Prexasertib: an investigational checkpoint kinase inhibitor for the treatment of high-grade serous ovarian cancer

Giulio Evangelisti, Fabio Barra, Melita Moioli, Paolo Sala, Sara Stigliani, Claudio Gustavino, Sergio Costantini, Simone Ferrero

Research output: Contribution to journalArticlepeer-review


Introduction: Patients with high-grade serous ovarian cancer (HGSOC) have a poor prognosis, and current chemotherapy regimens for treating advanced disease are far from satisfactory. Prexasertib (LY2606368) is a novel checkpoint kinase inhibitor (CHK) under investigation for the treatment of HGSOC. Data from a recent phase II trial showed promising efficacy and safety results for treating wild-type BRCA HGSOC. Areas covered: This article reviews the available data on the pharmacokinetics, pharmacodynamics, clinical efficacy, and safety of prexasertib in the treatment of HGSOC. Expert opinion: Until now, prexasertib demonstrated clinical activity in phase I and II clinical trial for treating wild-type BRCA HGSOC, whereas its promising efficacy as monotherapy and combined with olaparib in BRCA-mutated HGSOC has been preliminary evidenced only in phase I studies. Compared to other drugs of the same class, prexasertib showed a better tolerability profile, causing moderate hematological toxicity. Further studies are needed to confirm efficacy and safety profiles of prexasertib in combined regimens. New early clinical trials may investigate prexasertib administered with programmed cell death ligand 1 (PD-L1) and PI3 K inhibitors due to the preclinical evidence of a synergic action.

Original languageEnglish
Pages (from-to)779-792
Number of pages14
JournalExpert Opinion on Investigational Drugs
Issue number8
Publication statusPublished - Aug 2 2020


  • Checkpoint kinase 1
  • checkpoint kinase 2
  • CHK inhibitors
  • high-grade serous ovarian cancer
  • homologous recombination
  • LY2606368
  • olaparib
  • PARP inhibitors
  • prexasertib

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)


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