Talazoparib (Talzenna)

Other Medications · Approved since 2018

US Off-label EU EMA Approved ES Hospital use off-label in CRC Oral 3 Clinical Trials
PARP-1 PARP-2

Description

Talazoparib is a potent PARP inhibitor that has shown activity in colorectal cancer patients with specific genetic alterations, particularly those with homologous recombination deficiency or BRCA mutations. In CRC, this targeted therapy is utilized in patients whose tumors harbor DNA repair defects that make them vulnerable to PARP inhibition. The drug works by exploiting synthetic lethality in cancer cells that already have compromised DNA repair mechanisms.

Mechanism of Action

Talazoparib selectively inhibits poly(ADP-ribose) polymerase (PARP) enzymes, particularly PARP-1 and PARP-2, which are essential for single-strand DNA break repair. By blocking PARP function, the drug prevents repair of DNA damage, leading to accumulation of double-strand breaks that are lethal to cancer cells with defective homologous recombination repair pathways. This creates a synthetic lethal interaction that preferentially kills tumor cells while sparing normal cells with intact DNA repair mechanisms.

Molecular Targets

Side Effects

Anemia Neutropenia Thrombocytopenia Fatigue Nausea Headache Vomiting Alopecia Diarrhea Decreased appetite Abdominal pain Dizziness

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT05327010 Phase 2
Recruiting
Testing the Combination of the Anti-cancer Drugs ZEN003694 (ZEN-3694) and Talazoparib in Patients With Advanced Solid Tumors, The ComBET Trial
United States
NCT05725200 Phase 2
Recruiting
Study to Investigate Outcome of Individualized Treatment in Patients With Metastatic Colorectal Cancer
Norway
NCT03875313 Phase 1
Archived
Study of CB-839 (Telaglenastat) in Combination With Talazoparib in Patients With Solid Tumors
United States