Raltitrexed

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Raltitrexed
File:Raltitrexed.png
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Clinical data
AHFS/Drugs.comMicromedex Detailed Consumer Information
Routes of
administration
Intravenous
ATC code
Legal status
Legal status
  • UK: POM (Prescription only)
  • Not available in U.S.
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
PDB ligand
E number{{#property:P628}}
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Chemical and physical data
FormulaC21H22N4O6S
Molar mass458.489 g/mol
3D model (JSmol)
  (verify)

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

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.




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