Poly-ADP-ribosyl-polymerase inhibitor resistance mechanisms and their therapeutic implications

Curr Opin Obstet Gynecol. 2019 Feb;31(1):12-17. doi: 10.1097/GCO.0000000000000517.

Abstract

Purpose of review: Poly-ADP-ribosyl-polymerase (PARP) inhibitors are an increasingly-utilized therapy in women with high-grade serous ovarian carcinoma, but tumor resistance to PARP inhibitor monotherapy is inevitable.

Recent findings: PARP inhibitors have been most studied in patients with breast and ovarian cancers associated with deleterious germline BRCA1 or BRCA2 mutations, though their role has expanded to include use as maintenance therapy in women with platinum-sensitive high-grade serous ovarian cancer due to the high propensity of such cancers to have defects in DNA repair by homologous recombination. As mechanisms of PARP inhibitor resistance are elucidated, rationale combination strategies can be devised to extend therapeutic benefits and to abrogate resistance.

Summary: Mechanisms of resistance include restoration of homologous recombination repair proficiency, loss of cancer cell reliance on PARP, and increased intracellular signaling through cell growth pathways.

Publication types

  • Review

MeSH terms

  • BRCA1 Protein / drug effects
  • BRCA2 Protein / drug effects
  • Clinical Trials as Topic
  • Drug Resistance, Neoplasm / drug effects*
  • Female
  • Humans
  • Ovarian Neoplasms / drug therapy*
  • Ovarian Neoplasms / pathology
  • Phthalazines / pharmacology
  • Phthalazines / therapeutic use*
  • Piperazines / pharmacology
  • Piperazines / therapeutic use*
  • Poly(ADP-ribose) Polymerase Inhibitors / pharmacology
  • Poly(ADP-ribose) Polymerase Inhibitors / therapeutic use*

Substances

  • BRCA1 Protein
  • BRCA1 protein, human
  • BRCA2 Protein
  • Phthalazines
  • Piperazines
  • Poly(ADP-ribose) Polymerase Inhibitors
  • olaparib