A Single-center, Open-label, Fixed-sequence Trial to Investigate the Effect of Multiple-dose Aprocitentan on the Single-dose Pharmacokinetics of Combined Oral Contraceptives in Healthy Female Participants

The goal of this clinical trial is to learn if drug aprocitentan has an effect on hormonal contraceptives in healthy female volunteers. The main question it aims to answer is:
Does aprocitentan modify the fate of hormonal contraceptives in the body?
Trial participants will:
* Take a single dose of hormonal contraceptives (fixed combination) alone
* Take aprocitentan every day for 2 weeks
* Take a single dose of the same hormonal contraceptives at the same time as the 10th administration of aprocitentan.

开始日期2025-01-18

申办/合作机构

Idorsia Pharmaceuticals Ltd.

NCT05196399

/ Completed临床1期

A Single-center, Open-label, Randomized, Two-way Crossover Phase 1 Study to Compare the Single-dose Pharmacokinetics of Different Tablet Formulations of Aprocitentan in Healthy Subjects

The main purpose is to study the pharmacokinetics of aprocitentan (ACT-132577) using 2 different tablet formulations. The clinical pharmacology data will be used to determine bioequivalence of 2 different tablet formulations.

开始日期2022-02-02

申办/合作机构

Idorsia Pharmaceuticals Ltd.

NCT04252495

/ Completed临床1期

An Open-label Phase 1 Study to Investigate the Effect of Moderate Hepatic Impairment Due to Liver Cirrhosis on the Pharmacokinetics of a Single Dose of 25 mg Aprocitentan

This is a prospective, open-label, single-dose, Phase 1 study, to assess the effect of moderate hepatic impairment due to liver cirrhosis on the pharmacokinetics of aprocitentan (ACT-132577).

开始日期2020-06-26

申办/合作机构

Idorsia Pharmaceuticals Ltd.

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项与阿普昔腾坦相关的文献（医药）

2026-03-01·Pregnancy Hypertension-An International Journal of Womens Cardiovascular Health

Placental transfer of the novel endothelin-1 receptor antagonist aprocitentan

Article

作者: Kluivers, Anna C M ; Tan, Lunbo ; Danser, A H Jan ; van der Meeren, Lotte E ; Delahaye, Stephane ; Harhangi, Madhavi S ; Broekhuizen, Michelle

RATIONALE:

The vasoconstrictor endothelin-1 is elevated in preeclampsia, making endothelin receptor antagonists (ERAs) a logical therapeutic strategy. Here we evaluated the placental transfer of the novel ERA aprocitentan, which has recently been approved for hypertension treatment.

MATERIALS AND METHODS:

Dual-sided placental cotyledon perfusion was used to study transfer of aprocitentan, added maternally at a clinically relevant concentration of 150 ng/mL. Subsequently, these placentas were fetally exposed to endothelin-1. Antipyrine, which freely transfers to the fetal compartment, and fluorescein isothiocyanate [FITC]-dextran, which does not transfer, were used as comparator substances.

RESULTS:

After 3 h of perfusion, the fetal-to-maternal ratio for total (free + protein-bound) aprocitentan was 0.25 ± 0.04, while for free aprocitentan it was 0.42 ± 0.08. The fetal aprocitentan concentrations were too low to block the contractile effects of endothelin-1 in the fetal compartment, although experiments in isolated chorionic plate arteries confirmed that aprocitentan can block these effects when given at higher concentrations. After perfusion, 50-60% of aprocitentan was recovered in the maternal and fetal fluid compartments. Around 20-30% was present in tissue, as intact aprocitentan or as its hydrolysis product ACT-080803. Since the recovery of maternally applied antipyrine and FITC-dextran was 85-90%, while fetally applied FITC-dextran was fully recovered, the missing 10-15% is likely present in the intervillous space.

DISCUSSION:

Aprocitentan transfers across the human placental barrier, although its fetal levels following maternal application of 150 ng/mL were insufficient to block endothelin-1. Drug studies in isolated cotyledons should consider the intervillous space when calculating recovery.

