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Raltitrexed (United States: Not available): Drug information

Raltitrexed (United States: Not available): Drug information
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For additional information see "Raltitrexed (United States: Not available): Patient drug information"

For abbreviations, symbols, and age group definitions show table
Brand Names: Canada
  • Tomudex
Pharmacologic Category
  • Antineoplastic Agent, Antimetabolite;
  • Antineoplastic Agent, Antimetabolite (Antifolate)
Dosing: Adult

Note: Prior to treatment WBC should be >4,000/mm3, ANC >2,000/mm3, and platelets >100,000/mm3.

Colorectal cancer, advanced

Colorectal cancer, advanced: IV: 3 mg/m2 once every 3 weeks in the absence of toxicity.

Malignant pleural mesothelioma, advanced

Malignant pleural mesothelioma, advanced (off-label use): IV: 3 mg/m2 once every 3 weeks (in combination with cisplatin) until disease progression or unacceptable toxicity occurs (Ref).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

CrCl >65 mL/minute: No dosage adjustment necessary.

CrCl 55 to 65 mL/minute: Reduce dose to 75% of usual dose once every 4 weeks.

CrCl 25 to 54 mL/minute: Reduce dose to percentage of dose equivalent to CrCl once every 4 weeks (eg, reduce dose to 25% of usual dose for CrCl of 25 mL/minute)

CrCl <25 mL/minute: Do not administer (use is contraindicated in severe renal impairment)

Dosing: Liver Impairment: Adult

Preexisting impairment: Use is not recommended in clinical jaundice or decompensated liver disease.

Mild to moderate impairment: No dosage adjustment necessary; use with caution.

Severe impairment: Use is contraindicated.

Hepatotoxicity during treatment: Interrupt raltitrexed until hepatic enzymes return to grade 2 or lower.

Dosing: Obesity: Adult

American Society of Clinical Oncology guidelines for appropriate systemic therapy dosing in adults with cancer with a BMI ≥30 kg/m2 : Utilize patient's actual body weight for calculation of BSA- or weight-based dosing; manage regimen-related toxicities in the same manner as for patients with a BMI <30 kg/m2; if a dose reduction is utilized due to toxicity, may consider resumption of full, weight-based dosing (or previously tolerated dose level) with subsequent cycles only if dose escalations are allowed in the prescribing information, if contributing underlying factors (eg, hepatic or kidney impairment) are sufficiently resolved, AND if performance status has markedly improved or is considered adequate (Ref). Note: Once a dose reduction is made for some toxicities, the manufacturer recommends all subsequent dosing be administered at that reduced dosing level; refer to prescribing information for further information.

Dosing: Adjustment for Toxicity: Adult

Delay dose in subsequent cycles until recovery from toxicity. May consider administering leucovorin if appropriate. Once a dose reduction has been made, do not escalate dose in subsequent cycles.

Grade 4 GI toxicity (diarrhea or mucositis) or grade 3 GI toxicity in combination with grade 4 hematologic toxicity: Discontinue raltitrexed and manage with supportive measures (consider administering leucovorin).

Grade 3 hematologic toxicity (neutropenia or thrombocytopenia) or grade 2 GI toxicity (diarrhea or mucositis): Reduce dose by 25%.

Grade 4 hematologic toxicity (neutropenia or thrombocytopenia) or grade 3 GI toxicity (diarrhea or mucositis): Reduce dose by 50%.

Dosing: Older Adult

Refer to adult dosing; use with caution.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adults.

