SAN DIEGO, July 17, 2024 /PRNewswire/ -- Biotheryx, Inc., a biopharmaceutical company discovering and developing a portfolio of first-in-class protein degraders with a focus on validated targets in cancer and inflammatory diseases, today announced that the first patient has been dosed in its Phase 1 clinical trial evaluating BTX-9341, an investigational oral and bifunctional degrader of cyclin-dependent kinase 4 (CDK4) and cyclin-dependent kinase 6 (CDK6), as a monotherapy and in combination with fulvestrant for patients with advanced and/or metastatic hormone receptor positive (HR+)/human epidermal growth factor receptor 2 negative (HER2-) breast cancer who have previously received CDK4/6 inhibitor therapy either in the adjuvant or metastatic setting. .

圣地亚哥，2024年7月17日/PRNewswire/--生物制药公司Biotheryx，Inc.，一家发现和开发一流蛋白质降解剂组合的生物制药公司，专注于癌症和炎症性疾病的有效靶标，今天宣布，第一名患者已在其1期临床试验中服用BTX-9341，BTX-9341是一种细胞周期蛋白依赖性激酶4（CDK4）和细胞周期蛋白依赖性激酶6（CDK6）的研究性口服和双功能降解剂，作为单一疗法，并与氟维司群联合用于晚期和/或转移性激素受体阳性（HR+）/人表皮生长因子受体2阴性（HER2-）乳腺癌患者先前在辅助或转移环境中接受过CDK4/6抑制剂治疗的患者。。

'BTX-9341 is a potent and selective CDK4/6 degrader that has shown significant anti-tumor activity in both CDK4/6 inhibitor naïve and resistant preclinical models. We are optimistic that it will meet a critical unmet medical need for patients with HR+/HER2- breast cancer who have received prior CDK4/6 inhibitor therapy,' said Leah Fung, Ph.D., CEO of Biotheryx.

BTX-9341是一种有效的选择性CDK4/6降解剂，在CDK4/6抑制剂初始和耐药临床前模型中均显示出显着的抗肿瘤活性。Biotheryx首席执行官LeahFung博士说：“我们乐观地认为，它将满足先前接受过CDK4/6抑制剂治疗的HR+/HER2乳腺癌患者尚未满足的关键医疗需求。”。

'Dosing the first patient in this trial represents a significant milestone for Biotheryx, the patients we aim to serve and the scientists who have made this possible.'.

“在这项试验中给第一名患者服用药物，对于Biotheryx、我们旨在服务的患者以及使这成为可能的科学家来说，这是一个重要的里程碑。”。

The Phase 1 clinical trial will begin with dose escalation of BTX-9341 as a monotherapy, followed by a combination with fulvestrant and will conclude with dose expansion of BTX-9341 in combination with fulvestrant. The trial will assess safety, tolerability, pharmacokinetic and pharmacodynamic activity of BTX-9341 as a monotherapy and in combination with fulvestrant.

。该试验将评估BTX-9341作为单一疗法和与氟维司群联合使用的安全性，耐受性，药代动力学和药效学活性。

Once the recommended Phase 2 dose of the combination has been determined, there will be a formal evaluation of efficacy in an expansion cohort..

一旦确定了该组合的推荐2期剂量，将在扩展队列中对疗效进行正式评估。。

'We are thrilled to have dosed the first patient with BTX-9341 at The START Center for Cancer Research,' stated START Co-Founder and Co-Director of Clinical Research, Dr. Amita Patnaik, MD, FRCPC. 'BTX-9341 is a highly novel, first-in-class, potent and selective degrader of CDK4/6, representing an innovative therapeutic approach.

“我们很高兴在START癌症研究中心给第一位患者服用BTX-9341，”START联合创始人兼临床研究联合主任、FRCPC医学博士阿米塔·帕特奈克博士表示BTX-9341是一种高度新颖，一流，有效且选择性的CDK4/6降解剂，代表了一种创新的治疗方法。

It has the potential to transform the care of patients with advanced and/or metastatic HR+/HER2- breast cancer, particularly those who have received prior CDK4/6 inhibitor therapies. This milestone is perfectly aligned with START's mission to accelerate drug development and provide early access to cutting-edge anticancer therapies, bringing hope to patients and their families.'.

