- Potentially best-in-class MTA-cooperative PRMT5 inhibitor - - Demonstrates efficacy in pre-clinical models of glioblastoma and non-CNS tumor models with MTAP deletion - - Apeiron plans to file Investigational New Drug (IND) application for GT182 in mid-2024 - SAN FRANCISCO and SHANGHAI, China, Oct.

-潜在的一流的MTA合作PRMT5抑制剂-在具有MTAP缺失的胶质母细胞瘤和非CNS肿瘤模型的临床前模型中证明有效--Apeiron计划在2024年中期为GT182提交研究性新药（IND）申请-旧金山和中国上海，10月。

17, 2023 (GLOBE NEWSWIRE) -- GT Apeiron Therapeutics (‘Apeiron’), a biopharmaceutical company harnessing the power of artificial intelligence to develop targeted precision therapies for unmet medical needs, today announced the development candidate nomination of GTA182, a brain penetrant protein arginine methyltransferase 5 (PRMT5) inhibitor that exhibits methylthioadenosine (MTA) cooperativity resulting in high selectivity for MTAP-deleted cancer cells while sparing MTAP-expressing non-cancer cells.

172023（GLOBE NEWSWIRE）-GT Apeiron Therapeutics（'Apeiron'）是一家利用人工智能的力量为未满足的医疗需求开发针对性精确疗法的生物制药公司，今天宣布了GTA182的开发候选人提名，显示甲硫腺苷（MTA）协同作用的脑渗透蛋白精氨酸甲基转移酶5（PRMT5）抑制剂导致对MTAP缺失的癌细胞的高选择性，同时保留表达MTAP的非癌细胞。

This selectivity is expected to provide a more effective and safer treatment option for patients with MTAP-deleted cancers. “GTA182’s high selectivity for MTAP deleted cancers and its ability to cross the blood brain barrier make it a best-in-class candidate for advancement into clinical development for the potential treatment of CNS tumors as well as non-CNS indications,” said Fred Aswad, J.D., Ph.D., Senior Vice President of Biology and Translational Science.

预计这种选择性将为MTAP缺失癌症患者提供更有效和更安全的治疗选择。弗雷德·阿斯瓦德（Fred Aswad）博士说：“GTA182对MTAP缺失癌症的高选择性及其穿越血脑屏障的能力使其成为推进临床开发的最佳候选者，可用于潜在治疗中枢神经系统肿瘤以及非中枢神经系统适应症。，博士，生物与转化科学高级副总裁。

“Approximately 10% of solid tumors harbor MTAP deletions, including glioblastoma, lung, pancreatic, and bladder cancers all of which have limited treatment options and represent a significant unmet need for patients.” In preclinical studies, Apeiron has demonstrated that GTA182 is a potent and selective PRMT5 inhibitor exhibiting greater than 100-fold selectivity for MTAP deleted tumor cell lines.

“大约10%的实体瘤具有MTAP缺失，包括胶质母细胞瘤，肺癌，胰腺癌和膀胱癌，所有这些都有有限的治疗选择，并且代表了对患者的重大未满足需求。”在临床前研究中，Apeiron已经证明GTA182是一种有效的选择性PRMT5抑制剂，对MTAP缺失的肿瘤细胞系表现出大于100倍的选择性。

GTA182 is brain penetrant and has demonstrated tumor growth inhibition and tumor regression in in vivo pre-clinical models .

GTA182是脑渗透剂，并且已经在体内临床前模型中证明了肿瘤生长抑制和肿瘤消退。