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Folate-targeted chemotherapy

Christopher P Leamon1, Joseph A Reddy

  • 1Endocyte, Inc., 1205 Kent Ave., West Lafayette, IN 47906, USA. Leamon@Endocyte.com

Advanced Drug Delivery Reviews
|April 20, 2004
PubMed

Insights

Folate receptor targeted drug delivery utilizes folate-drug conjugates to deliver potent agents to cancer cells. This review covers preclinical screening, activity data, and emerging animal studies for these novel therapeutics.

Area of Science:

  • Oncology
  • Pharmacology
  • Drug Delivery

Background:

  • The folate receptor (FR) is a tumor-associated antigen.
  • FR binds folate and folate-drug conjugates with high affinity.
  • FR facilitates cellular uptake via endocytosis.

Purpose of the Study:

  • To review preclinical screening methods for folate-drug conjugates.
  • To summarize published activity data of various folate-drug conjugates.
  • To highlight emerging preclinical animal data for novel folate-drug conjugates.

Main Methods:

  • Review of preclinical screening strategies.
  • Compilation and summary of published conjugate activity.
  • Analysis of emerging animal data for novel compounds.

Main Results:

  • Folate-drug conjugates can deliver diverse payloads to FR-positive cells.
  • Attachment of potent small molecular weight agents to folate is a novel therapeutic approach.
  • Emerging animal data show promise for novel folate-drug conjugates.

Conclusions:

  • Folate-drug conjugates represent a promising targeted therapeutic strategy.
  • Preclinical evaluation is crucial for optimizing conjugate design and efficacy.
  • Further investigation in animal models is essential to advance this approach.

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