Shanghai (China) and Indianapolis (US) - March 22nd, 2024: Acerand Therapeutics (Acerand) announces the successful completion of the first patient enrollment in the Phase 1/2 clinical trial (ACE-106-001) of their groundbreaking selective PARP1 inhibitor (ACE-86225106 tablets).
ACE-106-001 is a first-in-human trial of Acerand's self-developed selective PARP1 inhibitor ACE-86225106. This trial consists of two phases: dose escalation and backfill module in phase 1, followed by the dose expansion module in phase 2. The primary objective is to evaluate the safety, tolerability, PK/PD profile, and pre-liminary efficacy of ACE-86225106 as a monotherapy. The leading investigators of this study are Professor Dingwei Ye and Jian Zhang from Fudan University Cancer Hospital. The study is conducted across multiple clinical institutions in China.
Remarks by Dr. Genshi Zhao, Acerand Co-Founder, President and CSO:
"This study is the first clinical trial of Acerand and represents an important milestone in our journey towards delivering transformative therapies to patients with unmet medical needs. While first-generation pan-PARP inhibitors have been approved for several indications (i.e., advanced ovarian, breast, prostate, and pancreatic cancers), their clinical utility has been limited by adverse effects. Highly selective PARP1 inhibitors hold promise in mitigating hematologic and gastrointestinal toxicities associated with inhibition of PARP2 and other PARP family members, potentially broadening the therapeutic window, enhancing patient compliance, and demonstrating improved efficacy."
About ACE-86225106：
ACE-86225106 is a novel, orally bioavailable, and highly selective inhibitor of poly (ADP-ribose) polymerase 1 (PARP1) developed by Acerand Therapeutics. It potently inhibits PARP1 in vitro with a potency similar to Olaparib, the first-generation pan-PARPi, and AZD5305, the second-generation PARP1 selective inhibitor under development, but does not significantly inhibit PARP2/3/5A/5B/6/7/12/14/15. In a DNA-PARP trapping assay, ACE-86225106 significantly induces DNA-PARP1 complex trapping, with no significant induction of DNA-PARP2 complex trapping, further validated its high PARP1 selectivity. Taken together, ACE-86225106, a highly selective and potent 2nd generation PARP1 inhibitor, is expected to demonstrate more robust clinical activity, better tolerability, and broader combination options, thereby improving the clinical outcomes for patients with advanced solid tumors as compared to the first-generation PARP inhibitors.
