A Phase 1 Open-label, 2-Part Crossover Study to Assess the Effect of Acid-reducing Agent Famotidine on the Pharmacokinetics of Afimetoran (BMS-986256) in Healthy Participants

The purpose of this study is to confirm there is no significant effect of gastric pH changes of famotidine on the drug levels of afimetoran in healthy participants.

开始日期2023-07-04

申办/合作机构

Bristol Myers Squibb Co.

NCT05901714

/ Completed临床1期

An Open-label, Single-sequence, Drug-drug Interaction Study in Healthy Participants to Assess the Effect of Phenytoin on the Pharmacokinetics of a Single Oral Dose of Afimetoran (BMS-986256) (Part 1) and the Effect of Steady-state Afimetoran on the Pharmacokinetics of Midazolam (Part 2)

This study will consist of 2 parts. The study will evaluate whether administration of phenytoin impacts the single-dose drug levels of afimetoran and BMT-271199 (Part 1) and will evaluate whether multiple administrations of afimetoran impact the drug levels of midazolam and 1-hydroxymidazolam (Part 2).

开始日期2023-06-14

申办/合作机构

Bristol Myers Squibb Co.

NCT04895696

/ Active, not recruiting临床2期

A Phase 2, Multicenter, Randomized, Double-blind, Placebo-Controlled, Study to Evaluate the Efficacy and Safety of Afimetoran in Participants With Active Systemic Lupus Erythematosus

The purpose of this study is to evaluate the effectiveness, safety and tolerability of Afimetoran in participants with active Systemic Lupus Erythematosus (SLE). The extension period will provide additional long-term safety and efficacy data and enable those participants initially randomized to placebo to receive treatment with Afimetoran.

开始日期2021-10-11

申办/合作机构

Bristol Myers Squibb Co.

100 项与 Afimetoran 相关的临床结果

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100 项与 Afimetoran 相关的转化医学

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100 项与 Afimetoran 相关的专利（医药）

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项与 Afimetoran 相关的文献（医药）

2025-08-01·JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY

Comparative effects of biologics and small molecule inhibitors on cutaneous disease activity in lupus erythematosus: A systematic review and network meta-analysis

Article

作者: Gou, David ; Sun, Wayne ; Rayner, Daniel G ; Xi, Cheng En ; Silang, Isabella ; Dutz, Jan P ; Khosravi-Hafshejani, Touraj

Meta-anal. of comparative effects of biologics and small mol. inhibitors on cutaneous disease activity in lupus erythematosus.Our review builds upon the limitations of previous network meta-analyses by including 29 more trials investigating 25 addnl. unique interventions in our analyses on CLASI-A scores.In addition to anifrolumab, deucravacitinib, and litifilimab, we identified superior efficacy of sifalimumab and daxdilimab compared to placebo-all of which target the type 1 interferon pathway. Litifilimab and daxdilimab inhibit BDCA2 and Ig-like transcript 7, resp., which reside on dendritic cells and stimulate the production of type 1 interferons.Meanwhile, sifalimumab directly inhibits interferon-, and anifrolumab and deucravacitinib target the interferon-receptor and tyrosine kinase 2, resp.-two proteins involved in the interferon signaling pathway.These findings support the continued investigation of the type 1 interferon pathway in the management of CLE.

2025-07-01·ACR open rheumatology

Safety, Tolerability, Efficacy, Pharmacokinetics, and Pharmacodynamics of Afimetoran, a Toll‐Like Receptor 7 and 8 Inhibitor, in Patients With Cutaneous Lupus Erythematosus: A Phase 1b Randomized, Double‐Blind, Placebo‐Controlled Study

Article

作者: Zhu, Lin ; Ignatenko, Stanislav ; Chadwick, Kristina D. ; Harrison, Melanie ; Bach, Thanh ; Saini, Jasmine ; Hosein, Fareeda ; Carayannopoulos, Leonidas N. ; Zhang, WanYing ; Krishna, Gopal ; Aras, Urvi ; Karabeber, Hazem ; Dawes, Michelle ; Baribaud, Frédéric

Objective:

There is an unmet need for safe and effective oral treatments for cutaneous lupus erythematosus (CLE). Afimetoran is an investigational, first‐in‐class, orally bioavailable, selective small molecule inhibitor of Toll‐like receptors (TLRs) 7 and 8. We investigated the safety, tolerability, efficacy, pharmacokinetics, and pharmacodynamics of afimetoran in patients with CLE.

