New Agent Taranabant Inhibits Food Intake and Stimulates Metabolism

Taranabant, a novel cannabinoid 1 (CB1) receptor inverse agonist, induces weight loss by reducing appetite by reducing caloric intake by 22% and increasing energy expenditure and fat oxidation, according to a compilation of research data from a new study.

Dr. Steven B. Heymsfield at Merck Research Laboratories in Rahway, New Jersey, stated that, using PET scanning, "our study showed that taranabant entered the brain and bound to the CB1 receptor, occupying about 30% on average of the CNS receptors." "This is the first CB1R drug study to show these relations in humans, a finding important in drug dosing concepts and in developing further understanding of side effects."

"Also," he added, "taranabant is thought to work outside the small area of the hypothalamus known to have important body weight regulatory effects. These novel actions provide new therapeutic opportunities for weight management given the very limited current repertoire of weight-loss drugs."

In a dose range-finding weight loss study, taranabant induced significant weight loss in obese subjects (BMI between 30 and 43), the authors report. The study was completed by 368 of the original 533 subjects who were randomly assigned to placebo or to taranabant up to 6 mg per day.

In the per-protocol analysis, mean weight changes from baseline to week 12 were -1.4 kg in the placebo group and -3.6, -4.3, -5.2, and -6.3 kg in groups assigned to taranabant 0.5 mg, 2 mg, 4 mg, and 6 mg, respectively.  Gastrointestinal-related adverse events and psychiatric symptoms were common, causing 32 affected subjects to discontinue treatment.
In a 24-hour food intake study that included 36 overweight and moderately obese participants (BMI 25 to 35), total calorie intake was reduced significantly by 22% in subjects randomly assigned to 12 mg taranabant in comparison with placebo. The active comparator sibutramine 30 mg led to a corresponding 12% reduction.

During 2-5 hours post-dose, compared with placebo, "the geometric mean ratio of peak resting energy expenditure after treatment with 12 mg of taranabant and 30 mg of sibutramine was 1.06 (p = .011) and 1.03 (p = .190), respectively," the investigators report.

Dr. Heymsfield’s group also noted a significant decrease in mean respiratory quotient following taranabant 12 mg, "suggesting increased fat metabolism."

"Such modest increases in energy expenditure, particularly when combined with appetite suppression, could exert profound effects on body weight over a period of months," the research team concludes.

Cell Metabolism Jan. 2008;7:68-78.

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