A Proof of Concept, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Effects of Tradipitant on Nausea and Vomiting After GLP-1R Agonist Administration in Healthy Overweight Class I or Class II Obese Volunteers

The goal of this study is to measure the effects of using Tradipitant after GLP-1R agonist use on nausea and vomiting in healthy overweight, class I, or class II obese volunteers. The study is placebo-controlled with two treatment arms.

开始日期2025-02-25

申办/合作机构

Vanda Pharmaceuticals, Inc.

NCT06836557

/ Recruiting临床3期

A Multicenter, Open Label, 3-Month Safety Study with Tradipitant in Patients with Idiopathic or Diabetic Gastroparesis

This is a multicenter, open label, 3-month safety study with tradipitant in patients with idiopathic and diabetic gastroparesis.

开始日期2024-01-09

申办/合作机构

Vanda Pharmaceuticals, Inc.

CTIS2023-503802-35-00

/ Recruiting临床3期

A MULTICENTER OPEN LABEL 3 MONTH SAFETY STUDY WITH TRADIPITANT IN PATIENTS WITH IDIOPATHIC OR DIABETIC GASTROPARESIS

开始日期2023-11-29

申办/合作机构

Vanda Pharmaceuticals, Inc.

100 项与曲地匹坦相关的临床结果

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100 项与曲地匹坦相关的转化医学

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100 项与曲地匹坦相关的专利（医药）

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项与曲地匹坦相关的文献（医药）

2024-12-01·Clinical gastroenterology and hepatology : the official clinical practice journal of the American Gastroenterological Association

The Efficacy of Tradipitant in Patients With Diabetic and Idiopathic Gastroparesis in a Phase 3 Randomized Placebo-Controlled Clinical Trial

Article

作者: Caleigh Kupersmith ; Darby Madonick ; Michael Camilleri ; Paula Moszczynski ; Mihael H. Polymeropoulos ; Changfu Xiao ; Anthony Lembo ; Michaela Fisher ; Jesse L. Carlin ; Sandra Smieszek ; Christos Polymeropoulos ; Gunther Birznieks

BACKGROUND:

Neurokinin receptor 1 antagonists are effective in reducing nausea and vomiting in chemotherapy-induced emesis. We investigated the safety and efficacy of tradipitant, a neurokinin receptor 1 antagonist, in patients with idiopathic and diabetic gastroparesis.

METHODS:

A total of 201 adults with gastroparesis were randomly assigned to oral tradipitant 85 mg (n = 102) or placebo (n = 99) twice daily for 12 weeks. Symptoms were assessed by a daily symptom dairy, Gastroparesis Cardinal Symptom Index scores, and other patient-reported questionnaires. Blood levels were monitored for an exposure-response analysis. The primary outcome was change from baseline to week 12 in average nausea severity, measured by daily symptom diary.

RESULTS:

The intention-to-treat (ITT) population did not meet the prespecified primary endpoint at week 12 (difference in nausea severity change drug vs placebo; P = .741) or prespecified secondary endpoints. Post hoc analyses were performed to control for drug exposure, rescue medications, and baseline severity inflation. Subjects with high blood levels of tradipitant significantly improved average nausea severity beginning at early time points (weeks 2-4). In post hoc sensitivity analyses, tradipitant treatment demonstrated strengthened effects, with statistically significant improvements in nausea at week 12.

CONCLUSIONS:

Although tradipitant did not reach significance in the ITT population, a pharmacokinetic exposure-response analysis demonstrated significant effects with adequate tradipitant exposure. When accounting for confounding factors such as baseline severity inflation and rescue medication, a statistically significant effect was also observed. These findings suggest that tradipitant has potential as a treatment for the symptom of nausea in gastroparesis. (ClincialTrials.gov, Number: NCT04028492).

2024-07-11·JOURNAL OF MEDICINAL CHEMISTRY

Occurrence of “Natural Selection” in Successful Small Molecule Drug Discovery

Article

作者: Zdrazil, Barbara ; Waldmann, Herbert ; Leeson, Paul D. ; Heinzke, A. Lina ; Pahl, Axel ; Leach, Andrew R. ; Young, Robert J.

Published compounds from ChEMBL version 32 are used to seek evidence for the occurrence of "natural selection" in drug discovery. Three measures of natural product (NP) character were applied, to compare time- and target-matched compounds reaching the clinic (clinical compounds in phase 1-3 development and approved drugs) with background compounds (reference compounds). Pseudo-NPs (PNPs), containing NP fragments combined in ways inaccessible by nature, are increasing over time, reaching 67% of clinical compounds first disclosed since 2010. PNPs are 54% more likely to be found in post-2008 clinical versus reference compounds. The majority of target classes show increased clinical compound NP character versus their reference compounds. Only 176 NP fragments appear in >1000 clinical compounds published since 2008, yet these make up on average 63% of the clinical compound's core scaffolds. There is untapped potential awaiting exploitation, by applying nature's building blocks─"natural intelligence"─to drug design.

2024-04-09·NEUROLOGY

Tradipitant Effective in the Reduction of Vomiting Associated with Motion Sickness Across Varied Sea Conditions (S3.003)

Article

作者: Birznieks, Gunther ; Kiely, Leah ; Polymeropoulos, Christos ; Goldberg, Abigail ; Xiao, Changfu ; Polymeropoulos, Mihael ; Bushman, Margaret ; Mourad, Raina ; Polymeropoulos, Vasilios ; Miller, Cameron ; Sutherland, Elizabeth ; Pham, Nikolas ; Morgan, Dane ; Davis, Tanner

OBJECTIVE:

The Motion Syros study was a multicenter, randomized, double-blind placebo-controlled study to evaluate the efficacy and safety of tradipitant for motion sickness.