Methods:

In this Phase 1b, randomized, double‐blind, placebo‐controlled study (NCT04493541), patients with CLE received afimetoran (30 mg once daily) or a placebo, in addition to select background medications, over 16 weeks. Safety and tolerability were mainly reported through adverse events (AEs). Pharmacokinetics were determined using plasma concentration–time data. Pharmacodynamic biomarkers and efficacy (CLE Disease Area and Severity Index‐Activity [CLASI‐A] scores) were exploratory end points.

Results:

Thirteen patients were randomized (afimetoran, n = 8; placebo, n = 5), and 12 patients completed treatment (1 discontinued afimetoran [COVID‐19 infection]). Afimetoran demonstrated a favorable safety profile compared with placebo (patients with AEs: 62.5% vs 80.0%), with mainly mild‐to‐moderate AEs. Plasma concentrations exceeded the projected targeted 24‐hour 90% inhibition concentration, supporting once‐ daily dosing. Pharmacodynamic analyses showed a rapid response to afimetoran by week 1 maintained throughout and beyond treatment, with reduced expression of TLR7/8 pathway–associated cytokines. All patients who received afimetoran had a change in the interferon‐1 gene signature (P < 0.0001) at week 16, with five of eight patients demonstrating a >50% improvement in CLASI‐A scores.

Conclusion:

These findings support afimetoran's potential as a once daily oral treatment for patients with CLE and suggest a possibly substantial therapeutic benefit, warranting further clinical investigation of afimetoran for lupus.

2023-12-18·Angewandte Chemie (International ed. in English)

Phenoxythiazoline (FTz)‐Cobalt(II) Precatalysts Enable C(sp²)–C(sp³) Bond‐Formation for Key Intermediates in the Synthesis of Toll‐like Receptor 7/8 Antagonists**

Article

作者: Chirik, Paul J. ; Kim, Junho ; Mills, L. Reginald ; Gygi, David ; Simmons, Eric M. ; Lee, Heejun ; Wisniewski, Steven R. ; Di Mare, Francesca

Abstract:

Evaluation of the relative rates of the cobalt‐catalyzed C(sp2)–C(sp3) Suzuki–Miyaura cross‐coupling between the neopentylglycol ester of 4‐fluorophenylboronic acid and N‐Boc‐4‐bromopiperidine established that smaller N‐alkyl substituents on the phenoxyimine (FI) supporting ligand accelerated the overall rate of the reaction. This trend inspired the design of optimal cobalt catalysts with phenoxyoxazoline (FOx) and phenoxythiazoline (FTz) ligands. An air‐stable cobalt(II) precatalyst, (FTz)CoBr(py)3 was synthesized and applied to the cross‐coupling of an indole‐5‐boronic ester nucleophile with a piperidine‐4‐bromide electrophile that is relevant to the synthesis of reported toll‐like receptor (TLR) 7/8 antagonist molecules including afimetoran. Addition of excess KOMe⋅B(OiPr)3 improved catalyst lifetime due to attenuation of alkoxide basicity that otherwise resulted in demetallation of the FI chelate. A first‐order dependence on the cobalt precatalyst and a saturation regime in nucleophile were observed, supporting turnover‐limiting transmetalation and the origin of the observed trends in N‐imine substitution.

项与 Afimetoran 相关的新闻（医药）

2026-04-16

·动脉网

贝利恩为BMS药物筹集3亿美元，以及其他生物融资

生物制药领域的私人融资加速，Beeline、Oricell、Terremoto、Harbinger、Neomorph、Adcendo 和 STORM 近期均获得了重要的融资轮次。Beeline Medicines 正式启动，并在 A 轮融资中筹集了 3 亿美元，由贝恩资本领投，同时从百时美施贵宝（BMS）获得了免疫学和炎症药物的管线授权。这家总部位于康涅狄格州斯坦福德和马萨诸塞州波士顿的初创公司目前有五种候选药物正在开发中。其主要候选药物 afimetoran（BMS-986256）是一种每日一次的口服 TLR7/8 抑制剂，正在进行针对系统性红斑狼疮（SLE）的二期临床试验，并在早期试验中显示出对皮肤型红斑狼疮（CLE）的潜力。针对 SLE 的三期临床计划正在筹备中。其他处于临床阶段的候选药物包括 BMS-986326，一种 IL-2-CD25 融合蛋白，正处于针对特应性皮炎及 SLE/CLE 的一期 b 阶段试验；以及 lomedeucitinib，一种口服 TYK2 抑制剂，正在进行针对银屑病的二期试验，类似于 BMS 已获批药物 Sotyktu。Beeline 由前 SpringWorks 首席执行官 Saqib Islam 领导，Badreddin Edris 担任首席运营官兼总裁。（摘要由动脉网AI生成）

