Analysis of Safety from a Human Clinical Trial with Pterostilbene

Abstract

Objectives. The purpose of this trial was to evaluate the safety of long-term pterostilbene administration in humans. Methodology. The trial was a prospective, randomized, double-blind placebo-controlled intervention trial enrolling patients with hypercholesterolemia (defined as a baseline total cholesterol ≥200 mg/dL and/or baseline low-density lipoprotein cholesterol ≥100 mg/dL). Eighty subjects were divided equally into one of four groups: (1) pterostilbene 125 mg twice daily, (2) pterostilbene 50 mg twice daily, (3) pterostilbene 50 mg + grape extract (GE) 100 mg twice daily, and (4) matching placebo twice daily for 6–8 weeks. Safety markers included biochemical and subjective measures. Linear mixed models were used to estimate primary safety measure treatment effects. Results. The majority of patients completed the trial (91.3%). The average age was 54 years. The majority of patients were females (71%) and Caucasians (70%). There were no adverse drug reactions (ADRs) on hepatic, renal, or glucose markers based on biochemical analysis. There were no statistically significant self-reported or major ADRs. Conclusion. Pterostilbene is generally safe for use in humans up to 250 mg/day.

Plant stilbenes induce endoplasmic reticulum stress and their anti-cancer activity can be enhanced by inhibitors of autophagy

“…Potential applications of stilbenes in the areas of aging and cancer have been investigated [21]. However, to date, there is not a recognized, FDAapproved therapeutic application of stilbenes in humans, although toxicity studies have shown pterostilbene to be safe to humans up to a dose of 250 mg/day [22]. …”

Pterostilbene surpassed resveratrol for anti-inflammatory application: Potency consideration and pharmacokinetics perspective

“…The aforementioned might explain why PTS is usually found to be more potent than RES in various previous reports (Yeo et al, 2013). Moreover, PTS displayed favourable safety profiles in both pre-clinical and clinical studies (Riche et al, 2013;Ruiz et al, 2009). Therefore, PTS appears to be a candidate with greater promise than RES for further development.…”

Involvement of the Nrf2 Pathway in the Regulation of Pterostilbene-Induced Apoptosis in HeLa Cells via ER Stress

“…In mice fed Pte for 28 days at doses up to 3000 mg/kg body weight/day, equivalent to 500 times the estimated mean human intake (25 mg/day), no significant toxic effects or adverse biochemical parameters were noted, compared to controls (35). Recent reports suggest that in humans Pte up to a dose of 250 mg/day does not have any adverse toxic effects on hepatic and renal functions, thereby emphasizing its importance as a safe drug (36).…”