2026-02-01·HYPERTENSION

Aprocitentan in Patients With Chronic Kidney Disease and Resistant Hypertension

Article

作者: Mann, Johannes ; Wang, Ji-Guang ; Sassi-Sayadi, Mouna ; Rossignol, Patrick ; Flamion, Bruno ; Flack, John M. ; Weber, Michael A. ; Schlaich, Markus P. ; Clozel, Martine ; Dreier, Roland F. ; Narkiewicz, Krzysztof

BACKGROUND::

Hypertension is a cause and consequence of chronic kidney disease (CKD). Resistant hypertension is common and often difficult to control in patients with CKD. This post hoc analysis evaluated the efficacy and safety of aprocitentan (with standardized background antihypertensive therapy) in patients with CKD and resistant hypertension, a group with high morbidity and mortality risk and limited treatment options.

METHODS::

The PRECISION study (Parallel-Group, Phase 3 Study With Aprocitentan in Subjects With Resistant Hypertension) consisted of part 1: 4-week, double-blind (aprocitentan 12.5 and 25 mg versus placebo); part 2: 32-week, single-blind (aprocitentan 25 mg); and part 3: 12-week, double-blind withdrawal (aprocitentan 25 mg versus placebo). In participants with CKD, aprocitentan’s effect on blood pressure (BP), urine albumin-to-creatinine ratio, and safety was evaluated.

RESULTS::

Of 730 participants in PRECISION, 147 had CKD categorized as KDIGO high risk or very high risk. At week 4, aprocitentan 12.5 mg, aprocitentan 25 mg, and placebo reduced office systolic BP by −13.5, −16.6, and −4.4 mm Hg, respectively; this was maintained with aprocitentan 25 mg to week 36 (−16.4 mm Hg). At week 4, reductions in nighttime ambulatory systolic BP were −9.6, −13.8, and −2.5 mm Hg, respectively. Changes in urine albumin-to-creatinine ratio were −47.1%, −59.6%, and −2.4%, respectively, maintained with aprocitentan 25 mg to week 36 (−61.6%). Aprocitentan was generally well tolerated (no change in potassium or estimated glomerular filtration rate); early peripheral edema was the most common adverse event.

CONCLUSIONS::

Aprocitentan was well tolerated; efficiently lowered BP, particularly nighttime ambulatory BP; and markedly reduced urine albumin-to-creatinine ratio in participants with CKD and resistant hypertension. Aprocitentan may confer considerable cardiovascular and kidney-protective benefits in these difficult-to-treat patients.

REGISTRATION::

URL: https://www.clinicaltrials.gov ; Unique identifier: NCT03541174.

2026-01-02·Current Hypertension Reviews

A New Drug for Resistant Hypertension: Aprocitentan

Article

作者: Chopra, Deepti ; Lhamo, Yangshen ; Sidhu, Jaspreet Kaur ; Goyal, Abhinav

Abstract::

Resistant hypertension (RH) is defined as uncontrolled blood pressure (BP) despite the use of three or more antihypertensive agents of different pharmacological classes. The treat-ment of resistant hypertension remains a challenge, as it is associated with a heightened risk of cardiovascular events. Many preclinical studies have demonstrated the importance of the endo-thelin pathway in resistant hypertension; however, the therapeutic application of endothelin an-tagonists in clinical practice has been limited due to various factors. Recently, in March 2024, the FDA approved aprocitentan, an orally active endothelin-1 (ET-1) receptor antagonist that inhibits the binding of ET-1 to ETA and ETB receptors. This is the first medication with a novel mechanism for the treatment of resistant hypertension. This review aims to summarise the avail-able evidence on the discovery, chemical nature, pharmacokinetics, pharmacodynamics, effi-cacy, and safety of the novel drug aprocitentan in the pharmacotherapy of resistant hyperten-sion. The landmark PRECISION trial demonstrated a significant BP-lowering effect with the use of the dual endothelin receptor antagonist aprocitentan in the treatment of resistant hyper-tension. Aprocitentan was shown to be particularly effective in patients over 75 years of age, those with a higher cardiovascular-risk profile, patients with diabetes, and individuals with ad-vanced chronic kidney disease (CKD). As a dual receptor antagonist, aprocitentan demonstrated a lower risk of fluid retention and vascular leakage, adverse effects previously observed with other endothelin receptor antagonists. Its mechanism of action, improved efficacy, and excellent tolerability make aprocitentan a promising therapeutic option for resistant hypertension. It may be particularly effective in the treatment of patients with comorbidities, such as diabetes and CKD.