2026-04-16

·药研网

被默克39亿收购后，又和BMS组建自免NewCo融资3亿，TLR7/8、TYK2、IL-2/8/10

4月16日，BMS宣布，将旗下五大药物资产注入全新生物科技公司 Beeline Medicines，开启精准免疫学的首次亮相。Bain Capital作为投资方，为Beeline提供约3亿美元启动资金，用于管线发展及市场推广。 Beeline Medicines的核心目标是推进精准免疫疗法，计划在未来一年内启动多项临床试验。该公司由经验丰富的行业人士 Saqib Islam 领衔，他曾担任SpringWorks Therapeutics的CEO，该公司是辉瑞的衍生企业，并于2024年以39亿美元被默克收购。 Beeline的核心药物为afimetoran，是首创的口服生物利用度强效小分子TLR7/8选择性抑制剂，在皮肤型红斑狼疮（CLE）患者中表现出良好的安全性，且与安慰剂组相比耐受性良好，从而实现了研究的主要目标。该药物已在CLE 1b期研究中完成概念验证，数据显示其药效快速且持久。2025年5月，FDA授予afimetoran快速通道资格，目前正推进系统性红斑狼疮（SLE）的2期临床试验，并计划在今年晚些时候完成，随后进入关键性3期研究。此外，Beeline还拥有 BMS-986326（IL-2/CD25融合蛋白，用于特应性皮炎、CLE及SLE）、BMS-986322（口服TYK2抑制剂，lomedeucitinib，用于银屑病及罕见免疫疾病）以及两款临床前生物制剂IL-8靶向BMS-986481、IL-10靶向BMS-986498，为未来临床开发储备潜力。 Beeline Medicines在官方声明中表示：“我们致力于推进自身免疫及炎症性疾病的精准疗法，将利用现有管线资产和未来临床试验，加速afimetoran等候选药物的研发与上市。” 自身免疫治疗赛道竞争激烈。Biogen近期在CLE中期临床试验中取得重要胜利，Gilead也斥资超20亿美元收购Ouro Medicines及其T细胞接合剂OM336，该药物目前正处于早期研发阶段，用于治疗多种自身免疫性疾病，包括血细胞减少症和血清阳性疾病。 Bain Capital作为投资方。此前，Bain Capital曾联合辉瑞孵化SpringWorks Therapeutics（2017年）和Cerevel Therapeutics（2018年），两家公司均已高价收购，这也为Beeline的潜力增添了信心。 End 声明：本公众号所有发文章(包括原创及转载文章)系出于传递更多信息之目的，且注明来源和作者。本公众号欢迎分享朋友圈或大群，谢绝媒体或机构未经授权以任何形式转载至其他平台。转载/商务/投稿 | 联系微信15618157102（sum_Gmi）商务合作稿件征集点击了解详情往期回顾 2026全球肥胖药企十强出炉一文读懂抗体：结构、分类与ADCC/ ADCP/ CDC机制