BACKGROUND:

Motion sickness is a common disorder affecting approximately 30% of travelers under usual circumstances. The sensory mismatch theory postulates that motion sickness is induced by a discordance between the visual, vestibular, and kinesthetic systems, leading to a constellation of symptoms including nausea and vomiting. Substance P activates NK1 receptors in the nucleus tractus solitarius inducing a cascade of symptoms. Tradipitant is a novel NK1 receptor antagonist being studied for the treatment of nausea and vomiting associated with motion sickness.

DESIGN/METHODS:

The Motion Syros study was a multicenter, randomized, double-blind, placebo-controlled study where 365 participants embarked on boat trips under varied sea conditions and received tradipitant 170 mg, tradipitant 85 mg, or placebo. Participants evaluated their symptoms at thirty-minute intervals during the expedition.

RESULTS:

Participants on tradipitant 170 mg or 85 mg had a significantly lower incidence of vomiting as compared to those on placebo across all boat trips (tradipitant 170 mg = 18.3%, tradipitant 85mg = 19.5%, placebo = 44.3%, p < .0001 for both dose comparisons against placebo, n = 365). A range of wave heights was represented across the various boat trips, eliciting variable degrees of severity of motion sickness and differing responses to tradipitant.

CONCLUSIONS:

Tradipitant has been confirmed to be effective in the reduction of vomiting associated with motion sickness across varied sea conditions with a range of wave heights. Motion sickness remains a significant unmet medical need, given existing treatments' limitations in alleviating symptoms and their frequent adverse effects. Disclosure: Dr. Polymeropoulos has received personal compensation for serving as an employee of Vanda Pharmaceuticals. An immediate family member of Dr. Polymeropoulos has received personal compensation in the range of $0-$499 for serving as an officer or member of the Board of Directors for Vanda. Dr. Polymeropoulos has stock in Vanda. Miss Bushman has received personal compensation for serving as an employee of Vanda Pharmaceuticals. Miss Bushman has stock in Vanda Pharmaceuticals. Mr. Morgan has stock in Vanda Pharmaceuticals. Ms. Sutherland has received personal compensation for serving as an employee of Vanda Pharmaceuticals. Ms. Sutherland has stock in Vanda Pharmaceuticals. Mr. Davis has received personal compensation for serving as an employee of Vanda Pharmaceuticals, Inc.. Mr. Davis has stock in Vanda Pharmaceuticals, Inc.. Mr. Pham has received personal compensation for serving as an employee of Vanda Pharmaceuticals. Mr. Pham has stock in Vanda Pharmaceuticals. Miss Kiely has received personal compensation for serving as an employee of Vanda Pharmaceuticals Inc.. Miss Kiely has stock in Vanda Pharmaceuticals Inc.. Ms. Goldberg has received personal compensation for serving as an employee of Vanda Pharmaceuticals Inc. Ms. Goldberg has stock in Vanda Pharmaceuticals Inc. Miss Mourad has received personal compensation for serving as an employee of Vanda Pharmaceuticals Inc.. Miss Mourad has stock in Vanda Pharmaceuticals Inc.. Miss Miller has received personal compensation for serving as an employee of Vanda Pharmaceuticals . Miss Miller has stock in Vanda Pharmaceuticals. Dr. Xiao has received personal compensation for serving as an employee of Vanda pharma. Dr. Xiao has stock in Vanda pharma. Dr. Polymeropoulos has received personal compensation for serving as an employee of Vanda Pharmaceuticals Inc. An immediate family member of Dr. Polymeropoulos has received personal compensation in the range of $0-$499 for serving as an officer or member of the Board of Directors for Vanda Pharmaceuticals Inc. Dr. Polymeropoulos has stock in Vanda Pharmaceuticals Inc. Mr. Birznieks has received personal compensation for serving as an employee of Vanda Pharmaceuticals. Dr. Polymeropoulos has received personal compensation for serving as an employee of Vanda Pharmaceuticals. Dr. Polymeropoulos has received personal compensation in the range of $0-$499 for serving as an officer or member of the Board of Directors for Vanda Pharmaceuticals .

102

项与曲地匹坦相关的新闻（医药）

2026-01-04

·药时空

两款新药年末获批 FDA 收官给药企送 "大礼"

