Talazoparib

What it is and how it works

Mechanism of Action Talazoparib is an inhibitor of PARP enzymes, including PARP1 and PARP2, which play a role in DNA repair. In vitro studies with cancer cell lines that harbored defects in DNA repair genes, including BRCA1 and BRCA2 , have shown that talazoparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting 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 .

Indications

is a poly (ADP-ribose) polymerase (PARP) inhibitor indicated for: Breast Cancer • As a single agent, for the treatment of adult patients with deleterious or suspected deleterious germline BRCA -mutated (g BRCA m) HER2-negative locally advanced or metastatic breast cancer. Select patients for therapy based on an FDA-approved companion diagnostic for TALZENNA. HRR Gene-mutated Metastatic Castration-Resistant Prostate Cancer (mCRPC) • In combination with enzalutamide for the treatment of adult patients with HRR gene-mutated metastatic castration-resistant prostate cancer (mCRPC). BRCA -mutated (g BRCA m) HER2-negative Locally Advanced or Metastatic Breast Cancer TALZENNA is indicated as a single agent for the treatment of adult patients with deleterious or suspected deleterious germline breast cancer susceptibility gene ( BRCA )-mutated (g BRCA m) human epidermal growth factor receptor 2 (HER2)-negative locally advanced or metastatic breast cancer. Select patients for therapy based on an FDA-approved companion diagnostic for TALZENNA .

Dosage and administration (summary)

• Take TALZENNA with or without food. Breast Cancer • The recommended dosage of TALZENNA is 1 mg taken orally once daily until disease progression or unacceptable toxicity. • For adverse reactions, consider dosing interruption or dose reduction. HRR Gene-mutated Metastatic Castration-Resistant Prostate Cancer (mCRPC) • The recommended dosage of TALZENNA is 0.5 mg taken orally once daily with enzalutamide until disease progression or unacceptable toxicity. • Patients should also receive a gonadotropic-releasing hormone (GnRH) analog concurrently or should have had bilateral orchiectomy.

Contraindications

None. None.

Warnings and precautions

• Myelodysplastic Syndrome/Acute Myeloid Leukemia (MDS/AML) : MDS/AML occurred in patients exposed to TALZENNA, and some cases were fatal. Monitor patients for hematological toxicity and discontinue if MDS/AML is confirmed. • Myelosuppression : TALZENNA may affect hematopoiesis and can cause anemia, neutropenia, and/or thrombocytopenia. • Embryo-Fetal Toxicity : TALZENNA can cause fetal harm. Advise of the potential risk to the fetus and to use effective contraception.

Pregnancy

Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action , TALZENNA can cause embryo-fetal harm when administered to a pregnant woman. There are no available data on TALZENNA use in pregnant women to inform a drug-associated risk.

Storage and supply

Storage Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F). .

Source: Talazoparib (Talzenna) — US FDA prescribing information, 2026-06-01, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.