A Phase 1/2 Open Label, Multicenter, Dose Escalation and Expansion Study of the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of HM43239 in Patients With Relapsed or Refractory Acute Myeloid Leukemia (AML)

The main purpose of this study is to identify a safe and potentially effective dose of tuspetinib to be used in future studies in study participants diagnosed with acute myeloid leukemia (AML), myelodysplastic syndromes with increased blasts grade 2 (MDS-IB2), or chronic myelomonocytic leukemia (CMML) that is relapsed or refractory after at least one line of prior therapy, or in study participants with newly diagnosed AML. Tuspetinib will be administered as a single agent or in combination with other drugs (venetoclax or venetoclax plus azacitidine), as specified for each part of the study.

开始日期2019-03-11

申办/合作机构

Aptose Biosciences, Inc.

100 项与 Tuspetinib 相关的临床结果

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100 项与 Tuspetinib 相关的转化医学

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100 项与 Tuspetinib 相关的专利（医药）

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项与 Tuspetinib 相关的文献（医药）

2026-09-01·NEUROIMAGE

Combined continuous theta burst transcranial ultrasound and magnetic stimulation for induction of cortical plasticity

Article

作者: Chen, Robert ; Chang, Hsin-Yun ; Shih, Yao-Chia ; Chen, Kai-Hsiang Stanley ; Chen, Gin-Shin ; Dong, Yan-Siou ; Nankoo, Jean-François ; Liu, Hao-Li ; Kuo, Yih-Chih Jacinta ; Yang, Wei-Chih

BACKGROUND:

Magnetic continuous theta burst stimulation (cTBS) is known to suppress human motor cortical excitability. Whether transcranial ultrasound stimulation (TUS) delivered in a continuous theta burst pattern (ctbTUS) produces similar inhibitory effects and whether co-applying ctbTUS with cTBS enhances these effects remains unclear.

METHODS:

Four stimulation conditions: ctbTUS + sham cTBS (ctbTUS), sham ctbTUS + cTBS (cTBS), sham ctbTUS + sham cTBS (sham), and ctbTUS + cTBS (cosTBS) were applied. Fifteen participants underwent neurophysiological testing with motor-evoked potentials (MEPs) recorded at 0, 10, 20, and 60 min post-stimulation, normalized to pre-intervention baselines. Additionally, 18 participants underwent resting-state functional MRI (rsfMRI) to assess functional connectivity (FC) between the hand representation of the motor cortex (M1) and other brain regions. Simulated skull density, transducer-skull space, and online-inhibition characteristics were evaluated as modulatory factors.

RESULTS:

ctbTUS induced inhibitory after-effects measured by MEP amplitude lasting up to 60 min (p = 0.001). However, cosTBS reduced this inhibition, although immediate MEP suppression remained (p = 0.024). rsfMRI revealed reduced FC between M1 and bilateral pre/post-central gyri and increased cerebellar FC after ctbTUS, but such after-stimulation patterns were absent after cosTBS. Higher pseudo-computed-tomography-derived skull density was associated with more negative ΔFC (or FC suppression, β = -0.844, p = 0.004). Participants with online inhibition showed greater offline MEP suppression (p = 0.004).

CONCLUSIONS:

ctbTUS induced inhibitory after-effects lasting up to 60 min but cosTBS decreased this suppression, likely via calcium-dependent plasticity or homeostatic plasticity effects. Skull density, and individual sensitivity to TUS are critical factors influencing TUS efficacy.

2026-05-20·Science Translational Medicine

Transcranial ultrasound stimulation of motor networks in Parkinson’s disease informed by local field potential dynamics

Article

作者: Chen, Robert ; Ding, Mandy Yi Rong ; Raies, Nasem ; Pichardo, Samuel ; Annirood, Regina ; Fasano, Alfonso ; Darmani, Ghazaleh ; Samuel, Nardin ; Lozano, Andres M. ; Vetkas, Artur ; Callister, Marcus ; Munhoz, Renato P. ; Kalia, Suneil K. ; Fomenko, Anton ; Grippe, Talyta ; Schall, Jeffrey D. ; Abrahao, Agessandro ; Nankoo, Jean-Francois ; Sarica, Can ; Hodaie, Mojgan ; Ramezanpour, Hamidreza ; Santyr, Brendan

Transcranial ultrasound stimulation (TUS) is a promising noninvasive technique for modulating deep brain targets and circuits with high spatial precision. For its successful clinical translation, confirmation of target engagement, together with a deeper understanding of the effects of TUS, is essential. To advance these goals, we obtained direct measures of neural activity using electrodes implanted in the subthalamic nucleus (STN) in patients with Parkinson’s disease (PD) during TUS of deep and superficial targets, guided by magnetic resonance imaging–based acoustic modeling and real-time neuronavigation. Seventeen patients were studied in the on-medication and off–deep brain stimulation states. Each patient received one active and one sham session in a randomized order, and 13 of 17 patients (76%) completed a third session, which was always active. Each active condition targeted a single site—either the primary motor cortex (M1), the globus pallidus internus (GPi), or the occipital cortex (control site)—with 10 patients per active target. TUS effects on the STN were found to be target specific. Stimulation of the M1 reduced STN beta oscillation activity compared with sham stimulation and was associated with improvements in motor signs. These effects were brain state specific, showing distinct modulation patterns at rest versus during movement. In contrast, TUS targeting the GPi increased beta activity relative to control conditions and did not improve motor signs. Our results provide mechanistic evidence that TUS can safely and selectively modulate pathological brain rhythms in the STN in PD, supporting its potential as a targeted, noninvasive therapeutic modality.

