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QuickView for Pemetrexed (compound)

Name: pemetrexed
PubChem Compound ID: 125891
Molecular formula: C20H19N5Na2O6
Molecular weight: 471.375 g/mol
Rolazar; Alimta; LY 231514; 150399-23-8; Tifolar; Pemetrexed disodium; LY 231514 disodium; L-Glutamic acid, N-(4-(2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrolo(2,3-d)pyrimidin-5-yl)ethyl)benzoyl)-, disodium salt
Name: pemetrexed
Name (isomeric): DB00642
Drug Type: small molecule
Pemetrexed Disodium; LY231514
Brand: Alimta
Category: Antimetabolites, Antimetabolites, Antineoplastic, Antineoplastic Agents, Enzyme Inhibitors, Folic Acid Antagonists
CAS number: 150399-23-8
Indication: Used in combination with cisplatin for the treatment of malignant pleural mesothelioma in adults whose disease is unresectable or who otherwise are not candidates for potentially curative surgery. Also used as a monotherapy for the treatment of 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 formyltra...
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Protein binding: 81%
Biotransformation: Metabolized by Cytochrome P450 Enzymes
Route of elimination: Pemetrexed is not metabolized to an appreciable extent and is primarily eliminated in the urine, with 70% to 90% of the dose recovered unchanged within the first 24 hours following administration.
Half Life: 3.5 hours
Clearance: 91.8 mL/min [Cancer patients with normal renal function receiving 0.2 to 838 mg/m2 infusion over a 10-minute period]
Affected organisms: Humans and other mammals
Drug interaction:
SulindacThe NSAID, sulindac, may increase the serum concentration of pemetrexed by decreasing its elimination. This interaction more prevalent in patients with mild to moderate renal insufficiency. Consider alternate therapy or monitor for pemetrexed toxicity during concomitant therapy.
KetoprofenThe NSAID, ketoprofen, may increase increase the serum concentration of pemetrexed by decreasing its renal clearance. Patients with mild to moderate renal insufficiency (CrCl 45-79 ml/min) should avoid use of ketoprofen within 2 days of a pemetrexed dose. Patients with better renal function do not appear to be at risk. Monitor for toxicity in all patients during concomitant therapy.
TolmetinTolmetin may decrease the renal excretion of Pemetrexed in patients with decreased creatinine clearance. Tolmetin may be withheld in these patients from 2 days before to 2 days after Pemetrexed administration.
Tiaprofenic acidTiaprofenic acid may decrease Pemetrexed excretion. Tiaprofenic acid should not be used around the time when Pemetrexed is administered.