Raltitrexed

Pronunciation: ral-tih-TREX-ed.

Generic name
raltitrexed
Drug class
Antimetabolite chemotherapy agent -- quinazoline folate analogue, thymidylate synthase inhibitor
Form
Powder for solution for infusion, 2 mg per vial
Route
Intravenous infusion
Legal status
Prescription-only, hospital/specialist chemotherapy use only

Availability and supply rules vary by country

Trade names by country: United Kingdom · Canada · Australia

Australia: Tomudex (5) · Full directory

What raltitrexed is and how it works

Raltitrexed is a chemotherapy medicine used in the palliative (symptom-control and life-extending, rather than curative) treatment of advanced colorectal (bowel) cancer, given by a cancer specialist as an infusion into a vein once every 3 weeks. (2) (4)

Raltitrexed is used when a standard 5-fluorouracil/folinic acid chemotherapy regimen is not tolerated or is otherwise unsuitable. It has a narrow margin between an effective dose and a toxic one, so your cancer team will calculate your exact dose individually from your body surface area and will check your blood counts and organ function closely before and during treatment.

Mechanism of action: how raltitrexed works

Raltitrexed is a quinazoline folate analogue transported into cells via the reduced folate carrier and extensively polyglutamated intracellularly, producing potent, prolonged inhibition of thymidylate synthase -- the key enzyme in de novo thymidine (and hence DNA) synthesis -- leading to DNA fragmentation and cell death. It is approximately 93% protein-bound and has a long terminal half-life, consistent with intracellular retention as polyglutamates. (2) (4)

What raltitrexed is used for

Advanced (metastatic) colorectal cancer

Used for the palliative treatment of advanced colorectal cancer, typically when 5-fluorouracil and folinic acid based chemotherapy is not tolerated or is considered inappropriate for the individual. (2) (4)

Before taking raltitrexed

Do not take / not appropriate for

  • Should not be given to anyone with a known serious allergic reaction to raltitrexed or any ingredient in the infusion. (all countries) (2)
  • Contraindicated during pregnancy and breastfeeding; pregnancy must be excluded before treatment starts. (all countries) (2) (4)
  • Contraindicated with severe kidney impairment (creatinine clearance below 25 mL/min) or severe liver impairment. (all countries) (2) (4)
  • Should not be combined with folic acid, folinic acid, or vitamin preparations containing these, except where a clinician specifically uses folinic acid to manage an overdose. (all countries) (2)

Tell your clinician about

  • Any history of reduced bone marrow function, poor general condition, or prior radiotherapy.
  • Any kidney or liver problems, even mild -- your dose and monitoring schedule depend heavily on these.
  • All other medicines, including any vitamin or folate-containing supplements.
  • Pregnancy, plans for pregnancy (for either partner), or breastfeeding -- effective contraception is needed during treatment and for at least 6 months afterward.
  • Your age -- older adults are more vulnerable to raltitrexed's toxic effects and need closer monitoring.
(2) (4)

How to take raltitrexed

  • Given only by, or under the close supervision of, a cancer specialist experienced in chemotherapy and in managing its toxicities.
  • Administered as a short (about 15-minute) infusion into a vein, diluted in a bag of saline or dextrose solution.
  • Not mixed with any other medicine in the same infusion container.
  • Given once every 3 weeks if no significant toxicity has developed since the previous dose.
(2)

Procedures and treatment changes

Tell the treating team before surgery, procedures, or any medicine change. Do not alter treatment without the responsible clinician. (1) (2) (3) (4) (5) (6)

Missed dose

Raltitrexed is scheduled and given by your cancer care team, not self-administered, so a 'missed dose' does not apply in the usual sense. Your team will decide the timing of your next cycle based on your blood counts and recovery from any side effects.

Overdose

Overdose is managed by the treating hospital team, typically with folinic acid (leucovorin) rescue and supportive care, plus close monitoring of blood counts and organ function. Seek immediate medical attention for any severe or unexpected symptoms after an infusion. (2)

Side effects

Side effects and their urgency vary; report severe, persistent, or concerning symptoms.

Nausea, vomiting, diarrhoea, and reduced appetite.

What to notice: Nausea, vomiting, diarrhoea, and reduced appetite.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (4)

Low white blood cell counts (leukopenia/neutropenia), low red blood cell counts (anaemia), and low platelet counts (thrombocytopenia).

What to notice: Low white blood cell counts (leukopenia/neutropenia), low red blood cell counts (anaemia), and low platelet counts (thrombocytopenia).

