In this review, we introduce the class of PARP inhibitors and current clinical applications; the importance of brain-penetrant drugs in the neuro-oncology setting; the rationale to combine PARP inhibitors with radiotherapy, chemotherapy and immunotherapy; the rationale to use PARP inhibitors within selected subgroups such as IDH-mutant gliomas; and review current and prospective clinical trials. The gene discussed is PARP1; the disease is central nervous system cancer.