Drug intelligence / Profile preview

Niraparib + pegylated liposomal doxorubicin

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous, Oral
01

Overview

Niraparib + pegylated liposomal doxorubicin is an investigational combination therapy for cancer treatment, particularly ovarian cancer. Niraparib is a potent and selective small molecule inhibitor of poly(ADP-ribose) polymerase (PARP) enzymes PARP-1 and PARP-2. By inhibiting these enzymes involved in DNA repair pathways—especially base excision repair—niraparib induces synthetic lethality in tumor cells with homologous recombination deficiency (such as those with BRCA mutations)[6][1]. Pegylated liposomal doxorubicin is a formulation of the anthracycline chemotherapeutic agent doxorubicin encapsulated in PEG-coated liposomes to enhance tumor targeting and reduce toxicity[3][5][8]. Doxorubicin works by intercalating DNA and inhibiting topoisomerase II activity[5]. The combination aims to exploit synergistic cytotoxicity by simultaneously impairing DNA repair (via PARP inhibition) and inducing DNA damage (via topoisomerase II inhibition), potentially improving efficacy while managing toxicity profiles[1].

Other names
PARP inhibitor + anthracycline liposome combination
02

Targets

PARP1 (Poly (adp-ribose) polymerase 1)PARP2 (Poly (adp-ribose) polymerase 2)Pol II (RNA polymerase II elongation factors)TOP2A (DNA topoisomerase II)

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