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (4)

Weakness/tiredness (asthenia) and fever, usually in the first week after an infusion.

What to notice: Weakness/tiredness (asthenia) and fever, usually in the first week after an infusion.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (4)

Rash, sometimes with itching.

What to notice: Rash, sometimes with itching.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (4)

Mouth sores (mucositis) and reversible increases in liver enzymes.

What to notice: Mouth sores (mucositis) and reversible increases in liver enzymes.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (2) (4)

Serious warnings

Signs of severe bone marrow suppression (low blood counts) — emergency

Symptoms: Fever, chills, or signs of infection; unusual bruising or bleeding; extreme tiredness or breathlessness.

Action: Contact your cancer care team or seek emergency care immediately -- severe drops in white blood cells or platelets can become life-threatening, especially if combined with diarrhoea. (2) (4)

Severe diarrhoea, vomiting, or mouth sores — emergency

Symptoms: Frequent watery diarrhoea, persistent vomiting, or a mouth too sore to eat or drink, especially together with fever or signs of low blood counts.

Action: Contact your cancer care team promptly -- severe gastrointestinal toxicity combined with low blood counts is a recognised cause of serious complications and may need same-day medical assessment. (2) (4)

Signs of a serious allergic reaction — emergency

Symptoms: Swelling of the face, lips, tongue, or throat; difficulty breathing; widespread rash or hives.

Action: Seek emergency medical help immediately. (2)

Worsening kidney or liver function — high caution

Symptoms: Reduced urine output, unusual swelling, yellowing of the skin/eyes, or marked fatigue.

Action: Your cancer team monitors kidney and liver function closely with blood tests before every cycle -- report any new symptoms between visits. (2) (4)

Interactions

  • Folic acid, folinic acid, and vitamin preparations containing these must not be taken alongside raltitrexed (except when a clinician uses folinic acid deliberately to manage an overdose), because they can interfere with how raltitrexed works. (2)
  • Because raltitrexed is partly cleared through active kidney tubular secretion, other medicines cleared the same way -- such as NSAID pain relievers -- carry a theoretical interaction risk, though clinical trial safety data did not show a clinically significant interaction with NSAIDs or warfarin in practice. (2) (4)

Pregnancy, breastfeeding, kidney/liver function, age

Pregnancy

Contraindicated. Pregnancy must be excluded before starting treatment and avoided during treatment and for at least 6 months afterward for either partner, because animal studies showed embryo loss and birth defects. (1) (2) (3) (4) (5) (6)

Breastfeeding

Contraindicated -- breastfeeding should not continue during treatment. (1) (2) (3) (4) (5) (6)

Children

Not recommended in children; safety and effectiveness have not been established in this age group. (1) (2) (3) (4) (5) (6)

Elderly

Older adults are more vulnerable to raltitrexed's toxic effects, largely because kidney function naturally declines with age, and require extra-careful monitoring. (1) (2) (3) (4) (5) (6)

Hepatic_impairment

Contraindicated in severe liver impairment; used with caution and close monitoring in mild-to-moderate impairment. (1) (2) (3) (4) (5) (6)

Renal_impairment

Contraindicated in severe kidney impairment (creatinine clearance below 25 mL/min); dose is reduced for creatinine clearance between 25 and 65 mL/min. (1) (2) (3) (4) (5) (6)

Monitoring

Before starting

  • Full blood count (white cells, neutrophils, platelets)
  • Liver function tests and bilirubin
  • Kidney function (creatinine clearance)
  • Pregnancy test where relevant

During treatment

  • Full blood count, liver enzymes, bilirubin, and creatinine before every 3-week cycle.
  • Weekly blood counts if gastrointestinal toxicity develops between cycles.
  • Closer clinical monitoring in older adults and anyone with reduced kidney or liver function.
(2)

Storage

Store unopened vials at or below 25C (77F), protected from light, in the original carton. Once reconstituted, the solution is chemically stable for 24 hours at 25C or 24 hours refrigerated at 2-8C -- prepared and used by hospital pharmacy/chemotherapy staff, not stored at home.

Professional information

Clinician-facing context only, sourced from the current UK SmPC and Health Canada product monograph; verify against the current full label before prescribing.

United Kingdom / European Union / Canada / Australia

Indication: Advanced colorectal cancer (palliative, second-line/alternative to 5-FU/folinic acid)

Dose summary: 3 mg/m2 IV over 15 minutes, every 3 weeks in the absence of toxicity. Dose escalation above 3 mg/m2 not recommended. Reduce dose for CrCl 25-65 mL/min; contraindicated for CrCl <25 mL/min. Contraindicated in severe hepatic impairment; caution and monitoring in mild-moderate hepatic impairment.

