talazoparib
Trade name: talzenna
Small moleculeapproved
Approved
Oct 16, 2018
Talazoparib (BMN 673) demonstrates excellent potency, inhibiting PARP1 and PARP2 enzyme activity. It inhibits PARP-mediated PARylation in a whole-cell assay and prevents proliferation of cancer cells carrying mutant BRCA1/2. Talazoparib is orally available, displaying favorable pharmacokinetic properties and remarkable antitumor efficacy in the BRCA1 mutant MX-1 breast cancer xenograft model following oral administration as a single-agent or in combination with chemotherapy agents such as temozolomide and cisplatin. Medivation (a subsidiary of Pfizer) is developing talazoparib (MDV 3800, formerly BMN 673 and LT 673) for the treatment of genetically defined cancers. On October 16, 2018, the FDA approved talazoparib (TALZENNA, Pfizer Inc.) for patients with deleterious or suspected deleterious germline BRCA-mutated (gBRCAm), HER2‑negative locally advanced or metastatic breast cancer. — NCATS
Clinical trial activity
107 trials · 83 clinical orgs · 1 marketing orgs
Phase 1
51
Phase 2
72
Phase 3
5
Phase 4
0
Earliest trial started Mar 1, 2010 (NCT01042379)
Timeline
Indications
Approved for
Studied for
- BRCA1 Protein · Phase 2
- Breast Neoplasms · Phase 3
- Carcinoma, Non-Small-Cell Lung · Phase 3
- Carcinoma, Ovarian Epithelial · Phase 2
- Carcinoma, Renal Cell · Phase 2
- Carcinoma, Squamous Cell · Phase 2
- Carcinoma, Transitional Cell · Phase 3
- Colorectal Neoplasms · Phase 2
- Endometrial Neoplasms · Phase 2
- Esophageal Neoplasms · Phase 1
- Fallopian Tube Neoplasms · Phase 2
- Gene Expression · Phase 2
- Glioblastoma · Phase 2
- Glioma · Phase 2
- Hamartoma · Phase 2
- Healthy Volunteers · Phase 1
- Hemangiosarcoma · Phase 2
- Hepatoblastoma · Phase 1/Phase 2
- Kidney Neoplasms · Phase 1/Phase 2
- Leukemia · Phase 1
- Leukemia, Lymphocytic, Chronic, B-Cell · Phase 1
- Leukemia, Myeloid, Acute · Phase 1/Phase 2
- Leukemia, Myelomonocytic, Chronic · Phase 1
- Lung Neoplasms · Phase 2
- Lyme Disease · Phase 2
- Lymphoma · Phase 3
- Lymphoma, Mantle-Cell · Phase 1
- Melanoma · Phase 2
- Mesothelioma · Phase 1
- Mutation · Phase 3
- Myelodysplastic Syndromes · Phase 1
- Neoplasm Metastasis · Phase 2
- Neoplasms · Phase 3
- Neoplasms, Germ Cell and Embryonal · Phase 1/Phase 2
- Neuroblastoma · Phase 1/Phase 2
- Neuroectodermal Tumors · Phase 1/Phase 2
- Neuroendocrine Tumors · Phase 1
- Osteosarcoma · Phase 1/Phase 2
- Ovarian Diseases · Early Phase 1
- Ovarian Neoplasms · Phase 3
- Pancreatic Neoplasms · Phase 2
- Paraganglioma · Phase 2
- Pheochromocytoma · Phase 2
- Polycythemia Vera · Phase 1
- Primary Myelofibrosis · Phase 1
- Prostatic Neoplasms · Phase 3
- Prostatic Neoplasms, Castration-Resistant · Phase 2
- PTEN Phosphohydrolase · Phase 2
- Rhabdoid Tumor · Phase 1/Phase 2
- Rhabdomyosarcoma · Phase 1/Phase 2
- Sarcoma · Phase 1/Phase 2
- Sarcoma, Ewing · Phase 1/Phase 2
- Small Cell Lung Carcinoma · Phase 2
- Squamous Cell Carcinoma of Head and Neck · Phase 2
- Stomach Neoplasms · Phase 2
- Thrombocytosis · Phase 1
- Triple Negative Breast Neoplasms · Phase 2
- Uterine Cervical Neoplasms · Phase 1
- Vaginal Neoplasms · Phase 1
- Wilms Tumor · Phase 1/Phase 2
Mechanism of action
- Poly [ADP-ribose] polymerase-1INHIBITOR
PARP1 inhibitor
Potent PARP1/2 inhibitor (PARP1 IC50 = 0.57 nmol/L). PARP1 Ki=1.2 nmol/L. PARP2 Ki= 0.85 nmol/L.