152

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2026-03-03

·终身学习-星辰如梦

【药品分享】罗伐昔替尼片——全球首创JAK/ROCK双靶点口服小分子抑制剂

罗伐昔替尼片是全球首个获批的JAK/ROCK双靶点抑制剂，填补了单JAK抑制剂难以改善纤维化的临床缺口；为不耐受芦可替尼或疗效不佳的骨髓纤维化患者提供新一线选择；cGVHD等自免适应症拓展潜力大，有望成为罕见血液/免疫疾病领域的重磅产品。基本信息研发与获批：正大天晴（中国生物制药旗下）自主研发的 1 类创新药、全球首创JAK/ROCK 双靶点口服小分子抑制剂；2026年2月28日获NMPA批准上市，用于中危-2/高危原发性骨髓纤维化(PMF)、真性红细胞增多症后MF(PPV-MF)、原发性血小板增多症后MF(PET-MF)成人一线治疗，缓解脾肿大与疾病相关症状；2024年7月提交NDA，目前仅中国获批，美国处于Ⅱ期临床。剂型：片剂，口服给药。作用机制：同时抑制JAK1/2与ROCK1/2：JAK-STAT通路异常是骨髓纤维化核心驱动，抑制后可缩脾、改善全身症状；ROCK通路参与纤维化与炎症，抑制后协同抗纤维化、优化骨髓微环境；对ROCK的抑制活性显著强于传统JAK抑制剂（如芦可替尼），双通路协同实现抗炎+抗纤维化双重效应。关键临床数据骨髓纤维化注册研究：第24周独立影像评估(IRC)脾脏体积缩小≥35%(SVR35)的比例达58.33%，显著优于羟基脲对照组(22.86%)；任意时间点SVR35达63.89%，平均持续8.31个月；总症状评分较基线下降≥50%的比例为77.78%(对照组54.29%)。安全性：总体耐受良好，≥3级不良事件发生率约40%，贫血约40%，治疗终止率仅6.7%，优于芦可替尼；常见不良反应包括贫血、血小板减少、乏力等。慢性移植物抗宿主病(cGVHD)：国内Ⅲ期临床，被CDE纳入突破性治疗；Ib/IIa 期显示多器官客观缓解率高，可降低激素依赖/难治患者的激素用量，结果发表于《Blood》。专利情况罗伐昔替尼(TQ05105)由正大天晴自主研发，构建了以核心化合物专利为基石、晶型/制剂/适应症为外围、全球多国布局的完整专利壁垒，保护期覆盖至2034年，并可通过专利期补偿延长。 1 化合物专利美国：US10561657B2（优先权日：2014-12-16）中国：ZL201580067048.0（PCT 进入中国）保护内容：罗伐昔替尼化学结构（JAK/ROCK 双靶点母核）；制备方法、药用组合物、盐型。到期时间：基础到期2034-12-16（自优先权日起20年）；可申请专利期补偿 (PTE)，最长可延长5年，补偿后总保护期不超过14年（自上市日起）。意义：全球唯一覆盖该双靶点结构的核心专利，2034年前无仿制药可合法上市。2 晶型专利：保护优势晶型（提高稳定性、溶解度、生物利用度）；防止竞争对手通过晶型规避核心专利。3 制剂专利：保护片剂处方、工艺、给药系统；覆盖上市剂型（罗伐昔替尼片）。4 适应症专利：保护骨髓纤维化(MF)、慢性移植物抗宿主病(cGVHD)等已获批/在研适应症的治疗方法；为后续适应症拓展（如 aGVHD、噬血细胞综合征）提供专利支撑。5 联合用药专利：保护罗伐昔替尼+ BET抑制剂/BCL-2抑制剂等联合方案；拓展临床应用，延长产品生命周期。仿制药与改良药风险1. 风险点专利悬崖风险：核心专利2034年到期后，仿制药大量上市，价格暴跌、市场份额被挤压。改良型新药(505(b)(2))冲击：竞争对手开发新剂型、新复方、新盐型罗伐昔替尼，通过快速审批上市，抢占市场。