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Pemetrexed
drug data and news
Pemetrexed drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Pemetrexed | ||
| Brand Names/Synonyms | Alimta; PEMETREXED; Pemetrexed; Pemetrexed Disodium; Pemetrexeddisodium | ||
| Indication | For the treatment of malignant pleural mesothelioma and locally advanced or metastatic non-small cell lung cancer (NSCLC) after prior chemotherapy | ||
| Sponsored links | Description | Not Available | |
| 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. | ||
| Pemetrexed News (When available) |
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 | ||
| Dosage Forms | POWDER FOR SOLUTION; Intravenous infusion | ||
| Drug_Category | Antineoplastic Agents; Antimetabolites; Enzyme Inhibitors; Folic Acid Antagonists; ATC:L01BA04 | ||
| 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. | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| 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 | ||
| Molecular Weight | 427.411 g/mol | ||
| Smiles String | C1=CC(=CC=C1CCC2=CNC3=C2C(=O)N=C(N3)N)C(=O)NC(CCC(=O)O)C(=O)O | ||
| Melting Point | Not Available | ||
| Water Solubility | Not Available | ||
| State | Solid | ||
| LogP/Hphobicity | Not Available | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Metabolized by Cytochrome P450 Enzymes | ||
| Half Life | 3.5 hours | ||
| Protein Binding [%] | 81% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Pemetrexed.html http://www.rxlist.com/cgi/generic3/alimta.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00573 | ||
| CAS Registry Number | 150399-23-8 | ||
| KEGG Compound ID | Not Available | ||
| PubChem ID | SID:197081 | ||
| PharmGKB ID | PA10810 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2253437 |
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