The Antifolates

Michele Visentin, Rongbao Zhao, I. David Goldman

Research output: Contribution to journalReview articlepeer-review

200 Scopus citations


This article focuses on the cellular, biochemical, and molecular pharmacology of antifolates and how a basic understanding of the mechanism of action of methotrexate, its cytotoxic determinants, mechanisms of resistance, and transport into and out of cells has led to the development of a new generation of antifolates, a process that continues in the laboratory and in the clinics. New approaches to folate-based cancer chemotherapy are described based on the targeted delivery of drugs to malignant cells.

Original languageEnglish (US)
Pages (from-to)629-648
Number of pages20
JournalHematology/Oncology Clinics of North America
Issue number3
StatePublished - Jun 2012


  • Antifolates
  • Folate receptor-mediated endocytosis
  • Folate receptors
  • Methotrexate
  • Pemetrexed
  • Pralatrexate
  • Proton-coupled folate transporter (PCFT)
  • Reduced folate carrier (RFC)

ASJC Scopus subject areas

  • Hematology
  • Oncology


Dive into the research topics of 'The Antifolates'. Together they form a unique fingerprint.

Cite this