Savolitinib: First Approval

Drugs. 2021 Sep;81(14):1665-1670. doi: 10.1007/s40265-021-01584-0.

Abstract

Savolitinib (Orpathys®; HUTCHMED, AstraZeneca) is a receptor tyrosine kinase mesenchymal epithelial transition factor (MET) inhibitor being developed for the treatment of metastatic non-small cell lung cancer (NSCLC), papillary and clear cell renal cell carcinoma (RCC), gastric cancer and colorectal cancer. Based on the results of a pivotal phase II trial in patients with NSCLC/pulmonary sarcomatoid carcinoma, savolitinib was recently granted approval in China (conditional on the results of a phase III trial) for the treatment of metastatic NSCLC with MET exon 14-skipping alterations in patients who have progressed after or who are unable to tolerate platinum-based chemotherapy. This article summarizes the milestones in the development of savolitinib leading to this first approval.

Publication types

  • Review

MeSH terms

  • Carcinoma, Non-Small-Cell Lung / drug therapy
  • Carcinoma, Non-Small-Cell Lung / genetics
  • Carcinoma, Renal Cell / drug therapy
  • China
  • Clinical Trials, Phase II as Topic
  • Colorectal Neoplasms / drug therapy
  • Drug Approval
  • Humans
  • Kidney Neoplasms / drug therapy
  • Lung Neoplasms / drug therapy
  • Lung Neoplasms / genetics
  • Neoplasm Metastasis / drug therapy
  • Pyrazines / therapeutic use*
  • Stomach Neoplasms / drug therapy
  • Triazines / therapeutic use*

Substances

  • Pyrazines
  • Triazines
  • 1-(1-(imidazo(1,2-a)pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-(1,2,3)triazolo(4,5-b)pyrazine