Raltitrexed
- Atc Codes:L01BA03
- CAS Codes:112887-68-0
- PHARMGKB ID:112887-68-0
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Tomudex; Belgium: Tomudex; Czech Republic: Tomudex; France: Tomudex; Hungary: Tomudex; Ireland: Tomudex; Italy: Tomudex; Latvia: Tomudex; Luxembourg: Tomudex; Poland: Tomudex; Portugal: Tomudex; Spain: Tomudex; UK: Tomudex.
North America
Canada: Tomudex.
Latin America
Brazil: Tomudex.
Drug combinations
Chemistry
Raltitrexed: C~21~H~22~N~4~O~6~S. Mw: 458.49. (1) L-Glutamic acid, N-[[5-[[(1,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]methylamino]-2-thienyl]carbonyl]-; (2) N-[5-[[(3,4-Dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]methylamino]-2-thenoyl]-L-glutamic acid. CAS-112887-68-0 (1996).
Pharmacologic Category
Antineoplastic Agents; Antimetabolites. (ATC-Code: L01BA03).
Mechanism of action
A folate analog which inhibits thymidylate synthase, blocking purine synthesis. This results in overall inhibition of DNA synthesis.
Therapeutic use
Treatment of advanced colorectal neoplasms.
Pregnancy and lactiation implications
Pregnancy should be avoided during, and for 6 months following treatment. Pregnant women should not handle this medication. Excretion in breast milk unknown (contraindicated in nursing women).
Unlabeled use
Undergoing clinical trials for a variety of neoplasms, including breast, colorectal non-small cell lung, ovarian and pancreatic cancers.
Contraindications
Hypersensitivity to raltitrexed or any component of the formulation. Uncontrolled diarrhea. Severe renal or hepatic impairment. Pregnancy or breast-feeding.
Warnings and precautions
Use with caution in malaise/weakness. Use with caution in history of gastrointestinal problems (particularly diarrhea), and in mild-to-moderate hepatic impairment. Therapy interruption required in hepatotoxicity. Use with caution in renal impairment, and in patients heavily pre-treated with chemotherapy or radiation, especially if myelosuppression, stomatitis, hepatic or renal toxicities persist. Folinic acid, folic acid, or folate-containing medications (e.g. multivitamins) may interfere with raltitrexed.