摘要：2025 年末，美国 FDA 接连批准两款重要新药：12 月 23 日核准 Agios 制药的口服药物 Aqvesme 用于治疗成人α或β地中海贫血相关贫血，12 月 30 日又为 Vanda 制药的晕车药 Nereus 亮绿灯。这两项审批均历经波折，却为特定患者群体带来新希望，也成为 FDA 年度监管工作的收官亮点。地中海贫血治疗突破：Aqvesme 减轻患者输血负担 Agios 制药的 Aqvesme（活性成分 mitapivat）获批之路并不顺畅。FDA 最初将审批日期从 9 月 7 日推迟至 12 月 7 日，需额外时间审查其风险评估与缓解策略（REMS），以应对潜在肝损伤风险。12 月初，因需完善 REMS 计划的标签文件，审批再次延后。这是 mitapivat 获得的第二项 FDA 批准。四年多前，该药物以 Pyrukynd 为商品名获批，用于治疗罕见遗传病丙酮酸激酶缺乏症引发的溶血性贫血。此次获批使适用人群大幅扩大，涵盖输血依赖型和非输血依赖型α或β地中海贫血成人患者。 Agios 首席执行官布莱恩・戈夫在圣诞夜电话会议中表示，Aqvesme 让患者摆脱了输血或皮下注射治疗的负担，也是首个能改善非输血依赖型患者生活质量的药物。该药将于 1 月底 REMS 计划实施后上市，年供应价 42.5 万美元，高于 Pyrukynd 的 33.5 万美元批发采购价。值得注意的是，Aqvesme 标签包含肝细胞损伤的黑框警告，患者用药前需接受肝功能检测，用药后 24 周内每四周检测一次。Agios 称，单独设立商品名可使 Aqvesme 的 REMS 计划仅适用于地中海贫血患者，避免与 Pyrukynd 的监管要求混淆。2025 年前三季度，Pyrukynd 销售额达 3400 万美元，三季度用药患者 149 人。四十载新突破：Nereus 成晕车治疗新选择 Vanda 制药的 Nereus（活性成分 tradipitant）则结束了晕车治疗四十余年无新药理疗法的局面。这款口服神经激肽-1（NK-1）受体拮抗剂的获批，距其因胃轻瘫适应症被 FDA 拒绝仅过去 15 个月。此前的完整回应函曾引发 Vanda 强烈不满，该公司抨击 FDA 延迟决策且未召开咨询委员会会议讨论药物价值。此次转机源于 12 月 4 日 FDA 解除部分临床暂停，认定晕车并非慢性疾病，Nereus 属于 "急性、事件驱动型疗法"，无需进行六个月的毒性研究。三项 III期临床试验为获批提供了有力支持，其中两项在船上开展。在一项 365 人参与的船载研究中，服用 Nereus 的患者呕吐发生率为 19%，而安慰剂组达 44%，该药对有晕车史患者的恶心症状也有改善作用。 Nereus将于未来数月上市，成为 Vanda 旗下第四款获批药物。该公司现有精神分裂症治疗药物 Fanapt（2024 年扩展用于双相 I 型障碍）、睡眠障碍药物 Hetlioz 和复发型多发性硬化症治疗药物 Ponvory。2025 年前三季度，Fanapt 销售额达 8400 万美元，同比增长 24%。 Vanda 并未放弃 tradipitant 的胃轻瘫适应症申请，同时正研究其用于预防 GLP-1 类减肥药引发的恶心呕吐。此外，FDA 将于1月7日决定是否批准 Hetlioz 用于时差反应障碍治疗。参考来源：https://www.fiercepharma.com/pharma/vandas-motion-sickness-drug-and-agios-thalassemia-treatment-make-grade-fda 识别微信二维码，可添加药时空小编请注明：姓名+研究方向！

