Shanghai, China and Indianapolis, US — 30 May, 2025: Acerand Therapeutics (Acerand), a clinical-stage biotech company focusing on the discovery and development of innovative small-molecule therapies in oncology and metabolic diseases, today announced preliminary clinical data of its self-developed novel and selective PARP1 inhibitor, ACE-86225106. These data will be presented as an abstract and poster at the 2025 American Society of Clinical Oncology (ASCO) Annual Meeting in Chicago, US, from 30 May to 3 June 2025.
The findings, derived from the ongoing dose escalation and backfill cohorts of the Phase 1/2 clinical trial ACE-106-001 (NCT06380660) show preliminary evidence of good tolerability and encouraging efficacy in patients with heavily pre-treated advanced solid tumors. Safety data indicated that ACE-86225106 is well tolerated at doses up to 30 mg QD, with no dose-limiting toxicities (DLTs) observed. And gastrointestinal and hematological adverse events were mild and manageable. PK profiles demonstrated approximately dose-proportional increases in drug exposure, with a flat PK curve and mild accumulation. Notably, partial response was observed at the lowest tested dose level of 5 mg QD and was further confirmed at higher dose levels, supporting early signs of clinical activity.
This multicenter, open-label, first-in-human study consists of two phases: “3+3” dose escalation module and backfill module in phase 1, followed by the dose expansion module in phase 2. The primary objectives are to evaluate the safety, tolerability, PK/PD profile, and preliminary efficacy of ACE-86225106 as monotherapy. The trial is being led by coordinating investigators Professor Dingwei Ye and Professor Jian Zhang of Fudan University Cancer Hospital.
The details of abstract information to be delivered by Acerand are as follows:
- Abstract Title: The efficacy and safety of a selective PARP1 inhibitor ACE-86225106 in patients with advanced solid tumors: Preliminary results from a first-in-human phase 1/2 study
- Abstract #: 3153
- Poster Bd #: 468
- Session type: Poster Session
- Session title: Developmental Therapeutics—Molecularly Targeted Agents and Tumor Biology
About ACE-86225106
ACE-86225106 is a novel, oral, and highly selective inhibitor of poly (ADP-ribose) polymerase 1 (PARP1) developed independently by Acerand Therapeutics. Preliminary clinical data indicate that ACE-86225106 is well tolerated and shows promising efficacy in heavily pre-treated advanced solid tumors. Preclinical studies showed significant inhibitory effect on PARP1 in vitro, which was comparable with the positive controls (Olaparib, the first-generation pan-PARPi, and AZD5305, the second-generation PARP1 selective inhibitor under development), and showed no significant inhibitory effect on PARP2/3/5A/5B/6/7/12/14/15. In a DNA-PARP trapping assay, ACE-86225106 showed significant induction of DNA-PARP1 complex trapping, with no significant induction of DNA-PARP2 complex trapping, reaffirming its high PARP1 selectivity. Collectively, these findings suggest that compared to first-generation PARP inhibitors, ACE-86225106 is expected to uphold its anti-tumor efficacy with potentially reduced hematological toxicity risks (i.e. anemia), extended therapeutic window, and greater flexibility for multiple combination therapy strategies, thereby improving the prognosis for patients with advanced solid tumor.
About Acerand Therapeutics
Acerand Therapeutics is a biotech company founded by an elite team of industry-leading scientists and drug developers. The company is dedicated to discovering and developing novel small-molecule therapies for oncology and metabolic diseases. With research and development hubs in Shanghai, China, and Indianapolis, Indiana, USA, Acerand leverages its proprietary innovation platform and operational efficiency to deliver a highly differentiated pipeline of drug candidates from discovery to clinical trials.
