitors (strong)
    Drug Categories cytochrome p-450 cyp2c8 inhibitors
    Drug Categories cytochrome p-450 cyp2c8 inhibitors (weak)
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 cyp3a4 inducers
    Drug Categories cytochrome p-450 cyp3a4 inducers (strength unknown)
    Drug Categories cytochrome p-450 enzyme inducers
    Drug Categories cytochrome p-450 enzyme inhibitors
    Drug Categories cytochrome p-450 substrates
    Drug Categories nephrotoxic agents
    Drug Categories selective cyclooxygenase 2 inhibitors (nsaids)
    (6 More Sources)

    Publications:

    Brzozowski et al., 2006, Prostaglandin/cyclooxygenase pathway in ghrelin-induced gastroprotection against ischemia-reperfusion injury., J. Pharmacol. Exp. Ther.
    Oitate et al., 2007, Covalent binding of rofecoxib, but not other cyclooxygenase-2 inhibitors, to allysine aldehyde in elastin of human aorta., Drug Metab. Dispos.
    Oitate et al., 2007, Mechanism for covalent binding of rofecoxib to elastin of rat aorta., J. Pharmacol. Exp. Ther.
    Oitate et al., 2006, Covalent binding of radioactivity from [14C]rofecoxib, but not [14C]celecoxib or [14C]CS-706, to the arterial elastin of rats., Drug Metab. Dispos.
    Brzozowska et al., 2004, Healing of chronic gastric ulcers in diabetic rats treated with native aspirin, nitric oxide (NO)-derivative of aspirin and cyclooxygenase (COX)-2 inhibitor., J. Physiol. Pharmacol.
    Pyrko et al., 2006, Downregulation of survivin expression and concomitant induction of apoptosis by celecoxib and its non-cyclooxygenase-2-inhibitory analog, dimethyl-celecoxib (DMC), in tumor cells in vitro and in vivo., Mol. Cancer
    Konturek et al., 2003, Influence of COX-2 inhibition by rofecoxib on serum and tumor progastrin and gastrin levels and expression of PPARgamma and apoptosis-related proteins in gastric cancer patients., Dig. Dis. Sci.
    Langman et al., 1999, Adverse upper gastrointestinal effects of rofecoxib compared with NSAIDs., JAMA
    Matheson et al., 2001, Rofecoxib: a review of its use in the management of osteoarthritis, acute pain and rheumatoid arthritis., Drugs
    Malmstrom et al., 1999, Comparison of rofecoxib and celecoxib, two cyclooxygenase-2 inhibitors, in postoperative dental pain: a randomized, placebo- and active-comparator-controlled clinical trial., Clin Ther
    Ehrich et al., 1999, Effect of specific COX-2 inhibition in osteoarthritis of the knee: a 6 week double blind, placebo controlled pilot study of rofecoxib. Rofecoxib Osteoarthritis Pilot Study Group., J. Rheumatol.
    Pascucci, 1999, COX-2-specific inhibition: implications for clinical practice., J Am Osteopath Assoc
    Hawkey et al., 2000, Comparison of the effect of rofecoxib (a cyclooxygenase 2 inhibitor), ibuprofen, and placebo on the gastroduodenal mucosa of patients with osteoarthritis: a randomized, double-blind, placebo-controlled trial. The Rofecoxib Osteoarthritis Endoscopy Multinational Study Group., Arthritis Rheum.
    Ashok et al., 2011, Selective cyclooxygenase-2 (COX-2) inhibitors and breast cancer risk., Breast
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Baron et al., 2008, Cardiovascular events associated with rofecoxib: final analysis of the APPROVe trial., Lancet
    Chakraborti et al., 2010, Progress in COX-2 inhibitors: a journey so far., Curr. Med. Chem.
    Lee YS et al., 2006, Genetically mediated interindividual variation in analgesic responses to cyclooxygenase inhibitory drugs., Clin Pharmacol Ther
    Grosser T, 2009, Variability in the response to cyclooxygenase inhibitors: toward the individualization of nonsteroidal anti-inflammatory drug therapy., J Investig Med
    Ebert et al., 2005, Protective role of heat shock protein 27 in gastric mucosal injury., J. Pathol.
  • ROFECOXIB   ELN

