Metabolic Therapeutics

ABP2111Na (Tablets) is a novel FIC dual GPR40 (also known as FFAR1) and GPR120 (also known as FFAR4) agonist that had been shown not only significantly to reduce the body weight, NASH, TG, LDL, and HbA1c in obese rats, but also to have hypolipidemic and hepatic function-improving effects in preclinical studies.

The Phase 1a/IIa clinical studies had been finished to evaluate the safety, tolerability, PK, PD and efficacy of ABP2111Na in participants with obesity or overweight in China, and already started Phase IIb in Jan. 2025. A total of 30 participants with obesity or overweight were enrolled in Phase IIa. In blind study, by Dec 20, 2024, only 3 of 30 participants (10.0%) had total 4 cases of possibly drug-related slight gastrointestinal AEs (such as vomiting and diarrhea), and each AE case happened only for few hours and well self-recovered without any treatment. All of possibly drug-related TEAEs were mild as grade 1 in severity, and ABP2111Na was well tolerated with excellent safety for all of 30 participants within 28 days of continuous administration. ABP2111Na showed dose-proportional PK within the dose range, the median Tmax was 1.8-3.0 h and mean T1/2 was 16.0-18.4 h on Day 28 across three of ABP2111Na dose ranges. After 4 weeks, mean changes from baseline body weight and BMI were -1.25% and -1.28% (n=10) in the first 50mg cohort, -3.31% and -3.16% (n=10) in the third 200mg cohort, respectively. Moreover, one participant in cohort 3 was significantly reduced -10.0% of weight and -10.2% of BMI without any drug-related AE within 4 weeks. For PK/PD, all of the ALT, AST, ALP, and TBIL tests for 3 cohorts were normal, and the TG and LDL showed a descending tendency, but did not cause any hypoglycemia.

Based on the clinical trial progress, the Clinical Phase III Study for obesity will start in Jun. 2025, in China. Moreover, the Phase I/IIa clinical bridging studies will be conducted in USA.