Pralatrexate (CAS: 146464-95-1) is a chemotherapy drug that belongs to the class of antifolate agents. It is chemically known as N-[[5-[Methyl(propyl)amino]-2-thiazolyl]methyl]-N-(4-[[2,4-diamino-6-pteridinyl)methyl]methylamino]-benzoyl]-L-glutamic acid, and its molecular formula is C23H23N9O5S with a formula weight of 539.55 g/mol. Pralatrexate is sold under the brand name Folotyn and was first approved by the FDA in 2009 for the treatment of patients with peripheral T-cell lymphoma (PTCL).
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Synonyms: PDX, 10-propargyl-10-deazaaminopterin, N10-propargyl-5,8-dideazafolic acid, PDX-101.
Health Benefits of Pralatrexate: Pralatrexate is primarily used for the treatment of peripheral T-cell lymphoma, which is a rare and aggressive form of non-Hodgkin's lymphoma. In preclinical studies, pralatrexate has demonstrated potential efficacy for the treatment of other types of tumors including bladder cancer, pancreatic cancer, and ovarian cancer. Additionally, pralatrexate has shown promise for treating MTX-resistant tumors, which are resistant to the widely used chemotherapy drug methotrexate.
Product Mechanism: Pralatrexate works by blocking folate metabolism in cancer cells, which inhibits DNA synthesis and cell division, ultimately leading to cell death. Pralatrexate is a folic acid analog and targets the folate receptor which is highly expressed in tumor cells. Once inside cancer cells, pralatrexate enters the folate metabolic pathway, causing a buildup of toxic metabolites that interfere with DNA synthesis.
Potential Effects: The primary effect of pralatrexate is the inhibition of cancer cell growth and the induction of apoptosis (programmed cell death) in cancer cells. Additionally, pralatrexate has been demonstrated to increase the sensitivity of cancer cells to other chemotherapeutic agents. In preclinical studies, pralatrexate has also shown promise as a radiosensitizer, meaning that it could enhance the efficacy of radiation therapy when used together.
Safety: Common side effects of pralatrexate include fatigue, anemia, nausea, vomiting, mucositis, loss of appetite, and diarrhea. More serious side effects include neutropenia, thrombocytopenia, and anemia. Pralatrexate can also cause liver damage and kidney damage in some patients. Therefore, patients taking pralatrexate should have regular blood tests to monitor their blood cell counts and liver and kidney function.
Side Effects and Dosing Information: Pralatrexate dosing is determined based on the patient's body surface area and their kidney function. The recommended dose of pralatrexate for PTCL is 30 mg/m2 given once weekly for six weeks in a row, followed by a one-week rest period. This cycle can be repeated up to six times. Doses of pralatrexate for other types of tumors have not been established. Patients should not receive pralatrexate if they have severe liver disease or severe kidney disease.
Conclusion: Pralatrexate is an antifolate agent used primarily for the treatment of peripheral T-cell lymphoma. It has demonstrated efficacy in this rare and aggressive form of cancer as well as potential efficacy for the treatment of other types of tumors. Pralatrexate works by blocking folate metabolism in cancer cells, which inhibits DNA synthesis and cell division. While pralatrexate is generally well-tolerated, it can cause a range of side effects, and patients taking pralatrexate should be closely monitored for any potential complications.