-Ultra-long-acting subcutaneous (SQ) injection formulation of small molecule ASC30 demonstrated a 36-day half-life in patients with obesity, supporting once monthly or less frequent administration.
-As previously disclosed, oral tablet formulation of small molecule ASC30 demonstrated potentially best-in-class 6.3% weight loss in patients with obesity after a four-week treatment.

Ascletis Pharma Inc.  announces positive interim results from its randomized, double-blind, placebo-controlled Phase Ib single subcutaneous (SQ) injection study (NCT06679959), conducted in the U.S., of small molecule ASC30 with three ultra-long-acting SQ injection formulations in patients with obesity (body mass index (BMI): 30-40 kg/m²).

The Phase Ib study investigated the half-life of three ultra-long-acting SQ injection formulations of ASC30 (100 mg, single injection), a small molecule GLP-1 receptor (GLP-1R) agonist, developed from Ascletis' ultra-long-acting platform (ULAP). In each cohort, eight patients received one formulation of ASC30 SQ injection and two patients were on volume-matched placebo.

One of the evaluated three formulations demonstrated a 36-day half-life in patients with obesity after a single SQ injection, supporting once monthly or less frequent administration. In addition, this formulation is a sterile solution for SQ injection and stable around neutral pH, allowing for potential co-formulation and co-administration with other drugs or drug candidates. This formulation of small molecule ASC30 SQ injection is advancing into further clinical trials to evaluate clinical efficacy at doses above 100 mg.

The other two formulations, which have different chemical and physical properties from the formulation mentioned above, also demonstrated ultra-long-acting potential in patients with obesity.   

As previously disclosed, the oral tablet formulation of small molecule ASC30 demonstrated potentially best-in-class 6.3% weight loss in patients with obesity after a four-week treatment (Press Release).

ASC30 SQ injection was generally well tolerated, demonstrating a favorable safety profile in the Phase Ib study. No serious adverse events (SAEs) were reported. There were no Grade 3 or higher adverse events (AEs) observed. The majority of gastrointestinal (GI)-related AEs were mild (Grade 1). There were no elevations of liver enzymes including alanine aminotransferase (ALT), aspartate aminotransferase (AST) and total bilirubin (TBL). There were no abnormal findings in laboratory tests, vital signs, ECGs (electrocardiograms, including QTc intervals), and physical exams. Most injection site reactions of ASC30 were mild. There were no Grade 3 or higher injection site reactions.

ASC30 was discovered and developed in-house at Ascletis as a first and only investigational small molecule GLP-1R biased agonist designed to be dosed once daily orally and once monthly or less frequent subcutaneously for the treatment of obesity.

"We are excited about the 36-day half-life of ASC30 SQ injection from our Phase Ib study of potentially first-in-class once-monthly injectable small molecule GLP-1R agonist to treat patients with obesity," said Jinzi Jason Wu, Ph.D., Founder, Chairman and CEO of Ascletis. "Once monthly or less frequent injection is critical in a market as large as obesity since it could save 75% or more devices and cartridges that are needed for once-weekly injectable medicines, in addition to enhanced compliance and convenience. Furthermore, ASC30 has the potential to offer both once-daily oral and once-monthly subcutaneous injection dosing options for patients, if approved."