Raltitrexed

drugbox
IUPAC_name = 2- [5- [methyl- [(2-methyl-4-oxo-1H- quinazolin-6-yl)methyl] amino] thiophen-2- yl] carbonylaminopentanedioic acid

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CAS_number = 112887-68-0
ATC_prefix = L01
ATC_suffix = BA03
ATC_supplemental =
PubChem = 104758
DrugBank = APRD00430
C=21 | H=22 | N=4 | O=6 | S=1
molecular_weight = 458.489 g/mol
bioavailability =
protein_bound =
metabolism =
elimination_half-life =
excretion =
pregnancy_AU =
pregnancy_US =
pregnancy_category =
legal_AU =
legal_UK = POM
legal_US =
legal_status = Not available in U.S.
routes_of_administration = Intravenous

Raltitrexed (brand name Tomudex) is an antimetabolite drug used in cancer chemotherapy. It is an inhibitor of thymidylate synthase, and is manufactured by AstraZeneca.

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 enzyme used in pyrimidine synthesis —thymidylate synthase (TS). Raltitrexed is fully active after polyglutamylation. Inhibition of L1210 cell growth i culture IC₅₀ = 9 nM, is one of the strongest antimetabolite in use.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.