Saturday, September 30, 2017

Drugs in Clinical Pipeline: SUVN-502 | 5-HT6 receptor antagonist | Treatment for Alzheimer's Disease

SUVN- 502 is a novel, potent, and selective 5-HT6 receptor antagonist with Ki of 1.71 nM and exhibited antagonist like inhibition with EC50 of 0.103 mM. SUVN-502 is effective in animal models of cognition. In microdialysis studies, SUVN-502 enhanced brain acetylcholine and glutamate levels in rat ventral hippocampus and frontal cortex. SUVN-502 has completed all regulatory safety and toxicity studies.

5-HT6 receptor a member of serotonin family predominates in brain regions associated with cognition and behavior. The blockade of 5-HT6 receptors leads to an improvement of cognitive performance in a wide variety of learning and memory paradigms.

Saturday, September 23, 2017

Drugs in Clinical Pipeline: CT1812 | Abeta Oligomers Receptor Antagonist | Treatment for Alzheimer's Disease

CT1812, works by a completely novel mechanism to stop the binding of toxic proteins that build up in the brains of Alzheimer's patients known as Abeta oligomers.

CT1812, a novel oligomer receptor antagonist is the only drug candidate that has demonstrated not only prevention but it also displaces binding of Abeta oligomers to receptors on brain cells. By stopping the initiating event in the Abeta oligomer cascade, this first-in-class drug candidate completely blocks downstream synaptotoxicity and restores memory to normal in aged transgenic mouse models of Alzheimer's disease.

Friday, September 15, 2017

Drugs in Clinical Pipeline: GRC 27864 | Microsomal Prostaglandin E Synthase-1 (mPGES-1) Inhibitor | Treatment for Chronic Inflammatory Diseases

GRC 27864 is a potent, selective, orally bioavailable inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1). Prostaglandins (PGs) are an important class of lipids related both to physiological and pathological conditions. Among them, prostaglandin E2 (PGE2) is a key mediator of inflammation, pain and fever, but it is also important for the protection of the gastrointestinal mucosa, nutriuresis, blood pressure regulation, and ovulation.

Microsomal prostaglandin E2 synthase-1 (mPGES-1) catalyzes the terminal step of prostaglandin E2 (PGE2) generation. mPGES-1 is strongly upregulated in inflamed tissues and overexpressed in tumors. mPGES-1 inhibitors may be safer anti-inflammatory agents overcoming the side effects of NSAIDs and COX-2 inhibitors.