Talazoparib

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.

• TALZENNA 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.ICD-10: C50.919

• None. None.contraindicated

• Take TALZENNA with or without food. ( 2.4 ) Breast Cancer • The recommended dosage of TALZENNA is 1 mg taken orally once daily until disease progression or unacceptable toxicity. ( 2.2 ) • For adverse reactions, consider dosing interruption or dose reduction. ( 2.5 ) 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. ( 2.3 ) • Patients should also receive a gonadotropic-releasing hormone (GnRH) analog concurrently or should have had bilateral orchiectomy. ( 2.3 ) 2.1 Patient Selection Information on the FDA-approved tests for the detection of genetic mutations is available at http://www.fda.gov/companiondiagnostics . g BRCA m HER2-negative Locally Advanced or Metastatic Breast Cancer Select patients for the treatment of advanced breast cancer with TALZENNA based on the presence of germline BRCA mutations [see Indications and Usage (1.1) , Clinical Studies (14.1) ] . HRR Gene-mutated Metastatic Castration-Resistant Prostate Cancer Select patients for the treatment of HRR gene-mutated mCRPC with TALZENNA based on the presence of alterations in genes directly or indirectly involved in HRR ( ATM , ATR , BRCA1 , BRCA2 , CDK12 , CHEK2 , FANCA , MLH1 , MRE11A , NBN , PALB2 , or RAD51C ) [see Indications and Usage (1.2) , Clinical Studies (14.2) ] . An FDA-approved test for the detection of HRR gene mutations for use with TALZENNA is not currently available.

• 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. ( 5.1 ) • Myelosuppression : TALZENNA may affect hematopoiesis and can cause anemia, neutropenia, and/or thrombocytopenia. ( 5.2 ) • Embryo-Fetal Toxicity : TALZENNA can cause fetal harm. Advise of the potential risk to the fetus and to use effective contraception. ( 5.3 , 8.1 , 8.3 ) 5.1 Myelodysplastic Syndrome/Acute Myeloid Leukemia Myelodysplastic Syndrome/Acute Myeloid Leukemia (MDS/AML), including cases with a fatal outcome, has been reported in patients who received TALZENNA. Overall, MDS/AML has been reported in 0.4% (3 out of 788) of solid tumor patients treated with TALZENNA as a single agent in clinical studies. In TALAPRO-2, MDS/AML occurred in 2 out of 511 (0.4%) patients treated with TALZENNA and enzalutamide and in 0 out of 517 (0%) patients treated with placebo and enzalutamide [see Adverse Reactions (6.1) ] . The durations of TALZENNA treatment in these 5 patients prior to developing MDS/AML were 0.3, 1, 2, 3, and 5 years. Most of these patients had received previous chemotherapy with platinum agents and/or other DNA damaging agents including radiotherapy. Do not start TALZENNA until patients have adequately recovered from hematological toxicity caused by previous chemotherapy. Monitor blood counts monthly during treatment with TALZENNA.

The following clinically significant adverse reactions are described elsewhere in the labeling: • Myelodysplastic Syndrome/Acute Myeloid Leukemia [see Warnings and Precautions (5.1) ] • Myelosuppression [see Warnings and Precautions (5.2) ] Most common adverse reactions (≥20%) as a single agent, including laboratory abnormalities, are: • Hemoglobin decreased, neutrophils decreased, lymphocytes decreased, platelets decreased, fatigue, glucose increased, aspartate aminotransferase increased, alkaline phosphatase increased, alanine aminotransferase increased, calcium decreased, nausea, headache, vomiting, alopecia, diarrhea, and decreased appetite. ( 6.1 ) Most common adverse reactions (≥10%) in combination with enzalutamide, including laboratory abnormalities, are: • Hemoglobin decreased, neutrophils decreased, lymphocytes decreased, fatigue, platelets decreased, calcium decreased, nausea, decreased appetite, sodium decreased, phosphate decreased, fractures, magnesium decreased, dizziness, bilirubin increased, potassium decreased, and dysgeusia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Pfizer Inc. at 1-800-438-1985 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

• Lactation : Advise women not to breastfeed. ( 8.2 ) • Renal Impairment : Reduce the dose and monitor for increased adverse reactions for patients with moderate or severe renal impairment. ( 2.6 , 8.7 ) 8.1 Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action [see Clinical Pharmacology (12.1) ] , 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. In an animal reproduction study, the administration of talazoparib to pregnant rats during the period of organogenesis caused fetal malformations and structural skeletal variations and embryo-fetal death at maternal exposures that were 0.24 times the AUC in patients receiving the recommended dose of 1 mg daily (see Data ) . Apprise pregnant women and females of reproductive potential of the potential risk to a fetus. The background risk of major birth defects and miscarriage for the indicated population is unknown. In the general U.S. population, the estimated background risks of major birth defects and miscarriage in clinically recognized pregnancies are 2% to 4% and 15% to 20%, respectively. Data Animal Data In an embryo-fetal development toxicity study, pregnant rats received oral doses of 0.015, 0.05, and 0.15 mg/kg/day talazoparib during the period of organogenesis.