2026-01-02

·化学经纬

2025年度FDA 获批新药汇总

点击上方蓝字关注我们早研早知道 2025年即将迎来尾声，截止当前，已有 44 款新药于2025年获得 FDA 批准上市，更有两款待批。近日，Chris De Savi 对此做了海报汇总。从药物形态来看，小分子获得大丰收！有超四分之三新药（32/46，包括两款待批）为小分子药物，这有赖于激酶抑制剂（13 款），尤其是对突变体抑制剂的开发做出的贡献。此外，11 款抗体药物、3 款核苷酸药物。而多肽类药物仅 1 款，没有环肽，有些低于预期，期待不久有新的突破。 EARLY R&D TALKING 小分子获批新药 01 1.1 药物名称：Grafapex 有效活性成分：Treosulfan 由利奥制药首研，由美迪斯制药申请上市；在免疫抑制和肿瘤治疗领域，与氟达拉滨联合使用，作为治疗急性髓系白血病和骨髓增生异常综合征的异基因造血干细胞移植的预备方案；一种粉末制剂，用于静脉注射。作用机制：一种DNA烷基化试剂 1.2 药物名称：JOURNAVX有效活性成分：Suzetrigine 由美国福泰制药公司开发和商业化；神经系统和骨骼肌系统治疗领域，一种用于治疗中度至重度急性疼痛的口服片剂；靶点：电压门控钠离子通道亚基α Nav1.8 1.3 药物名称：Gomekli 有效活性成分：Mirdametinib 由SpringWorks治疗公司研发和商业化；在肿瘤治疗领域，用于治疗有症状的丛状神经纤维瘤不能完全切除的1型神经纤维瘤病；口服胶囊；靶点：MAPK/ERK激酶1/2 1.4 药物名称：Romvimza 有效活性成分：vimseltinib 由Deciphera制药研发和申请上市；在肿瘤治疗领域，用于治疗有症状的腱鞘巨细胞瘤，手术切除可能导致功能限制恶化或严重并发症；一种口服胶囊制剂。作用机制：一种集落刺激因子1抑制剂 1.5 药物名称：Blujepa 有效活性成分：Gepotidacin 由葛兰素史克首研与申请上市；在泌尿生殖与感染系统治疗领域，用于治疗无并发症的尿路感染；一种口服速释制剂；作用机制：DNA 拓扑异构酶II/IV 抑制剂 1.6 药物名称：Vanrafia 有效活性成分：Atrasentan 由雅培制药首研，并由诺华商业化开发；在泌尿生殖系统治疗领域，用于降低成人原发性免疫球蛋白A肾病疾病快速进展风险的蛋白尿；一种口服片剂；作用机制：内皮素A型受体拮抗剂 1.7 药物名称：Avmapki Fakzynja Co-Pack 有效活性成分：Avutometinib/Defactinib 由 Verastem首研和商业化开发；在肿瘤治疗领域，用于治疗 KRAS 突变的复发性低级别浆液性卵巢癌（LGSOC）；联合用药的口服制剂；作用机制：靶向 RAF/MEK/FAK 的抑制剂 1.8 药物名称：Tryptyr 有效活性成分：Acoltremon 由 Avizorex 制药首研，并由 Alcon实验室公司商业化开发；在眼科治疗领域，用于治疗干眼症的症状和体征；一种滴眼液；作用机制：TRPM8 钙离子通道激活剂 1.9 药物名称：Ibtrozi 有效活性成分：Taletrectinib 由第一三共首研，并由 Nuvation 生物商业化开发；在肿瘤治疗领域，用于治疗局部晚期或转移性ROS1阳性非小细胞肺癌；一种口服制剂；作用机制：ROS1/泛-TRK抑制剂 1.10 药物名称：Zegfrovy 有效活性成分：Sunvozertinib 由江苏迪哲医药股份有限公司首研和商业化开发；在肿瘤肿瘤领域，用于治疗经FDA批准的试验检测到表皮生长因子受体外显子20插入突变的局部晚期或转移性非小细胞肺癌，在铂基化疗期间或之后疾病进展；口服片剂；作用机制：EGFR外显子20插入突变抑制剂 1.11 药物名称：Ekterly 有效活性成分：Sebetralstat 由 KalVista制药首研和商业化开发；在皮肤病治疗领域，用于治疗遗传学血管水肿的急性发作；一种口服片剂；作用机制：血管舒缓素B1 抑制剂 1.12 药物名称：Anzupgo 有效活性成分：Delgocitinib 由日本烟草公司首研，并由Leo制药商业化开发；在免疫调节皮肤病治疗领域，用于当局部皮质类固醇不可取或产生不充分的反应时，治疗中度至重度慢性手部湿疹；一种局部涂抹的溶液剂；作用机制：泛-JAK 酪氨酸激酶抑制剂 1.13 药物名称：Sephience 有效活性成分：Sepiapterin 由 PTC 治疗公司首研和商业化开发；在内分泌与代谢治疗领域，用于结合苯丙氨酸限制饮食，治疗头孢氨喋呤反应性苯丙酮尿患者的高苯丙氨酸血症；一种口服粉末制剂；作用机制：苯丙氨酸羟化酶激活剂 1.14 药物名称：Vizz 有效活性成分：Aceclidine 由 Lenz 治疗公司首研和商业化；在眼科治疗领域，用于治疗老花眼；一种眼科用液体制剂；作用机制：胆碱能受体激动剂 1.15 药物名称：Modeyso 有效活性成分：Dordaviprone 由 Oncoceutics 公司首研，并由 Chimerix 制药公司商业化开发；在肿瘤治疗领域，用于治疗弥漫性中线胶质瘤，携带H3 K27M突变，在既往治疗后病情进展；一种口服胶囊制剂；作用机制：多巴胺D2 受体拮抗剂；酪蛋白溶解线粒体基质肽酶蛋白水解亚基激活剂。 