    Interaction Score: 14.2

    Interaction Types & Directionality:
    other/unknown

    Interaction Info:

    PMIDs:
    17620346 17164475 16679386


    Sources:
    DrugBank

  • ROFECOXIB   GHRL

    Interaction Score: 1.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16868036


    Sources:
    NCI

  • ROFECOXIB   PTGS2

    Interaction Score: 1.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name rofecoxib,Vioxx
    Novel drug target Established target
    Specific Action of the Ligand Inhibition

    PMIDs:
    10580458 11398914 10566562 10555907 10643177 10693877 20724158 11752352 18922570 20166930 16678543 19602986


    Sources:
    PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

  • ROFECOXIB   IL10

    Interaction Score: 0.84

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15613743


    Sources:
    NCI

  • ROFECOXIB   BIRC5

    Interaction Score: 0.56

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16707021 14627349


    Sources:
    NCI

  • ROFECOXIB   HSPB1

    Interaction Score: 0.43

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16041694


    Sources:
    NCI

  • ROFECOXIB   BAX

    Interaction Score: 0.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14627349


    Sources:
    NCI

  • ROFECOXIB   ALDH1A1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DrugBank: DB00533

    • Version: 5.1.7

    Alternate Names:
    ROFECOXIB DrugBank Drug Name
    162011-90-7 CAS Number
    Vioxx Drug Brand

    Drug Info:
    Drug Type small molecule
    Drug Groups approved
    Drug Groups investigational

    Publications:
    Oitate et al., 2007, Covalent binding of rofecoxib, but not other cyclooxygenase-2 inhibitors, to allysine aldehyde in elastin of human aorta., Drug Metab. Dispos.
    Oitate et al., 2007, Mechanism for covalent binding of rofecoxib to elastin of rat aorta., J. Pharmacol. Exp. Ther.
    Oitate et al., 2006, Covalent binding of radioactivity from [14C]rofecoxib, but not [14C]celecoxib or [14C]CS-706, to the arterial elastin of rats., Drug Metab. Dispos.

  • TdgClinicalTrial: ROFECOXIB

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications NSAID
    Drug Class small molecule
    FDA Approval withdrawn

    Publications:

  • NCI: ROFECOXIB

    • Version: 14-September-2017

    Alternate Names:
    C1832 NCI drug code

    Drug Info:

    Publications:
    Brzozowska et al., 2004, Healing of chronic gastric ulcers in diabetic rats treated with native aspirin, nitric oxide (NO)-derivative of aspirin and cyclooxygenase (COX)-2 inhibitor., J. Physiol. Pharmacol.
    Pyrko et al., 2006, Downregulation of survivin expression and concomitant induction of apoptosis by celecoxib and its non-cyclooxygenase-2-inhibitory analog, dimethyl-celecoxib (DMC), in tumor cells in vitro and in vivo., Mol. Cancer
    Brzozowski et al., 2006, Prostaglandin/cyclooxygenase pathway in ghrelin-induced gastroprotection against ischemia-reperfusion injury., J. Pharmacol. Exp. Ther.

  • NCI: VIOXX

    • Version: 14-September-2017

    Alternate Names:
    C1832 NCI drug code

    Drug Info:

    Publications:
    Konturek et al., 2003, Influence of COX-2 inhibition by rofecoxib on serum and tumor progastrin and gastrin levels and expression of PPARgamma and apoptosis-related proteins in gastric cancer patients., Dig. Dis. Sci.

  • PharmGKB: rofecoxib

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Lee YS et al., 2006, Genetically mediated interindividual variation in analgesic responses to cyclooxygenase inhibitory drugs., Clin Pharmacol Ther
    Grosser T, 2009, Variability in the response to cyclooxygenase inhibitors: toward the individualization of nonsteroidal anti-inflammatory drug therapy., J Investig Med

  • DTC: ROFECOXIB

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL122 ChEMBL Drug ID

    Drug Info:

    Publications:

  • TTD: Rofecoxib

    • Version: 2020.06.01

    Alternate Names:
    D05VLS TTD Drug ID

    Drug Info:

    Publications:

  • GuideToPharmacology: 178100242

    • Version: 29-September-2020

    Alternate Names:
    ROFECOXIB GuideToPharmacology Ligand Name

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL122

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL122

    • Version: chembl_23

    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.

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