Nucleus: The Chemical Blogspace Blog

VIVUS, Inc on 7. January 201, announced positive results from a phase 2 study evaluating the safety and efficacy of Qnexa®, an investigational drug, for the treatment of obstructive sleep apnea (OSA). VIVUS recently completed phase 3 development of Qnexa for the treatment of obesity and submitted a New Drug Application (NDA) to the FDA for that indication. The OSA- study announced  demonstrated statistically significant improvement in the apnea/hypopnea index (“AHI” – a measure of the severity of sleep apnea) in patients with OSA treated with Qnexa for 28 weeks.

OSA is a sleep-related breathing disorder that involves a decrease or complete halt in airflow despite an ongoing effort to breathe. OSA is associated with an increased risk of hypertension, diabetes, stroke, sudden cardiac death and all-cause mortality. Currently, there are no approved pharmacologic treatments for OSA and current treatment approaches are limited to devices or surgery, so if approved by the FDA, Qnexa®  not only reduce the weight  but also significantly improve sleep apnea.

Ref : http://ir.vivus.com/releasedetail.cfm?ReleaseID=434708

We knew that Lorcaserin, is a serotonergic weight-loss drug developed by Arena Pharmaceuticals. It is currently undergoing the final phase of clinical trials in preparation for submission for FDA approval.

Lorcaserin is a selective 5-HT2C receptor agonist and in vitro testing of the drug showed reasonable selectivity for 5-HT2C over other related targets 5-HT2C receptors are located almost exclusively in the brain, and can be found in the choroid plexus, cortex, hippocampus, cerebellum, amygdala, thalamus, and hypothalamus.

Mode of action : Arena believes that the activation of 5-HT2C receptors in the hypothalamus promotes weight loss through appetite suppression, and this is supported by animal studies, but it is unclear whether the dose range used in human trials will be sufficient to demonstrate the same level of weight loss. While it is generally thought that 5-HT2C receptors help to regulate appetite as well as mood, motor behavior, and endocrine secretion, the exact mechanism of appetite regulation is not yet known.

Arena reported positive, highly significant top-line results in September 2009. Arena will also present new data analyses from lorcaserin’s successful Phase 3 pivotal program in oral and poster sessions. In an independent clinical symposium, expert academic scientists and physicians will spotlight the 5HT-2C mechanism for weight management. As per the claim by the company, the positive results from the Phase 3 pivotal program highlight lorcaserin’s potential to provide physicians with a treatment option that combines three important attributes – efficacy, safety and tolerability. Hope in the days to come will have a drug to treat obesity too…

The Purple Mangosteen (Garcinia mangostana), colloquially known simply as “the mangosteen“, is a tropical evergreen tree, believed to have originated in the Sunda Islands and the Moluccas of Indonesia. The tree grows from 7 to 25 m (20–80 ft) tall. The rind (exocarp) of the edible fruit is deep reddish purple when ripe. Botanically an aril, the fragrant edible flesh can be described as sweet and tangy, citrusy with peach flavor and texture.

Mangosteen is typically advertised and marketed as part of an emerging category of novel functional foods sometimes called “superfruits” presumed to have a combination of 1) appealing subjective characteristics, such as taste, fragrance and visual qualities, 2) nutrient richness, 3) antioxidant strength and 4) potential impact for lowering risk against human diseases.

Though the antioxidant strength was known earlier, a recent study by Dr. Jay Udani and co workers is interesting and as per the claim by the authors, mangosteen juice has anti-inflammatory properties which could prove to be valuable in preventing the development of heart disease and diabetes in obese patients. For people drinking over half a liter of mangosteen juice a day, the degree of reduction in CRP levels was statistically significant – a reduction of 1.33mg/L compared to an increase of 0.9mg/L in the placebo group. Inflammation, as measured here by CRP, is a predictor of cardiovascular disease and a precursor of metabolic syndrome. Reducing inflammation in obese people is a treatment goal, and a natural treatment may be preferable to other treatments which may carry the risk of side effect. Though further studies with a larger population are required to confirm and further define the benefits of this juice, which was safe at all dosages tested its a good achievement. More…