- Poly [ADP-ribose] polymerase 2INHIBITOR
PARP2 inhibitor
Approval history
- approvedPriority reviewOct 16, 2018
Chemistry & pharmacology
Loading structure…
SMILES
Cn1ncnc1[C@H]1c2n[nH]c(=O)c3cc(F)cc(c23)N[C@@H]1c1ccc(F)cc1- Mol. weight
- 380.36 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL3137320 ↗
- WikipediaTalazoparib ↗
- NCATS9QHX048FRV ↗
- ChEMBLCHEMBL3137318 ↗
Also known as
- bmn 673
- bmn 673
- bmn 673
- bmn 673
- bmn-673
- bmn-673
- bmn 673ts
- bmn 673ts
- talazoparib
- talazoparib
- talazoparib
- talazoparib
- talazoparib
- talazoparib tosylate
- talazoparib tosylate
- talazoparib tosylate
- talazoparib tosylate
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06762808 | Phase 2 | Jun 1, 2025 | Genentech, University of Texas at Houston |
| NCT06844383 | Phase 2 | Apr 30, 2025 | Harvard University, Memorial Sloan-Kettering Cancer Center, Pfizer, Prostate Cancer Clinical Trials Consortium |
| NCT06582628 | Phase 2 | Jul 5, 2024 | Fundacion Oncosur, Universidad Complutense de Madrid |
| NCT06218628 | Phase 1 | Apr 5, 2024 | Temple University |
| NCT05873192 | Phase 2 | Sep 30, 2023 | University of Texas at Houston |
| NCT05898399 | Phase 1/Phase 2 (Phase 2) | Jun 30, 2023 | Artios |
| NCT05425862 | Phase 1 | Oct 21, 2022 | Peter MacCallum Cancer Centre |
| NCT05319249 | Phase 1/Phase 2 (Phase 2) | Sep 30, 2022 | German Cancer Research Center |
| NCT05725200 | Phase 2 | Sep 27, 2022 | University of Oslo |
| NCT05327010 | Phase 2 | Aug 4, 2022 | National Cancer Institute (NCI), University of Texas at Houston |
| NCT05101551 | Phase 1 | Mar 31, 2022 | Stanford University |
| NCT05288127 | Phase 2 | Mar 8, 2022 | Cancer Research Malaysia, Pfizer, University of Malaya |
| NCT05071937 | Phase 2 | Jan 31, 2022 | Case Western Reserve University, Pfizer, University of Pittsburgh, Zenith Epigenetics |
| NCT05142241 | Phase 2 | Jan 14, 2022 | National Cancer Institute (NCI), National Institutes of Health (NIH) |
| NCT05097599 | Phase 2 | Oct 21, 2021 | Strata Oncology |
| NCT04756765 | Phase 2 | Sep 30, 2021 | Pfizer, Stanford University |
| NCT05059522 | Phase 3 | Sep 29, 2021 | Pfizer |
| NCT05053854 | Phase 1 | Sep 27, 2021 | Peter MacCallum Cancer Centre |
| NCT04991480 | Phase 1/Phase 2 (Phase 2) | Sep 13, 2021 | Artios, Tennessee Oncology, PLLC, University of Texas at Houston |
| NCT04819243 | Phase 2 | Sep 1, 2021 | Sungkyunkwan University |
Showing 20 of 107 trials
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Organizations
Research & Development (83)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Pfizer | For profit | 47 | 14 | 4 | 2013 |
| National Cancer Institute (NCI) | Government | 18 | 10 | 2 | 2013 |
| Medivation | For profit | 16 | 12 | 3 | 2010 |
| University of Texas at Houston | Academic/Hospital | 10 | 7 | 2 | 2014 |
| Harvard University | Academic/Hospital | 7 | 5 | 2 | 2016 |
| Biomarin | For profit | 4 | 0 | 2 | 2014 |
| Genentech | For profit | 4 | 0 | 1 | 2020 |
| Memorial Sloan-Kettering Cancer Center | Academic/Hospital | 4 | 3 | 1 | 2019 |
| National Institutes of Health (NIH) | Government | 3 | 0 | 1 | 2015 |
| Peter MacCallum Cancer Centre | Academic/Hospital | 3 | 3 | 2 | 2021 |
| Southwest Oncology Group | Academic/Hospital | 3 | 2 | 1 | 2017 |
| Stanford University | Academic/Hospital | 3 | 3 | 2 | 2015 |
| Artios | For profit | 2 | 2 | 1 | 2021 |
| Astellas | For profit | 2 | 0 | 2 | 2019 |
| Calithera Biosciences | For profit | 2 | 1 | 1 | 2019 |
| Case Western Reserve University | Academic/Hospital | 2 | 2 | 1 | 2020 |
| Foundation Medicine | For profit | 2 | 0 | 1 | 2020 |
| Hoosier Cancer Research Network | Academic/Hospital | 2 | 0 | 1 | 2021 |
| Indiana University | Academic/Hospital | 2 | 2 | 2 | 2019 |
| Myrexis Inc. | For profit | 2 | 0 | 1 | 2014 |
83 organizations
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