It is a folate analog metabolic inhibitor indicated for: ? Locally Advanced or Metastatic Nonsquamous Non-Small Cell Lung Cancer: Initial treatment in combination with cisplatin. Maintenance treatment of patients whose disease has not progressed after four cycles of platinum-based first-line chemotherapy. ? After prior chemotherapy as a single agent. ? Mesothelioma: in combination with cisplatin.
Pemetrexed is a folate analog metabolic inhibitor that disrupts folate-dependent metabolic processes essential for cell replication. In vitro studies show that Pemetrexed inhibits thymidylate synthase (TS), dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase (GARFT), which are folate-dependent enzymes involved in the de novo biosynthesis of thymidine and purine nucleotides. Pemetrexed is taken into cells by membrane carriers such as the reduced folate carrier and membrane folate binding protein transport systems. Once in the cell, Pemetrexed is converted to polyglutamate forms by the enzyme folylpolyglutamate synthetase. The polyglutamate forms are retained in cells and are inhibitors of of TS and GARFT.
Combination use in Non-Small Cell Lung Cancer and Mesothelioma: Recommended dose of ALIMTA is 500 mg/m2 i.v. on Day 1 of each 21-day cycle in combination with cisplatin 75 mg/m2 i.v. beginning 30 minutes after ALIMTA administration. ? Single-Agent use in Non-Small Cell Lung Cancer: Recommended dose of ALIMTA is 500 mg/m2 i.v. on Day 1 of each 21-day cycle. ? Dose Reductions: Dose reductions or discontinuation may be needed based on toxicities from the preceding cycle of therapy.
Ibuprofen increases exposure (AUC) of Pemetrexed. In patients with creatinine clearance between 45mL/min and 79mL/min
Avoid administration of Ibuprofen for 2 days before, the day of, and 2 days following administration of Pemetrexed.
Monitor patients more frequently for myelosuppression, renal, and gastrointestinal toxicity, if concomitant administration of Ibuprofen cannot be avoided.
History of severe hypersensitivity reaction to pemetrexed.Premedication regimen: Instruct patients to take folic acid and vitamin B12. Pretreatment with dexamethasone or equivalent reduces cutaneous reaction. ? Bone marrow suppression: Reduce doses for subsequent cycles based on hematologic and nonhematologic toxicities. ? Renal function: Do not administer when CrCl <45 mL/min. ? NSAIDs with renal insufficiency: Use caution in patients with mild to moderate renal insufficiency (CrCl 45-79 mL/min). ? Lab monitoring: Do not begin next cycle unless ANC ?1500 cells/mm3 , platelets ?100,000 cells/mm3 ,and CrCl ?45 mL/min. ? Pregnancy: Fetal harm can occur when administered to a pregnant woman. Women should be advised to use effective contraception measures to prevent pregnancy during treatment with it.
fatigue,nausea,and anorexia. Additional common adverse reactions when used in combination with cisplatin include vomiting,neutropenia,leukopenia, anemia,stomatitis/pharyngitis,thrombocytopenia,and constipation
Pregnancy Category D. There is positive evidence of human fetal risk,but the benefits from use in pregnant women may be acceptable despite the risk (e.g.,if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective). Lactation: Advise women not to breastfeed during treatment with Pemetrexed and for 1 week after the final dose
No drugs are approved for the treatment of Pemetrexed overdose. Based on animal studies, administration of leucovorin may mitigate the toxicities of Pemetrexed overdosage. It is not known whether pemetrexed is dialyzable.
Store below 30°C in a cool and dry place, away from sunlight. Keep out of the reach of children.
Store below 30°C in a cool and dry place, away from sunlight. Keep out of the reach of children.
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