Berlin, Germany, May 15, 2023 – Bayer announced today initiation of dosing in a Phase I first-in-human clinical study with 225Ac-PSMA-Trillium (BAY 3563254), a next-generation targeted alpha therapy. The investigational candidate, labeled with actinium-225 and comprising a novel PSMA (prostate-specific membrane antigen) -targeting small molecule with a customized albumin-binding moiety, is designed to improve therapeutic efficacy and reduce side effects in normal organs such as salivary glands.

2023年5月15日，德国柏林——拜耳公司今天宣布，在第一阶段的人体临床研究中，开始使用225Ac PSMA延龄草（BAY 3563254），这是一种下一代靶向α疗法。用锕-225标记并包含具有定制白蛋白结合部分的新型PSMA（前列腺特异性膜抗原）靶向小分子的研究候选物旨在提高治疗效果并减少唾液腺等正常器官的副作用。

The dose-escalation study (NCT06217822) will evaluate the safety, tolerability and efficacy of 225Ac-PSMA-Trillium in patients with advanced metastatic castration resistant prostate cancer (mCRPC).“Despite recent advances in the treatment landscape for prostate cancer, there is still a high unmet need for novel precision therapy options to improve outcomes for patients with metastatic castration-resistant prostate cancer,” said Fred Saad, MD, FRCS, Professor and Chairman of Surgery at University of Montreal and Director of Genitourinary Oncology at University of Montreal Hospital Center (CHUM), Canada.

剂量递增研究（NCT06217822）将评估225Ac-PSMA延龄草在晚期转移性去势抵抗性前列腺癌（mCRPC）患者中的安全性，耐受性和有效性。“尽管前列腺癌治疗领域取得了最新进展，但仍然需要新的精确治疗方案来改善转移性去势抵抗性前列腺癌患者的预后，”蒙特利尔大学外科教授兼主席、加拿大蒙特利尔大学医院中心（CHUM）泌尿生殖肿瘤主任弗雷德·萨阿德（FredSaad）说。

“225Ac-PSMA-Trillium is a novel approach, which could provide a new treatment to address this unmet need in mCRPC.”“Targeted radionuclide therapy is a strategic pillar of precision oncology at Bayer, holding the promise to shift the treatment paradigm for patients, including those whose disease has developed resistance to other treatments,” said Dominik Ruettinger, M.D., Ph.D., Head of Research and Early Development for Oncology at Bayer.

“225Ac-PSMA延龄草是一种新方法，可以提供一种新的治疗方法来解决mCRPC中未满足的需求。”“靶向放射性核素治疗是拜耳精密肿瘤学的战略支柱，有望改变患者的治疗模式，包括那些疾病对其他治疗产生耐药性的患者，”拜耳肿瘤学研究和早期发展负责人多米尼克·鲁廷格博士说。

“We are excited to announce initiation of the Phase I and dosing of the first patient with 225Ac-PSMA-Trillium. With its unique design, we believe it could offer a meaningful benefit for patients with metastatic prostate cancer, and we look forwar.

“我们很兴奋地宣布，第一个使用225Ac PSMA延龄草的患者开始了第一阶段的治疗，并开始给药。凭借其独特的设计，我们相信它可以为转移性前列腺癌患者提供有意义的益处，我们期待着战争。