>10%:

Dermatologic: Skin rash (14%)

Gastrointestinal: Abdominal pain (17% to 18%), anorexia (26% to 28%), constipation (13% to 15%), diarrhea (37% to 38%; grades 3/4: 11%), mucous membrane abnormality (12%), nausea (57% to 58%; grades 3/4: ≤12%), stomatitis (11%; grades 3/4: 2%), vomiting (37% to 38%; grades 3/4: ≤12%)

Hematologic & oncologic: Anemia (15% to 18%; grades 3/4: 7% to 8%), leukopenia (including neutropenia: 20% to 22%; grades 3/4: 12% to 13%)

Hepatic: Increased serum alanine aminotransferase (14% to 15%), increased serum aspartate aminotransferase (16% to 18%)

Nervous system: Asthenia (46% to 49%)

Miscellaneous: Fever (2% to 23%)

1% to 10%:

Cardiovascular: Cardiac abnormality (2%; including heart failure), cardiac arrhythmia (3%; including atrial fibrillation, sinus tachycardia, supraventricular tachycardia), peripheral edema (10%)

Dermatologic: Alopecia (6%), cellulitis (3%), diaphoresis (3% to 4%), pruritus (3%)

Endocrine & metabolic: Dehydration (6% to 7%), hypokalemia (2%), weight loss (6%)

Gastrointestinal: Dysgeusia (6%), dyspepsia (6%), flatulence (2% to 3%), xerostomia (2% to 3%)

Genitourinary: Urinary tract infection (3%)

Hematologic & oncologic: Thrombocytopenia (5% to 6%; grades 3/4: 4%)

Hepatic: Hyperbilirubinemia (2% to 3%), increased serum alkaline phosphatase (2% to 3%)

Infection: Infection (3%), sepsis (2% to 3%)

Nervous system: Chills (4%), depression (3%), dizziness (4% to 5%), headache (6%), hypertonia (<2%), insomnia (3% to 4%), malaise (4%), pain (4%), paresthesia (2% to 3%)

Neuromuscular & skeletal: Arthralgia (<2%), myalgia (3%)

Ophthalmic: Conjunctivitis (2% to 3%)

Renal: Increased serum creatinine (2% to 3%)

Respiratory: Dyspnea (4% to 5%), flu-like symptoms (6% to 8%), increased cough (5%), pharyngitis (4% to 5%)

Frequency not defined: Dermatologic: Desquamation

Postmarketing:

Gastrointestinal: Gastrointestinal hemorrhage

Hepatic: Acute hepatic failure (Raderer 2000), hepatotoxicity (including increased gamma-glutamyl transferase) (Massacesi 2003)

Respiratory: Interstitial pneumonitis (Schallier 2000)

Contraindications

Hypersensitivity to raltitrexed or any component of the formulation; severe renal and/or hepatic impairment; pregnancy or breastfeeding; use in patients who may become pregnant; use in children (<18 years of age).

Warnings/Precautions

Concerns related to adverse effects:

• Bone marrow suppression: Neutropenia, leukopenia, anemia, and thrombocytopenia may occur; neutropenia and thrombocytopenia may be severe. Bone marrow suppression is typically mild to moderate and generally occurs 7 to 14 days after treatment; recovery usually occurs by day 21. Use with caution in patients with preexisting bone marrow suppression.

• Gastrointestinal toxicity: Diarrhea, mucositis, and stomatitis may occur. Severe diarrhea with concomitant hematologic toxicity (neutropenia) may be life-threatening.

• Hepatotoxicity: Asymptomatic and self-limiting reversible ALT and AST elevations may occur.

• Malaise/weakness: May cause malaise/weakness; caution patients concerning operation of machinery/driving.

Special populations:

• Older adult: Use with caution in older adult patients. Monitor closely, especially for GI toxicity, such as diarrhea or mucositis.

• Radiation therapy recipients: Use with caution in patients who have received prior radiation therapy.

Product Availability

Not available in the US

Generic Equivalent Available: US

Yes

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Reconstituted, Intravenous:

Tomudex: 2 mg (1 ea)

Administration: Adult

IV: Administer as an infusion over 15 minutes.

When used in combination with cisplatin for malignant pleural mesothelioma (off-label use), administer raltitrexed first, followed by cisplatin (Ref).

Hazardous Drugs Handling Considerations

This medication is not on the NIOSH (2024) list; however, it meets the criteria for a hazardous drug. Raltitrexed contains manufacturer's special handling information and is a cytotoxic drug (per product labeling).

Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2023; NIOSH 2024; USP-NF 2020).

Use: Labeled Indications

Note: Not approved in the US.