1.16 药物名称：Hernexeos 有效活性成分：Zongertinib 由勃林格殷格翰首研和商业化开发；在肿瘤治疗领域，用于治疗不可切除或转移的非鳞状非小细胞肺癌，其肿瘤有HER2酪氨酸激酶结构域激活突变，经FDA批准的试验检测，并且先前接受过全身治疗；一种口服片剂；作用机制：HER2 激酶抑制剂 1.17 药物名称：Brinsupri 有效活性成分：Brensocatib 由阿斯利康首研，并由阿斯利康和 Insmed公司共同商业化开发；在呼吸系统感染治疗领域，用于治疗非囊性纤维化支气管扩张症；一种口服片剂；作用机制：二肽基肽酶（DPP1）抑制剂 1.18 药物名称：Wayrilz 有效活性成分：Rilzabrutinib 由 Principia 生物制药首研，并由 Sanofi 商业化开发；在血液系统治疗领域，用于治疗对免疫球蛋白、抗d治疗或皮质类固醇反应不充分的持续性或慢性免疫性血小板减少症；一种口服片剂；作用机制：酪氨酸激酶（BTK）抑制剂 1.19 药物名称：Forzinity 有效活性成分：Elamipretide 由 Stealth 生物治疗公司首研和开发；在心血管与内分泌代谢治疗领域，用于改善体重至少30公斤的Barth综合征患者的肌肉力量；一种皮下注射肽类制剂；作用机制：线粒体卡罗酯结合 1.20 药物名称：Inluriyo 有效活性成分：Imlunestrant 由礼来制药首研和商业化开发；在肿瘤和泌尿治疗系统，用于治疗雌激素受体阳性，人表皮生长因子受体2阴性，雌激素受体1突变的晚期或转移性乳腺癌，在至少一种内分泌治疗后疾病进展；口服片剂；作用机制：一种雌激素受体（ER）拮抗剂降解剂 1.21 药物名称：Palsonify 有效活性成分：Paltusotine 由 Crinetics 制药公司首研和商业化开发；在肿瘤和内分泌代谢系统治疗领域，用于治疗肢端肥大症的成人谁有不充分的反应，手术和/或谁是不适合的选择；一种口服片剂；作用机制：生长抑素2受体激动剂 1.22 药物名称：Rhapsido 有效活性成分：Remibrutinib 由诺华首研与商业化开发；在皮肤病免疫调节治疗领域，用于治疗成人慢性自发性荨麻疹，尽管H1抗组胺治疗仍有症状；一种口服片剂；作用机制：BTK抑制剂 1.23 药物名称：Jascayd 有效活性成分：Nerandomilast 由勃林格殷格翰首研和商业化开发；在免疫调节呼吸道系统治疗领域，用于治疗特发性肺纤维化；一种口服片剂；作用机制：磷酸二酯酶4B（PDE4）抑制剂 1.24 药物名称：Lynkuet 有效活性成分：Elinzanetant 由葛兰素史克首研，并由拜耳商业化开发；在内分泌与代谢和心血管系统治疗领域，用于治疗更年期引起的中重度血管舒缩症状；一种口服凝胶制剂；作用机制：神经肽（NK）-1/3 受体拮抗剂 1.25 药物名称：Komzifti 有效活性成分：Ziftomenib 由密西根大学首研，并由 KuRa肿瘤公司进一步商业化开发；在内分泌与代谢和肿瘤治疗领域，用于治疗成人复发或难治性急性髓性白血病伴核磷蛋白1易感突变，且没有令人满意的替代治疗方案；一种口服胶囊；作用机制：menin 抑制剂，可阻断menin和赖氨酸[K]特异性甲基转移酶2A（KMT2A）的相互作用。 1.26 药物名称：Hyrnuo 有效活性成分：Sevabertinib 由拜耳首研和商业化开发；在肿瘤治疗领域，用于治疗局部晚期或转移性非鳞状非小细胞肺癌，肿瘤具有活化HER2酪氨酸激酶结构域激活突变的患者接受全身治疗；口服片剂；作用机制：HER2/EGFR 抑制剂 1.27 药物名称：Nuzolvence 有效活性成分：Zoliflodacin 由阿斯利康首研开发，随后继续由 Entasis 继续开发优化，最终由 Innoviva 专科治疗公司与全球抗生素研究与开发伙伴关系（GARDP）之间公私合作开发；在抗菌感染治疗领域，用于治疗由淋病奈瑟菌引起的无并发症泌尿生殖道淋病；一种口服抗生素；作用机制：细菌II 型拓扑异构酶抑制剂 1.28 药物名称：Cardamyst 有效活性成分：Etripamil 由 Milestone 制药首研和商业化开发；在心血管系统治疗领域，用于治疗阵发性室熵性心动过速发作；一种鼻腔系统喷雾剂；作用机制：钙离子通道阻断剂 1.29 药物名称：Myqorzo 有效活性成分：Aficamten 由 Cytokinetics 制药首研和商业化开发；在心血管系统治疗领域，用于治疗有症状的阻塞性肥厚性心肌病；一种口服胶囊；作用机制：肌球蛋白抑制剂 1.30 药物名称：Kygevvi 有效活性成分：Doxecitine/Doxribtimine 由哥伦比亚大学首研，并由 UCB 商业化开发；在内分泌与代谢和肌肉骨骼系统治疗领域，用于治疗 12 岁或以下开始出现症状的胸苷激酶2缺乏症患者；一种合成核苷，联合用药，口服溶液剂粉末；作用机制：脱氧核苷疗法两款待批小分子药物（不知道为什么？） 1.31 药物名称：Relacorilant 有效活性成分：Relacorilant 由 Corcept 制药首研；在内分泌与代谢治疗领域，用于治疗库氏综合征；口服胶囊；作用机制：糖皮质激素受体拮抗剂 1.32 药物名称：Tradipitant 有效活性成分：Tradipitant 由礼来首研；用于治疗晕动病；作用机制：NK1拮抗剂 EARLY R&D TALKING 获批抗体药物 02 2.1 药物名称：Datroway 有效活性成分：Datopotamab deruxtecan 由第一三共制药首研，并由阿斯利康和第一三共制药联合开发并商业化；在肿瘤治疗领域，用于治疗不可切除或转移性，HR-阳性、HER2阴性的乳腺癌，既往接受过基于内分泌的治疗和化疗的不可切除或转移性疾病。一种用于静脉注射的抗体偶联药物（ADC）。