它有可能改变晚期和/或转移性HR+/HER2乳腺癌患者的护理，特别是那些先前接受过CDK4/6抑制剂治疗的患者。这一里程碑与START的使命完全一致，即加速药物开发，尽早获得尖端抗癌疗法，为患者及其家人带来希望。”。

In preclinical studies, orally administered BTX-9341 demonstrated in vivo CDK4/6 degradation and improved anti-tumor activity as a monotherapy compared to current standard of care treatment regimens. BTX-9341 also demonstrated synergies with selective estrogen receptor degraders including fulvestrant, elacestrant and camizestrant in CDK4/6 naïve and resistant models..

在临床前研究中，与目前的标准治疗方案相比，口服BTX-9341作为单一疗法表现出体内CDK4/6降解和改善的抗肿瘤活性。BTX-9341在CDK4/6幼稚和耐药模型中也显示出与选择性雌激素受体降解剂（包括氟维司群，elacestrant和camizestrant）的协同作用。。

About BTX-9341

关于BTX-9341

BTX-9341 is a first-in-class, oral degrader of CDK4/6, important targets for a range of cancers and clinically validated in HR+/HER2- breast cancer. In preclinical breast cancer models, BTX-9341 demonstrated superiority to CDK4/6 inhibitors through potent and highly selective catalytic degradation of CDK4 and CDK6, robust inhibition of Cyclin E and CDK2 transcription, cell cycle arrest and ultimately superior in vivo efficacy in breast cancer xenografts.

BTX-9341是CDK4/6的一流口服降解剂，CDK4/6是一系列癌症的重要靶标，并在HR+/HER2乳腺癌中得到临床验证。在临床前乳腺癌模型中，BTX-9341通过对CDK4和CDK6的有效和高选择性催化降解，对细胞周期蛋白E和CDK2转录的强烈抑制，细胞周期停滞以及最终在乳腺癌异种移植物中具有优异的体内功效，证明了其优于CDK4/6抑制剂。

Beyond this increased efficacy potential, BTX-9341 is differentiated from CDK4/6 inhibitor approaches through the ability to overcome key resistance mechanisms that limit the impact of inhibitors in second line HR+/HER2- breast cancer..

除了这种增加的疗效潜力之外，BTX-9341通过克服限制抑制剂在二线HR+/HER2-乳腺癌中影响的关键耐药机制的能力与CDK4/6抑制剂方法有所区别。。

About Biotheryx, Inc.

关于Biotheryx，Inc。

Biotheryx is a clinical-stage biopharmaceutical company discovering and developing a portfolio of first-in-class protein degraders, including bifunctional degraders and molecular glues. Our focus is on deploying the differentiated potential of degraders towards validated targets in cancer and inflammatory disease.

Biotheryx是一家临床阶段的生物制药公司，发现并开发了一流的蛋白质降解剂组合，包括双功能降解剂和分子胶。我们的重点是将降解物的分化潜力部署到癌症和炎症性疾病的有效靶点。

Members of our founding and scientific teams previously developed the IMiDs, the first U.S. Food and Drug Administration (FDA) approved modulators of Cereblon, the most widely validated E3 ligase involved in protein degradation, and we have applied our expertise in Cereblon binding to build our proprietary PRODEGY platform.

我们的创始团队和科学团队的成员先前开发了IMiDs，这是美国食品和药物管理局（FDA）批准的第一种脑蛋白调节剂，是参与蛋白质降解的最广泛验证的E3连接酶，我们已经将我们在脑蛋白结合方面的专业知识应用于构建我们专有的PRODEGY平台。

Biotheryx's clinical program, BTX-9341, a bifunctional degrader of CDK4 and CDK6, began a Phase 1 clinical trial in the third quarter of 2024. Biotheryx's pipeline also includes BTX-10908, a first-in-class degrader of SOS1 for pan-KRAS mutant cancers and PDE4 degraders for inflammatory diseases. For more information, please visit biotheryx.com and engage with us on LinkedIn..

Biotheryx的临床项目BTX-9341是CDK4和CDK6的双功能降解剂，于2024年第三季度开始了1期临床试验。Biotheryx的管道还包括BTX-10908，它是用于泛KRAS突变癌症的SOS1的一流降解剂，以及用于炎症性疾病的PDE4降解剂。欲了解更多信息，请访问biotheryx.com并在LinkedIn上与我们联系。。