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Human PK study with SRT501


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#1 malbecman

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Posted 20 June 2011 - 05:41 PM


I guess my desire to see more human studies is being fulfilled. :-D

Note that they were able to detect resveratrol in the liver and a marker for apotosis in the malignant tissue did appear to be increased by 39%.......


Cancer Prev Res (Phila). 2011 Jun 16. [Epub ahead of print]
Phase I randomised double-blind pilot study of micronized resveratrol(SRT501) in patients with hepatic metastases - safety, pharmacokinetics and pharmacodynamics.
Howells LM, Berry DP, Elliott PJ, Jacobson EW, Hoffmann E, Hegarty B, Brown K, Steward W, Gescher AJ.
Source
1Dept of Cancer Studies, Univ of Leicester.
Abstract
The phytochemical resveratrol has undergone extensive preclinical investigation for its putative cancer chemopreventive properties. Low systemic availability of the parent compound due to rapid and extensive metabolism, may confound its usefulness as a potential agent to prevent malignancies in organs remote from the site of absorption. Micronization allows increased drug absorption, thus increasing availability. Here we describe a pilot study of SRT501, micronized resveratrol, given at 5.0 g daily for 14 days, to patients with colorectal cancer and hepatic metastases scheduled to undergo hepatectomy. The purpose of the study was to assess the safety, pharmacokinetics and pharmacodynamics of the formulation. SRT501 was found to be well tolerated. Mean plasma resveratrol levels following a single dose of SRT501 administration were 1942±1422 ng/mL, exceeding those published for equivalent doses of non-micronized resveratrol by 3.6-fold. Resveratrol was detectable in hepatic tissue following SRT501 administration (up to 2287 ng/g). Cleaved caspase-3, a marker of apoptosis, was significantly increased by 39% in malignant hepatic tissue following SRT501 treatment, compared to tissue from the placebo-treated patients. SRT501 warrants further clinical exploration to assess its potential clinical utility.

PMID: 21680702
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