作用机制：DNA 拓扑异构酶I和细胞表面糖蛋白Trop-2 抑制剂剂， 2.2 药物名称：penpulimab-kcqx 有效活性成分：penpulimab-kcqx（派安普利单抗）由中山康方生物制药公司首研，并由Akeso生物制药申请美国上市；在肿瘤治疗领域，用于与顺铂或卡铂和吉西他滨联合治疗复发或转移性非角化性鼻咽癌（NPC）的成人患者，或在铂基化疗和至少一种其他先前治疗线上或之后单独使用；一种单克隆抗体静脉注射剂；作用机制：程序性死亡受体-1（PD-1）阻断抗体 2.3 药物名称：Imaavy 有效活性成分：Nipocalimab 由Momenta制药公司首研，并由强生旗下杨森生物科技商业化开发；在免疫调节治疗领域，用于治疗广泛性重症肌无力；一种静脉注射单克隆抗体；作用机制：靶向 Fc γ受体和转运体的 IgG 单克隆受体。 2.4 药物名称：Emrelis 有效活性成分：Telisotuzumab vedotin 由艾伯维首研和商业化；在肿瘤治疗领域，用于治疗在先前接受系统性治疗后仍处于局部晚期或转移状态、且存在高 c-Met 蛋白表达的非鳞状非小细胞肺癌（NSCLC）患者；用于静脉注射的单克隆抗体偶联物（ADC）；作用机制：c-Met 定向抗体和微管抑制剂偶联物。 2.5 药物名称：Enflonsia 有效活性成分：Clesrovimab 由默沙东首研和商业化开发；在感染治疗领域，用于预防呼吸道合胞病毒（RSV）下呼吸道疾病的新生儿和出生在或进入其第一个RSV季节的婴儿；一种肌肉注射单克隆抗体；作用机制：呼吸道合胞病毒F单克隆抗体 2.6 药物名称：Andembry 有效活性成分：Garadacimab 由 CSL公司首研和商业化开发；在皮肤病治疗领域，用于防止遗传性血管性水肿的发作；一种皮下注射单克隆抗体；作用机制：凝血因子XIIa催化结合区域结合单克隆抗体 2.7 药物名称：Lynozyfic 有效活性成分：Linvoseltamab 由再生元首研，并由 Regeneron 商业化开发；在肿瘤治疗领域，用于治疗复发或难治性多发性骨髓瘤，治疗前至少接受过四种治疗，包括蛋白酶体抑制剂、免疫调节剂和抗CD38单克隆抗体；一种静脉注射双特异性抗体；作用机制：CD3、BCMA 双特异性抗体 2.8 药物名称：Keytruda Qlex 有效活性成分：pembrolizumab and berahyaluronidase alfa-pmph 由默沙东首研和商业化开发；在肿瘤治疗领域，用于静脉注射派姆单抗的成人和儿童（12岁及以上）实体瘤适应症的治疗；作用机制：PD-1 抑制剂 2.9 药物名称：Voyxact 有效活性成分：Sibeprenlimab 由Visterra 公司首研，并由Otsuka 制药商业化开发；在免疫调节和泌尿生殖系统治疗领域，用于降低原发性免疫球蛋白A 肾病中有疾病进展危险的成人的蛋白尿；皮下注射剂；作用机制：靶向B细胞成熟抗原的IgG2单克隆抗体 2.10 药物名称：Lerochol 有效活性成分：Lerodalcibep-liga 由 Adnexus治疗公司首研，并由 Lib 治疗公司商业化开发；在内分泌与代谢和心血管系统治疗领域，用于降低成人高胆固醇血症患者的低密度脂蛋白胆固醇，包括杂合子家族性高胆固醇血症，作为饮食和运动的辅助；一种皮下注射融合蛋白；作用机制：PCSK9 抑制剂 2.11 药物名称：Exdensur 有效活性成分：Depemokimab-ulaa 由葛兰素史克首研与商业化开发；在呼吸系统治疗领域，用于治疗以嗜酸性粒细胞表型为特征的严重哮喘，作为一种附加的维持治疗；一种皮下注射剂；作用机制：IL-5 拮抗单克隆抗体 EARLY R&D TALKING 获批核苷酸药物 03 3.1 药物名称：Qfitlia 有效活性成分：Fitusiran 由美国奥尼兰姆首研，并由Genzyme公司申请上市商业化；在血液系统治疗领域，用于预防或减少血友病A或B出血发作的频率；该药物主要活性成分 Fitusiran，是一种抗凝血酶定向的双链小干扰核苷酸（siRNA），它与含有三天线乙酰半乳糖胺（GaINAc）片段的配体共价连接，如上图。一种皮下注射剂；作用机制：抗凝血酶导向的 siRNA 3.2 药物名称：Dawnzera 有效活性成分：Donidalorsen 由Ionis制药公司首研和商业化开发；在皮肤病感染治疗领域，用于防止遗传性血管性水肿的发作；一种皮下注射剂；作用机制：靶向血管舒缓素B1的反寡义核苷酸 3.3 药物名称：Redemplo 有效活性成分：Plozasiran 由美国箭头公司首研与商业化开发；在内分泌与代谢治疗领域，用于降低家族性乳糜微粒血症综合征成人的甘油三酯；一致皮下注射剂；作用机制：载脂蛋白C3靶向的小干扰RNA（siRNA）疗法。 EARLY R&D TALKING 总结与展望 02 整体来看，这是小分子药物“雄起”的一年。其中，在肿瘤-血液-实体瘤领域有 16 款小分子药物；在疼痛-神经-眼科治疗领域 3 款小分子药物；免疫-皮肤病领域 3 款小分子药物；心血管-代谢-罕见病领域有 7 款小分子药物；也有 2 款抗感染类小分子药物；在抗体生物制剂方面总共 11 款药物，以及 3 款核苷酸类药物。整体来看，激酶抑制剂类继续领跑，共 13 款药物；新药高度集中在肿瘤、免疫、代谢三大领域。而罕见病、遗传病适应症成为差异化突破口。期待环肽药物厚积薄发！图片来源：Linkedin，by Chris De Savi 参考资源： 1.https://www.fda.gov/drugs/novel-drug-approvals-fda/novel-drug-approvals-2025 2.摩熵医药数据库（原药融云）检索

