Drug intelligence / Profile preview

irinotecan liposomal (Merrimack Pharmaceuticals)

Development stage
Approved
Lead developer
Merrimack Pharmaceuticals
Modality
Small Molecules, Liposomes → Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

Irinotecan liposomal is a **liposomal formulation of irinotecan**, a topoisomerase I inhibitor, designed to improve delivery and prolong systemic exposure of the active drug. Encapsulation in a lipid bilayer vesicle (liposome) enables higher circulating concentrations, greater tumor uptake, and extended exposure to the active metabolite SN-38, enhancing antitumor activity at potentially lower doses compared to conventional irinotecan[1][4][7]. **Mechanism of action:** Irinotecan and SN-38 bind to the topoisomerase I–DNA complex, preventing re-ligation of single-strand DNA breaks during replication, resulting in double-strand DNA breakage and cell death. The formulation is used primarily in the **treatment of metastatic pancreatic adenocarcinoma in combination with fluorouracil and leucovorin**, including now as first-line therapy combined with oxaliplatin (NALIRIFOX regimen)[5]. It is being investigated for other gastrointestinal and solid tumors[3][4].

Brand names
Onivyde
Other names
irinotecan liposomeirinotecan liposome injectionliposomal irinotecan
02

Targets

TOP1 (DNA Topoisomerase I)

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