Talazoparib (BMN 673)
Catalog No.S7048 Synonyms: LT-673
Molecular Weight(MW): 380.35
Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.
Cited by 79 Publications
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|Description||Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.|
|Features||Most potent and selective PARPi reported thus far.|
BMN-673 selectively binds to PARP and prevents PARP-mediated DNA repair of single strand DNA breaks via the base-excision repair pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability and eventually leads to apoptosis. BMN 673 selectively kills cancer cells with BRCA-1 or BRCA-2 mutations. BMN 673 demonstrates single-agent cytotoxicityin BRCA-1 mutant (MX-1, IC50 = 0.3 nM) and BRCA-2 mutant cells (Capan-1, IC50 = 5 nM). In contrast, in MRC-5 normal human fibroblastand other tumor cell lines with wild-type BRCA-1 and BRCA-2 genes, IC50 of BMN 673 ranges between 90 nM and 1.9 μM.  In cultured human cancer cells, BMN 673 also significantly enhances the cytotoxic efficacy of both Temozolomide and SN-38. Off-target molecular screening did not identify significant non-specific activity for this class of PARP inhibitors. 
|In vivo||In rat pharmacokinetic studies, BMN 673 displays >50% oralbioavailability and pharmacokinetic properties that enable singledaily dosing. In MX-1 xenograft tumor model studies, daily oral dosingof BMN 673 significantly enhances the antitumor effects ofcytotoxic therapies in a dose-dependent manner. |
|In vitro||DMSO||38 mg/mL warmed (99.9 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03974217||Recruiting||Drug: Talazoparib||Leukemia||Dana-Farber Cancer Institute|Pfizer||August 1 2019||Phase 1|
|NCT03901469||Recruiting||Drug: ZEN003694|Drug: Talazoparib||Triple Negative Breast Cancer||Zenith Epigenetics|Pfizer||June 26 2019||Phase 2|
|NCT03911973||Recruiting||Drug: Gedatolisib|Drug: Talazoparib||TNBC - Triple-Negative Breast Cancer||Kari Wisinski|Pfizer|Big Ten Cancer Research Consortium||April 17 2019||Phase 1|Phase 2|
|NCT03875313||Recruiting||Drug: CB-839|Drug: Talazoparib||Solid Tumor|Clear Cell Renal Cell Carcinoma|TNBC - Triple-Negative Breast Cancer|Colorectal Cancer|CRC|RCC|ccRCC||Calithera Biosciences Inc||March 22 2019||Phase 1|Phase 2|
|NCT03672773||Recruiting||Drug: Talazoparib|Drug: Temozolomide||Recurrent Extensive Stage Small Cell Lung Carcinoma|Refractory Extensive Stage Small Cell Lung Carcinoma||Jonsson Comprehensive Cancer Center|Translational Research in Oncology|National Cancer Institute (NCI)||October 31 2018||Phase 2|
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Frequently Asked Questions
Which solvent do you recommend to dilute the inhibitor for in vivo study in mice?
BMN673 (S7048) can be dissolved in vehicle (10% DMAc, 6% Solutol, and 84% PBS) according to the paper: http://clincancerres.aacrjournals.org/content/19/18/5003.full. Quote from Method and Material section "Xenograft experiments: BMN 673 (various doses as indicated), or vehicle (10% DMAc, 6% Solutol, and 84% PBS) was administered by oral gavage"