Active Ingredient History
Raltegravir (RAL, Isentress, formerly MK-0518) is an antiretroviral drug produced by Merck & Co., used to treat HIV and it is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in patients 4 weeks of age and older. Raltegravir inhibits the catalytic activity of HIV-1 integrase, an HIV-1 encoded enzyme that is required r viral replication. Inhibition of integrase prevents the covalent insertion, or integration, of unintegrated linear HIV-1 DNA into the host cell genome preventing the formation of the HIV-1 provirus. The provirus is required to direct the production of progeny virus, so inhibiting integration prevents propagation of the viral infection. Raltegravir did not significantly inhibit human phosphoryl transferases including DNA polymerases α, β, and γ. Coadministration with others drugs that are strong inducers of UGT1A1, such as rifampin, may result in reduced plasma concentrations of raltegravir. The most common adverse reactions of moderate to severe intensity (≥2%) are insomnia, headache, dizziness, nausea and fatigue. Severe, potentially life-threatening, and fatal skin reactions have been reported. This include cases of Stevens-Johnson syndrome and toxic epidermal necrolysis. Hypersensitivity reactions have also been reported and were characterized by rash, constitutional findings, and sometimes, organ dysfunction, including hepatic failure. The major mechanism of clearance of raltegravir in humans is UGT1A1-mediated glucuronidation. NCATS
Drug Pricing (per unit)
Note: This drug pricing data is preliminary, incomplete, and may contain errors.
Combination drugs
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
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| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
Acquired Immunodeficiency Syndrome (Phase 4)
Amyotrophic Lateral Sclerosis (Phase 1)
Antiretroviral Therapy, Highly Active (Phase 2)
Bone Diseases, Metabolic (Phase 4)
Cardiovascular Diseases (Phase 4)
Cognitive Dysfunction (Phase 1)
Depression (Phase 1)
Endothelial Cells (Phase 4)
Fatty Liver (Phase 4)
Head and Neck Neoplasms (Early Phase 1)
Healthy Volunteers (Phase 4)
Hepacivirus (Phase 1)
Hepatitis C (Phase 4)
Hepatitis C, Chronic (Phase 4)
HIV (Phase 4)
HIV-1 (Phase 4)
HIV Seropositivity (Phase 4)
HTLV-I Infections (Early Phase 1)
Hypercholesterolemia (Phase 1)
Hyperlipidemias (Phase 3)
Hypertriglyceridemia (Phase 3)
Infections (Phase 3)
Inflammation (Phase 4)
Infusions, Intravenous (Phase 2)
Leukemia (Phase 2)
Leukemia-Lymphoma, Adult T-Cell (Phase 1/Phase 2)
Lipodystrophy (Phase 2)
Liver Cirrhosis (Phase 2)
Liver Cirrhosis, Biliary (Phase 2)
Liver Failure (Phase 1/Phase 2)
Liver Transplantation (Phase 1/Phase 2)
Metabolic Syndrome (Phase 4)
Multiple Sclerosis, Relapsing-Remitting (Phase 2)
Neoplasms (Phase 4)
Non-alcoholic Fatty Liver Disease (Phase 4)
Osteoporosis (Phase 4)
Paraparesis, Tropical Spastic (Early Phase 1)
Pharmacokinetics (Phase 1)
Pregnancy (Phase 2/Phase 3)
Quality of Life (Phase 4)
Renal Insufficiency, Chronic (Phase 3)
Tuberculosis (Phase 4)
Viremia (Phase 3)
| Trial | Phase | Start Date | Organizations | Indications |
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