Colorectal cancer, advanced: Treatment of advanced colorectal cancer.

Use: Off-Label: Adult

Malignant pleural mesothelioma, advanced

Medication Safety Issues
Sound-alike/look-alike issues:

Raltitrexed may be confused with methotrexate, PEMEtrexed, PRALAtrexate.

Tomudex may be confused with Temodal.

High alert medication:

The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drugs (chemotherapeutic agent; parenteral and oral; contraindicated in pregnancy) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Acute Care, Community/Ambulatory Care, and Long-Term Care Settings).

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

5-Aminosalicylic Acid Derivatives: May increase myelosuppressive effects of Myelosuppressive Agents. Risk C: Monitor

Abrocitinib: May increase immunosuppressive effects of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid

Antithymocyte Globulin (Equine): Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Antithymocyte Globulin (Equine). Specifically, these effects may be unmasked if the dose of cytotoxic chemotherapy is reduced. Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Antithymocyte Globulin (Equine). Specifically, infections may occur with greater severity and/or atypical presentations. Risk C: Monitor

Antithyroid Agents: Myelosuppressive Agents may increase neutropenic effects of Antithyroid Agents. Risk C: Monitor

Baricitinib: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Baricitinib. Risk X: Avoid

BCG Products: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of BCG Products. Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of BCG Products. Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Brincidofovir: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Brincidofovir. Risk C: Monitor

Brivudine: May increase adverse/toxic effects of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid

Chikungunya Vaccine (Live): Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Chikungunya Vaccine (Live). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Chikungunya Vaccine (Live). Risk X: Avoid

Chloramphenicol (Ophthalmic): May increase adverse/toxic effects of Myelosuppressive Agents. Risk C: Monitor

Chloramphenicol (Systemic): Myelosuppressive Agents may increase myelosuppressive effects of Chloramphenicol (Systemic). Risk X: Avoid

Cladribine: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Cladribine. Risk X: Avoid

CloZAPine: Myelosuppressive Agents may increase adverse/toxic effects of CloZAPine. Specifically, the risk for neutropenia may be increased. Risk C: Monitor

Coccidioides immitis Skin Test: Coadministration of Immunosuppressants (Cytotoxic Chemotherapy) and Coccidioides immitis Skin Test may alter diagnostic results. Management: Consider discontinuing cytotoxic chemotherapy several weeks prior to coccidioides immitis skin antigen testing to increase the likelihood of accurate diagnostic results. Risk D: Consider Therapy Modification

COVID-19 Vaccine (Inactivated Virus): Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of COVID-19 Vaccine (Inactivated Virus). Risk C: Monitor

COVID-19 Vaccine (mRNA): Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of COVID-19 Vaccine (mRNA). Management: Give a 3-dose primary series for all patients aged 6 months and older taking immunosuppressive medications or therapies. Booster doses are recommended for certain age groups. See CDC guidance for details. Risk D: Consider Therapy Modification

COVID-19 Vaccine (Subunit): Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of COVID-19 Vaccine (Subunit). Risk C: Monitor

Deferiprone: Myelosuppressive Agents may increase neutropenic effects of Deferiprone. Management: Avoid the concomitant use of deferiprone and myelosuppressive agents whenever possible. If this combination cannot be avoided, monitor the absolute neutrophil count more closely. Risk D: Consider Therapy Modification

Dengue Tetravalent Vaccine (Live): Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Dengue Tetravalent Vaccine (Live). Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Dengue Tetravalent Vaccine (Live). Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Denosumab: May increase immunosuppressive effects of Immunosuppressants (Cytotoxic Chemotherapy). Management: Consider the risk of serious infections versus the potential benefits of coadministration of denosumab and cytotoxic chemotherapy. If combined, monitor patients for signs/symptoms of serious infections. Risk D: Consider Therapy Modification

Deucravacitinib: May increase immunosuppressive effects of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid

Etrasimod: May increase immunosuppressive effects of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid

Fexinidazole: Myelosuppressive Agents may increase myelosuppressive effects of Fexinidazole. Risk X: Avoid