生物类似药/后续新药竞争：新一代JAK/ROCK 抑制剂、双特异性抗体等后续产品上市，替代罗伐昔替尼。2. 应对策略 1）生命周期管理(LCM)：适应症拓展：加速cGVHD、aGVHD、噬血细胞综合征等新适应症临床与上市，延长产品生命周期。剂型改良：开发长效缓释、口服纳米、皮下注射等新剂型，申请改良型新药专利，构建新壁垒。联合疗法：推进罗伐昔替尼 + 其他药物联合方案临床，形成独家联合治疗标准。 2）仿制药防御：专利链接：在中国、美国及时登记核心 + 外围专利，利用专利链接制度延迟仿制药上市。专利期补偿最大化：争取最长5年PTC/PTE，将实际市场独占期延长至2040年左右。3）产品迭代：启动下一代 JAK/ROCK 抑制剂、双靶点/多靶点药物研发，构建产品管线梯队，应对后续竞争。其他药品分享链接如下，欢迎点击查看： Ormeloxifene OTF慢性体重管理的新型药物-Tirzepatide新型的非阿片类小分子镇痛药-Suzetrigine奥麦利昔芬口腔薄膜立项调研报告纳米技术双氯芬酸乳胶剂药学研究2025年9月药品批准信息快讯（八）——利斯的明透皮贴剂分享2025年9月药品批准信息快讯（九）——米托坦片分享CDE-《化学仿制药参比制剂目录（第一百批）》（征求意见稿）[附: 药品分享——阿达苏(洛沙平吸入剂)]药品分享-塞来昔布盐酸曲马多片药品分享——伐莫洛龙口服混悬液【药品分享】盐酸菲优拉生片【药品分享】拉坦噻吗滴眼液【药品分享】Baxdrostat 片【药品分享】Omecamtiv Mecarbil缓释片【药品分享】曲地匹坦（Rolapitant）【药品分享】Zasocitinib 胶囊【药品分享】甲磺酸阿帕替尼片【药品分享】巴氯芬口服溶液【药品分享】奥德昔巴特胶囊【药品分享】扎维吉泮鼻喷雾剂【药品分享】左羟丙哌嗪糖浆【药品分享】利丙双卡因凝胶贴膏【药品分享】司来吉兰改良型新药（缓释片）【药品分享】复方甘菊利多卡因凝胶【药品分享】盐酸索安非托片【药品分享】地塞米松口溶膜【药品分享】盐酸来罗西利片【药品分享】马来酸噻吗洛尔凝胶【药品分享】褪黑素颗粒【药品分享】罗氟司特乳膏【药品分享】盐酸芬戈莫德胶囊【药品分享】示踪用盐酸米托蒽醌注射液【药品分享】美洛昔康纳米晶注射液【药品分享】Clascoterone 5%外用溶液【药品分享】马来酸依那普利口服溶液【药品分享】注射用双氯芬酸钠利多卡因【药品分享】马来酸依那普利叶酸片—复方降压药【药品分享】依曲帕米鼻喷雾剂—用于治疗成人阵发性室上性心动过速的可自行给药鼻喷雾剂【药品分享】奥卡西平口服混悬液—一款可用于儿童的钠通道调节类抗癫痫药【药品分享】泊沙康唑口服混悬液——一种常用的抗真菌药物【药品分享】舒沃替尼片【药品分享】依伏卡塞片——第二代口服拟钙剂【药品分享】西诺氨酯片——第三代抗癫痫发作药物【药品分享】匹妥布替尼片——非共价可逆 BTK 抑制剂（用于复发 / 难治套细胞淋巴瘤（MCL））【药品分享】贝美前列素【产品分享】达普司他片【药品分享】水合氯醛糖浆——镇静催眠药【产品分享】苏沃雷生（Suvorexant）——全球首个食欲素受体拮抗剂类催眠药【药品分享】贝沙罗汀【药品分享】地夫可特干混悬剂——一种糖皮质激素类药物【药品分享】伊卢多啉片——治疗成人腹泻型肠易激综合征（IBS‑D）的首创口服阿片受体调节剂【药品分享】卢美哌隆胶囊——一种新型的非典型抗精神病药物【药品分享】奥氟格列隆片——口服非肽类小分子 GLP-1 受体激动剂【药品分享】苯磺酸克利加巴林胶囊——一种新型的治疗神经病理性疼痛的药物【药品分享】苯磺酸美洛加巴林片——治疗周围神经病理性疼痛（PNP）的第三代钙离子通道调节剂【药品分享】Iberdomide胶囊——一款新一代cereblon（CRBN）E3连接酶调节剂（CELMoD）化合物【药品分享】酒石酸伐尼克兰鼻喷雾剂——一种用于治疗干眼症的西药【药品分享】赛沃替尼片——中国首个获批的高选择性 