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Pemetrexed: profile and news
New drug to aid SA fight against asbestos-linked cancer May 4, 2006 Point Therapeutics Reports First Quarter 2006 Financial Results ... May 9, 2006 Coley Pharmaceutical Group Reports First Quarter Financial Results May 11, 2006 Millennium Achieves First Quarter 2006 Non-GAAP Profitability and ... Apr 27, 2006 Lilly Reports Q1 EPS of $.77, or 13% Growth Apr 20, 2006 Other information Indication For the treatment of malignant pleural mesothelioma and locally advanced or metastatic non-small cell lung cancer (NSCLC) after prior chemotherapy Pharmacology Preclinical studies have shown that pemetrexed inhibits the in vitro growth of mesothelioma cell lines (MSTO-211H, NCI-H2052). Studies with the MSTO-211H mesothelioma cell line showed synergistic effects when pemetrexed was combined concurrently with cisplatin. Mechanism Of Action Pemetrexed is an antifolate containing the pyrrolopyrimidine-based nucleus that exerts its antineoplastic activity by disrupting folate-dependent metabolic processes essential for cell replication. In vitro studies have shown that pemetrexed inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), all folate-dependent enzymes involved in the de novo biosynthesis of thymidine and purine nucleotides. Pemetrexed is transported into cells by both 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 TS and GARFT. Polyglutamation is a time- and concentration-dependent process that occurs in tumor cells and, to a lesser extent, in normal tissues. Polyglutamated metabolites have an increased intracellular half-life resulting in prolonged drug action in malignant cells. Drug Category Antineoplastic Agents; Antimetabolites; Enzyme Inhibitors; Folic Acid Antagonists; ATC:L01BA04 Brand Names/Synonyms Alimta; PEMETREXED; Pemetrexed; Pemetrexed Disodium; Pemetrexeddisodium Dosage Forms POWDER FOR SOLUTION; Intravenous infusion Absorption Not Available Interactions -->Interactions for Pemetrexed: ALIMTA is primarily eliminated unchanged renally as a result of glomerular filtration and tubular secretion. Concomitant administration of nephrotoxic drugs could result in delayed clearance of ALIMTA. Concomitant administration of substances that are also tubularly secreted (e.g., probenecid) could potentially result in delayed clearance of ALIMTA. Although ibuprofen (400 mg qid) can be administered with ALIMTA in patients with normal renal function (creatinine clearance ³80 mL/min), caution should be used when administering ibuprofen concurrently with ALIMTA to patients with mild to moderate renal insufficiency (creatinine clearance from 45 to 79 mL/min). Patients with mild to moderate renal insufficiency should avoid taking NSAIDs with short elimination half-lives for a period of 2 days before, the day of, and 2 days following administration of ALIMTA. In the absence of data regarding potential interaction between ALIMTA and NSAIDs with longer half-lives, all patients taking these NSAIDs should interrupt dosing for at least 5 days before, the day of, and 2 days following ALIMTA administration. If concomitant administration of an NSAID is necessary, patients should be monitored closely for toxicity, especially myelosuppression, renal, and gastrointestinal toxicity. Drug/Laboratory Test Interactions None known. Chemical IUPAC Name 2-[4-[2-(4-amino-2-oxo-3,5,7-triazabicyclo[4.3.0]nona-3,8,10-trien-9-yl)ethyl]benzoyl]aminopentanedioic acid Chemical Formula C20H21N5O6 Half Life 3.5 hours Drug Type Approved Drug # Accession No APRD00573 CAS Registry Number 150399-23-8 |
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