Overview
Rofecoxib is used for the treatment of osteoarthritis, rheumatoid arthritis, acute pain in adults, and primary dysmenorrhea, as well as acute treatment of migraine attacks with or without auras. Rofecoxib is a solid. This compound belongs to the stilbenes. These are organic compounds containing a 1,2-diphenylethylene moiety. Stilbenes (C6-C2-C6 ) are derived from the common phenylpropene (C6-C3) skeleton building block. The introduction of one or more hydroxyl groups to a phenyl ring lead to stilbenoids. Rofecoxib has a half-life of 17 hours and its mean oral bioavailability at therapeutically recommended doses of 125, 25, and 50 mg is approximately 93%. The proteins that rofecoxib target include elastin and prostaglandin G/H synthase 2. Cytochrome P450 1A2, Cytochrome P450 3A4, Cytochrome P450 2C9, Cytochrome P450 2C8, and Prostaglandin G/H synthase 1 are known to metabolize rofecoxib. On September 30, 2004, Merck voluntarily withdrew rofecoxib from the market because of concerns about increased risk of heart attack and stroke associated with long-term, high-dosage use.
Indication
For the treatment of osteoarthritis, rheumatoid arthritis, acute pain in adults, and primary dysmenorrhea, as well as acute treatment of migraine attacks with or without auras.
Associated Conditions
No associated conditions information available.
Research Report
Rofecoxib (DB00533): A Comprehensive Monograph on a Paradigm-Shifting COX-2 Inhibitor
Executive Summary
Rofecoxib, a small molecule drug developed by Merck & Co. and marketed as Vioxx, represents one of the most consequential narratives in modern pharmaceutical history. Launched in 1999 as a selective cyclooxygenase-2 (COX-2) inhibitor, it was heralded as a major therapeutic advancement, offering potent anti-inflammatory and analgesic effects for conditions like osteoarthritis and rheumatoid arthritis with a significantly improved gastrointestinal (GI) safety profile compared to traditional nonsteroidal anti-inflammatory drugs (NSAIDs).[1] This promise of "safer" pain relief propelled it to blockbuster status, with over 80 million prescriptions worldwide.[3]
The trajectory of Rofecoxib was irrevocably altered by findings from two pivotal clinical trials. The Vioxx Gastrointestinal Outcomes Research (VIGOR) trial, while confirming the drug's GI benefits, simultaneously revealed an unexpected and alarming fivefold increase in the risk of myocardial infarction compared to the non-selective NSAID naproxen.[4] This initial safety signal was intensely debated, with the manufacturer initially attributing the finding to a cardioprotective effect of naproxen rather than a cardiotoxic effect of Rofecoxib. However, the definitive evidence emerged from the Adenomatous Polyp Prevention on Vioxx (APPROVe) trial. Though designed to study colon polyp prevention, APPROVe demonstrated that long-term use of Rofecoxib at a standard therapeutic dose nearly doubled the risk of serious thrombotic cardiovascular events compared to placebo.[6]
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2013/01/08 | Not Applicable | Completed | Hospital Universitario Pedro Ernesto | ||
2009/02/16 | Phase 2 | Terminated | Oslo University Hospital | ||
2008/04/14 | Phase 4 | Terminated | |||
2008/03/18 | Phase 3 | Completed | |||
2008/03/18 | Phase 4 | Completed | |||
2007/12/06 | Phase 3 | Completed | |||
2006/10/11 | Phase 2 | Completed | National Cancer Institute, Naples | ||
2005/12/07 | Not Applicable | Completed | |||
2005/12/05 | Phase 4 | Completed | |||
2005/09/12 | Phase 4 | Completed |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| No FDA approvals found for this drug. | |||||
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
| No EMA approvals found for this drug. | |||
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No HSA approvals found for this drug. | |||||
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| No TGA approvals found for this drug. | |||||
Health Canada Drug Approvals
Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
|---|---|---|---|---|---|
| VIOXX TAB 12.5MG | merck frosst canada & cie, merck frosst canada & co. | 02241107 | Tablet - Oral | 12.5 MG / TAB | 11/8/1999 |
| VIOXX TAB 25MG | merck frosst canada & cie, merck frosst canada & co. | 02241108 | Tablet - Oral | 25 MG / TAB | 11/8/1999 |
| VIOXX SUSPENSION 12.5MG/5ML | merck frosst canada & cie, merck frosst canada & co. | 02241109 | Suspension - Oral | 12.5 MG / 5 ML | 5/8/2000 |
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
|---|---|---|---|---|---|
| No CIMA AEMPS (Spain) approvals found for this drug. | |||||
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Philippines FDA approvals found for this drug. | |||||
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Saudi SFDA approvals found for this drug. | |||||
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Malaysia NPRA approvals found for this drug. | |||||
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
|---|---|---|---|---|---|
| No UK EMC drug information found for this drug. | |||||
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