MET 酪氨酸激酶抑制剂【药品分享】盐酸阿夫唑嗪缓释片——一种用于治疗良性前列腺增生（BPH）的 α1 - 受体阻滞剂【药品分享】索格列净片——全球首个获批的SGLT1/SGLT2 双重抑制剂【药品分享】奥吡卡朋胶囊——新一代的儿茶酚-氧位-甲基转移酶抑制剂（COMT）【药品分享】奎扎替尼片——一种口服高选择性 FLT3 抑制剂【药品分享】硫酸拉罗替尼胶囊 / 口服溶液——全球首个高选择性口服 TRK 抑制剂【药品分享】司帕生坦片——成人IgA肾病领域首个非免疫抑制疗法【药品分享】黄体酮阴道栓剂/阴道缓释凝胶剂——主要用于辅助生殖技术（ART）中的黄体支持【药品分享】替戈拉生片——首款国产钾离子竞争性酸阻滞剂类药物（P-CAB）【药品分享】拉坦前列烯酯滴眼剂——一种新型眼科用药【药品分享】布比卡因脂质体注射液——一种长效局部麻醉药【药品分享】甲磺酸加诺沙星片——一种喹诺酮类抗菌药【药品分享】磷酸芦可替尼乳膏——中国首款且唯一获批的白癜风治疗靶向药【药品分享】甲磺酸洛美他派胶囊——全球唯一口服MTP抑制剂【药品分享】依达拉奉口服混悬液——肌萎缩侧索硬化症（ALS，渐冻人症）新药【药品分享】依达拉奉右莰醇舌下片——全球卒中领域首个获FDA突破性疗法认定的舌下脑保护剂【药品分享】马来酸氟诺替尼片——JAK2/FLT3/CDK6 三靶点抑制剂【药品分享】普拉替尼胶囊——国内首个获批的高选择性 RET（转染重排）酪氨酸激酶抑制剂【药品分享】右美托咪定舌下膜——新型 α₂肾上腺素受体激动剂舌下膜剂【药品分享】卡匹色替片——全球首个获批上市的AKT抑制剂【药品分享】库莫西利胶囊——全球首个CDK2/4/6抑制剂【药品分享】赛贝曲司他片——全球首个HAE急性发作口服疗法【药品分享】KYGEVVI（Doxecitine/Doxribtimine）——全球首款且唯一获批的TK2d针对性治疗药物【药品分享】Forzinity（Elamipretide）注射剂——全球首个用于治疗Barth综合征的药物【药品分享】Brinsupri（Brensocatib, 布伦索卡替布）片——全球首个获批上市的二肽基肽酶1（DPP-1）抑制剂【药品分享】维立西呱片——全球首个心衰适应症的可溶性鸟苷酸环化酶（sGC）刺激剂【药品分享】盐酸哌罗匹隆片——非典型抗精神病药【药品分享】盐酸托泊替康胶囊/注射用盐酸托泊替康——经典的拓扑异构酶Ⅰ抑制剂类抗肿瘤药【药品分享】阿普昔腾坦片——全球首个获批用于难治性高血压的口服双重内皮素受体拮抗剂（ERA）【药品分享】注射用盐酸依拉环素——全球首个氟环素类抗生素【药品分享】奥洛格列净胶囊——国内首款抑制SGLT1与SGLT2的1类创新药【药品分享】盐酸匹米替尼胶囊——国内首个、全球首个获批的腱鞘巨细胞瘤（TGCT）系统性靶向药，高选择性CSF-1R抑制剂【药品分享】布地奈德肠溶胶囊——全球首个、中国唯一获批用于原发性IgA肾病对因治疗的靶向药物【药品分享】艾拉莫德片——中国原研、全球首个上市的小分子抗风湿药（csDMARD）【药品分享】索托克拉片——新一代BCL2抑制剂【药品分享】利奈昔巴特片——口服、选择性、可逆性回肠胆汁酸转运体（IBAT/ASBT）抑制剂【药品分享】多替诺雷片——高选择性URAT1抑制剂【药品分享】瑞普泊肽片——口服GLP‑1/GIP双靶点激动剂【药品分享】硫酸索西美雷塞片——口服、强效的KRAS G12C共价抑制剂免责声明：本文仅作医药信息传播分享，并不构成投资或决策建议。

