C-7 Progesterone Analogues and MDRl in Breast Cancer

Abstract

In the course of the past year, we have completed a meta-analysis of published studies, which confirms the expression and prognostic role of the MDR 1 mechanism of resistance in human breast cancer. In our effort to obtain effective inhibitors of this mechanism, we have synthesized some novel progesterone analogs. Among these, PgA4 is in vitro about 30-fold more potent a MDR1 inhibitor than the parental compound. Obtaining an MTD in vivo is limited by PgA4 low water solubility. We have defined a cyclodextrin-based formulation which, because of increased PgA4 solubility and decreased local tissue toxicity, will allow the in vivo administration of repeated and higher doses of PgA4.

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Document Details

Document Type
Technical Report
Publication Date
Sep 01, 1997
Accession Number
ADA338786

Entities

People

  • Robert R. Clarke

Organizations

  • Georgetown University

Tags

DTIC Thesaurus Topics

  • Analogs
  • Breast Cancer
  • Carbon Carbon Composites
  • Cells
  • Chemical Analysis
  • Chemistry
  • Chemotherapy
  • Drug Resistance
  • Inhibitors
  • Macrocyclic Compounds
  • Materials
  • Oxidation
  • Progesterone
  • Resistance
  • Solubility
  • Test And Evaluation
  • Toxicity

Fields of Study

  • Chemistry

Readers

  • Oncology (Cancer Research).
  • Organic Chemistry
  • Solar Photovoltaics and Thermoelectric Devices.