Drug intelligence / Profile preview

niraparib + carboplatin

Development stage
Discontinued
Lead developer
GSK
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Niraparib + carboplatin is a **combination therapy** of the small molecule PARP inhibitor **niraparib** and the **platinum-based chemotherapy agent** carboplatin. Niraparib acts by selectively inhibiting poly(ADP-ribose) polymerase (PARP)-1 and PARP-2, enzymes crucial for the base excision repair pathway of single-strand DNA breaks. In tumors deficient in homologous recombination repair (such as those with BRCA1/2 mutations or other forms of homologous recombination deficiency), inhibition of PARP leads to accumulation of DNA damage and cell death (synthetic lethality). Carboplatin exerts cytotoxic effects by forming inter- and intra-strand DNA crosslinks, thus inhibiting DNA replication and transcription, which triggers apoptosis in rapidly dividing tumor cells. The combination is being studied in advanced solid tumors with homologous recombination deficiency where synergistic effects on DNA damage-based cytotoxicity are hypothesized.

Other names
niraparib plus carboplatinniraparib and carboplatin
02

Targets

DNADAT (Dopamine plasma membrane transport protein)NET (Norepinephrine Transporter)PARP1 (Poly (adp-ribose) polymerase 1)PARP2 (Poly (adp-ribose) polymerase 2)SERT (Sodium-dependent serotonin transporter)Pol II (RNA polymerase II elongation factors)

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