Resistance patterns with tyrosine kinase inhibitors in melanoma: new insights

Curr Opin Oncol. 2012 Mar;24(2):150-4. doi: 10.1097/CCO.0b013e32834fca92.

Abstract

Purpose of review: After years of therapeutic approaches with limited effects in metastatic melanoma, new inhibitors of serine-threonine and tyrosine kinases have demonstrated impressive clinical efficacy and improved survival.

Recent findings: This review explains the molecular background for the development of specific kinase inhibitors and briefly summarizes their clinical impact on advanced melanoma.

Summary: Despite robust early clinical efficacy, the antiproliferative effect of these kinase inhibitors is limited. The resistance mechanisms are explored currently and will help to identify new targets for melanoma therapy.

Publication types

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

MeSH terms

  • Antineoplastic Agents / therapeutic use*
  • Drug Resistance, Neoplasm* / genetics
  • Genes, ras / genetics
  • Humans
  • Indoles / therapeutic use
  • Melanoma / drug therapy*
  • Melanoma / genetics
  • Protein Kinase Inhibitors / therapeutic use*
  • Protein-Serine-Threonine Kinases / antagonists & inhibitors*
  • Proto-Oncogene Proteins B-raf / genetics
  • Skin Neoplasms / drug therapy*
  • Skin Neoplasms / genetics
  • Sulfonamides / therapeutic use
  • Vemurafenib

Substances

  • Antineoplastic Agents
  • Indoles
  • Protein Kinase Inhibitors
  • Sulfonamides
  • Vemurafenib
  • BRAF protein, human
  • Protein-Serine-Threonine Kinases
  • Proto-Oncogene Proteins B-raf