On March 22, 2024 Acerand Therapeutics (Acerand) reported 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) (Press release, Acerand Therapeutics, MAR 22, 2024, View Source [SID1234641764]).

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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 coordinating investigators leading this study are Professor Dingwei Ye and Jian Zhang from Fudan University Cancer Hospital. The study is being conducted simultaneously across multiple clinical institutions nationwide.

Remarks by Dr. Genshi Zhao, Acerand Co-Founder, President and CSO:

"This study is the first clinical trial of Acerand and represents a crucial milestone in our journey towards developing innovative small-molecule anti-tumor drug independently. While first-generation pan-PARP inhibitors have been approved for several indications (i.e., advanced ovarian, breast, prostate, and pancreatic cancers), their clinical optimal dose has been limited by adverse effects, limiting the therapeutic window. Highly selective PARP1 inhibitors hold promise in mitigating hematologic toxicity associated with PARP2 inhibition, potentially broaden the therapeutic window, enhancing patient compliance, and demonstrating improved efficacy."

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. It 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) and extended therapeutic window, thereby improving the prognosis for patients with advanced solid tumor.