Treating cancer with medicines that tightly attach to their targets via covalent bonds is not a new concept in drug discovery, but it is picking up pace. Some companies are trying to improve this approach as they employ covalency to address elusive targets. These efforts, at least the publicly known ones, are focused on small molecules.

用通过共价键与其靶标紧密结合的药物治疗癌症并不是药物发现的新概念，但它正在加快步伐。一些公司正在尝试改进这种方法，因为它们使用共价来解决难以捉摸的目标。这些努力，至少是众所周知的努力，都集中在小分子上。

Enlaza Therapeutics is working to bring covalency to biologic therapies and it has raised $100 million for efforts that include work in one of the hottest areas of cancer drug research..

Enlaza Therapeutics正在努力为生物疗法带来共价性，它已经筹集了一亿美元，用于包括癌症药物研究最热门领域之一的工作。。

The Series A financing announced Tuesday was led by the life sciences group of J.P. Morgan.

周二宣布的A系列融资由摩根大通生命科学集团牵头。

The binding of a drug is a chemical reaction between the drug and its target. Most drug interactions can be characterized by “on rates” when they are bound to their targets, and “off rates” when they are dissociated from them, said Sergio Duron, CEO of La Jolla, California-based Enlaza. Small molecules are cleared from the body relatively quickly, which is why these drugs must typically be taken daily.

药物的结合是药物与其靶标之间的化学反应。总部位于加利福尼亚州拉霍亚的Enlaza首席执行官塞尔吉奥·杜龙（SergioDuron）说，大多数药物相互作用的特征是，当它们与目标结合时，它们会“开率”，而当它们与目标分离时，它们会“关率”。小分子相对较快地从体内清除，这就是为什么这些药物通常必须每天服用的原因。

Protein drugs, such as antibodies, stay around longer, which means dosing can be less frequent. These biologic drugs also offer better targeting specificity compared to small molecules..

蛋白质药物，如抗体，停留时间更长，这意味着给药频率可能较低。与小分子相比，这些生物药物还具有更好的靶向特异性。。

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With the Rise of AI, What IP Disputes in Healthcare Are Likely to Emerge?

随着人工智能的兴起，医疗保健领域可能会出现哪些知识产权纠纷？

Munck Wilson Mandala Partner Greg Howison shared his perspective on some of the legal ramifications around AI, IP, connected devices and the data they generate, in response to emailed questions.

Munck Wilson Mandala合伙人格雷格·豪森（GregHowison）在回答电子邮件中提出的问题时，分享了他对人工智能、IP、连接设备及其产生的数据产生的一些法律后果的看法。

Enlaza named its covalent biologic platform technology “War-Lock.” This technology develops drugs that are nonreactive when they are circulating in the body. But when they find their target, this proximity activates them, leading the molecule to form a covalent bond. The War-Lock platform is based on technologies licensed from the University of California, San Francisco, and The Scripps Research Institute.

Enlaza将其共价生物平台技术命名为“战争锁”。这项技术开发的药物在体内循环时无反应。但当它们找到目标时，这种接近会激活它们，导致分子形成共价键。War Lock平台基于加利福尼亚大学旧金山分校和斯克里普斯研究所许可的技术。

Duron said the research involved using non-natural amino acids that are nonreactive until they are in forced proximity to a target. The research, published in the journal Cell in 2020, sparked the idea of applying this strategy to proteins, Duron said..

杜伦说，这项研究涉及使用非天然氨基酸，这些氨基酸在被迫接近目标之前是无反应的。Duron说，这项研究于2020年发表在《细胞》杂志上，引发了将这一策略应用于蛋白质的想法。。

Unlike small molecules, which mostly work by blocking their targets, Enlaza’s biologic drugs carry therapeutic payloads. Enlaza’s initial focus is cancer, where its research interests include antibody drug conjugates (ADCs). These drugs consist of a toxic drug payload chemically linked to an antibody that targets the delivery of the therapy to cancer cells.

与主要通过阻断其靶标起作用的小分子不同，Enlaza的生物药物具有治疗有效载荷。Enlaza最初的重点是癌症，其研究兴趣包括抗体-药物偶联物（ADC）。这些药物由与抗体化学连接的有毒药物有效载荷组成，该抗体靶向将治疗递送至癌细胞。

However, sometimes the drug payload is released early, which leads to adverse effects elsewhere in the body. One way drug companies are trying to improve ADCs is with better linkers..

