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EP0057 + olaparib
- Development stage
- Phase 2
- Lead developer
- Ellipses Pharma
- Modality
- Small Molecules, Nanoparticles → Drug Delivery Systems
- Administration
- Intravenous, Oral
01
Overview
EP0057 + olaparib is an investigational drug combination for cancer therapy. **EP0057** is a nanoparticle-drug conjugate consisting of a cyclodextrin-linked camptothecin, facilitating improved delivery and accumulation of the cytotoxic camptothecin in tumor tissue[3]. **Olaparib** is a small molecule inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes (PARP1 and PARP2); inhibition of these enzymes blocks DNA repair mechanisms, particularly in tumor cells with BRCA mutations, promoting cell death[2][4]. The combination aims to enhance antitumor activity: EP0057 induces DNA damage, and olaparib inhibits DNA repair, leading to synthetic lethality. This combination is being developed primarily for small cell lung cancer and advanced ovarian cancer[1][3][5][7].
- Other names
- camptothecin nanoparticle drug conjugate + olaparibEP0057 + Lynparza
02
Targets
PARP1 (Poly (adp-ribose) polymerase 1)PARP2 (Poly (adp-ribose) polymerase 2)TOP1 (DNA Topoisomerase I)
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