Ascletis Reports Encouraging Results from ASC30 Trials for Obesity Treatment
Ascletis Pharma Inc. has recently announced positive topline results from its Phase Ia single ascending dose (SAD) clinical trial involving the ASC30 oral tablet, aimed at treating obesity. The SAD study, which enrolled 40 patients with a body mass index (BMI) between 30 and 40 kg/m², evaluated five different dosage cohorts: 2 mg, 5 mg, 10 mg, 20 mg, and 40 mg. The outcomes of this study indicate that the ASC30 tablet exhibits dose-proportional pharmacokinetic (PK) characteristics and an impressive half-life (t1/2) of up to 60 hours, supporting the feasibility of a once-daily or even less frequent oral dosing regimen.
An important finding from the study is the comparability of ASC30's PK properties to other existing small molecule oral GLP-1 receptor (GLP-1R) agonists, suggesting that ASC30 could potentially outperform its competitors in the market. For instance, data revealed the drug exposure of a 5 mg ASC30 single dose is 2.2 times greater than that of a 6 mg dose of orforglipron, which highlights its superiority.
Particularly noteworthy was the significant data collected in Cohort 5, where the 40 mg ASC30 dose was administered under both fasting and fed conditions. The results demonstrated that the pharmacokinetics remained largely unchanged regardless of food intake, indicating that patients could take the ASC30 tablet without the constraints of food or water, simplifying the administration protocol for users.
Regarding safety, the ASC30 oral tablet was well tolerated throughout the study. Adverse events reported were mostly mild (grade 1) to moderate (grade 2), with gastrointestinal issues being the most prevalent. Encouragingly, there were no serious adverse effects or higher-grade complications recorded during the trial. Furthermore, liver enzyme levels such as alanine aminotransferase (ALT) and aspartate aminotransferase (AST) remained within normal ranges, underscoring the drug's favorable safety profile.
The ASC30 oral tablet has been formulated to be stable at room temperature, enhancing its therapeutic use. Animal studies indicate a relative oral bioavailability of 99%, with preliminary evidence supporting weekly dosing intervals for enhanced patient compliance. Notably, ASC30 has been designed as a biased small molecule GLP-1R agonist, allowing it to serve dual functions: it can be administered as a once-monthly injection or as an oral tablet taken daily.
As the trial progresses, Dr. Jinzi Jason Wu, the Founder and CEO of Ascletis, expressed his excitement over the potential impact of the ASC30 oral tablet. "With superior pharmacokinetic properties demonstrated in the SAD study, we are eager to share the forthcoming efficacy data from our Phase Ib multiple ascending dose (MAD) trial by the end of March this year," he stated. The Phase Ib trial involves additional cohorts focusing on various dosing strategies over a 28-day period, and results from these studies will provide further insight into the weight loss outcomes and overall safety of the ASC30 oral tablet.
Unique to ASC30 is its characteristic of being the first and only small molecule GLP-1R biased agonist, which means it can be effectively dosed both subcutaneously and orally. The investigational drug has shown promising in vitro potency against GLP-1R compared to orforglipron, further solidifying its potential position in the obesity treatment landscape.
As the landscape for obesity treatments continues to evolve, Ascletis's ASC30 oral tablet stands out due to its promising PK and safety profile, potentially making it a game-changer in obesity management. With ongoing trials and future data releases, stakeholders and patients alike are closely monitoring the developments of this groundbreaking treatment option.
An important finding from the study is the comparability of ASC30's PK properties to other existing small molecule oral GLP-1 receptor (GLP-1R) agonists, suggesting that ASC30 could potentially outperform its competitors in the market. For instance, data revealed the drug exposure of a 5 mg ASC30 single dose is 2.2 times greater than that of a 6 mg dose of orforglipron, which highlights its superiority.
Particularly noteworthy was the significant data collected in Cohort 5, where the 40 mg ASC30 dose was administered under both fasting and fed conditions. The results demonstrated that the pharmacokinetics remained largely unchanged regardless of food intake, indicating that patients could take the ASC30 tablet without the constraints of food or water, simplifying the administration protocol for users.
Regarding safety, the ASC30 oral tablet was well tolerated throughout the study. Adverse events reported were mostly mild (grade 1) to moderate (grade 2), with gastrointestinal issues being the most prevalent. Encouragingly, there were no serious adverse effects or higher-grade complications recorded during the trial. Furthermore, liver enzyme levels such as alanine aminotransferase (ALT) and aspartate aminotransferase (AST) remained within normal ranges, underscoring the drug's favorable safety profile.
The ASC30 oral tablet has been formulated to be stable at room temperature, enhancing its therapeutic use. Animal studies indicate a relative oral bioavailability of 99%, with preliminary evidence supporting weekly dosing intervals for enhanced patient compliance. Notably, ASC30 has been designed as a biased small molecule GLP-1R agonist, allowing it to serve dual functions: it can be administered as a once-monthly injection or as an oral tablet taken daily.
As the trial progresses, Dr. Jinzi Jason Wu, the Founder and CEO of Ascletis, expressed his excitement over the potential impact of the ASC30 oral tablet. "With superior pharmacokinetic properties demonstrated in the SAD study, we are eager to share the forthcoming efficacy data from our Phase Ib multiple ascending dose (MAD) trial by the end of March this year," he stated. The Phase Ib trial involves additional cohorts focusing on various dosing strategies over a 28-day period, and results from these studies will provide further insight into the weight loss outcomes and overall safety of the ASC30 oral tablet.
Unique to ASC30 is its characteristic of being the first and only small molecule GLP-1R biased agonist, which means it can be effectively dosed both subcutaneously and orally. The investigational drug has shown promising in vitro potency against GLP-1R compared to orforglipron, further solidifying its potential position in the obesity treatment landscape.
As the landscape for obesity treatments continues to evolve, Ascletis's ASC30 oral tablet stands out due to its promising PK and safety profile, potentially making it a game-changer in obesity management. With ongoing trials and future data releases, stakeholders and patients alike are closely monitoring the developments of this groundbreaking treatment option.
Topics Health）
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