Synonyms: BMN-673 | BMN673 | Talzenna®
talazoparib is an approved drug (FDA (2018), EMA (2019))
Compound class:
Synthetic organic
Comment: Talazoparib is a PARP inhibitor [8], inhibiting both PARP1 and PARP2 [1,8]. The compound is bioavailable as the tosylate salt (PubChem CID 56966514).
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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No information available. |
Summary of Clinical Use |
Following a positive outcome from Phase 3 clinical trial NCT01945775 [3,5,7], talazoparib received FDA approval in October 2018 as a treatment for patients with deleterious/suspected deleterious germline BRCA-mutated, HER2 negative locally advanced or metastatic breast cancers [4]. In June 2023, FDA approval was expanded to include treatment of homologous recombination repair (HRR) gene-mutated metastatic castration-resistant prostate cancer (mCRPC). |
Mechanism Of Action and Pharmacodynamic Effects |
Talazoparib is a poly ADP ribose polymerase (PARP) inhibitor. PARP is involved in repairing single-strand DNA breaks (nicks). In cells with mutations in other DNA repair enzymes such as the BRCA and PALB2 (Q86YC2) mutations in breast, ovarian and prostate cancers [2], PARP becomes more important for the DNA repair process. In such malignant cells, inhibition of PARP may therefore result in cell death due to accumulated DNA damage. Some PARP inhibitors cause irreversible binding of the enzyme to the DNA in addition to catalytic inhibition [6]. This may result in accumulation of toxic PARP-DNA complexes. |