2026-02-28

·新药信息合集

新药合集—1月全球新药汇总

1月全球获批新药清单全球共有84款新药（含新适应症）获批上市，中国（包括中国内地及中国香港）约有34种，是本月新药获批最多的地区。美国约有8种。欧洲药品管理局约有13种，是全球创新药上市的核心市场。加拿大约有7种。其他地区（如韩国、马来西亚、沙特阿拉伯等）共约有22种。 •肿瘤领域：这是最主要的适应症领域，包括治疗套细胞淋巴瘤的新药匹妥布替尼、治疗非小细胞肺癌的新药阿美替尼、治疗非霍奇金淋巴瘤的新药苯达莫司汀、治疗急性髓系白血病的新药奎扎替尼、治疗子宫内膜癌的新药度伐利尤单抗，等多种恶性肿瘤。 •其他重要领域： ⭐代谢性疾病：以治疗糖尿病为代表的新药甘精胰岛素。 ⭐免疫系统疾病：治疗湿疹血小板减少伴免疫缺陷综合征的新药Etuvetidigene autotemcel等罕见免疫疾病。 ⭐心血管疾病：治疗高血压的新药阿普昔腾坦。 1月全球提交申请新药清单 75款药物提交上市申请，中国提交38款，美国约有16款，欧洲药品管理局约有14款，日本约有5款，其他地区（如加拿大、澳大利亚等）共约有2种。 •肿瘤领域：治疗肌层浸润性膀胱癌的新药申请数量突出，显示对肿瘤精准诊断的需求增加。还有治疗急性淋巴细胞白血病的新药泊那替尼、治疗多发性骨髓瘤的新药特立妥单抗、治疗胆道癌的新药恩沃利单抗、治疗肝细胞癌的新药阿帕替尼等消化系统恶性肿瘤受到关注。 •其他重要领域： ⭐代谢性疾病：糖尿病依然是重要的治疗领域，有治疗1型糖尿病的新药替利珠单抗、治疗2型糖尿病的新药普卢格列汀+二甲双胍或德谷胰岛素+利拉鲁肽等。 ⭐罕见病与特殊适应症：治疗腱鞘巨细胞瘤的新药坦鲁扑拜单抗等罕见疾病也有新药申请。 1月首次进入 Ⅲ 期临床的新药清单 30款药物进入III期临床，中国内地约13种，占据绝对主导地位，美国约有4种，欧洲药品管理局约有3种，其它有10种。 •肿瘤领域：治疗去势抵抗性前列腺癌的新药DB-1311、治疗上皮样肉瘤的新药HH2853等难治性肿瘤继续推进研发。 •其他重要领域： ⭐免疫系统疾病：治疗特应性皮炎的新药度普利尤单抗-GS101等免疫性皮肤病是重点研发领域。 ⭐神经系统疾病：治疗亨廷顿舞蹈病的新药Votoplam、治疗多发性硬化的新药Frexalimab皮下注射等神经系统疾病显示出较高研发热度。 ⭐代谢性疾病：治疗甲基丙二酸血症的新药羟钴胺(新适应症)-华润双鹤等代谢性疾病受到关注。 ⭐眼科疾病：治疗高眼压和开角型青光眼的新药HUC3-637等眼科疾病有新突破。 1月研发进度终止新药 7款药物终止研发，其中有 36款新药研发终止，1 款新药适应症研发终止。终止阶段：终止项目涉及临床III期、II期和I期。终止原因：涵盖实体瘤、胰腺癌、妇科肿瘤等多种恶性肿瘤，说明肿瘤药物研发仍面临较大挑战。 ⭐血液系统疾病：颅内出血等血液系统相关并发症的治疗研究遇到困难。 ⭐遗传性疾病：如共济失调毛细血管扩张综合征等遗传性疾病的治疗研发因疗效不佳等原因终止。 END