Filgotinib: May increase immunosuppressive effects of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid

Folic Acid: May decrease therapeutic effects of Raltitrexed. Risk X: Avoid

Inebilizumab: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Inebilizumab. Risk C: Monitor

Influenza Virus Vaccines: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Influenza Virus Vaccines. Management: Administer influenza vaccines at least 2 weeks prior to initiating chemotherapy if possible. If vaccination occurs less than 2 weeks prior to or during chemotherapy, revaccinate at least 3 months after therapy discontinued if immune competence restored. Risk D: Consider Therapy Modification

Leflunomide: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Leflunomide. Management: Increase the frequency of chronic monitoring of platelet, white blood cell count, and hemoglobin or hematocrit to monthly, instead of every 6 to 8 weeks, if leflunomide is coadministered with immunosuppressive agents, such as cytotoxic chemotherapy. Risk D: Consider Therapy Modification

Lenograstim: Antineoplastic Agents may decrease therapeutic effects of Lenograstim. Management: Avoid the use of lenograstim 24 hours before until 24 hours after the completion of myelosuppressive cytotoxic chemotherapy. Risk D: Consider Therapy Modification

Leucovorin Calcium-Levoleucovorin: May decrease therapeutic effects of Raltitrexed. Risk X: Avoid

Linezolid: May increase myelosuppressive effects of Myelosuppressive Agents. Risk C: Monitor

Lipegfilgrastim: Antineoplastic Agents may decrease therapeutic effects of Lipegfilgrastim. Management: Avoid concomitant use of lipegfilgrastim and myelosuppressive cytotoxic chemotherapy. Lipegfilgrastim should be administered at least 24 hours after the completion of myelosuppressive cytotoxic chemotherapy. Risk D: Consider Therapy Modification

Multivitamins/Minerals (with ADEK, Folate, Iron): May decrease therapeutic effects of Raltitrexed. Specifically, the folic acid contained in multivitamins is responsible for this potential interaction. Risk X: Avoid

Mumps- Rubella- or Varicella-Containing Live Vaccines: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Mumps- Rubella- or Varicella-Containing Live Vaccines. Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Mumps- Rubella- or Varicella-Containing Live Vaccines. Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Nadofaragene Firadenovec: Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Nadofaragene Firadenovec. Specifically, the risk of disseminated adenovirus infection may be increased. Risk X: Avoid

Natalizumab: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Natalizumab. Risk X: Avoid

Ocrelizumab: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Ocrelizumab. Risk C: Monitor

Ofatumumab: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Ofatumumab. Risk C: Monitor

Olaparib: Myelosuppressive Agents may increase myelosuppressive effects of Olaparib. Risk C: Monitor

Palifermin: May increase adverse/toxic effects of Antineoplastic Agents. Specifically, the duration and severity of oral mucositis may be increased. Management: Do not administer palifermin within 24 hours before, during infusion of, or within 24 hours after administration of myelotoxic chemotherapy. Risk D: Consider Therapy Modification

Pidotimod: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Pidotimod. Risk C: Monitor

Pimecrolimus: May increase immunosuppressive effects of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid

Piperacillin: May increase hypokalemic effects of Antineoplastic Agents. Risk C: Monitor

Pneumococcal Vaccines: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Pneumococcal Vaccines. Risk C: Monitor

Poliovirus Vaccine (Live/Trivalent/Oral): Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Poliovirus Vaccine (Live/Trivalent/Oral). Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Poliovirus Vaccine (Live/Trivalent/Oral). Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Polymethylmethacrylate: Immunosuppressants (Cytotoxic Chemotherapy) may increase hypersensitivity effects of Polymethylmethacrylate. Management: Use caution when considering use of bovine collagen-containing implants such as the polymethylmethacrylate-based Bellafill brand implant in patients who are receiving immunosuppressants. Consider use of additional skin tests prior to administration. Risk D: Consider Therapy Modification

Promazine: May increase myelosuppressive effects of Myelosuppressive Agents. Risk C: Monitor

Pyrimethamine: May increase adverse/toxic effects of Raltitrexed. Risk C: Monitor