Renal context: Mild-to-moderate renal impairment (CrCl 25-65 mL/min) reduces raltitrexed plasma clearance by approximately 50% and requires dose reduction; severe impairment is a contraindication. (2) (4)

Mechanism of action

Hepatic guidance

Mild-to-moderate hepatic impairment reduced plasma clearance by less than 25% in studied patients; severe hepatic impairment is a contraindication.

Overdose note

Overdose is managed with supportive care and folinic acid (leucovorin) rescue plus intensive monitoring of blood counts, renal, and hepatic function, given the risk of life-threatening myelosuppression and GI toxicity. (2) (4)

Frequently asked questions

Is raltitrexed (Tomudex) available in the US, UK, Europe, Canada, Australia, and New Zealand?

It is authorised and available in the UK, the European Union (via national authorisations in member states), Canada, and Australia. It is not approved or marketed in the United States -- a live check of the FDA's DailyMed database returns no results for raltitrexed, and pemetrexed is used instead in US practice. Its current availability in New Zealand could not be confirmed from official sources. (1) (2) (3) (4) (5) (6)

Why can't I take folic acid or folinic acid supplements while on raltitrexed?

Folic acid, folinic acid, and similar vitamin preparations can interfere with how raltitrexed works and are contraindicated during treatment, except when your clinical team deliberately uses folinic acid to manage an overdose. (2)

What blood tests do I need before each raltitrexed treatment cycle?

Your care team will typically check a full blood count (white cells, neutrophils, and platelets), liver enzymes and bilirubin, and kidney function (creatinine) before each cycle, since raltitrexed can cause serious drops in blood counts and needs dose adjustment if kidney function is reduced. If you develop diarrhoea or mouth soreness, more frequent blood-count checks may be needed. (2)

What is the mechanism of action of raltitrexed?

Raltitrexed is a quinazoline folate analogue transported into cells via the reduced folate carrier and extensively polyglutamated intracellularly, producing potent, prolonged inhibition of thymidylate synthase -- the key enzyme in de novo thymidine (and hence DNA) synthesis -- leading to DNA fragmentation and cell death. It is approximately 93% protein-bound and has a long terminal half-life, consistent with intracellular retention as polyglutamates. (2) (4)

What is the generic name of Raltitrexed?

The generic name is raltitrexed. (2)

What class of drug is raltitrexed?

Raltitrexed is classed as: Antimetabolite chemotherapy agent -- quinazoline folate analogue, thymidylate synthase inhibitor. (2)

References

  1. DailyMed search for 'raltitrexed' -- zero drug labels foundU.S. Food and Drug Administration / DailyMed (NIH) · United States · accessed 2026-07-30 · source 1
  2. Tomudex 2 mg powder for solution for infusion -- Summary of Product Characteristicselectronic medicines compendium (emc), United Kingdom -- Hospira UK Limited (Pfizer) · United Kingdom · accessed 2026-07-30 · source 2
  3. Raltitrexed: List of nationally authorised medicinal products -- PSUSA/00002605/202509European Medicines Agency (EMA) -- PSUR single assessment (PSUSA) and list of nationally authorised medicinal products · European Union · accessed 2026-07-30 · source 3
  4. TOMUDEX (raltitrexed disodium for injection) Product MonographHealth Canada product monograph, Pfizer Canada Inc. · Canada · accessed 2026-07-30 · source 4
  5. Tomudex powder for solution for infusion 2 mg/vial -- ARTG entry 194724Therapeutic Goods Administration (TGA), Australia · Australia · accessed 2026-07-30 · source 5
  6. Medsafe product database search for raltitrexed/Tomudex -- no data sheet or product listing foundMedsafe (New Zealand regulator) product/application search -- no result located · New Zealand · accessed 2026-07-30 · source 6

Brand names by country

Single-ingredient raltitrexed names are shown separately by country. Product availability, strengths, and supply rules can change; combination products are not included here.

Priority countries

United Kingdom

  • Tomudex (2)MHRA licensed emc smpc confirmed · 2 mg/vial · Hospira UK Limited (Pfizer)

Canada

  • TOMUDEX

Australia

  • Tomudex (5)TGA ARTG active confirmed · 2 mg/vial · Hospira Australia Pty Ltd
View brands in additional countries.

European Union

Tomudex (3)

This page provides general reference information about raltitrexed and is not a substitute for advice from the cancer specialist managing your treatment. All dosing and treatment decisions should be made with your oncology team.

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