Olaparib for the treatment of breast cancer

Research output: Contribution to journalReview article

Abstract

INTRODUCTION: Mutations in BRCA1 and BRCA2 genes account for around 2-3% of breast cancer events and more than 10% of triple negative breast cancers. Olaparib (Lynparza®), an orally administered PARP inhibitor, demonstrated clinical benefit in a phase III trial for mutated BRCA-positive HER2 negative metastatic breast cancer. Areas covered: This review gives an overview of available preclinical and clinical data regarding olaparib, including its chemistry, mechanism of action, pharmacokinetics and pharmacodynamics, and evidence supporting antitumor efficacy and safety profile in breast cancer patients. Expert commentary: Olaparib improves progression-free survival in germline BRCA mutated HER2 negative metastatic breast cancer patients as compared to standard chemotherapy, with a manageable toxicity profile. Efficacy is of clinical relevance especially in the context of triple negative breast cancer. However, several aspects, such as sequencing or combination of these agents with other anticancer agents and identification of appropriate biomarkers, still need to be clearly defined.

Original languageEnglish
Pages (from-to)519-530
Number of pages12
JournalExpert Review of Anticancer Therapy
Volume18
Issue number6
DOIs
Publication statusPublished - Jun 2018

Fingerprint

Triple Negative Breast Neoplasms
Breast Neoplasms
BRCA2 Gene
BRCA1 Gene
Therapeutics
Antineoplastic Agents
Disease-Free Survival
Pharmacokinetics
Biomarkers
Safety
Drug Therapy
Mutation
olaparib
Poly(ADP-ribose) Polymerase Inhibitors
Breast Cancer 3

Keywords

  • Antineoplastic Agents/adverse effects
  • BRCA1 Protein/genetics
  • BRCA2 Protein/genetics
  • Breast Neoplasms/drug therapy
  • Disease-Free Survival
  • Female
  • Humans
  • Phthalazines/adverse effects
  • Piperazines/adverse effects
  • Poly(ADP-ribose) Polymerase Inhibitors/adverse effects
  • Receptor, ErbB-2/metabolism

Cite this

Olaparib for the treatment of breast cancer. / Griguolo, Gaia; Dieci, Maria Vittoria; Guarneri, Valentina; Conte, PierFranco.

In: Expert Review of Anticancer Therapy, Vol. 18, No. 6, 06.2018, p. 519-530.

Research output: Contribution to journalReview article

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abstract = "INTRODUCTION: Mutations in BRCA1 and BRCA2 genes account for around 2-3{\%} of breast cancer events and more than 10{\%} of triple negative breast cancers. Olaparib (Lynparza{\circledR}), an orally administered PARP inhibitor, demonstrated clinical benefit in a phase III trial for mutated BRCA-positive HER2 negative metastatic breast cancer. Areas covered: This review gives an overview of available preclinical and clinical data regarding olaparib, including its chemistry, mechanism of action, pharmacokinetics and pharmacodynamics, and evidence supporting antitumor efficacy and safety profile in breast cancer patients. Expert commentary: Olaparib improves progression-free survival in germline BRCA mutated HER2 negative metastatic breast cancer patients as compared to standard chemotherapy, with a manageable toxicity profile. Efficacy is of clinical relevance especially in the context of triple negative breast cancer. However, several aspects, such as sequencing or combination of these agents with other anticancer agents and identification of appropriate biomarkers, still need to be clearly defined.",
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AU - Griguolo, Gaia

AU - Dieci, Maria Vittoria

AU - Guarneri, Valentina

AU - Conte, PierFranco

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AB - INTRODUCTION: Mutations in BRCA1 and BRCA2 genes account for around 2-3% of breast cancer events and more than 10% of triple negative breast cancers. Olaparib (Lynparza®), an orally administered PARP inhibitor, demonstrated clinical benefit in a phase III trial for mutated BRCA-positive HER2 negative metastatic breast cancer. Areas covered: This review gives an overview of available preclinical and clinical data regarding olaparib, including its chemistry, mechanism of action, pharmacokinetics and pharmacodynamics, and evidence supporting antitumor efficacy and safety profile in breast cancer patients. Expert commentary: Olaparib improves progression-free survival in germline BRCA mutated HER2 negative metastatic breast cancer patients as compared to standard chemotherapy, with a manageable toxicity profile. Efficacy is of clinical relevance especially in the context of triple negative breast cancer. However, several aspects, such as sequencing or combination of these agents with other anticancer agents and identification of appropriate biomarkers, still need to be clearly defined.

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