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Roche’s oral GLP-1 receptor agonist CT-996 has weight loss of -6.1% within four weeks

Roche has reported positive topline results from two arms of an ongoing multi-part Phase I clinical trial for CT-996, an investigational, once-daily, oral small molecule GLP-1 receptor agonist being developed for the treatment of both type 2 diabetes and obesity. The data showed that treatment with CT-996 in participants with obesity and without type 2 diabetes resulted in a clinically meaningful placebo-adjusted mean weight loss of -6.1% within four weeks (p <0.001). The full study data will be presented at an upcoming medical meeting.


CT-996 was well tolerated, with mostly mild or moderate gastrointestinal-related adverse events, consistent with the safety profile of the incretin drug class. There were no treatment

discontinuations related to the study drug. The study results also showed that blood levels of CT-996 were largely unaffected either during fasting or after a standardised high-fat meal. Thus, the company believes, CT-996 could potentially be dosed without regard to meal timing, thereby affording greater dosing flexibility for patients. Based on the study data, CT-996 is anticipated to be used not only as a therapy for achieving glycaemic control and inducing weight loss, but also potentially for oral weight maintenance therapy following weight loss induced by injectables.


CT-996 is an investigational, once-daily, oral small molecule GLP-1 receptor agonist being developed for the treatment of both type 2 diabetes and obesity. Unlike the endogenous GLP-1 hormone, CT-996 is specifically designed to be a biased GLP-1 receptor agonist that activates cAMP signalling with minimal-to-no beta-arrestin recruitment. These finely tuned signalling properties are expected to lead to strong glycaemic control, significant weight loss and good tolerability.


The CT-996-201 trial is a multi-part, multi-cohort Phase I randomised, double-blind, placebo-controlled, single- and multiple- ascending dose study designed to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of CT-996 in otherwise-healthy adults who are overweight or obese, with and without type 2 diabetes. Part 1 was a single ascending dose in 40 participants with overweight or obesity (completed); part 2 was a multiple ascending dose in three sequential cohorts of a total of 25 participants with obesity without type 2 diabetes (completed); part 3 is a multiple ascending dose study in two sequential cohorts of 30 participants with obesity and type 2 diabetes (planned to be initiated in Q4 2024).


The primary endpoint of the trial is safety and tolerability of CT-996; secondary endpoints include the assessment of the pharmacokinetics of CT-996, along with its effect on body weight and glucose homeostasis. Based on the current Phase I results, CT-996 will advance into Phase II clinical development.


"We are pleased to see the clinically meaningful weight loss in people treated with our oral GLP-1 therapy CT-996, which could eventually help patients address both chronic weight management and glycaemic control indications,” said Dr Levi Garraway, Roche’s Chief Medical Officer and Head of Global Product Development. “Following our data for CT-388, this is the second positive readout in less than three months from our growing metabolic pipeline, which includes both oral and injectable options to address patients' needs across a spectrum of related diseases."

 

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