Niraparib (Zejula)

Other Medications · Approved since 2017

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

Description

Niraparib is an oral PARP (poly ADP-ribose polymerase) inhibitor that has shown activity in colorectal cancer, particularly in patients with homologous recombination deficiency. In CRC treatment, niraparib is being explored as maintenance therapy following oxaliplatin-based chemotherapy and in combination with EGFR inhibitors like panitumumab for advanced or metastatic disease. The drug shows particular promise in colorectal cancers with PALB2 mutations and other DNA repair defects.

Mechanism of Action

Niraparib selectively inhibits PARP-1 and PARP-2 enzymes, which are essential for single-strand DNA break repair through the base excision repair pathway. By blocking PARP function, the drug causes accumulation of DNA damage that leads to synthetic lethality in cancer cells with defective homologous recombination repair, such as those with BRCA1/2, PALB2, or other DNA repair gene mutations.

Molecular Targets

Side Effects

Thrombocytopenia Anemia Neutropenia Fatigue Nausea Constipation Vomiting Abdominal pain Mucositis Diarrhea Decreased appetite Headache Insomnia

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

Clinical Trials

NCT05412706 Phase 2
Archived
Niraparib Maintenance Treatment in mCRC With a Partial o Complete Response After Oxaliplatin-based Induction Therapy
Multiple
NCT05169437 Phase 2
Terminated
Niraparib in the Treatment of Patients With Advanced PALB2 Mutated Tumors
United States
NCT03983993 Phase 2
Active, not recruiting
Niraparib and Panitumumab in Patients With Advanced or Metastatic Colorectal Cancer
United States