Raltitrexed

Raltitrexed

File:Raltitrexed.svg
Clinical data
ATC code	L01BA03 (WHO)
Identifiers
IUPAC name 2-[5-[methyl- [(2-methyl-4-oxo-1H- quinazolin-6-yl)methyl] amino] thiophen-2- yl] carbonylaminopentanedioic acid
CAS Number	112887-68-0
PubChem CID	104758
DrugBank	APRD00430
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C21H22N4O6S
Molar mass	458.489 g/mol

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Overview

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

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.