Drug intelligence / Profile preview

SI-10

Development stage
Preclinical
Lead developer
Baylor College of Medicine
Modality
Small Molecules
01

Overview

SI-10 is a small molecule inhibitor of Steroid Receptor Coactivator-3 (SRC-3), also known as Nuclear receptor coactivator 3 (NCOA3). It is being investigated as a potential therapeutic strategy for aggressive and ibrutinib-resistant mantle cell lymphoma (MCL) and other B-cell lymphomas. SRC-3 is a transcriptional coactivator that is frequently overexpressed in the lymph nodes of B-cell non-Hodgkin's lymphoma patients and plays a critical role in driving tumor progression and drug resistance. SI-10 has demonstrated dose-dependent cytotoxicity in MCL cell lines and significant in vivo efficacy, extending survival in ibrutinib-resistant murine models and human patient-derived xenograft (PDX) models with low toxicity.

02

Targets

NCOA3 (Nuclear receptor coactivator 3)

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