– Bayer announced today initiation of a Phase I clinical trial with BAY 3670549, an investigational highly selective G-protein-coupled inwardly rectifying potassium channel 4 (GIRK4) inhibitor, which has the potential to help control the electrical activity of heart cells in patients with atrial fibrillation (AFib).

– 拜耳今天宣布启动BAY 3670549的I期临床试验，这是一种研究中的高选择性G蛋白偶联内向整流钾通道4（GIRK4）抑制剂，有可能帮助控制心房颤动（AFib）患者的心脏细胞电活动。

This investigative approach for rapid cardioversion to normal sinus rhythm is aiming to enable immediate treatment without the need for anesthesia/sedation and electrical shock and to significantly reduce the patients’ time spent in hospital. The first-in-human dose escalation study in a randomized, double-blind, placebo-controlled, group-comparison design will investigate the safety, tolerability, pharmacokinetics and pharmacodynamics of BAY 3670549 in healthy participants.

这种快速转复为正常窦性心律的探究方法旨在实现无需麻醉/镇静和电击即可立即治疗，并显著减少患者住院时间。首次人体剂量递增研究将以随机、双盲、安慰剂对照、组间比较的设计，评估BAY 3670549在健康受试者中的安全性、耐受性、药代动力学和药效学。

AFib is the most common type of cardiac arrhythmia (irregular heart rhythm), affecting more than 60 million people worldwide, and a significant risk factor for stroke and heart failure..

房颤是最常见的心律失常（心跳不规律）类型，影响全球超过6000万人，并且是中风和心力衰竭的重要风险因素。

“Initiating clinical development of our investigational GIRK4 inhibitor marks an important milestone of our ambition transforming atrial fibrillation treatment with a fast-acting, effective and well tolerated first-line pharmacological therapy for acute cardioversion, alleviating the burdens of electrical cardioversion on patients, physicians and healthcare systems”, said Andrea Haegebarth, Ph.D., Global Head of Research and Early Development for Cardiovascular, Renal, Immunology at Bayer’s Pharmaceuticals Division.

“启动我们正在研究的GIRK4抑制剂的临床开发，标志着我们在实现心房颤动治疗转型这一雄心中的重要里程碑，这是一种快速起效、有效且耐受性良好的一线急性心脏复律药物疗法，能够减轻电复律给患者、医生和医疗系统带来的负担，”拜耳制药部门心血管、肾脏和免疫学全球研发负责人Andrea Haegebarth博士表示。

“We look forward to advancing the program through clinical development, which will strengthen Bayer’s cardiovascular portfolio and advance research efforts to the benefit of a broad patient population in need for novel and better medicines.”.

“我们期待通过临床开发推进该项目，这将加强拜耳的心血管产品组合，并推动研究工作，造福需要新型和更好的药物的广大患者群体。”

The current gold standard to treat acute AFib episodes is electric cardioversion (ECV). This is an effective but resource-intensive and logistically challenging procedure, which is normally scheduled in advance and typically requires sedation or even anesthesia to safely deliver an electrical shock to the patient and restore the heart to its normal sinus rhythm..

目前治疗急性房颤发作的金标准是电复律 (ECV)。这是一种有效但资源密集且在后勤上具有挑战性的程序，通常需要提前安排，并且通常需要镇静甚至麻醉，以安全地对患者施加电击并使心脏恢复到正常的窦性心律。

On the other hand, currently available anti-arrhythmic drugs (AADs), which are commonly used for the management of symptomatic AFib, can’t be applied to broad patient populations due to a number of contraindications (such as for patients with structural heart disease) and safety risks, including abnormal heart rhythms and sudden death.

另一方面，目前可用的抗心律失常药物（AADs），通常用于治疗有症状的房颤，由于许多禁忌症（例如对于患有结构性心脏病的患者）和包括心律异常及猝死在内的安全风险，无法广泛应用于患者群体。

Additionally, they show limited, short-term efficacy, require close monitoring and bear the risk of serious side effects..

此外，它们显示出有限的、短期的有效性，需要密切监测，并且存在严重副作用的风险。

Investigational GIRK4 inhibitor (BAY 3670549) is derived from Bayer’s strategic research alliance with the Broad Institute.

调查性GIRK4抑制剂（BAY 3670549）源自拜耳与博德研究所的战略研究联盟。

About GIRK4 inhibitor (BAY 3670549)

关于GIRK4抑制剂（BAY 3670549）

BAY 3670549 is an investigational highly selective G-protein-coupled inwardly rectifying potassium channel 4 (GIRK4) inhibitor with potential to help control the electrical activity of heart cells in patients with atrial fibrillation (AFib).