2026-05-01·TOXICOLOGY AND APPLIED PHARMACOLOGY

Tussilagone inhibits MRGPRX2-mediated mast cell degranulation and suppresses pseudo-allergic reactions

Article

作者: Cao, Yong-Xiao ; Mi, Yan-Ni ; Huang, Ting-Ting ; Yan, Ping-Ping ; Attiogbe, Mawusse K I

Mas-related G protein-coupled receptor X2 (MRGPRX2) is a crucial target in pseudo-allergic reactions. Tussilagone (Tus), the main bioactive component derived from Tussilago farfara, has anti-inflammatory effects, but its potential inhibitory effects on pseudo-allergic responses remain unclear. This research aimed to evaluate the inhibitory role of Tus on pseudo-allergic reactions and its underlying mechanism. In vivo Systemic pseudo-allergic reactions and passive cutaneous anaphylaxis (PCA) models were established to assess the effects of Tus. In vitro, mast cell (LAD2) degranulation, inflammatory cytokine release, and signaling pathway protein expression were assessed. Calcium influx was measured in MRGPRX2-expressing HEK293 cells. The results showed that Tus significantly attenuated Tween 80- and substance P (SP)-induced systemic pseudo-allergy and PCA reactions. It also suppressed mast cell degranulation and decreased production of tumor necrosis factor-alpha (TNF-α), Interleukin-8 (IL-8) and monocyte chemotactic protein-1 (MCP-1). In MRGPRX2-expressing HEK293 cells, Tus suppressed Tween 80- and SP-induced Ca²⁺ influx. Mechanistically, Tus inhibited tolimidone-induced Lyn kinase activation and suppressed SP-and Tween 80-induced β-hexosaminidase release, exhibiting an inhibitory profile comparable to that of the Lyn/Btk antagonist bosutinib. Additionally, Tus attenuated the phosphorylation levels of MRGPRX2 downstream signal molecules, including Btk, PLCγ1, PKC, p38 MAPK, IκB-α and NF-κB (p65). In conclusion, Tus attenuates SP-and Tween 80-induced mast cell activation and pseudo-allergic reactions by targeting the Lyn/Btk/PLCγ1 and p38/NF-κB pathways, highlighting its therapeutic potential for pseudo-allergy.