免疫疗法并购快速通道临床2期临床3期

2026-04-15

·药明康德

产业新闻 | 3亿美元A轮融资！新锐推进小分子疗法2期研究；超1亿美元！新锐开发创新AKT抑制剂

3亿美元A轮融资！新锐推进小分子疗法2期研究 Beeline Medicines今日宣布正式亮相，该公司致力于开发精准疗法以改善自身免疫性及炎症性疾病患者的治疗前景。该公司最初成立于2025年7月，其初始产品组合包括从百时美施贵宝（Bristol Myers Squibb）引进的五个研发项目。这些候选疗法均基于明确机制设计，具有高度选择性，旨在为多种免疫介导疾病患者带来更持久的健康获益。在Bain Capital领投的3亿美元A轮融资支持下，Beeline Medicines计划推进精准治疗策略的发展，为亟需创新疗法的患者群体带来新的治疗选择。在研发管线方面，公司正推进一系列以经过验证的生物学机制为基础的精准疗法，通过优化分子设计并采用高效的临床开发策略，重点解决未满足的医疗需求。其中，主打项目afimetoran是一种选择性小分子TLR7/8抑制剂，具有每日一次口服给药的潜力，正在开发用于治疗狼疮，并已在皮肤型红斑狼疮的1b期研究中获得早期临床概念验证；该药物还在2025年5月获得美国FDA授予的系统性红斑狼疮快速通道资格，目前针对系统性红斑狼疮的2期研究正在进行，预计将于2026年下半年完成。此外，公司还在推进IL-2-CD25融合蛋白BMS-986326，用于治疗特应性皮炎及狼疮，通过提高对调节性T细胞的选择性以改善疗效与给药间隔；TYK2变构抑制剂lomedeucitinib则在斑块型银屑病的2期研究中获得积极概念验证结果，并有望进一步拓展至罕见免疫疾病。与此同时，公司还布局两项处于IND阶段的下一代生物制品项目，分别靶向IL-18和IL-10通路，以应对包括胃肠道炎症性疾病在内的多种炎症性疾病。超1亿美元！新锐开发创新AKT抑制剂 Terremoto Biosciences今日宣布完成1.08亿美元C轮融资。本轮融资由RA Capital Management、Deep Track Capital、Osage University Partners以及BeOne Medicines等新投资方参与，现有投资者OrbiMed、Third Rock Ventures、Novo Holdings和Cormorant Asset Management亦继续跟投。公司表示，此次融资将用于推进其在肿瘤学及罕见病领域的研发管线，加速候选疗法进入临床开发阶段。 Terremoto的核心肿瘤项目TER-2013目前正在开展1期临床试验，主要针对携带PIK3CA、AKT或PTEN基因变异的实体瘤患者，这些分子异常在多种癌症中具有重要作用，在HR阳性乳腺癌患者中尤为常见。此外，公司还在推进另一项候选疗法TER-4480，用于治疗遗传性出血性毛细血管扩张症（HHT）。该疾病是一种罕见的遗传性出血性疾病，由异常血管形成引起，目前尚无获批疗法。该项目预计将于今年晚些时候进入临床阶段。两项管线均围绕关键调控蛋白AKT展开。研究表明，在AKT1、AKT2和AKT3三种结构相似的亚型中，AKT1在疾病进展中发挥主导作用，而AKT2则与皮疹及葡萄糖稳态紊乱等不良反应相关。基于先进的药物化学技术，Terremoto开发了一类新型AKT1选择性抑制剂，旨在避免传统PI3K/AKT通路抑制剂因PI3Kα或AKT2抑制所带来的毒性限制，从而实现更深、更持久的治疗效果并改善耐受性。参考资料： [1] Terremoto Biosciences Closes $108 Million Series C Financing to Advance Selective AKT1-Inhibitors in Oncology and Hereditary Hemorrhagic Telangiectasia. Retrieved April 15, 2026 from https://www.businesswire.com/news/home/20260415685181/en/Terremoto-Biosciences-Closes-%24108-Million-Series-C-Financing-to-Advance-Selective-AKT1-Inhibitors-in-Oncology-and-Hereditary-Hemorrhagic-Telangiectasia [2] Beeline Medicines Debuts to Deliver Category-Leading Precision Therapies for People Living with Autoimmune and Inflammatory Diseases. Retrieved April 15, 2026 from https://www.globenewswire.com/news-release/2026/04/15/3274299/0/en/Beeline-Medicines-Debuts-to-Deliver-Category-Leading-Precision-Therapies-for-People-Living-with-Autoimmune-and-Inflammatory-Diseases.html 免责声明：本文仅作信息交流之目的，文中观点不代表药明康德立场，亦不代表药明康德支持或反对文中观点。本文也不是治疗方案推荐。如需获得治疗方案指导，请前往正规医院就诊。版权说明：欢迎个人转发至朋友圈，谢绝媒体或机构未经授权以任何形式转载至其他平台。转载授权请在「药明康德」微信公众号回复“转载”，获取转载须知。分享，点赞，在看，聚焦全球生物医药健康创新

100 项与 Afimetoran 相关的药物交易

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研发状态

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适应症	最高研发状态	国家/地区	公司	日期
系统性红斑狼疮	临床2期	美国	Bristol Myers Squibb Co.	2021-10-11
系统性红斑狼疮	临床2期	中国	Bristol Myers Squibb Co.	2021-10-11
系统性红斑狼疮	临床2期	日本	Bristol Myers Squibb Co.	2021-10-11
系统性红斑狼疮	临床2期	阿根廷	Bristol Myers Squibb Co.	2021-10-11
系统性红斑狼疮	临床2期	澳大利亚	Bristol Myers Squibb Co.	2021-10-11
系统性红斑狼疮	临床2期	巴西	Bristol Myers Squibb Co.	2021-10-11
系统性红斑狼疮	临床2期	智利	Bristol Myers Squibb Co.	2021-10-11
系统性红斑狼疮	临床2期	哥伦比亚	Bristol Myers Squibb Co.	2021-10-11
系统性红斑狼疮	临床2期	法国	Bristol Myers Squibb Co.	2021-10-11
系统性红斑狼疮	临床2期	德国	Bristol Myers Squibb Co.	2021-10-11