Drug intelligence / Profile preview

niraparib + temozolomide

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Niraparib + temozolomide is an investigational combination therapy consisting of two small molecule drugs used primarily in oncology clinical trials. Niraparib is a potent, selective oral inhibitor of poly(ADP-ribose) polymerase 1 and 2 (PARP1/2), enzymes involved in DNA repair. Temozolomide is an oral alkylating agent that induces DNA damage by methylation, leading to tumor cell death. The rationale for combining these agents is based on the hypothesis that PARP inhibition potentiates the cytotoxic effects of temozolomide by blocking DNA repair pathways, thereby increasing cancer cell sensitivity to alkylating damage. This combination has been studied in advanced cancers such as glioblastoma and Ewing sarcoma, with early-phase trials demonstrating tolerability at adjusted doses and preliminary antitumor activity[1][3][4][5][6]. The most common toxicities are hematologic (thrombocytopenia, neutropenia, anemia). Clinical development continues for recurrent/progressive glioblastoma and other solid tumors.

Other names
niraparib + temozolomide
02

Targets

DNAPARP2 (Poly (adp-ribose) polymerase 2)

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