Pemetrexed

Pemetrexed

File:Pemetrexed.svg
Clinical data
[[Regulation of therapeutic goods |Template:Engvar data]]	EU EMA: by INN US FDA: Pemetrexed
Pregnancy category	US: D (Evidence of risk)
Routes of administration	IV
ATC code	L01BA04 (WHO)
Legal status
Legal status	UK: POM (Prescription only) US: ℞-only
Pharmacokinetic data
Bioavailability	NA
Protein binding	81%
Metabolism	Negligible
Elimination half-life	3.5 hours
Excretion	Renal
Identifiers
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
CAS Number	137281-23-3
PubChem CID	60843
DrugBank	APRD00573
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C20H21N5O6
Molar mass	427.411 g/mol

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Overview

Pemetrexed (brand name Alimta®) is a chemotherapy drug manufactured and marketed by Eli Lilly and Company. Its indications are the treatment of pleural mesothelioma as well as non-small cell lung cancer.

History

The molecular structure of pemetrexed was developed by Edward C. Taylor at Princeton University and clinically developed by Indianapolis based drug maker, Eli Lilly and Company.

Mechanism of action

Pemetrexed is chemically similar to folic acid and is in the class of chemotherapy drugs called folate antimetabolites. It works by inhibiting three enzymes used in purine and pyrimidine synthesis—thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyl transferase (GARFT). By inhibiting the formation of precursor purine and pyrimidine nucleotides, pemetrexed prevents the formation of DNA and RNA, which are required for the growth and survival of both normal cells and cancer cells.

Clinical use

In February 2004, the Food and Drug Administration approved pemetrexed for treatment of malignant pleural mesothelioma, a type of tumor of the lining of the lung, in combination with cisplatin. In July 2004, the FDA granted approval as a second-line agent for the treatment of non-small cell lung cancer. Trials are currently testing it against esophagus and other cancers.

Patients are required to be on folic acid and vitamin B12 supplementation when they are on pemetrexed therapy. (In clinical trials for mesothelioma, folic acid and B12 supplementation reduced the frequency of adverse events.) It is also recommended for patients to be on a steroid (e.g. dexamethasone 4mg twice daily) on the day prior, day of, and day after pemetrexed infusion to avoid skin rashes.

External links

• Alimta website
• Alimta / Pemetrexed Virtual Cancer Centre
• NCI Drug Information Summary on Pemetrexed Disodium