• AC-101 demonstrated a favorable safety and tolerability profile in healthy subjects in single, food effect, and multiple dose cohorts

• No serious or severe AEs occurred during the study. All TRAEs are classified as Grade 1, and resolved without concomitant medication.

• AC-101 was readily absorbed following oral administration, and the exposure increased in a proportional manner with ascending doses following a single dose of AC-101 (up to 600 mg)

• AC-101 robustly inhibited inflammatory cytokines IL-1β and IL-6 downstream of RIPK2 at doses of 100-200mg QD.

Suzhou China, April 26, 2024 - Accro Bioscience (Suzhou) Limited (Accropeutics), a clinical-stage biotech company with a focus on molecular mechanisms of regulated cell death and related pathogenesis in human diseases, today announces positive results at the completion of the Phase I study of its drug candidate AC-101 in healthy human subjects. The Phase I trial was a single center, randomized, double-blind, placebo-controlled, single and multiple ascending dose study following oral administration in healthy human subjects, to evaluate the safety, tolerability, pharmacokinetics and the effects of food of AC-101.

In the Single Ascending Dosage (SAD) part, 30 healthy subjects were randomized and AC-101 was evaluated against placebo (n=10) using single oral administration at escalating doses. This study demonstrated that AC-101 had a significant safety range, from 50 to 600 mg, and the maximum tolerated dose was not reached. The exposure of AC-101 increased in a proportional manner with ascending doses following a single dose of AC-101. No serious or severe adverse events or dose-limiting toxicities leading to study discontinuation were observed. All TRAEs are classified as Grade 1.

12 healthy subjects were randomized into Fasted or Fed cohorts, and no abnormal findings were observed in Food Effect study of AC-101.

In the Multiple Ascending Dosage (MAD) part, 24 healthy subjects were randomized into three dosage cohorts of 50, 100, and 200mg, and AC-101 was evaluated against placebo (n=6) using multiple oral administration from Day 1 to Day 7. The PK profile from MAD study demonstrated no accumulation of AC-101 for the 50 and 100mg cohorts, mild accumulation (1.8 folds) for the 200mg cohorts at the steady state.  Biomarkers indicated 100-200mg QD may well cover the potential therapeutic effect dosages. No serious or severe adverse events or dose-limiting toxicities leading to study discontinuation were observed. All TRAEs are classified as Grade 1.

Based on the preclinical profile together with these Phase I results, Accropeutics intends to advance AC-101 into Phase Ib/IIa studies in IBD patients in Q4, 2024.

Dr. Xiaohu Zhang, co-founder and CEO of Accropeutics said, "We are thrilled to achieve the important milestones of AC-101 in the Phase I study. We look forward to evaluating AC-101 for more safety and preliminary efficacy data for IBD patients in a phase Ib/IIa study. We will work diligently to move the program forward, in the hope that it would one day provide safe and efficacious new treatment options for IBD patients worldwide.”

About RIPK2

Receptor interacting protein kinase 2 (RIP2 or RIPK2) is a member of the receptor interacting serine/threonine protein kinase family. Dysregulation of NOD/RIPK2 dependent signaling pathways is associated with human diseases, such as inflammatory bowel disease (IBD) and sarcoidosis.

About AC-101

AC-101 was developed from the company's drug discovery platform targeting "regulatory cell death and inflammation". Preclinical studies show that AC-101 effectively inhibits the release of the NOD-RIPK2 dependent inflammatory factors and significantly protects tissue damage in IBD models. AC-101 is one of the leading RIPK2 asset worldwide.

About Accropeutics

Accropeutics is a clinical-stage biotech company with a core focus on molecular mechanisms of regulated cell death and related pathogenesis in human diseases. The Company has developed a robust portfolio with innovative compounds in various stages spanning from lead optimization to clinical trials. The RIPK1 inhibitor AC-003 completed phase I clinical trials in China and the United States in August 2023, and the clinical trials for aGVHD patients have been initiated; The RIPK2 inhibitor AC-101 has completed Phase I in Australia with excellent safety and PK/PD data; AC-201, a selective TYK2/JAK1 inhibitor with huge potential for treating inflammatory and autoimmune diseases, has completed Phase I in Australia and China, and is currently undergoing Phase II clinical trials in China. The company has multiple compounds in the PCC and preclinical research and development stages. Accropeutics owns global rights of all its assets with 17 patents issued in China, Japan, Korea, US and EU.