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Pemetrexed



Pemetrexed
Systematic (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
Identifiers
CAS number 137281-23-3
ATC code L01BA04
PubChem 60843
DrugBank APRD00573
Chemical data
Formula C20H21N5O6 
Mol. mass 427.411 g/mol
Pharmacokinetic data
Bioavailability NA
Protein binding 81%
Metabolism Negligible
Half life 3.5 hours
Excretion Renal
Therapeutic considerations
Licence data

EU US

Pregnancy cat.

D(US)

Legal status

POM(UK) -only(US)

Routes IV

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.

Additional recommended knowledge

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 in 2004 year.

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.

 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Pemetrexed". A list of authors is available in Wikipedia.
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