Raltitrexed

Intravenous
Advanced colorectal cancer

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

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.

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

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).

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. Assess for signs of gastrointestinal toxicity.

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

Description: 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 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.

Cytotoxic Chemotherapy

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.