BAY 3670549 是一种研究性高选择性 G 蛋白偶联内向整流钾通道 4 (GIRK4) 抑制剂，有可能帮助控制心房颤动 (AFib) 患者的心脏细胞电活动。

GIRK4 channels are specialized proteins that regulate the electrical activity of heart cells by facilitating the flow of potassium ions (K+) in response to the neurotransmitter acetylcholine (ACh). This mechanism is particularly crucial during the later phases of the heart’s electrical signaling, specifically during so-called atrial effective refractory period (AERP).

GIRK4通道是一种特殊蛋白质，通过在神经递质乙酰胆碱（ACh）的作用下促进钾离子（K+）的流动来调节心肌细胞的电活动。这一机制在心脏电信号传导的后期阶段尤为重要，特别是在所谓的房性有效不应期（AERP）期间。

Increased activity of these channels shortens the AERP in the atria (the upper chambers of the heart), thereby reducing the recovery time after each heartbeat. This alteration in recovery time can contribute to the onset and persistence of AFib..

这些通道活动的增加会缩短心房（心脏的上部腔室）的AERP，从而减少每次心跳后的恢复时间。这种恢复时间的改变可能会促使房颤的发生和持续。

About Atrial fibrillation

关于心房颤动

AFib is one of the most common sustained cardiac rhythm disorders (arrhythmias). It results from rapid, disorganized electrical signals in the upper chambers (atria) of the heart, causing them to quiver and contract quickly and irregularly. As a result, the atria do not empty completely, and blood does not flow properly, causing blood clots to form.

心房颤动是最常见的心律失常（心律不齐）之一。它是由心脏上腔（心房）中快速而无序的电信号引起的，导致心房颤抖并快速而不规则地收缩。结果，心房无法完全排空，血液不能正常流动，从而导致血栓形成。

These blood clots can break loose and travel to the brain, resulting in a stroke..

这些血块可能会脱落并移动到大脑，导致中风。

The prevalence of AFib continues to increase globally. Projection studies show that the number of people with AFib will rise to 15.9 million in 2050 in America and 17.9 million in 2060 in Europe.

房颤的患病率在全球范围内持续增加。预测研究表明，到2050年，美国房颤患者人数将上升至1590万，而到2060年，欧洲将达到1790万。

People with AFib are 5 times more likely to suffer a stroke than people without AFib.

患有房颤的人中风的可能性是无房颤人群的五倍。

AFib-related strokes are also associated with a 50% likelihood of death within one year.

与房颤相关的中风在一年内死亡的可能性也达到50%。

About Bayer’s Commitment in Cardiovascular Diseases

关于拜耳在心血管疾病方面的承诺

Bayer is a leader in cardiology and is advancing a portfolio of innovative treatments in cardiovascular (CV) diseases of high unmet medical need. The strategy is to unlock the strong potential of the future CV market by transforming Bayer’s portfolio into precision cardiology, addressing the high CV disease burden, and driving the long-term growth.

拜耳在心脏病学领域处于领先地位，正在推进一系列针对高未满足医疗需求的心血管（CV）疾病的创新治疗方案。其战略是通过将拜耳的产品组合转型为精准心脏病学，解决心血管疾病带来的沉重负担，并推动长期增长，从而释放未来心血管市场的巨大潜力。

Bayer’s portfolio already includes several innovative products as well as compounds in various stages of preclinical and clinical development..

拜耳的产品组合已经包括几种创新产品，以及处于临床前和临床开发不同阶段的化合物。

About Bayer

关于拜耳

Bayer is a global enterprise with core competencies in the life science fields of health care and nutrition. In line with its mission, “Health for all, Hunger for none,” the company’s products and services are designed to help people and the planet thrive by supporting efforts to master the major challenges presented by a growing and aging global population.

拜耳是一家在医疗保健和营养等生命科学领域具有核心竞争力的全球性企业。秉承“人人健康，无人饥饿”的使命，公司的产品和服务旨在帮助人类和地球繁荣发展，支持应对不断增长和老龄化的全球人口所带来的重大挑战。

Bayer is committed to driving sustainable development and generating a positive impact with its businesses. At the same time, the Group aims to increase its earning power and create value through innovation and growth. The Bayer brand stands for trust, reliability and quality throughout the world. In fiscal 2024, the Group employed around 93,000 people and had sales of 46.6 billion euros.

拜耳致力于通过其业务推动可持续发展并产生积极影响。同时，集团旨在通过创新和增长提高盈利能力并创造价值。拜耳品牌在全球范围内代表信任、可靠性和质量。在2024财年，该集团拥有约93,000名员工，销售额达466亿欧元。