Resistance to Poly (ADP-Ribose) Polymerase Inhibitors (PARPi): Mechanisms and Potential to Reverse

Curr Oncol Rep. 2022 Dec;24(12):1685-1693. doi: 10.1007/s11912-022-01337-6. Epub 2022 Nov 8.

Abstract

Purpose of review: This review will focus on the most common mechanisms for poly (ADP-ribose) polymerase inhibitors' (PARPi) resistance and the main strategies for overcoming acquired or de novo PARPi resistance.

Recent findings: Initial approvals for PARPi as part of treatment for advanced epithelial ovarian cancer (EOC) started in 2014 with patient with recurrent cancer characterized by BRCA mutations in the 3rd and 4th line and now have approvals for front-line maintenance in both the BRCA mutated and BRCAwt populations. As with all therapies, patients will eventually develop resistance to treatment. The most common mechanisms for PARPi resistance include reversion mutations, methylation events, and restoration of homologous recombination deficiency (HRD) through combinations and targeting replication stress. As more and more patients receive initial treatment (and potential retreatment with PARPi), we need to better understand the mechanisms in which tumors acquire PARPi resistance.

Keywords: BRCA mutation; Epithelial ovarian cancer; Homologous recombination deficiency; Niraparib; Olaparib; PARP inhibitor resistance; PARP inhibitors; Restoration of homologous recombination proficiency; Rucaparib.

Publication types

  • Review

MeSH terms

  • Adenosine Diphosphate / therapeutic use
  • Female
  • Humans
  • Neoplasm Recurrence, Local / drug therapy
  • Ovarian Neoplasms* / drug therapy
  • Ovarian Neoplasms* / genetics
  • Ovarian Neoplasms* / pathology
  • Poly(ADP-ribose) Polymerase Inhibitors* / pharmacology
  • Poly(ADP-ribose) Polymerase Inhibitors* / therapeutic use
  • Ribose / therapeutic use

Substances

  • Poly(ADP-ribose) Polymerase Inhibitors
  • Ribose
  • Adenosine Diphosphate