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| Systematic (IUPAC) name | |
|---|---|
| N-[(5-{methyl[(2-methyl-4-oxo-1,4-dihydroquinazolin-6-yl)methyl]amino}-2-thienyl)carbonyl]-L-glutamic acid | |
| Identifiers | |
| CAS number | 112887-68-0 |
| ATC code | L01BA03 |
| PubChem | 104758 |
| DrugBank | APRD00430 |
| Chemical data | |
| Formula | C21H22N4O6S |
| Mol. mass | 458.489 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status | |
| Routes | Intravenous |
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Raltitrexed (brand name Tomudex) is an antimetabolite drug used in cancer chemotherapy. It is an inhibitor of thymidylate synthase, and is manufactured by AstraZeneca.[1]
Uses
Used in treatment of colorectal cancer since 1998.
Mechanism of action
Raltitrexed is chemically similar to folic acid and is in the class of chemotherapy drugs called folate antimetabolites. It works by inhibiting Dihydrofolate reductase, an enzyme used in the synthesis of tetrahydrofolate, thereby preventing the synthesis of thymidylate. Raltitrexed is fully active after polyglutamylation. By inhibiting the formation of precursor pyrimidine nucleotides, raltitrexed prevents the formation of DNA and RNA, which are required for the growth and survival of both normal cells and cancer cells.
Inhibition of L1210 cell growth in culture IC50 = 9 nM, is one of the strongest antimetabolites in use.
Structure and phase I clinical trial described in 1986.[2]
References
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