Drug intelligence / Profile preview

SRT501

Development stage
Phase 1
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

SRT501 is a micronized oral formulation of resveratrol, a naturally occurring polyphenol, developed by Sirtris (a GSK Company). The micronization process was designed to enhance the bioavailability and absorption of resveratrol, which typically exhibits poor pharmacokinetic properties in standard formulations. SRT501 acts as an activator of Sirtuin 1 (SIRT1), a NAD+-dependent deacetylase that regulates various metabolic, inflammatory, and cell-survival pathways. The drug was evaluated in Phase 1 and Phase 2 clinical trials for several indications, including colorectal cancer with hepatic metastases, type 2 diabetes, and multiple myeloma. However, GSK discontinued the development of SRT501 in 2010 following safety concerns, specifically the occurrence of acute renal failure in patients during a Phase 2 trial for multiple myeloma.

Other names
micronized resveratrol
02

Targets

SIRT1 (NAD-dependent protein deacetylase sirtuin-1)SIRT5 (NAD-dependent protein deacylase sirtuin-5, mitochondrial)SIRT3 (NAD-dependent protein deacetylase sirtuin-3)

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