Rabies Vaccine: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Rabies Vaccine. Management: Complete rabies vaccination at least 2 weeks before initiation of immunosuppressant therapy if possible. If combined, check for rabies antibody titers, and if vaccination is for post exposure prophylaxis, administer a 5th dose of the vaccine. Risk D: Consider Therapy Modification

Ritlecitinib: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Ritlecitinib. Risk X: Avoid

Ropeginterferon Alfa-2b: Myelosuppressive Agents may increase myelosuppressive effects of Ropeginterferon Alfa-2b. Management: Avoid coadministration of ropeginterferon alfa-2b and other myelosuppressive agents. If this combination cannot be avoided, monitor patients for excessive myelosuppressive effects. Risk D: Consider Therapy Modification

Ruxolitinib (Topical): Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Ruxolitinib (Topical). Risk X: Avoid

Sipuleucel-T: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Sipuleucel-T. Management: Consider reducing the dose or discontinuing the use of immunosuppressants, such as cytotoxic chemotherapy, prior to initiating sipuleucel-T therapy. Risk D: Consider Therapy Modification

Sphingosine 1-Phosphate (S1P) Receptor Modulators: May increase immunosuppressive effects of Immunosuppressants (Cytotoxic Chemotherapy). Risk C: Monitor

Tacrolimus (Topical): Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Tacrolimus (Topical). Risk X: Avoid

Talimogene Laherparepvec: Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Talimogene Laherparepvec. Specifically, the risk of infection from the live, attenuated herpes simplex virus contained in talimogene laherparepvec may be increased. Risk X: Avoid

Tertomotide: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Tertomotide. Risk X: Avoid

Tofacitinib: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Tofacitinib. Risk X: Avoid

Typhoid Vaccine: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Typhoid Vaccine. Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Typhoid Vaccine. Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Ublituximab: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Ublituximab. Risk C: Monitor

Upadacitinib: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Upadacitinib. Risk X: Avoid

Vaccines (Live): Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Vaccines (Live). Specifically, the risk of vaccine-associated infection may be increased. Vaccines (Live) may decrease therapeutic effects of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid

Vaccines (Non-Live/Inactivated/Non-Replicating): Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Vaccines (Non-Live/Inactivated/Non-Replicating). Management: Give non-live/inactivated/non-replicating vaccines at least 2 weeks prior to starting chemotherapy when possible. Patients vaccinated less than 14 days before or during chemotherapy should be revaccinated at least 3 months after therapy is complete. Risk D: Consider Therapy Modification

Yellow Fever Vaccine: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Yellow Fever Vaccine. Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Yellow Fever Vaccine. Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Zoster Vaccine (Live/Attenuated): Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Zoster Vaccine (Live/Attenuated). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Zoster Vaccine (Live/Attenuated). Risk X: Avoid

Reproductive Considerations

Use is contraindicated in patients who may become pregnant during treatment. Pregnancy should be excluded prior to treatment. Pregnancy should be avoided during treatment and for 6 months after the last raltitrexed dose if either partner is receiving treatment.

Pregnancy Considerations

Use is contraindicated in patients who are pregnant.

Pregnant patients should not handle this medication.

Breastfeeding Considerations

Use in breastfeeding patients is contraindicated by the manufacturer.

Dietary Considerations

Avoid folic acid, folinic acid (leucovorin calcium), and multivitamins with folic acid close to and during administration.

Monitoring Parameters

CBC with differential (at baseline, prior to each treatment, or weekly if GI toxicity observed); hepatic function tests and serum creatinine (at baseline and prior to each treatment). Monitor for signs of GI toxicity. Evaluate pregnancy status prior to use in patients who may become pregnant.

The American Society of Clinical Oncology hepatitis B virus (HBV) screening and management provisional clinical opinion (ASCO [Hwang 2020]) recommends HBV screening with hepatitis B surface antigen, hepatitis B core antibody, total Ig or IgG, and antibody to hepatitis B surface antigen prior to beginning (or at the beginning of) systemic anticancer therapy; do not delay treatment for screening/results. Detection of chronic or past HBV infection requires a risk assessment to determine antiviral prophylaxis requirements, monitoring, and follow-up.

