Talazoparib
Talazoparib is a potent PARP1/2 inhibitor that traps the PARP-DNA complex on damaged DNA, preventing repair and causing irreparable double-strand breaks and cell death specifically in tumor cells with homologous recombination deficiency (HRD) such as BRCA1/2-mutated cancers. It is approved for the treatment of HER2-negative locally advanced or metastatic breast cancer in patients with germline BRCA mutations, and is under investigation in other BRCA-associated tumors. Its high PARP-trapping potency provides superior cytotoxicity in BRCA-deficient cells compared to earlier PARP inhibitors.
Masse moléculaire
380,4000 g/mol
LogP
2,30
TPSA
84,20 Ų
Règle des 5 de Lipinski
Conforme
Aires thérapeutiques
Mécanisme d'action
Inhibits poly(ADP-ribose) polymerase (PARP) enzymes involved in DNA single-strand break repair, exploiting homologous recombination deficiency in cancer cells to cause synthetic lethality.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Inhibits poly(ADP-ribose) polymerase (PARP) enzymes involved in DNA single-strand break repair, exploiting homologous recombination deficiency in cancer cells to cause synthetic lethality.
Structure 2D
Cite this structure
Embed this structure
SMILES
Cn1ncnc1[C@H]1c2n[nH]c(=O)c3cc(F)cc(c23)N[C@@H]1c1ccc(F)cc1
InChI
InChI=1S/C19H14F2N6O/c1-27-18(22-8-23-27)15-16(9-2-4-10(20)5-3-9)24-13-7-11(21)6-12-14(13)17(15)25-26-19(12)28/h2-8,15-16,24H,1H3,(H,26,28)/t15-,16-/m1/s1
Molecular Formula
C19H14F2N6O
HBD / HBA
2 / 7
Liaisons Rotatives
2
Atomes Lourds
28
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
Foire aux questions
Talazoparib is a potent PARP1/2 inhibitor that traps the PARP-DNA complex on damaged DNA, preventing repair and causing irreparable double-strand breaks and cell death specifically in tumor cells with homologous recombination deficiency (HRD) such as BRCA1/2-mutated cancers. It is approved for the treatment of HER2-negative locally advanced or metastatic breast cancer in patients with germline BRCA mutations, and is under investigation in other BRCA-associated tumors. Its high PARP-trapping potency provides superior cytotoxicity in BRCA-deficient cells compared to earlier PARP inhibitors.
Inhibits poly(ADP-ribose) polymerase (PARP) enzymes involved in DNA single-strand break repair, exploiting homologous recombination deficiency in cancer cells to cause synthetic lethality.
Yes, Talazoparib is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL3137320. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 135565082. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.
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