Sticking it to KRAS: Covalent Inhibitors Enter the Clinic

Cancer Cell. 2020 Jan 13;37(1):3-4. doi: 10.1016/j.ccell.2019.12.009.

Abstract

Drugs that target KRAS 12C covalently, AMG 510 and MRTX849, are now in the clinic. Recent papers describe development of these compounds, their selectivity and properties, early clinical data, and potential combination therapies. These papers herald a new era in Ras research, with improved drugs and strategies certain to follow.

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Drug Design
  • Drug Evaluation, Preclinical
  • Genes, ras*
  • Humans
  • Mice
  • Mutation
  • Neoplasms / drug therapy
  • Piperazines / pharmacology*
  • Proto-Oncogene Proteins p21(ras) / antagonists & inhibitors*
  • Pyridines / pharmacology*
  • Pyrimidines / pharmacology*
  • Signal Transduction / drug effects
  • Translational Research, Biomedical
  • Treatment Outcome

Substances

  • Antineoplastic Agents
  • KRAS protein, human
  • Piperazines
  • Pyridines
  • Pyrimidines
  • sotorasib
  • Proto-Oncogene Proteins p21(ras)