Mechanism of Action

Raltitrexed is a folate analogue that selectively inhibits thymidylate synthase, blocking purine synthesis. This results in an overall inhibition of DNA synthesis.

Pharmacokinetics (Adult Data Unless Noted)

Distribution: Vss: 548 L

Protein binding: 93%

Metabolism: Undergoes extensive intracellular metabolism to active polyglutamate forms; appears to be little or no systemic metabolism of the drug

Half-life elimination: Triphasic; Beta: ~2 hours; Terminal: 198 hours

Excretion: Urine (~50% as unchanged drug); feces (~15%)

Pharmacokinetics: Additional Considerations (Adult Data Unless Noted)

Altered kidney function: Plasma clearance is reduced approximately 50% in patients with CrCl 25 to 65 mL/minute.

Hepatic function impairment: Mild to moderate impairment results in a reduction in plasma clearance of less than 25%.

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AR) Argentina: Tomudex;
  • (AT) Austria: Tomudex;
  • (AU) Australia: Tomudex;
  • (BE) Belgium: Tomudex;
  • (BG) Bulgaria: Tomudex;
  • (BR) Brazil: Tomudex;
  • (CN) China: Sai wei jian;
  • (CZ) Czech Republic: Tomudex;
  • (ES) Spain: Tomudex;
  • (FI) Finland: Tomudex;
  • (FR) France: Tomudex;
  • (GB) United Kingdom: Tomudex;
  • (HK) Hong Kong: Tomudex;
  • (HU) Hungary: Tomudex;
  • (IE) Ireland: Tomudex;
  • (IT) Italy: Tomudex;
  • (KR) Korea, Republic of: Tomudex;
  • (LV) Latvia: Tomudex;
  • (MX) Mexico: Tomudex;
  • (NO) Norway: Tomudex;
  • (NZ) New Zealand: Tomudex;
  • (PH) Philippines: Tomudex;
  • (PL) Poland: Tomudex;
  • (PT) Portugal: Tomudex;
  • (RU) Russian Federation: Tomudex;
  • (SG) Singapore: Tomudex;
  • (SK) Slovakia: Tomudex;
  • (TR) Turkey: Tomudex;
  • (UY) Uruguay: Tomudex;
  • (ZA) South Africa: Tomudex
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  3. Hwang JP, Feld JJ, Hammond SP, et al. Hepatitis B virus screening and management for patients with cancer prior to therapy: ASCO provisional clinical opinion update. J Clin Oncol. 2020;38(31):3698-3715. doi:10.1200/JCO.20.01757 [PubMed 32716741]
  4. Massacesi C, Santini D, Rocchi MB, et al. Raltitrexed-induced hepatotoxicity: multivariate analysis of predictive factors. Anticancer Drugs. 2003;14(7):533-541. doi:10.1097/00001813-200308000-00005 [PubMed 12960737]
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  7. Schallier D, Neyns B, De Mey J, Meysman M. Raltitrexed-related pulmonary toxicity. Acta Oncol. 2000;39(4):537-538. doi:10.1080/028418600750013474 [PubMed 11041118]
  8. Tomudex (raltitrexed) [product monograph]. Kirkland, Quebec, Canada: Pfizer Canada Inc; December 2021.
  9. United States Pharmacopeia. <800> Hazardous Drugs—Handling in Healthcare Settings. In: USP-NF. United States Pharmacopeia; July 1, 2020. Accessed January 16, 2025. doi:10.31003/USPNF_M7808_07_01
  10. van Meerbeeck JP, Gaafar R, Manegold C, et al, “Randomized Phase III Study of Cisplatin With or Without Raltitrexed in Patients With Malignant Pleural Mesothelioma: An Intergroup Study of the European Organisation for Research and Treatment of Cancer Lung Cancer Group and the National Cancer Institute of Canada,” J Clin Oncol, 2005, 23(28):6881-9. [PubMed 16192580]
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