128

项与 Tuspetinib 相关的新闻（医药）

2026-07-07

·分子药讯

医药信息整理-2026.07.07

Zymeworks 将收购 Theravance Biopharma, Inc. 2026年7月6日，该收购将YUPELRI ® (revefenacin) 纳入 Zymeworks 的产品组合，该药由Theravance Biopharma和Mylan联合研发，最初于2018年11月在美国获准用于治疗成人慢性阻塞性肺病（COPD），是首款获得美国FDA批准的每日一次雾化型长效毒蕈碱受体拮抗剂。 Ipsen 斥资高达 17.5 亿美元收购 Kartos，押注血液癌症领域 Ipsen 收购的核心是一款 MDM2 阻断剂navtemadlin，MDM2是一种抑制关键肿瘤抑制因子p53表达的蛋白质，navtemadlin旨在恢复这种表达。Kartos正在测试将navtemadlin作为JAK抑制剂ruxolitinib的附加疗法，用于治疗高危骨髓纤维化。据 Ipsen 首席执行官 David Loew 表示，该药物“最早可能在 2028 年”面向患者上市。 Talawar Therapeutics 与 JATT II Acquisition Corp. 宣布达成最终业务合并协议，旨在创建一家上市生物技术公司，开发针对免疫炎症疾病的潜在同类最佳双特异性抗体 Talawar是首家为开发和商业化Khanda Therapeutics, L.P.（"Khanda"）发现的资产而成立的公司，目前正在开发TALA-125，这是一种用于治疗特应性皮炎的新型抗IL-13 × 抗IL-18双特异性抗体，预计将于2027年第一季度进入临床阶段。此次超额认购的2.25亿美元以及私募股权投资（"PIPE"）及其在交易完成时可供合并公司使用的现金，预计将资助TALA-125直至2028年下半年的2b期概念验证研究数据公布。 INTENT Biologics 的 PEP Biologic™ 获 FDA 突破性疗法认定，用于其即将进入 3 期临床的旗舰适应症 INTENT Biologics 是一家临床阶段的生物技术公司，致力于开发针对具有重大未满足医疗需求严重疾病的首创外泌体生物疗法。该公司今日宣布，美国食品药品监督管理局（FDA）已授予 PEP Biologic™ 用于治疗糖尿病足溃疡（DFU）的突破性疗法认定（IND 019567）。这代表了 INTENT Biologics 的又一重大监管里程碑，并进一步加强了 PEP Biologic 的开发路径，建立在先前获得 FDA 快速通道认证的基础上，反映了 DFU 的严重未满足需求，以及 PEP Biologic 新型再生作用机制在解决慢性、不愈合伤口、烧伤和溃疡的潜在治疗潜力。 Aptose Biosciences 宣布完成被 Hanmi Pharmaceutical 收购 2026年6月30日，Aptose Biosciences Inc. 是一家临床阶段的精准肿瘤学公司，正在开发一种基于tuspetinib (TUS) 的三联一线疗法，用于治疗新诊断的急性髓系白血病 (AML) 患者，今日宣布完成根据安排计划（于2025年11月19日和2026年2月24日宣布）的安排，HS North America Ltd.（“买方”）——Hanmi Pharmaceutical Co. Ltd.的全资子公司（“Hanmi”，与买方合称“Hanmi买方”）收购了Aptose所有已发行且流通的普通股（“普通股”），其中未被Hanmi买方或其各自关联方当前持有或控制的部分（“安排”）。 92Bio 公司为铂耐药卵巢癌 NTB-928 的 1 期临床试验首位患者给药 92Bio, Inc. (www.92biotech.com) 是一家开发下一代T细胞衔接抗体（TCEs）的临床阶段生物技术公司，今日宣布在评估NTB-928治疗铂耐药性卵巢癌的1期临床试验中，首位患者已完成给药。该试验在美国多个中心进行，首位患者在首席研究员Geraldine O'Sullivan Coyne医学博士的指导下，于START纽约-长岛中心完成给药。NTB-928结合了亲和力调节的抗CD3部分与亲和力依赖的FOLR1结合臂，以实现肿瘤与正常组织的区分选择性。这种双机制设计能够有效杀伤FOLR1过表达的卵巢癌细胞，同时保护表达微量FOLR1的正常组织——这是针对该抗原的传统方法的一个关键局限。值得注意的是，FOLR1在超过75%的卵巢癌中呈过表达状态。支持NTB-928差异化选择性特征的临床前数据已发表于《Oncoimmunology》（Avanzino等，2022年）。 Neurocrine Biosciences 启动针对 4 岁以下经典型先天性肾上腺皮质增生症患儿的Crinecerfont 二期研究 2026年7月1，Neurocrine Biosciences, Inc. 今日宣布启动其2期临床研究，旨在评估crinecerfont在3个月至4岁以下患有经典型先天性肾上腺皮质增生症（CAH）儿童中的安全性和耐受性。Crinecerfont（商品名：CRENESSITY®）在美国已获批作为辅助治疗方案，用于控制4岁及以上经典型CAH成人和儿童患者体内的雄激素水平。Crinecerfont于2024年获得美国食品药品监督管理局批准，标志着经典型先天性肾上腺皮质增生症（CAH）患者在70多年来首次取得的治疗进展。它是一种强效且选择性的口服促肾上腺皮质激素释放因子1型受体（CRF1）拮抗剂，通过非糖皮质激素机制，从源头上减少升高的促肾上腺皮质激素（ACTH）分泌，从而降低下游过量的肾上腺雄激素。 