Metabolism

After administration of TALZENNA 1 mg orally once daily as a single agent (the recommended dosage for breast cancer), the mean [% coefficient of variation (CV%)] AUC and maximum observed plasma concentration (C max ) of talazoparib at steady-state was 208 (37%) ng.hr/mL and 16.4 (32%) ng/mL, respectively. The mean (CV%) steady-state C trough was 3.53 (61%) ng/mL.

• Oct 16, 2018NDANDA211651Pfizer
• Mar 7, 2024NDANDA217439Pfizer

1. 1Anaemia26315%
2. 2Neoplasm Progression17110%
3. 3Death17010%
4. 4Fatigue1156.8%
5. 5Off Label Use965.7%
6. 6Thrombocytopenia945.5%
7. 7Haemoglobin Decreased784.6%
8. 8Platelet Count Decreased734.3%
9. 9Febrile Neutropenia684.0%
10. 10Malignant Neoplasm Progression673.9%
11. 11Pancytopenia663.9%
12. 12Nausea613.6%
13. 13Neutropenia543.2%
14. 14Asthenia533.1%
15. 15Dyspnoea492.9%

The 10 most recently updated of 121 ClinicalTrials.gov registrations naming Talazoparib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Presurgical Phase II Study of Talazoparib in Combination With Enzalutamide in Prostate Cancer
  Recruiting · Phase 2 · Interventional · 30 enrolled · M.D. Anderson Cancer Center
  NCT05873192updated 2026-06-12
• Talazoparib in Treating Patients With Recurrent, Refractory, Advanced, or Metastatic Cancers and Alterations in the BRCA Genes
  Active not recruiting · Phase 2 · Interventional · 150 enrolled · M.D. Anderson Cancer Center
  NCT02286687updated 2026-06-12
• Testing Maintenance Therapy for Small Cell Lung Cancer in Patients With SLFN11 Positive Biomarker
  Active not recruiting · Phase 2 · Interventional · 103 enrolled · National Cancer Institute (NCI)
  NCT04334941updated 2026-06-05
• TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer
  Recruiting · Phase 2 · Interventional · 4,200 enrolled · American Society of Clinical Oncology
  NCT02693535updated 2026-05-29
• Study of Onivyde With Talazoparib or Temozolomide in Children With Recurrent Solid Tumors and Ewing Sarcoma
  Recruiting · Phase 1 · Phase 2 · Interventional · 90 enrolled · St. Jude Children's Research Hospital
  NCT04901702updated 2026-05-19
• Measuring the Effects of Talazoparib in Patients With Advanced Cancer and DNA Repair Variations
  Recruiting · Phase 2 · Interventional · 36 enrolled · National Cancer Institute (NCI)
  NCT04550494updated 2026-05-13
• Testing the Combination of the Anti-cancer Drugs ZEN003694 (ZEN-3694) and Talazoparib in Patients With Advanced Solid Tumors, The ComBET Trial
  Recruiting · Phase 2 · Interventional · 88 enrolled · National Cancer Institute (NCI)
  NCT05327010updated 2026-05-13
• Phase Ia/Ib Talazoparib + Tazemetostat for mCRPC
  Active not recruiting · Phase 1 · Interventional · 35 enrolled · Dana-Farber Cancer Institute
  NCT04846478updated 2026-05-12
• I-SPY TRIAL: Neoadjuvant and Personalized Adaptive Novel Agents to Treat Breast Cancer
  Recruiting · Phase 2 · Interventional · 5,000 enrolled · QuantumLeap Healthcare Collaborative
  NCT01042379updated 2026-05-06
• Evaluation of Talazoparib, a PARP Inhibitor, in Patients With Somatic BRCA Mutant Metastatic Breast Cancer: Genotyping Based Clinical Trial
  Recruiting · Phase 2 · Interventional · 30 enrolled · Massachusetts General Hospital
  NCT03990896updated 2026-05-06

Frequently asked questions

How does Talazoparib work?

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.

What is Talazoparib used for?

According to FDA labeling, Talazoparib carries indications including: TALZENNA 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Talazoparib?

Talazoparib is classified as Poly (ADP-ribose) polymerase (PARP) inhibitors, Poly(ADP-Ribose) Polymerase Inhibitor, Poly(ADP-Ribose) Polymerase Inhibitors, Decreased DNA Integrity, Increased Cellular Death.

What are the brand names for Talazoparib?

Talazoparib is marketed under brand names including Talzenna.

What are the contraindications for Talazoparib?

Talazoparib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.