上市批准寡核苷酸免疫疗法

2026-01-02

·BioSpace

Vanda Ends 40-Year Motion Sickness Drug Drought with FDA Approval for Nereus

Gargonia/ iStock Jefferies analysts envision a steady launch curve that could ultimately drive meaningful sales from people who are dissatisfied with existing treatments. The FDA has approved Vanda Pharmaceuticals’ tradipitant for the prevention of vomiting induced by motion. The company filed for FDA approval after linking the oral neurokinin-1 receptor antagonist, which Vanda will sell as Nereus, to significant reductions in vomiting in two Phase III real-world provocation studies conducted on boats. In one trial, vomiting incidence was 18.3% to 19.5% with Nereus versus 44.3% with placebo. Vomiting rates were 10.4% to 18.3% with Nereus versus 37.7% on placebo in the second study. Vanda said the approval marks the first time in over 40 years that a new pharmacologic treatment for motion sickness has come to market. Nereus will compete with dramamine, an over-the-counter antihistamine drug that prevents and treats motion sickness symptoms including nausea, vomiting and dizziness. Jefferies analysts identified a detail of the approval that could differentiate Nereus. “Encouragingly, Nereus’ label is for the prevention of vomiting caused by motion, rather than the symptoms of motion sickness (e.g. nausea, vomiting, and dizziness) like dramamine,” the analysts said in a note to investors. The label permits patients to take Nereus around 60 minutes before an event expected to cause vomiting induced by motion. Patients need to take the medicine on an empty stomach, meaning at least one hour before or two hours after a full meal, but otherwise analysts said the “front page label looks clean/simple.” Vanda’s assessment of the market opportunity for Nereus includes two to three million U.S. patients who take dramamine every month, the analysts said. The lack of innovation in the motion sickness drug field means there may be some pent-up demand for Nereus. “We envision a steady launch curve as awareness builds over time, with some contribution from patients who have been waiting for an alternative to existing therapies,” the analysts said. “A modest penetration among dissatisfied users or patients who currently avoid travel (due to inadequate symptom control) could drive meaningful sales in theory.” Vanda is yet to share the list price for Nereus, but Jefferies analysts expect a premium over existing OTC treatments. The company hopes to be well prepared for launch ahead of the 2026 summer season, the analysts said, and plans to focus on digital advertising and direct-to-consumer outreach rather than building a large prescriber‑focused sales force. The analysts’ overview of the launch plan aligns with comments by Vanda CEO Mihael Polymeropoulos. On an earnings call in October 2025, Polymeropoulos described the strategy for both Nereus and jet lag drug Hetlioz. “We’re developing a quite elaborate strategy that will become very consumer-centric, focusing on concierge service for supplying the drug to both of them,” Polymeropoulos said. “Our recent experiences with direct-to-consumer campaigns, but also the elevation of brand awareness of the company, are going to be very important and have been strategically designed to be in place in advance of those launches.” The FDA could rule on Hetlioz in jet lag by Jan. 7. The back-to-back regulatory actions follow the creation of a collaborative framework to resolve disputes between the FDA and Vanda, which sued the agency in April amid rejections, a partial hold and other setbacks. The FDA lifted the partial hold on tradipitant last month. Vanda’s approval was one of a clutch of authorizations over the holiday period. The FDA also approved Agios Pharmaceuticals’ Aqvesme for the treatment of anemia in adults with alpha- or beta-thalassemia, and expanded the labels of Roche’s cancer drug Lunsumio and Boehringer Ingelheim’s pulmonary fibrosis medicine Jascayd .

临床3期上市批准临床结果

100 项与曲地匹坦相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11728	曲地匹坦	-	DB12580

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
晕动病	美国	Vanda Pharmaceuticals, Inc.	2025-12-30

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
胃轻瘫	申请上市	美国	Vanda Pharmaceuticals, Inc.	2023-12-04
新型冠状病毒感染	临床3期	美国	Vanda Pharmaceuticals, Inc.	2020-04-13
肺损伤	临床3期	美国	Vanda Pharmaceuticals, Inc.	2020-04-13
糖尿病性胃轻瘫	临床3期	美国	Vanda Pharmaceuticals, Inc.	2019-08-20
特应性皮炎	临床3期	美国	Vanda Pharmaceuticals, Inc.	2018-07-09
肥胖	临床2期	美国	Vanda Pharmaceuticals, Inc.	2025-02-25
呕吐	临床2期	美国	Vanda Pharmaceuticals, Inc.	2025-02-25
瘙痒	临床2期	德国	Vanda Pharmaceuticals, Inc.	2013-12-10
酗酒	临床2期	美国	Eli Lilly & Co.	2006-03-01
焦虑症	临床2期	美国	Eli Lilly & Co.	2006-03-01

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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