HUTCHMED 宣布 ORPATHYS® 获 NMPA 批准用于治疗 MET 扩增的胃癌患者 2026年7月2日，和黄医药今日宣布，ORPATHYS ®（Savolitinib）的新药上市申请（NDA）已获得中国国家药品监督管理局（“NMPA”）条件性批准，用于治疗至少接受过两种既往系统治疗失败的MET扩增局部晚期或转移性胃癌或胃食管结合部（GC/GEJ）腺癌患者。ORPATHYS®（savolitinib）是一种强效且高度选择性的MET酪氨酸激酶抑制剂（TKI），由阿斯利康与和黄医药联合开发，并由阿斯利康商业化。MET是一种在正常细胞发育中发挥关键作用的酪氨酸激酶受体。ORPATHYS®可阻断因突变（如外显子14跳跃突变或其他点突变）、基因扩增或蛋白质过表达而导致的MET受体酪氨酸激酶通路异常激活。 Genentech 的 Divarasib 在非小细胞肺癌的头对头 III 期临床试验中优于已获批的KRAS G12C 抑制剂罗氏集团成员Genentech今日宣布，III期Krascendo 1研究取得积极结果。该研究评估了在既往接受过治疗的KRAS G12C非小细胞肺癌（NSCLC）患者中，作为下一代在研KRAS G12C抑制剂的divarasib，与已获批的第一代KRAS G12C抑制剂sotorasib或adagrasib的疗效对比。该研究达到了主要和关键次要终点，divarasib在无进展生存期（PFS）和总生存期（OS）方面均实现了具有临床意义和统计学显著性的改善。divarasib的安全性与此前数据保持一致，未发现新发现，最常见的治疗相关事件均可控且可逆。 PureTech 旗下实体 Celea Therapeutics 完成 1.8 亿美元融资，旨在推进氘代吡非尼酮作为治疗特发性肺纤维化（IPF）的潜在新标准疗法 PureTech Health plc是一家致力于将科学转化为生命价值、将创新转化为价值的生物治疗公司，欣然注意到其初创实体Celea Therapeutics（简称“Celea”）今日宣布完成1.8亿美元的融资。参与方包括RA Capital Management、拜耳旗下的Leaps以及创始人PureTech Health，此外还有一家大型美国医疗保健基金和一家领先的主权财富基金。此次融资所得资金将支持计划于2026年第三季度初启动的deupirfenidone（LYT-100）III期SURPASS-IPF临床试验。这是一种在研的下一代抗纤维化药物，有望成为特发性肺纤维化（IPF）患者的新标准疗法。计划中的关键性3期SURPASS-IPF试验是一项全球性、随机、双盲、头对头试验，直接比较deupirfenidone 825 mg TID与pirfenidone 801 mg TID在未接受背景治疗的IPF成人患者中的疗效。主要有效性终点是第52周绝对用力肺活量较基线的变化，这将评估deupirfenidone相对于pirfenidone的优效性。Celea预计将于2026年第三季度初启动3期SURPASS-IPF试验。 Revolution Medicines 在 2026 年 ESMO 胃肠道癌症大会上展示 Zoldonrasib 联合疗法治疗 RAS G12D 转移性胰腺癌的 1/2 期临床数据 2026年7月2日，Revolution Medicines, Inc. 是一家处于临床后期阶段的肿瘤学公司，致力于为RAS依赖型癌症患者开发靶向疗法。该公司今日公布了两项1/2期临床试验的结果，这些试验评估了其口服RAS(ON) G12D选择性共价抑制剂zoldonrasib在RAS G12D转移性胰腺导管腺癌（PDAC）患者联合治疗方案中的表现。这些结果将在今日的2026年欧洲内科肿瘤学会（ESMO）胃肠道癌症大会的论文宣读环节中展示，内容包括zoldonrasib联合标准疗法化疗在初治患者中的应用，以及zoldonrasib联合daraxonrasib（该公司开发的口服RAS(ON)多性向选择性抑制剂）在既往接受过治疗的患者中的应用。 Safety and Efficacy of Zoldonrasib Plus Chemotherapy in Patients with First Line RAS G12D Metastatic Pancreatic Cancer (Abstract #340O) Safety and Efficacy of Zoldonrasib Plus Daraxonrasib in Patients with Second Line-Plus RAS G12D Metastatic Pancreatic Cancer (Abstract #341O) 诺华获得欧洲委员会批准，Itvisma® 用于治疗脊髓性肌萎缩症（SMA） 2026年7月2日，诺华今日宣布，欧洲委员会（EC）已批准Itvisma®（onasemnogene abeparvovec）用于治疗患有5q脊髓性肌萎缩症（SMA）且生存运动神经元1（SMN1）基因存在双等位基因突变的2岁及以上儿童、青少年和成人。随着该批准的通过，Itvisma成为目前欧盟内首个且唯一获批用于这一广泛SMA人群的基因替代疗法。Itvisma是一种基于腺相关病毒9（AAV9）的基因疗法，其独特设计旨在通过提供人类SMN1基因的功能拷贝，改善运动功能，从而解决SMA的遗传根源，实现持续的SMN蛋白表达，仅需一次性鞘内注射。Itvisma最常见的副作用包括上呼吸道感染、发热、呕吐、头痛和肝酶升高。STEER和STRENGTH研究的结果已发表在《自然医学》杂志上。来源：智慧芽新药情报库

