Pemetrexed

Pemetrexed

Pemetrexed ball-and-stick model

Pathway of tetrahydrofolate and antimetabolites

Information about Pemetrexed

Pemetrexed is a parenterally administered folate antagonist and antineoplastic agent, used in the treatment of non-small cell lung cancer and malignant mesothelioma.

Liver safety of Pemetrexed

Pemetrexed therapy has been associated with moderate rates of serum enzyme elevations during therapy, but has not been convincingly linked to instances of acute, clinically apparent liver injury.

Mechanism of action of Pemetrexed

Pemetrexed (pem" e trex' ed) is a folic acid analog which acts as an antagonist to the enzymes involved in folate dependent synthetic pathways such as thymidine synthase, dihydrofolate reductase and glycinamide ribonucleotide formyltransferase. Inhibition of these enzymes leads to decrease in intracellular thymidine and purine which interferes with DNA synthesis and leads to apoptotic cell death in rapidly dividing cells. In vitro and in vivo studies have shown that pemetrexed inhibits growth of mesothelioma and non-small cell lung cancer cell lines, and clinical trials in advanced forms of these cancers have shown improvements in overall survival times in pemetrexed treated subjects.

FDA approval information for Pemetrexed

Pemetrexed was approved for use in the United States in 2004. Current indications are for locally advanced or metastatic nonsquamous, non-small cell lung cancer (NSCLC) and for malignant pleural mesothelioma, usually in combination with other antineoplastic agents (such as cisplatin) and with folic acid and vitamin B12 supplementation.

Dosage and administration for Pemetrexed

Pemetrexed is available in single use vials of 100 or 500 mg as a powder for reconstitution under the brand name Alimta. The recommended dose is 500 mg/m2 intravenously on day 1 of each 21 day cycle.

Side effects of Pemetrexed

Pemetrexed shares common side effects with other folate antagonists such as fatigue, nausea, vomiting, anorexia, diarrhea, alopecia, bone marrow suppression, and rash. Uncommon, but potentially serious adverse events include febrile neutropenia, infections, dehydration, renal failure, arrhythmias and peripheral neuropathy.

• Dailymed label info on Pemetrexed
• FDA Pemetrexed