DGIdb - ROFECOXIB Drug Record

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FDA Approval	withdrawn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:

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

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

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational

ROFECOXIB Drug Record

ROFECOXIB chembl:CHEMBL122

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: other/unknown

Interaction Info:

PMIDs: 17620346 17164475 16679386

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16868036

Sources: NCI

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15613743

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16707021 14627349

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16041694

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 14627349

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

DrugBank: DB00533

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

TdgClinicalTrial: ROFECOXIB

Alternate Names:

Drug Info: Drug Indications NSAID Drug Class small molecule FDA Approval withdrawn

Publications:

NCI: ROFECOXIB

Alternate Names: C1832 NCI drug code

Drug Info:

NCI: VIOXX

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

Alternate Names:

Drug Info:

DTC: ROFECOXIB

Alternate Names: CHEMBL122 ChEMBL Drug ID

Drug Info:

Publications:

TTD: Rofecoxib

Alternate Names: D05VLS TTD Drug ID

Drug Info:

Publications:

GuideToPharmacology: 178100242

Alternate Names: ROFECOXIB GuideToPharmacology Ligand Name

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL122

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL122

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

other/unknown

PMIDs:
17620346 17164475 16679386

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
16868036

Sources:
NCI

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

Interaction Types & Directionality:

n/a

PMIDs:
15613743

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
16707021 14627349

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
16041694

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
14627349

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

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

Drug Info:

Drug Indications NSAID

Drug Class small molecule

FDA Approval withdrawn

Alternate Names:

C1832 NCI drug code

Alternate Names:

C1832 NCI drug code

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.

Alternate Names:

CHEMBL122 ChEMBL Drug ID

Alternate Names:

D05VLS TTD Drug ID

Alternate Names:

ROFECOXIB GuideToPharmacology Ligand Name