2026-07-06

·BioSpace

Aptose Biosciences Announces Completion of Acquisition by Hanmi Pharmaceutical

June 30, 2026 -- Aptose Biosciences Inc. (“Aptose” or the “Company”) (TSX: APS and OTC: APTOF), a clinical-stage precision oncology company developing a tuspetinib (TUS)-based triple drug frontline therapy to treat patients with newly diagnosed acute myeloid leukemia (AML), today announced the closing of the plan of arrangement (announced on November 19, 2025 and February 24, 2026) pursuant to which HS North America Ltd. (the “Purchaser”), a wholly owned subsidiary of Hanmi Pharmaceutical Co. Ltd. (“Hanmi”, and together with the Purchaser, the “Hanmi Purchasers”) acquired all of the issued and outstanding common shares of Aptose (the “Common Shares”) that were not currently owned or controlled by the Hanmi Purchasers or their respective affiliates (the “Arrangement”). Under the terms of the amended and restated arrangement agreement among Aptose and the Hanmi Purchasers dated February 23, 2026, Aptose shareholders, other than the Hanmi Purchasers and their respective affiliates that hold any Common Shares, will receive C$2.41 in cash per Common Share, which represents a premium of 28% over Aptose’s 30-day VWAP of C$1.88 on the Toronto Stock Exchange (“TSX”) for the period immediately preceding entering into the Arrangement Agreement. The Arrangement received approval from the Company’s shareholders at a special meeting held on March 31, 2026, and the Arrangement received final court approval on the same date. The Arrangement has also received the necessary regulatory approvals in Korea. As a result of the Arrangement, the Common Shares are expected to be delisted from the TSX at the close of trading on or about July 3, 2026. The Company has submitted an application to cease to be a reporting issuer under applicable Canadian securities laws and to otherwise terminate the Company’s public reporting requirements in the United States and Canada. Aptose Biosciences is a clinical-stage biotechnology company committed to developing precision medicines addressing unmet medical needs in oncology, with an initial focus on hematology. The Company's small molecule cancer therapeutics pipeline includes products designed to provide single agent efficacy and to enhance the efficacy of other anti-cancer therapies and regimens without overlapping toxicities. The Company’s lead clinical-stage compound tuspetinib (TUS), is an oral kinase inhibitor that has demonstrated activity as a monotherapy and in combination therapy in patients with relapsed or refractory acute myeloid leukemia (AML) and is being developed as a frontline triplet therapy in newly diagnosed AML. Hanmi Pharmaceutical Co., Ltd. is a research-driven pharmaceutical company headquartered in Seoul, South Korea, and serves as the core operating subsidiary of Hanmi Science, the Group’s holding company. Founded in 1973, Hanmi is committed to developing innovative therapies that address significant unmet medical needs across oncology, metabolic and rare diseases, immunology, and inflammation. Hanmi Pharmaceutical’s pipeline spans innovative biologics and small-molecule candidates, supported by proprietary drug development platforms and a portfolio of established medicines. As part of the Hanmi Science Group, Hanmi Pharmaceutical actively pursues global partnerships and licensing collaborations with leading multinational pharmaceutical companies to advance its therapies to patients worldwide. The content above comes from the network. if any infringement, please contact us to modify.

