BOSTON--(BUSINESS WIRE)--Anagenex, a pioneering drug discovery company pairing large-scale data generation with proprietary artificial intelligence (AI) to discover the next generation of small molecule medicines, today announced the company has nominated PRMT5 and MAT2A as its first two preclinical programs.

波士顿--（商业新闻短讯）--开创性的药物发现公司Angenex将大规模数据生成与专有人工智能（AI）相结合，以发现下一代小分子药物，今天宣布该公司已提名PRMT5和MAT2A作为其前两个临床前项目。

PRMT5 is an essential gene required for cell survival. Inhibition of the metabolic protein MAT2A leads to PRMT5 inhibition. Both of these proteins are viewed as potential cancer therapeutic targets..

PRMT5是细胞存活所需的必需基因。代谢蛋白MAT2A的抑制导致PRMT5抑制。这两种蛋白质都被视为潜在的癌症治疗靶点。。

Anagenex has built a platform that pairs large-scale data generation enabled by artificial intelligence (AI) to find and develop hits to multiple targets simultaneously, exploring entire pathways to identify the most promising compounds to modify disease biology.

Angenex建立了一个平台，该平台可以将人工智能（AI）支持的大规模数据生成配对，以同时发现和开发多个目标的命中，探索整个途径，以确定最有希望的化合物来改变疾病生物学。

Anagenex prioritizes targets with clear human validation. Targets with a human biomarker are four times more likely to be approved, however hundreds remain un-drugged because these often belong to novel target classes or challenging mechanisms. Synthetic lethal oncology, a situation in which loss of function of two genes together result in cell death, while loss of either gene alone does not, is a particularly fruitful area for targets because they often come with an associated human biomarker and massive unmet medical need persists..

Angenex通过明确的人为验证确定目标的优先级。具有人类生物标志物的靶标被批准的可能性是其四倍，然而数百个靶标仍未被药物治疗，因为这些靶标通常属于新的靶标类别或具有挑战性的机制。。。

Anagenex’s first programs addressing PRMT5 and MAT2A fit this validated human target hypothesis. PRMT5 is a pan-essential gene and MAT2A inhibition leads to inhibition of PRMT5. Both leverage MTAP deletion, a gene that is lost in 15% of all solid tumors, providing a unique mechanism to target therapies exclusively to tumors.

Angenex的第一个针对PRMT5和MAT2A的程序符合这一经过验证的人类目标假说。PRMT5是一个泛必需基因，MAT2A抑制导致PRMT5的抑制。两者都利用MTAP缺失，该基因在所有实体瘤的15%中丢失，为仅针对肿瘤的治疗提供了独特的机制。

While competitive programs are showing value in the clinic, Anagenex’s unique platform has been able to identify highly novel compounds for these targets which it believes will help patients by increasing selectivity and brain penetrance..

虽然竞争性项目在临床上显示出价值，但Angenex的独特平台能够为这些目标识别出高度新颖的化合物，它认为这些化合物将通过提高选择性和大脑渗透率来帮助患者。。

“Today none of the programs in the clinic have been able to unlock the majority of patients who might be eligible for PRMT5 and MAT2A inhibitors,” said Ryan Kruger, Chief Scientific Officer of Anagenex. “PRMT5 needs to be hit extremely effectively but hitting PRMT5 in normal tissue creates dose-limiting side-effects.

Angenex首席科学官瑞安·克鲁格（RyanKruger）说：“今天，诊所中没有一个项目能够解锁大多数可能有资格使用PRMT5和MAT2A抑制剂的患者。”。“PRMT5需要非常有效地打击，但在正常组织中打击PRMT5会产生剂量限制性副作用。

MTAP loss provides us with a magic bullet to inhibit PRMT5 only in tumor cells either through the inhibition of MAT2A or through inhibition of PRMT5 directly.”.