然而，有时药物有效载荷会提前释放，从而导致身体其他部位的不良反应。制药公司试图改进ADC的一种方法是使用更好的链接器。。

Using covalency to achieve selective and specific attachment to cancer cells could offer another way to improve ADCs. Enlaza aims to achieve high clearance of its drugs so they do not stay around and cause side effects, Duron said. But during the time an Enlaza cancer drug is in the body, it would have a long residency time on its target via the covalent bond..

使用共价实现对癌细胞的选择性和特异性附着可以提供另一种改善ADC的方法。Duron说，Enlaza的目标是实现其药物的高清除率，以便它们不会停留在周围并引起副作用。但是，在Enlaza抗癌药物进入体内的过程中，它通过共价键在其靶标上会有很长的停留时间。。

“This is not just another ADC,” Duron said. “This is a different strategy to approach what is a very, very hot field right now where everyone is innovating on linker/payload strategies, and we are innovating on a different part of that molecule.”

“这不仅仅是另一个ADC，”Duron说。“这是一个不同的策略，以接近目前非常非常热门的领域，每个人都在链接器/有效负载策略上创新，我们正在该分子的不同部分进行创新。”

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A Personalized Approach to Medication Nonadherence

个性化的药物不依从性方法

At the Abarca Forward conference earlier this year, George Van Antwerp, managing director at Deloitte, discussed how social determinants of health and a personalized member experience can improve medication adherence and health outcomes.

在今年早些时候的Abarca Forward会议上，德勤董事总经理乔治·范安特卫普（GeorgevanAntwerp）讨论了健康的社会决定因素和个性化的会员体验如何改善药物依从性和健康结果。

Enlaza launched in 2022 backed by $61 million in seed financing led by Avalon Ventures. That capital was used to translate the science from an academic paper into a drug discovery engine. Duron said Enlaza has achieved preclinical proof of concept, demonstrating better safety and efficacy for its covalent biologic drugs.

Enlaza成立于2022年，由Avalon Ventures领导的6100万美元种子融资支持。该资金用于将科学从学术论文转化为药物发现引擎。Duron说，Enlaza已经取得了临床前概念验证，证明其共价生物药物具有更好的安全性和有效性。

With the financing, the company will continue to develop its pipeline with the goal of reaching the clinic. Duron declined to offer a specific timeline, but said he expects “at least a couple of development candidates” will progress to clinical testing over the next several years..

通过融资，该公司将继续开发其管道，以达到诊所的目标。Duron拒绝提供具体的时间表，但表示他预计“至少有几个开发候选人”将在未来几年内进入临床测试阶段。。

The company isn’t disclosing its targets yet. But Duron said the War-Lock approach could be applied to other types of cancer drugs, such as radioligand therapies. As a platform technology, War-Lock also has potential applications in other therapeutic areas, such as autoimmune diseases. Now that the startup has emerged from semi-stealth mode, it is looking for potential biopharmaceutical industry partners interested in exploring applications of the technology.

该公司尚未披露其目标。但杜伦说，战争锁定方法可以应用于其他类型的癌症药物，如放射性配体疗法。作为一种平台技术，战争锁在其他治疗领域也有潜在的应用，如自身免疫性疾病。现在，这家初创公司已经摆脱了半隐形模式，它正在寻找有兴趣探索该技术应用的潜在生物制药行业合作伙伴。

Duron said he’s looking to work with companies “that can enable our pipeline and be aligned with our vision of covalent protein drugs.”.

Duron说，他希望与“能够使我们的生产线与共价蛋白质药物的愿景保持一致”的公司合作。

Besides J.P. Morgan, other participants in Enlaza’s new financing include earlier investors Frazier Life Sciences, Avalon Ventures, Lightspeed Venture Partners, and Samsara BioCapital. New investors in the startup include Amgen Ventures, Regeneron Ventures, Bregua Corporation, Pappas Capital, and Alexandria Venture Investments..

除摩根大通外，Enlaza新融资的其他参与者包括早期投资者Frazier Life Sciences、Avalon Ventures、Lightspeed Venture Partners和轮回生物资本。这家初创公司的新投资者包括安进风险投资公司（Amgen Ventures）、Regeneron Ventures、Bregua Corporation、Pappas Capital和亚历山大风险投资公司（Alexandria Venture Investments）。。

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抗体-药物偶联物

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cancer

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Sergio Duron

Sergio Duron

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