2026-06-21

·药明康德

针对妇科肿瘤，创新ADC展现治疗潜力；不依赖于特定突变，三联癌症疗法获积极临床进展…… | 一周盘点

本期看点： 1. Zymeworks公司公布了其抗体偶联药物（ADC）ZW191的1期临床试验新数据，该药在铂类耐药卵巢癌（PROC）及子宫内膜癌患者中展现出显著的抗肿瘤活性。 2. Aptose Biosciences公司公布了tuspetinib联用标准剂量的venetoclax和azacitidine（TUS+VEN+AZA）三联疗法治疗新确诊的急性髓系白血病（AML）患者的1/2期试验的新数据。 ZW191：公布1期临床试验的新数据 Zymeworks公司公布了其ADC疗法ZW191的1期临床试验新数据。ZW191靶向叶酸受体α（FRα），该靶点在约75%的高级别浆液性卵巢癌和约70%的肺腺癌中表达。ZW191具有独特的设计，可高效进入FRα阳性细胞，并释放Zymeworks开发的具旁观者效应的载荷——拓扑异构酶I抑制剂ZD06519。此次公布的结果显示，ZW191在铂类耐药卵巢癌及子宫内膜癌患者中展现出显著的抗肿瘤活性。截至2026年3月9日的数据，在疗效可评估的PROC患者中，FRα阳性与阴性肿瘤患者的确认客观缓解率（cORR）分别达到78.6%和47.4%，疾病控制率（DCR）分别为100.0%和89.5%；整体PROC人群的cORR为58.8%。FRα阴性子宫内膜癌患者的cORR为40.0%，DCR为80.0%。两癌种队列的缓解出现较早且随时间加深，中位缓解持续时间尚未达到，中位无进展生存期（PFS）为7.6个月。此外，该药物具备良好的耐受性特征和较宽的治疗窗口，支持继续开展临床开发。 Tuspetinib：公布1/2期联合治疗试验数据 Aptose Biosciences公司公布了其针对新确诊的急性髓系白血病患者开展的1/2期TUSCANY试验的新数据。这些患者接受了不同剂量的tuspetinib联用标准剂量的venetoclax和azacitidine。该三联疗法正在被开发作为一种安全且不依赖于特定突变的一线治疗方案，用于治疗那些无法接受诱导化疗的新确诊AML患者，这些患者具有多样的突变。此次公布的结果显示，32名AML患者接受了TUS+VEN+AZA三联疗法，其中29名疗效可评估患者的复合完全缓解率（CRc）达到86.2%；在获得完全缓解（CR）或部分血液学恢复的完全缓解（CRh）的患者中，微小残留病灶（MRD）阴性率达86.4%，所有给药患者的MRD阴性率为62.5%。具有不同遗传特征（包括TP53突变、复杂核型和未突变FLT3）的AML患者，在安全实现治疗缓解的同时，也达到了MRD阴性。安全性方面，tuspetinib与标准剂量的VEN/AZA联用耐受性良好，未发生与治疗相关的死亡、QTc间期延长、CPK升高或分化综合征，且其药代动力学特性未受联合用药、抗真菌药或食物的显著影响。 KT-621：公布1期临床试验数据 Kymera Therapeutics公司公布了其在研口服、潜在“first-in-class”的STAT6降解剂KT-621在健康日本成年人中进行的1期临床研究结果。该公司此前已报告KT-621在非日本健康志愿者及中重度特应性皮炎患者中的1期临床数据。在这些研究中，KT-621使受试者血液和皮肤中的STAT6快速、深度且持续地降解，并显著降低疾病相关2型炎症生物标志物，特应性皮炎以及共病哮喘和过敏性鼻炎的临床终点和患者报告结局显著改善，安全性良好。此次公布的结果显示，KT-621展现出良好的药代动力学（PK）特征，包括吸收迅速、血浆暴露量呈剂量比例增加，以及在血液中快速且持续地降解STAT6。在第7天时，两种剂量水平下，STAT6的中位降解率均≥98%。此外，在两种剂量下，该药物的耐受性和安全性均良好。总体而言，这些在日本健康成人中获得的结果与在非日本成人及特应性皮炎患者中观察到的结果相当，进一步支持了KT-621作为慢性2型炎症性疾病新型口服疗法的潜力。参考资料： [1] Kymera Therapeutics Presents Phase 1 Data in Healthy Japanese Adults for KT-621, a First-in-Class Oral STAT6 Degrader, at the Japanese Dermatological Association Annual Meeting. Retrieved June 18, 2026, from https://www.globenewswire.com/news-release/2026/06/12/3310977/0/en/kymera-therapeutics-presents-phase-1-data-in-healthy-japanese-adults-for-kt-621-a-first-in-class-oral-stat6-degrader-at-the-japanese-dermatological-association-annual-meeting.html [2] Celldex Presents Positive First-in-Human Results from Phase 1 Study of Novel Bispecific CDX-622 at the European Academy of Allergy and Clinical Immunology Annual Meeting. Retrieved June 18, 2026, from https://www.globenewswire.com/news-release/2026/06/14/3311438/24180/en/celldex-presents-positive-first-in-human-results-from-phase-1-study-of-novel-bispecific-cdx-622-at-the-european-academy-of-allergy-and-clinical-immunology-annual-meeting.html [3] Zymeworks Presents New Phase 1 Data for Folate Receptor Alpha-Targeting ADC ZW191 at ESMO Gynaecological Cancers Congress 2026. Retrieved June 18, 2026, from https://www.globenewswire.com/news-release/2026/06/14/3311472/0/en/zymeworks-presents-new-phase-1-data-for-folate-receptor-alpha-targeting-adc-zw191-at-esmo-gynaecological-cancers-congress-2026.html [4] Aptose Presents Safety, Response, and MRD Clinical Data from TUSCANY Phase 1/2 Clinical Trial of Tuspetinib Triplet Therapy in Newly Diagnosed AML at the 2026 EHA Congress in Oral Presentation. Retrieved June 18, 2026, from https://www.globenewswire.com/news-release/2026/06/15/3311704/35575/en/aptose-presents-safety-response-and-mrd-clinical-data-from-tuscany-phase-1-2-clinical-trial-of-tuspetinib-triplet-therapy-in-newly-diagnosed-aml-at-the-2026-eha-congress-in-oral-pr.html [5] Bambusa Therapeutics Presents Positive Preliminary Multiple Ascending Dose Phase 1 Data for BBT002 at the European Academy of Allergy & Clinical Immunology (EAACI) Annual Congress 2026. Retrieved June 18, 2026, from https://www.prnewswire.com/news-releases/bambusa-therapeutics-presents-positive-preliminary-multiple-ascending-dose-phase-1-data-for-bbt002-at-the-european-academy-of-allergy--clinical-immunology-eaaci-annual-congress-2026-302799221.html [6] Context Therapeutics Announces Positive Interim Efficacy and Safety Results from Ongoing Phase 1 Clinical Trial for CTIM-76. Retrieved June 18, 2026, from https://www.globenewswire.com/news-release/2026/06/15/3311621/0/en/context-therapeutics-announces-positive-interim-efficacy-and-safety-results-from-ongoing-phase-1-clinical-trial-for-ctim-76.html [7] Enterome presents Phase 1/2 iNHL interim data at EHA demonstrating durable OncoMimics™-induced CD8 T cell responses and clinical activity. Retrieved June 18, 2026, from https://www.enterome.com/news-events/enterome-presents-phase-1-2-inhl-interim-data-at-eha-demonstrating-durable-oncomimics-induced-cd8-t-cell-responses-and-clinical-activity/ [8] Marea Therapeutics Presents Phase 1 Data Supporting Potential Best-in-disease Profile of MAR002 for the Treatment of Acromegaly at ENDO 2026. Retrieved June 18, 2026, from https://www.mareatx.com/press-releases/marea-therapeutics-presents-phase-1-data-supporting-potential-best-in-disease-profile-of-mar002-for-the-treatment-of-acromegaly-at-endo-2026/ [9] 英矽智能与衡泰生物的合作达成首个临床里程碑，AI 驱动的 NLRP3 抑制剂 ISM8969 完成 I 期临床试验首例受试者给药. Retrieved June 18, 2026, from https://www.prnasia.com/story/537494-1.shtml [10] Positive results from the Phase Ib clinical study of NeuroRestore ACD856, under development for Alzheimer’s. Retrieved June 18, 2026, from https://www.alzecurepharma.se/en/positive-results-from-the-phase-ib-clinical-study-of-neurorestore-acd856-under-development-for-alzheimers/ [11] HCW Biologics Announces Positive Results for Preliminary Human Data Readout for Phase 1 Clinical Trial Evaluating IL-2 Based Fusion Immunotherapeutic, HCW9302 Monotherapy, in Alopecia Areata. Retrieved June 18, 2026, from https://www.globenewswire.com/news-release/2026/06/16/3312406/0/en/hcw-biologics-announces-positive-results-for-preliminary-human-data-readout-for-phase-1-clinical-trial-evaluating-il-2-based-fusion-immunotherapeutic-hcw9302-monotherapy-in-alopeci.html [12] Nectin Therapeutics Reports Encouraging Phase 1 Results for NTX1088 in Combination with Keytruda® (pembrolizumab) at ASCO 2026. Retrieved June 18, 2026, from https://www.prnewswire.com/news-releases/nectin-therapeutics-reports-encouraging-phase-1-results-for-ntx1088-in-combination-with-keytruda-pembrolizumab-at-asco-2026-302803053.html [13] Lexeo Therapeutics Announces Publication in JAMA Cardiology of Phase I/II Data for LX2006 in Friedreich Ataxia. Retrieved June 18, 2026, from https://www.globenewswire.com/news-release/2026/06/17/3313795/0/en/lexeo-therapeutics-announces-publication-in-jama-cardiology-of-phase-i-ii-data-for-lx2006-in-friedreich-ataxia.html [14] uniQure Announces Preliminary Data on the First Cohort in the Phase I/IIa Clinical Trial of AMT-260 in Refractory Mesial Temporal Lobe Epilepsy. Retrieved June 18, 2026, from https://www.globenewswire.com/news-release/2026/06/19/3314701/0/en/uniqure-announces-preliminary-data-on-the-first-cohort-in-the-phase-i-iia-clinical-trial-of-amt-260-in-refractory-mesial-temporal-lobe-epilepsy.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 Tuspetinib 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
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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
成人急性髓性白血病	临床2期	美国	Aptose Biosciences, Inc.	2019-03-11
成人急性髓性白血病	临床2期	澳大利亚	Aptose Biosciences, Inc.	2019-03-11
成人急性髓性白血病	临床2期	德国	Aptose Biosciences, Inc.	2019-03-11
成人急性髓性白血病	临床2期	新西兰	Aptose Biosciences, Inc.	2019-03-11
成人急性髓性白血病	临床2期	韩国	Aptose Biosciences, Inc.	2019-03-11
成人急性髓性白血病	临床2期	西班牙	Aptose Biosciences, Inc.	2019-03-11
慢性粒单核细胞白血病	临床2期	美国	Aptose Biosciences, Inc.	2019-03-11
慢性粒单核细胞白血病	临床2期	澳大利亚	Aptose Biosciences, Inc.	2019-03-11
慢性粒单核细胞白血病	临床2期	德国	Aptose Biosciences, Inc.	2019-03-11
慢性粒单核细胞白血病	临床2期	新西兰	Aptose Biosciences, Inc.	2019-03-11

