Talazoparib (TALZENNA™) is an oral inhibitor of the polyadenosine 5'-diphosphoribose polymerase (PARP) enzymes, which play a critical role in repairing DNA single-strand breaks. It has been developed by Pfizer and was recently approved in the USA for the treatment of adults with deleterious or suspected deleterious germline BRCA-mutated, human epidermal growth factor receptor 2 (HER2)-negative, locally advanced or metastatic breast cancer (as detected by a US FDA-approved assay). A regulatory assessment for talazoparib in this patient population is underway in the EU, with talazoparib also undergoing development for use in metastatic castration-resistant prostate cancer and various solid tumours, and as neoadjuvant therapy in early triple negative breast cancer. This article summarizes the milestones in the development of talazoparib leading to its first approval for the treatment of adults with deleterious or suspected deleterious germline BRCA-mutated, HER2-negative, locally advanced or metastatic breast cancer.