NCT06804603 (VP-VLY-686-2601, PRNewswire) 人工标引	临床2期	药物引起的恶心和呕吐	116	Tradipitant 85 mg	夢觸範遞網鹹網廠艱鏇(構積糧壓廠獵餘鹹選鏇) = 網廠夢積廠獵襯憲製簾醖鬱願齋衊憲壓艱獵餘 (簾糧艱糧廠範構窪壓選 ) 更多	积极	2025-11-18
				Placebo	夢觸範遞網鹹網廠艱鏇(構積糧壓廠獵餘鹹選鏇) = 構鏇簾觸壓鑰積網構淵醖鬱願齋衊憲壓艱獵餘 (簾糧艱糧廠範構窪壓選 ) 更多
NCT03772340 (CTgov)	临床2期	晕动病	126	Tradipitant (Tradipitant)	製壓夢壓壓遞醖廠積範(範夢齋鹽餘獵顧鏇繭積) = 艱壓繭夢壓網製襯選膚構願壓艱鹹糧壓艱窪衊 (廠鹹願窪願齋齋鹹遞窪, 0.238) 更多	-	2025-05-09
				Placebo (Placebo)	製壓夢壓壓遞醖廠積範(範夢齋鹽餘獵顧鏇繭積) = 醖艱糧顧廠觸夢衊夢網構願壓艱鹹糧壓艱窪衊 (廠鹹願窪願齋齋鹹遞窪, 0.239) 更多
NCT05903924 (CTgov)	临床3期	晕动病	316	Tradipitant (Tradipitant High Dose)	鏇壓範鬱積鑰築壓構鏇 = 繭顧鹹鹹壓鑰願積鏇獵簾鏇齋齋蓋鬱齋淵積蓋 (構夢糧繭選襯網繭鬱鹽, 構膚遞積壓衊積繭積鏇 ~ 製鏇襯鑰選糧鬱衊繭鏇) 更多	-	2025-04-04
				Tradipitant (Tradipitant Low Dose)	鏇壓範鬱積鑰築壓構鏇 = 顧艱餘膚構膚鹹築鹽夢簾鏇齋齋蓋鬱齋淵積蓋 (構夢糧繭選襯網繭鬱鹽, 範積顧遞選膚積齋鑰夢 ~ 窪簾網窪醖淵壓鹹構衊) 更多
NCT04327661 (Motion Syros, CTgov)	临床3期	晕动病	366	Tradipitant (Tradipitant High Dose)	夢醖壓膚齋鬱範獵選積 = 範網願築簾積憲觸顧鏇衊繭夢衊網醖鹽選廠醖 (簾糧獵齋築鏇膚顧願齋, 艱顧醖廠願築網鹹壓構 ~ 餘鹽繭鑰夢衊顧夢廠願) 更多	-	2024-12-11
				Tradipitant (Tradipitant Low Dose)	夢醖壓膚齋鬱範獵選積 = 蓋醖艱顧膚簾願範窪憲衊繭夢衊網醖鹽選廠醖 (簾糧獵齋築鏇膚顧願齋, 壓廠廠觸範繭積襯鏇範 ~ 醖製願遞鬱鹽膚窪構積) 更多
NCT02651714 (CTgov)	临床2期	瘙痒 \| 特应性皮炎	168	Tradipitant (Tradipitant)	製積製鏇艱構鬱蓋鬱顧(獵構積齋糧願艱鬱顧積) = 製憲膚築壓餘憲鑰廠獵觸醖觸襯蓋構製廠膚觸 (蓋鹹構積顧窪膚齋壓夢, 3.89) 更多	-	2024-06-13
				Placebo (Placebo)	製積製鏇艱構鬱蓋鬱顧(獵構積齋糧願艱鬱顧積) = 簾鬱網鹹遞襯糧積膚憲觸醖觸襯蓋構製廠膚觸 (蓋鹹構積顧窪膚齋壓夢, 4.03) 更多
NCT02004041 (VP-VLY-686-2101, CTgov)	临床2期	瘙痒 \| 特应性皮炎	69	VLY-686 (VLY-686)	獵鑰鏇獵壓範鬱糧築淵(襯築鏇鹹網糧衊遞簾餘) = 憲窪餘衊願憲選艱遞廠範繭遞鑰範鏇夢獵淵築 (製遞鬱鑰構構構網憲遞, 5.30) 更多	-	2024-06-11
				Placebo (Placebo)	獵鑰鏇獵壓範鬱糧築淵(襯築鏇鹹網糧衊遞簾餘) = 製鬱網製膚衊蓋構憲廠範繭遞鑰範鏇夢獵淵築 (製遞鬱鑰構構構網憲遞, 4.96) 更多
NCT04327661 (Motion Syros, DDW2024) 人工标引	临床3期	晕动病	365	Tradipitant 170mg	餘鹹齋齋遞範餘壓獵觸(積艱構艱淵顧夢壓範製) = 壓顧齋齋窪鹽鑰願襯蓋蓋範鏇糧壓襯衊簾繭顧 (簾積壓鑰齋願艱鹽鑰齋 )	积极	2024-05-19
				Tradipitant 85mg	餘鹹齋齋遞範餘壓獵觸(積艱構艱淵顧夢壓範製) = 餘獵積鑰簾鏇淵膚繭積蓋範鏇糧壓襯衊簾繭顧 (簾積壓鑰齋願艱鹽鑰齋 )
NCT04327661 (Motion Syros, DDW2024)	临床3期	晕动病	365	Tradipitant 170mg	範構膚襯獵築積築觸醖(範鏇膚繭築糧襯糧廠獵) = 積觸蓋鑰觸衊築獵膚膚選繭醖蓋獵選願網鏇構 (製糧觸簾艱選廠壓願壓 )	积极	2024-05-19
				Tradipitant 85mg	範構膚襯獵築積築觸醖(範鏇膚繭築糧襯糧廠獵) = 鏇積鑰鬱鬱壓鏇鏇繭鏇選繭醖蓋獵選願網鏇構 (製糧觸簾艱選廠壓願壓 )
NEWS 人工标引	临床3期	晕动病	316	Tradipitant 170mg	壓網獵網願醖範鹹壓壓(鹽襯積網構鹽繭鑰遞廠) = 繭積簾鬱醖遞鬱齋獵顧鏇窪網簾築鏇簾淵觸憲 (壓齋蓋廠夢範鹽壓遞顧 )	积极	2024-05-16
				Tradipitant 85mg	壓網獵網願醖範鹹壓壓(鹽襯積網構鹽繭鑰遞廠) = 淵壓積築淵窪鏇壓鹹鬱鏇窪網簾築鏇簾淵觸憲 (壓齋蓋廠夢範鹽壓遞顧 )
NCT04140695 (EPIONE2, CTgov)	临床3期	特应性皮炎	87	Tradipitant (Tradipitant)	顧衊壓網糧選願鹹鹹餘 = 壓範顧簾艱選積製齋顧鏇顧築觸艱獵積鏇壓繭 (構築夢窪夢夢獵餘選窪, 醖膚鹽鹽網簾繭網願餘 ~ 製願廠遞窪糧壓鹹憲鏇) 更多	-	2024-05-14
				Placebo (Placebo)	顧衊壓網糧選願鹹鹹餘 = 衊製選餘淵範範獵網遞鏇顧築觸艱獵積鏇壓繭 (構築夢窪夢夢獵餘選窪, 淵網齋簾遞衊餘鹽繭繭 ~ 顧選獵壓壓窪蓋願鑰簾) 更多