Drug intelligence / Profile preview

olaparib + topotecan

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Olaparib + topotecan is an experimental combination of two small-molecule anticancer drugs. **Olaparib** is a poly(ADP-ribose) polymerase (PARP) inhibitor that impairs DNA repair in tumor cells, particularly those with homologous recombination deficiency (e.g., BRCA mutations). **Topotecan** is a topoisomerase I inhibitor that induces DNA damage by interfering with DNA relegation during replication. The combination aims to enhance antitumor activity by combining PARP inhibition with DNA-damaging chemotherapy, exploiting synthetic lethality and synergistic cytotoxicity seen in preclinical and early clinical studies for various advanced solid tumors, especially ovarian cancer[1][2]. Development as a regimen has focused on investigational use, with studies limited by overlapping haematological toxicity[1].

02

Targets

PARP2 (Poly (adp-ribose) polymerase 2)TOP1 (DNA Topoisomerase I)

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