Generic Medicine Info
Indications and Dosage
Advanced colorectal cancer
Adult: 3 mg/m2 via infusion over 15 minutes once every 3 weeks in the absence of toxicity. Dosage is individualised based on the gastrointestinal and haematological toxicity. Refer to detailed product guidelines for dose adjustments according to toxicity.
Renal Impairment
CrCl (mL/min) Dosage
55-65 Reduce to 75% once every 4 weeks.
25-54 Reduce to 50% once every 4 weeks.
<25 Contraindicated.
Hepatic Impairment
Severe: Contraindicated.
Reconstitute with 4 mL of sterile water for injection to a concentration of 0.5 mg/mL. Further dilute with 50-250 mL of 0.9% NaCl or 5% dextrose in water.
Severe renal and hepatic impairment. Pregnancy and lactation. Concomitant use with folinic acid, folic acid, or vitamin preparations containing these agents.
Special Precautions
Patient with bone marrow suppression, poor general condition, and have undergone radiation therapy. Elderly. Mild to moderate renal and hepatic impairment.
Adverse Reactions
Significant: Bone marrow suppression (e.g. neutropenia, leucopenia, anaemia, thrombocytopenia), nausea, vomiting, diarrhoea, mucositis, stomatitis, malaise, weakness.
Eye disorders: Conjunctivitis.
Gastrointestinal disorders: Mouth ulceration, 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 concomitant haematologic toxicity (e.g. neutropenia).
Patient Counseling Information
This medicine may cause malaise or weakness, if affected, do not drive or operate machinery.
Monitoring Parameters
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. Assess for signs of gastrointestinal toxicity.
Drug Interactions
Potentially Fatal: Diminished therapeutic effect with folinic acid, folic acid, or vitamin preparations containing these agents.
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.
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.
Chemical Structure

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 135400182, Raltitrexed. https://pubchem.ncbi.nlm.nih.gov/compound/Raltitrexed. Accessed Jan. 27, 2021.

Store intact vials below 25°C. Protect from light. Reconstituted solutions and diluted solutions for infusion are stable between 2-8°C for 24 hours. This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
MIMS Class
Cytotoxic Chemotherapy
ATC Classification
L01BA03 - raltitrexed ; Belongs to the class of antimetabolites, folic acid analogues. Used in the treatment of cancer.
Anon. Raltitrexed. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 20/10/2020.

Buckingham R (ed). Raltitrexed. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/10/2020.

Joint Formulary Committee. Raltitrexed. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/10/2020.

Tomudex 2 mg Powder for Solution for Infusion (Hospira UK Limited). MHRA. https://products.mhra.gov.uk/. Accessed 20/10/2020.

Disclaimer: This information is independently developed by MIMS based on Raltitrexed from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2024 MIMS. All rights reserved. Powered by MIMS.com
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