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Pemetrexed
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DRUG INFO
Pemetrexed
Drug Name:
Pemetrexed
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:
DrugBank: Interactions for Pemetrexed
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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Pemetrexed News
(When available)
Press appeal success grants 'an extra three months of life' Dec 21, 2005
HoldTheFrontPage.co.uk, The paper published the pictures and stories of six men who have the disease, and who will die soon without the Tyneside-developed drug Alimta, available on ...
Cancer linked to building materials affect many Dec 18, 2005
Xinhua, US-based Eli Lilly announced over the weekend that it has introduced Alimta, the world's first medication to treat the asbestos-related malign pleural ...
Full text of David Cameron's speech on the NHS Jan 4, 2006
Guardian Unlimited, And new ones are coming on stream the whole time. Alimta, for lung cancer. Velcade, for myeloma. And, of course, Femara and Herceptin for breast cancer.[6]. ...
Hana Biosciences Announces 2006 Corporate Goals; Key 2005 ... Jan 5, 2006
Business Wire (press release), Compared to currently available antifolates such as methotrexate or pemetrexed (Alimta(R); Eli Lilly) in preclinical studies, Talotrexin enters into cells up ...
Oncology Nursing Society Presents Mesothelioma Victims with Hope ... Jan 2, 2006
PR Web (press release), The new antifolate pemetrexed (Alimta) has been shown to improve outcomes when combined with more standard chemotherapeutic agents such as platins and ...
Don Peasley Dec 17, 2005
Northwest Herald, His father points with pride to his son's success in discovering two drugs – Alimta and Gemzar – marketed by Eli Lilly and amounting to more than $1 ...
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