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CT-996 is an investigational, once-daily oral small molecule agonist of the glucagon-like peptide 1 receptor (GLP-1 receptor) being developed for the treatment of obesity and type 2 diabetes. Unlike endogenous GLP-1 hormone or peptide-based GLP-1 analogs, CT-996 is a signal-biased agonist that selectively activates cAMP signaling with minimal-to-no beta-arrestin recruitment at the GLP-1 receptor. This bias is designed to enhance glycemic control and promote significant weight loss while potentially improving tolerability compared to other agents in its class. In Phase I clinical trials, CT-996 demonstrated robust reductions in body weight (up to a placebo-adjusted mean of -6.1% after four weeks) and improvements in glucose homeostasis among participants with obesity or type 2 diabetes. The drug was generally well tolerated; most adverse events were mild or moderate gastrointestinal symptoms typical for incretin-based therapies. Rapid dose escalation increased GI side effects such as nausea and GERD; slower titration improved tolerability but reduced efficacy[1][2][6][8][9].
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