Drug intelligence / Profile preview

sepantronium

Development stage
Phase 2
Lead developer
Astellas Pharma Global Development, Inc.
Modality
Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Sepantronium is a small-molecule proapoptotic agent developed as an antineoplastic drug. Its primary mechanism of action is the selective inhibition of survivin (BIRC5), a member of the inhibitor of apoptosis (IAP) gene family that is overexpressed in many cancers and associated with aggressive tumor phenotypes and poor prognosis. By suppressing survivin expression in a dose- and time-dependent manner, sepantronium induces apoptosis and autophagy in cancer cells. It has demonstrated potent antitumor activity across various human cancer cell lines regardless of p53 status, with notable efficacy in non-Hodgkin's lymphoma, hormone-refractory prostate cancer, ovarian cancer, sarcoma, non-small-cell lung cancer (NSCLC), breast cancer, leukemia, and melanoma[1][2][3]. Sepantronium was investigated primarily as its bromide salt form (sepantronium bromide/YM155). Despite promising preclinical results and early-phase clinical trials showing tolerability when administered intravenously—often by continuous infusion—later-stage trials failed to show significant clinical benefit. All development for oncology indications has been discontinued[3][6][7].

Other names
sepantronium bromidesepantronium cationsepantronium ion
02

Targets

Baculoviral IAP repeat-containing protein 5 promoter

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