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Pemetrexed

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Revision as of 16:17, 18 August 2006 by Phil E.Stein (talk | contribs) (revert to 83)(diff) ← Previous revision | Latest revision (diff) | Newer revision → (diff) Pharmaceutical compound
Pemetrexed
File:Pemetrexed.jpg
Clinical data
Routes of
administration
IV
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityNA
Protein binding81%
MetabolismNegligible
Elimination half-life3.5 hours
ExcretionRenal
Identifiers
IUPAC name
  • 2- nona-3,8,10-trien-9-yl)ethyl] benzoyl] aminopentanedioic acid
CAS Number
PubChem CID
DrugBank
CompTox Dashboard (EPA)
ECHA InfoCard100.205.735 Edit this at Wikidata
Chemical and physical data
FormulaC20H21N5O6
Molar mass427.411 g/mol g·mol

Pemetrexed (brand name Alimta®) is a chemotherapy drug. 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.

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 ..

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