Pralatrexate
- Atc Codes:L01BA05
- CAS Codes:146464-95-1
- PHARMGKB ID:146464-95-1
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
North America
USA: Folotyn.
Drug combinations
Chemistry
Pralatrexate: C~23~H~23~N~7~O~5~. Mw: 477.48. (2S)-2-[[4-[(1RS)-1-[(2,4-diaminopteridin-6-yl)methyl]but-3-ynyl]benzoyl]amino]pentanedioic acid. CAS-146464-95-1.
Pharmacologic Category
Antineoplastic Agents; Antimetabolite; Antifolate. (ATC-Code: L01BA05).
Mechanism of action
Pralatrexate is a folate analog metabolic inhibitor that competitively inhibits dihydrofolate reductase. It is also a competitive inhibitor for polyglutamylation by the enzyme folylpolyglutamyl synthetase. This inhibition results in the depletion of thymidine and other biological molecules, the synthesis of which depends on single carbon transfer.
Therapeutic use
Treatment of patients with relapsed or refractory peripheral T-cell lymphoma (PTCL). This indication is based on overall response rate. Clinical benefit such as improvement in progression-free survival or overall survival has not been demonstrated.
Pregnancy and lactiation implications
Can cause fetal harm when administered to a pregnant woman. Women should be advised against breastfeeding while being treated with pralatrexate.
Unlabeled use
Contraindications
None known to date.
Warnings and precautions
Thrombocytopenia, neutropenia, and anemia may occur. Mucositis has been reported (if ≥grade 2 mucositis is observed, omit or modify dose). Can cause fetal harm. Use caution in patients with moderate-to-severe renal function impairment. Elevated liver function test abnormalities may present (may require dose modification). Patients should be instructed to take folic acid and receive vitamin B~12~ to potentially reduce treatment-related hematological toxicity and mucositis. Dermatologic reactions have been reported in clinical studies and post-marketing safety reports.