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irinotecan + olaparib
- Development stage
- Unknown
- Lead developer
- AstraZeneca
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Irinotecan + olaparib is an investigational combination therapy consisting of two small molecule drugs: irinotecan, a topoisomerase I inhibitor, and olaparib, a poly(ADP-ribose) polymerase (PARP) inhibitor. Irinotecan interferes with DNA replication by inhibiting topoisomerase I, leading to DNA strand breaks and cell death. Olaparib inhibits PARP enzymes involved in single-strand DNA break repair; this inhibition leads to accumulation of DNA damage and synthetic lethality in tumor cells with defective homologous recombination repair mechanisms. Preclinical studies have shown that combining these agents can potentiate anti-tumor effects, particularly in cancers with deficiencies in DNA repair pathways such as BRCA-mutated tumors. The combination has been evaluated primarily in early-phase clinical trials for advanced colorectal cancer and pancreatic ductal adenocarcinoma (PDAC), but significant toxicities have limited its further development[1][2][3].
- Brand names
- Camptosar (irinotecan)Lynparza (olaparib)
- Other names
- irinotecan + olaparib
02
Targets
PARP1 (Poly (adp-ribose) polymerase 1)TOP1 (DNA Topoisomerase I)
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