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Talzenna (Talazoparib Tosylate)

Pfizer Inc. · FDA-approved approved Small molecule Verified Quality 75/100

PARP1/PARP2 inhibitor causing DNA damage, decreased proliferation, and apoptosis in BRCA-mutated cancers.

Talazoparib is a PARP inhibitor indicated for gBRCAm HER2-negative breast cancer as monotherapy and HRR gene-mutated mCRPC with enzalutamide. It demonstrates linear pharmacokinetics with a 90-hour half-life and primarily renal excretion, requiring dose adjustment in moderate-to-severe renal impairment. P-gp inhibitors significantly increase talazoparib exposure and require dose reduction or avoidance. FDA-approved companion diagnostics are required for patient selection in both indications.

At a glance

Generic nameTalazoparib Tosylate
SponsorPfizer Inc.
Drug classPARP inhibitor
TargetPARP1 and PARP2 enzymes
ModalitySmall molecule
Therapeutic areaOncology
PhaseFDA-approved
Annual revenue182

Mechanism of action

Talazoparib inhibits poly(ADP-ribose) polymerase enzymes (PARP1 and PARP2) that play a role in DNA repair. In vitro studies with cancer cell lines harboring defects in DNA repair genes, including BRCA1 and BRCA2, have shown that talazoparib-induced cytotoxicity involves inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes. This results in DNA damage, decreased cell proliferation, and apoptosis. Talazoparib anti-tumor activity was observed in patient-derived xenograft breast cancer models bearing mutated BRCA1 or mutated BRCA2 or wild type BRCA1 and BRCA2.

Approved indications

Common side effects

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Patents

PatentExpiryType

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SourceUsed for
FDA Orange BookPatents + exclusivity
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