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Raltitrexed

Antimetabolite · Antineoplastic

AntimetaboliteAntineoplastic
CDSCO approved
EXCRETION
not curated
INTERACTIONS
none in our sources
PREGNANCY
Avoid (teratogenic in animal studies).
FDA category + note

Mechanism

Raltitrexed is a folate analog transported into cells primarily via the reduced folate transporter. Once inside, it undergoes polyglutamation. This polyglutamated form exhibits increased inhibitory potency against folate-dependent enzymes required for purine and thymidylate synthesis, thereby interfering with DNA synthesis and cellular proliferation.

Indications

Advanced colorectal cancer

Dosing

Renal adjustment
Avoid if creatinine clearance less than 30 mL/minute. Reduce dose in mild to moderate impairment (consult product literature).
Hepatic adjustment
Manufacturer advises caution (increased risk of accumulation).

Contraindications

  • Creatinine clearance less than 30 mL/minute
  • Pregnancy
  • Breast-feeding

Pregnancy & lactation

Pregnancy

Avoid (teratogenic in animal studies).

Lactation

Discontinue breast-feeding.

Related guidelines

Other Antimetabolite drugs

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Sources: BNF·Verified: 2026-05-10 · House clinical team