Drug intelligence / Profile preview

SRT501 + bortezomib

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

SRT501 + bortezomib is a combination therapy investigated for the treatment of relapsed and/or refractory multiple myeloma. SRT501 is a micronized oral formulation of resveratrol, a natural polyphenol with proposed cancer-preventive and cytotoxic effects, primarily acting as a Sirtuin Enzyme 1 (SIRT1) activator. Bortezomib is a proteasome inhibitor with established use in multiple myeloma. The rationale for the combination is potential synergy between bortezomib's proteasome inhibition and resveratrol's SIRT1 activation and additional inhibition of cellular signaling pathways (such as nuclear factor kappa B, AKT, and STAT3). In phase 2 studies, the combination achieved low response rates but was associated with significant renal toxicity – the trial was terminated early due to safety concerns including serious renal adverse events[1][3][5].

Other names
bortezomib + SRT501micronized resveratrol + bortezomib
02

Targets

SIRT1 (NAD-dependent protein deacetylase sirtuin-1)PSMB9 (Immunoproteasome subunit beta type-1i)PSMB1 (26S Proteasome (β1-Subunit))PSMB5 (Proteasome subunit beta Type-5)

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