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Raltitrexed



Raltitrexed
Systematic (IUPAC) name
2-[5-[methyl- [(2-methyl-4-oxo-1H- quinazolin-6-yl)methyl] amino] thiophen-2- yl] carbonylaminopentanedioic 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  ?
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Excretion  ?
Therapeutic considerations
Pregnancy cat.

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Legal status
Routes  ?

Raltitrexed (brand name Tomudex®) is a chemotherapy drug manufactured AstraZeneca Company, is an antimetabolite used in chemotherapy. It is an inhibitor of thymidylate synthase.

Additional recommended knowledge

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.



 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Raltitrexed". A list of authors is available in Wikipedia.
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