MTAP丢失为我们提供了一个神奇的子弹，通过抑制MAT2A或直接抑制PRMT5，仅在肿瘤细胞中抑制PRMT5。”。

The most effective PRMT5 compounds in the clinic are 74-fold selective for tumors over regular cells, but preclinical and clinical data suggests that at least 250-fold selectivity is needed to provide treatment benefit to most patients. Brain penetrance is also important because 40% of patients in the primary indication, Non-Small Cell Lung Carcinoma (NSCLC), experience progression to brain metastases that are often fatal..

临床上最有效的PRMT5化合物对肿瘤的选择性是常规细胞的74倍，但临床前和临床数据表明，需要至少250倍的选择性才能为大多数患者提供治疗益处。脑外显率也很重要，因为40%的主要适应症非小细胞肺癌（NSCLC）患者会进展为脑转移，这通常是致命的。。

Anagenex has developed a series of scaffolds with extreme selectivity, and preliminary work is demonstrating that some of those are brain penetrant. Anagenex is targeting to nominate one of these programs as a development candidate in 2H 2025.

Angenex开发了一系列具有极高选择性的支架，初步工作表明其中一些是脑渗透剂。Angenex计划在2025年下半年提名其中一个项目作为发展候选人。

“Essentially all of the competitive compounds targeting PRMT5 and MAT2A are exploring the same scaffolds,” stated Kruger. “Simply rehashing chemistry others have explored won’t generate the breakthroughs patients need. Fortunately, our platform has discovered several scaffolds that are completely unrelated to those currently being clinically evaluated, giving us a fresh endeavor to help patients in a whole range of cancers.”.

克鲁格说：“基本上所有针对PRMT5和MAT2A的竞争性化合物都在探索相同的支架。”。“简单地重新使用其他人探索过的化学物质不会产生患者所需的突破。幸运的是，我们的平台已经发现了几种与目前正在进行临床评估的支架完全无关的支架，这为我们提供了一种新的努力来帮助患有各种癌症的患者。”。

In parallel to the announcement of the targets within Anagenex’s synthetic lethal oncology portfolio, the Company is planning to expand into immunology in 2024, leveraging its unique discovery platform to solve the most challenging immune disorders. This follows Anagenex’s initiation of a partnership with Nimbus Therapeutics across a variety of targets, which was previously announced in late-2023..

。此前，Angenex与Nimbus Therapeutics在多个目标上建立了合作伙伴关系，此前于2023年底宣布。。

“Our platform is uniquely suited to finding chemical matter for any target, fulfilling our mission to find a molecule for every malady,” said Nicolas Tilmans, Anagenex CEO. “The true power of our platform is in the scalability, and its capability to screen many targets in parallel, then investigate them with up to 100 million target-focused compounds.

Angenex首席执行官尼古拉斯·蒂尔曼（NicolasTilmans）表示：“我们的平台非常适合为任何目标寻找化学物质，完成了我们为每种疾病寻找分子的使命。”。“我们平台的真正力量在于可扩展性，它能够并行筛选多个目标，然后用多达1亿个目标化合物对其进行调查。

This scale of early-stage compound investigation ensures that we will generate multiple compounds that will make it to the clinic.”.

这种规模的早期化合物研究确保了我们将产生多种化合物，使其进入临床。”。

About Anagenex

关于Angenex

Anagenex is pairing large-scale data generation with AI to discover the next generation of small molecule medicines. Driven by over 300 billion proprietary measurements, Anagenex's precision small molecule discovery platform leverages AI to design and custom chemistry to synthesize 100M target-specific molecules for testing in two weeks, creating a virtuous cycle between real lab experiments and computational tools.

Angenex正在将大规模数据生成与人工智能相结合，以发现下一代小分子药物。在3000多亿专有测量的推动下，Angenex的精密小分子发现平台利用人工智能设计和定制化学，在两周内合成100万个目标特定分子进行测试，从而在真实的实验室实验和计算工具之间形成良性循环。

Led by a team of highly experienced scientists and engineers, the company’s pipeline is focused on synthetic lethal oncology. Learn more about us at www.anagenex.com or connect with us on LinkedIn..

在经验丰富的科学家和工程师团队的带领下，该公司的管道专注于合成致命肿瘤学。有关我们的更多信息，请访问www.anagenex.com或通过LinkedIn与我们联系。。