Pemetrexed: A novel antifolate agent enters clinical practice

Victoria Kut, Jyoti D. Patel, Athanassios Argiris*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

17 Scopus citations


Pemetrexed (Alimta®, Eli Lilly) is a multitargeted antifolate that inhibits at least three enzymes in the nucleic acid synthetic pathways. The US Food and Drug Administration recently approved pemetrexed, in combination with cisplatin, for the first-line treatment of advanced malignant pleural mesothelioma. Moreover, pemetrexed was recently shown to be as efficacious as docetaxel (Taxotere®, Aventis in the second-line treatment of non-small cell lung cancer, and its toxicity profile was preferable. The main toxicity seen with pemetrexed is myelosuppression, which is considerably reduced by coadministration of folic acid and vitamin B12. Multiple Phase II clinical trials have demonstrated that pemetrexed has promising single-agent activity in many other solid tumors, including head and neck, breast and colorectal cancers. Combination regimens consisting of pemetrexed and other chemotherapeutics or novel molecular-targeted agents are currently under investigation. Future studies will better define and likely expand the role of pemetrexed for the treatment of cancer.

Original languageEnglish (US)
Pages (from-to)511-522
Number of pages12
JournalExpert review of anticancer therapy
Issue number4
StatePublished - Aug 2004


  • Antifolate
  • Mesothelioma
  • Non-small cell lung cancer
  • Pemetrexed
  • Solid tumors

ASJC Scopus subject areas

  • Oncology
  • Pharmacology (medical)


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