Studies with RP 56976 (taxotere): a semisynthetic analogue of taxol

J Natl Cancer Inst. 1991 Feb 20;83(4):288-91. doi: 10.1093/jnci/83.4.288.

Abstract

RP 56976 (taxotere), a new semisynthetic analogue of taxol, is a potentially important chemotherapeutic agent for the treatment of cancer. We report here that this drug is a potent inhibitor of cell replication and, like taxol, promotes the in vitro assembly of stable microtubules in the absence of guanosine triphosphate and induces microtubule-bundle formation in cells. Compared with taxol, RP 56976 is slightly more active as a promoter of tubulin polymerization. As an inhibitor of cell replication, RP 56976 is 2.5-fold more potent than taxol in J774.2 and P388 cells and at least 5-fold more potent in taxol-resistant cells.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Alkaloids / pharmacology*
  • Alkaloids / toxicity
  • Animals
  • Cell Survival / drug effects
  • Cells, Cultured
  • Cricetinae
  • Cricetulus
  • Docetaxel
  • Guanosine Triphosphate / metabolism
  • Leukemia, Lymphoid / drug therapy
  • Leukemia, Lymphoid / pathology
  • Microtubules / drug effects
  • Paclitaxel
  • Structure-Activity Relationship
  • Taxoids*
  • Tumor Cells, Cultured

Substances

  • Alkaloids
  • Taxoids
  • Docetaxel
  • Guanosine Triphosphate
  • Paclitaxel