Drug intelligence / Profile preview

SAHA-OBP

Development stage
Preclinical
Modality
Small Molecules
Administration
Not Established In Humans, In Vitro Studies: Not Applicable
01

Overview

SAHA-OBP is a small molecule prodrug of suberoylanilide hydroxamic acid (SAHA, also known as vorinostat) that is specifically designed to be activated by high levels of reactive oxygen species (ROS), which are typically elevated in cancer cells. The drug chemically incorporates a 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl carbonyl (OBP) group, which is cleaved in the presence of hydrogen peroxide. This releases active SAHA only in the tumor microenvironment, leading to selective activation in cancer cells and sparing normal tissue. The released SAHA inhibits histone deacetylases (HDACs), resulting in accumulation of acetylated histones and the induction of apoptosis in malignant cells. SAHA-OBP demonstrates selective cytotoxicity against various cancer cell lines (HeLa, MCF-7, MDA-MB-231, B16-F10) and does not show significant toxicity toward non-cancerous cells. It has also shown efficacy in multicellular tumor spheroid models as an antitumor agent[1][2][13].

02

Targets

HDAC1 (Histone Deacetylase 1)

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