On November 3, 2023 Acerand Therapeutics reported the approval of their next generation PARP1 selective inhibitor, ACE-86225106, for a first-in-human, open-label, multi-center Phase I/II study by the Center for Drug Evaluation of China National Medical Products Administration (Press release, Acerand Therapeutics, NOV 3, 2023, View Source [SID1234641763]).
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ACE-86225106 is a next generation PARP1 selective inhibitor with excellent in vitro and in vivo activity. Its markedly increased selectivity over other PARP isoforms, especially PARP2 and PARP3, has significantly improved its safety profile in in vitro and in vivo studies. Its differentiated pharmacokinetic property may result in better tolerability and more durable clinical activity. The low projected human dose in combination with high starting first in human dose could lead to rapid identification of recommended phase 2 dose. Due to its excellent potency, selectivity, and pharmacokinetic properties, ACE-86225106 can be used as a single agent and more importantly as a preferred combination partner with chemotherapies and targeted therapies in treating multiple solid tumors.
Given these promising data, Acerand Therapeutics will promptly initiate phase 1 dose escalation study in patients in China followed by the US to further assess the potential of ACE-86225106 as an effective mono- or combination therapy for treating different types of cancers, especially those with BRCA mutations or other homologous recombination deficiency.
Remarks by Dr. Genshi Zhao, Acerand Co-Founder, President and CSO:
We are very excited to begin clinical trials for our PARP1 inhibitor, ACE-86225106. The first-generation PARP inhibitors are known to have serious hematological and gastrointestinal toxicities due to the lack of selectivity over PARP2 and other isoforms. These serious toxicities have limited their clinical utility, especially in combination therapies. With its markedly increased selectivity over PARP2, significantly improved safety profile, excellent in vitro and in vivo potency, and PK profile, ACE-86225106 is expected to have great potential as a safer and more effective treatment option for cancer patients. We are confident that ACE-86225106’s clinical performance will greatly benefit cancer patients in China and elsewhere.