Raltitrexed

CrCl (mL/min)	Dosage
<25	Contraindicated.
25-54	Reduce to 50% once every 4 weeks.
55-65	Reduce to 75% once every 4 weeks.

Severe: Contraindicated.

Powder for solution for infusion: Reconstitute vial with 4 mL of sterile water for injection to a concentration of 0.5 mg/mL. Further dilute with 50-250 mL of NaCl 0.9% or dextrose 5% in water.

Severe renal and hepatic impairment. Pregnant or women who may become pregnant during treatment. Lactation. Concomitant use with calcium folinate, folic acid, or vitamin preparations containing these agents.

Patient with preexisting bone marrow suppression, poor general condition, and those who have undergone radiation therapy. Mild to moderate renal and hepatic impairment. Elderly.

Significant: Bone marrow suppression (e.g. neutropenia, leucopenia, anaemia, thrombocytopenia), diarrhoea, mucositis, stomatitis, malaise, weakness, ALT/AST elevations.
Eye disorders: Conjunctivitis.
Gastrointestinal disorders: Mouth ulceration, nausea, vomiting, constipation, dyspepsia, abdominal pain, gastrointestinal bleeding.
General disorders and administration site conditions: Asthenia, fever, pain, peripheral oedema.
Hepatobiliary disorders: Hyperbilirubinaemia.
Infections and infestations: Flu-like syndrome, cellulitis, sepsis.
Investigations: Increased transaminases, alkaline phosphatase; weight loss.
Metabolism and nutrition disorders: Anorexia, dehydration.
Musculoskeletal and connective tissue disorders: Arthralgia.
Nervous system disorders: Headache, hypertonia, taste perversion.
Skin and subcutaneous tissue disorders: Rash, pruritus, alopecia, sweating.
Potentially Fatal: Severe diarrhoea with neutropenia.

This medicine may cause malaise or weakness, if affected, do not drive or operate machinery.

Monitor CBC with differential at baseline, before each treatment, or weekly in the occurrence of gastrointestinal toxicity; hepatic function and serum creatinine at baseline and before each treatment. Closely monitor for signs of gastrointestinal toxicity (e.g. diarrhoea, mucositis).

Potentially Fatal: Diminished therapeutic effect with calcium folinate, folic acid, or vitamin preparations containing these agents.

Description:
Mechanism of Action: Raltitrexed, a folate analogue which causes inhibition of DNA synthesis and cell death by acting as a direct and specific thymidylate synthase inhibitor.
Pharmacokinetics:
Distribution: Plasma protein binding: 93%.
Metabolism: Metabolised intracellularly into active polyglutamate forms.
Excretion: Mainly via urine (approx 50% as unchanged drug); faeces (approx 15%). Terminal elimination half-life: 198 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 135400182, Raltitrexed. https://pubchem.ncbi.nlm.nih.gov/compound/Raltitrexed. Accessed Feb. 24, 2026.

Powder for solution for infusion: Store intact vials below 25°C. Protect from light. Reconstituted solutions and diluted solutions for infusion: Store between 2-8°C for 24 hours. This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.

Cytotoxic Chemotherapy

L01BA03 - raltitrexed ; Belongs to the class of antimetabolites, folic acid analogues. Used in the treatment of cancer.

Brayfield A, Cadart C (eds). Raltitrexed. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/02/2026.

Joint Formulary Committee. Raltitrexed. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/02/2026.

Raltitrexed. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 11/02/2026.

Tomudex 2 mg Powder for Solution for Infusion (Hospira UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 11/02/2026.