Active Ingredient History
Capecitabine is a fluoropyrimidine carbamate with antineoplastic activity. It is an orally administered systemic prodrug which is converted to 5-fluorouracil (5-FU). Both normal and tumor cells metabolize 5-FU to 5-fluoro-2’-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). These metabolites cause cell injury by two different mechanisms. First, FdUMP and the folate cofactor, N5-10-methylenetetrahydrofolate, bind to thymidylate synthase (TS) to form a covalently bound ternary complex. This binding inhibits the formation of thymidylate from 2’-deoxyuridylate. Thymidylate is the necessary precursor of thymidine triphosphate, which is essential for the synthesis of DNA, so that a deficiency of this compound can inhibit cell division. Second, nuclear transcriptional enzymes can mistakenly incorporate FUTP in place of uridine triphosphate (UTP) during the synthesis of RNA. This metabolic error can interfere with RNA processing and protein synthesis. Most common adverse reactions (≥30%) were diarrhea, hand-and-foot syndrome, nausea, vomiting, abdominal pain, fatigue/weakness, and hyperbilirubinemia. The concentration of 5-fluorouracil is increased and its toxicity may be enhanced by leucovorin. NCATS
Drug Pricing (per unit)
Note: This drug pricing data is preliminary, incomplete, and may contain errors.
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 |
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Breast Neoplasms (approved 1998)
Candidiasis (approved 1971)
Colorectal Neoplasms (approved 1998)
Endocarditis (approved 1971)
Meningitis, Cryptococcal (approved 1971)
Pulmonary Infarction (approved 1971)
Urinary Tract Infections (approved 1971)
Antifungal Agents (Phase 4)
Astrocytoma (Phase 2/Phase 3)
Brain Neoplasms (Phase 1/Phase 2)
Breast Neoplasms (Phase 2)
Carcinoma, Hepatocellular (Phase 1)
Carcinoma, Non-Small-Cell Lung (Phase 1)
Colorectal Neoplasms (Phase 1/Phase 2)
Cryptococcus (Phase 2)
Digestive System Neoplasms (Phase 1/Phase 2)
Glioblastoma (Phase 2/Phase 3)
Glioma (Phase 1)
Gliosarcoma (Phase 1)
Head and Neck Neoplasms (Phase 2)
HIV (Phase 2/Phase 3)
HIV Infections (Phase 3)
Leukemia, Myeloid, Acute (Phase 1)
Lung Neoplasms (Phase 2)
Lymphoma (Phase 1)
Melanoma (Phase 1)
Meningitis, Cryptococcal (Phase 4)
Methylation (Phase 1)
Myelodysplastic Syndromes (Phase 1)
Neoplasms (Phase 1/Phase 2)
Oligodendroglioma (Phase 2/Phase 3)
Ovarian Neoplasms (Phase 1)
Pancreatic Neoplasms (Phase 1)
Sarcoma (Phase 1)
Triple Negative Breast Neoplasms (Phase 1)
Urinary Bladder Neoplasms (Phase 2)
Trial | Phase | Start Date | Organizations | Indications |
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