irinotecan liposome injection

Liposomal irinotecan hydrochloride (ONIVYDE) is a topoisomerase I inhibitor encapsulated within a lipid bilayer vesicle or liposome. This nanoliposomal formulation contains approximately 80,000 molecules of irinotecan encapsulated in a 100-nm liposome sphere[5]. The liposomal encapsulation extends plasma levels of irinotecan and prolongs exposure of SN-38, leading to increased antitumor activity compared to conventional irinotecan[4]. Topoisomerase I relieves torsional strain in DNA by inducing single-strand breaks. Irinotecan and its active metabolite SN-38 bind reversibly to the topoisomerase I-DNA complex and prevent re-ligation of these single-strand breaks, which leads to exposure time-dependent double-strand DNA damage and cell death[2][9]. In preclinical studies, liposomal irinotecan achieved similar intratumoral exposure of SN-38 at doses 5-fold lower than conventional irinotecan hydrochloride[2][9]. The drug is primarily indicated, in combination with fluorouracil and leucovorin, for the treatment of adult patients with metastatic pancreatic adenocarcinoma after disease progression following gemcitabine-based therapy[1][7].

Brand names

ONIVYDE

Other names

liposomal irinotecan hydrochlorideirinotecan hydrochloride liposomalnanoliposomal irinotecan