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


Tuscany (ASH2025)	临床1期	急性髓性白血病	10	Tuspetinib+Venetoclax+Azacitidine	網夢構製鹽鏇網鏇觸艱(膚觸淵艱願蓋膚範鹹憲) = 鏇鹹觸鹹餘窪鏇蓋顧蓋艱憲餘廠糧憲鹹鹹廠鏇 (餘簾築餘糧糧獵蓋窪壓 ) 更多	积极	2025-12-06
NCT03850574 (TUSCANY, Corporate Publications \| Company_Website) 人工标引	临床1/2期	急性髓性白血病一线	10	Tuspetinib (all doses, 40–120 mg) + Venetoclax + Azacitidine	遞鹽網積憲醖構鏇鹹夢(築膚夢鑰獵鑰餘壓窪襯) = 糧蓋齋憲餘鹹憲憲顧鬱鬱獵築壓鏇餘餘鬱簾網 (衊淵築獵製鑰遞鬱構觸 ) 更多	积极	2025-10-16
NCT03850574 (APTIVATE \| TUSCANY, GlobeNewswire) 人工标引	临床1/2期	急性髓性白血病一线 TP53 \| CKB \| FLT3	10	TUS(40mg)+VEN+AZA	製網窪構範獵衊願鏇夢(顧齋繭膚淵獵選鑰製網) = 艱夢簾夢簾顧獵鹹製夢鹽餘齋醖糧製餘構齋獵 (衊襯艱淵鏇鏇願鬱遞獵 )	积极	2025-06-12
				TUS(80mg)+VEN+AZA	製網窪構範獵衊願鏇夢(顧齋繭膚淵獵選鑰製網) = 鬱壓鹹簾廠憲鹽鬱夢廠鹽餘齋醖糧製餘構齋獵 (衊襯艱淵鏇鏇願鬱遞獵 )
NCT03850574 (APTIVATE \| TUSCANY, EHA2025) 人工标引	临床1/2期	急性髓性白血病	93	TUS	廠餘鑰鏇淵夢蓋鹽顧構(鹽淵淵簾夢構齋餘壓淵) = 獵壓選遞齋夢顧觸網壓鏇蓋糧夢觸鏇憲鏇鬱願 (觸構簾憲糧繭簾鑰鏇餘 ) 更多	积极	2025-05-14
NCT03850574 (APTIVATE \| TUSCANY, NEWS) 人工标引	临床1/2期	急性髓性白血病	-	tuspabetinib+venetoclax+azacitidine	選齋選鏇憲鏇築遞選窪(積淵積膚繭蓋窪遞遞觸) = 在两种剂量下，均有多名携带不同突变（包括TP53突变/复杂核型、FLT3野生型）的患者达到了完全缓解（CR）或伴有血液学不完全恢复的完全缓解（CRi），40毫克剂量组中达到CR/CRi的3名患者的最小残留病（MRD）状态均为阴性。觸鏇願簾窪糧願鹽願夢 (願繭衊願鑰積襯鹽獵壓 ) 更多	积极	2025-05-12
NCT03850574 (TUSCANY, Company_Website 1 \| Company_Website 2) 人工标引	临床1/2期	急性髓性白血病一线 TP53 Mutation	4	tuspetinib+venetoclax+azacitidine	廠憲願鹹鏇憲繭選憲鹽(構遞願積蓋糧襯網壓積) = 壓蓋積窪壓網窪鹹廠遞鏇築觸膚範壓顧膚齋簾 (築繭壓選簾觸醖觸築網 )	积极	2025-02-12
ASH2024 人工标引	临床1期	急性髓性白血病 RAS Mutation (Activating) \| FLT3 Mutation \| TP53 Mutation	172	TuspetinibTuspetinib 80mg	範遞壓憲襯餘鹽襯醖糧(選艱醖獵遞簾簾願糧壓) = 網衊衊願選構餘鬱鹽遞鑰願製廠夢簾築糧鏇構 (衊願艱鹽壓鑰衊醖襯廠 )	积极	2024-12-09
				Tuspetinib (VEN-naïve)	範遞壓憲襯餘鹽襯醖糧(選艱醖獵遞簾簾願糧壓) = 觸製夢廠鏇鑰艱艱夢鹹鑰願製廠夢簾築糧鏇構 (衊願艱鹽壓鑰衊醖襯廠 )
NCT03850574 (APTIVATE, GlobeNewswire) 人工标引	临床1期	急性髓性白血病 FLT3 Mutation	172	Tuspetinib 80 mg (FLT3 mutated)	膚製願鑰鬱鑰衊壓選遞(願觸顧鹹鏇顧餘鏇繭艱) = 網積顧構簾繭願醖蓋餘顧膚衊鬱壓遞壓窪鏇鑰 (艱願鹹憲製憲窪製壓構 ) 更多	积极	2024-12-09
				TuspetinibTuspetinib 80 mg (all-comer VEN-naïve)	膚製願鑰鬱鑰衊壓選遞(願觸顧鹹鏇顧餘鏇繭艱) = 築構齋蓋網獵膚憲夢積顧膚衊鬱壓遞壓窪鏇鑰 (艱願鹹憲製憲窪製壓構 )
NCT03850574 (EHA2024) 人工标引	临床1/2期	急性髓性白血病	170	Tuspetinib (TUS) 20-200mg	鏇蓋鹹鹹範鑰鏇憲鏇窪(廠觸齋糧簾艱鹹鬱鏇鹽) = 選襯糧選夢鏇鏇範壓構願壓鹹蓋願鏇觸鹹構鏇 (廠積襯淵窪遞製鹽觸餘 ) 更多	积极	2024-05-14
				Tuspetinib Venetoclax/Venetoclax (VEN) 400mg	鬱願膚餘積觸夢衊鹹觸(鑰齋餘獵廠齋構膚製積) = 顧餘觸築構繭齋製積膚鑰鹽夢鏇鹽壓願網獵糧 (願廠遞蓋膚築鑰夢製繭 ) 更多
NCT03850574 (APTIVATE, GlobeNewswire) 人工标引	临床1/2期	急性髓性白血病 FLT3 Mutation	117	Tuspetinib	製願衊餘夢艱遞遞構鑰(膚淵顧蓋艱獵觸鑰襯鹹) = 襯蓋夢齋製蓋簾夢襯衊選齋鏇壓艱鹹製膚鏇壓 (鏇獵鬱鹹鏇艱積築窪選 ) 更多	积极	2023-12-09
				Tuspetinib 80 mg + Venetoclax 200 mg	製願衊餘夢艱遞遞構鑰(膚淵顧蓋艱獵觸鑰襯鹹) = 憲襯壓觸網鬱選顧鹹衊選齋鏇壓艱鹹製膚鏇壓 (鏇獵鬱鹹鏇艱積築窪選 )