Development of the Commercial Manufacturing Process for Ipatasertib

Chimia (Aarau). 2021 Aug 25;75(7-8):605-613. doi: 10.2533/chimia.2021.605.

Abstract

Ipatasertib is a potent small molecule Akt kinase inhibitor currently being tested in Phase III clinical trials for the treatment of metastatic castration-resistant prostate cancer and triple negative metastatic breast cancer. In this paper an overview of the development achievements towards the commercial manufacturing process is given. The convergent synthesis consists of ten steps with eight isolated intermediates and utilizes a wide range of chemical techniques and technologies to build-up this complex drug. All three stereocenters are introduced using enzyme or metal catalysis.

MeSH terms

  • Antineoplastic Combined Chemotherapy Protocols*
  • Humans
  • Male
  • Neoplasms* / drug therapy
  • Piperazines / therapeutic use
  • Pyrimidines / therapeutic use

Substances

  • Piperazines
  • Pyrimidines
  • ipatasertib