Design and tumor targeting of anthracyclines able to overcome multidrug resistance: A double-advantage approach

Waldemar Priebe, Roman Perez-Soler

Research output: Contribution to journalReview article

60 Scopus citations

Abstract

A novel 'double-advantage approach' to developing more effective chemotherapies will be reviewed. This approach is based on a presumption that analogs designed on a sound hypothesis, and combined with a rationally selected drug delivery system, will optimize antitumor activity by creating drugs that are more active and that can be more specifically targeted to tumors. In the design of drugs superior to doxorubicin, we have focused on typical multidrug resistance and new anthracycline analogs, whose uptake is not affected by P-glycoprotein. Analysis of structural elements of anthracyclines affecting activity against multidrug resistant tumors and affinity for liposomes will be discussed. Annamycin, a lipophilic anthracycline analog, was selected for further preclinical development as a liposomal formulation and demonstrated, in the initial biological evaluation, high activity against tumors resistant to doxorubicin.

Original languageEnglish (US)
Pages (from-to)215-234
Number of pages20
JournalPharmacology and Therapeutics
Volume60
Issue number2
DOIs
Publication statusPublished - 1993
Externally publishedYes

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Keywords

  • Antitumor agents
  • anamycin
  • anthracyclines
  • doxorubicin
  • drug design
  • multidrug resistance

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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