2026-02-26

·BioSpace

Idorsia reports strong 2025 results with QUVIVIQ sales more than doubling – further sales growth ahead with multiple pipeline catalysts in 2026

Ad hoc announcement pursuant to Art. 53 LR Idorsia delivers on its upgraded 2025 guidance , with strong QUVIVIQ sales growth, disciplined investment, and a significantly improved bottom line. Focused investment in Idorsia’s pipeline of first-in-class medicines to drive future growth, with key readout for daridorexant in pediatric insomnia imminent and Lucerastat registration study advancing in Fabry’s disease. Allschwil, Switzerland – February 26, 2026 Idorsia Ltd (SIX: IDIA) announces strong financial and operational results for the full year 2025, setting a new base for further growth ahead and a catalyst rich 2026. Srishti Gupta, MD, Chief Executive Officer of Idorsia, commented: “2025 marked a year of disciplined execution and renewed momentum for Idorsia. We delivered on our upgraded guidance, more than doubled QUVIVIQ sales, and significantly strengthened our financial position – demonstrating that focused investment and commercial excellence can go hand in hand. At the same time, we continued the next phase of growth: positioning TRYVIO/JERAYGO as the first treatment to target a new pathway in hypertension in decades and progressing our pipeline, including the upcoming readout of the pediatric insomnia study and the registrational program for lucerastat in Fabry disease. With multiple catalysts ahead, we enter 2026 with clarity, confidence, and a clear path toward sustainable growth.” QUVIVIQ ® (daridorexant) Global 2025 net sales grow to CHF 134 million, reflecting outstanding year-over-year momentum – with continued strong growth ahead. QUVIVIQ continues to reshape the insomnia treatment landscape, and we are investing to accelerate its trajectory toward blockbuster status. Growth will be driven by expanded global reach through partnerships targeting general practitioners, strategic commercial alliances, additional public reimbursement wins, potential U.S. descheduling, adoption of innovative digital and distribution models, and the initiation of a U.S. label-enhancing study focused on daytime functioning. New opportunity to transform the treatment paradigm in pediatric insomnia with results expected in Q2 2026 from the Phase 2 study for daridorexant – the only dual orexin receptor antagonist in development for this population with high unmet need. TRYVIO™ / JERAYGO™ (aprocitentan) TRYVIO is available in the US and used in the top 25 hypertension centers. Robust on-market experience among leading experts indicates “PRECISION-like” double-digit blood pressure reductions and confirms the tolerability pro diverse patient groups. Regulatory success in 2025 – JERAYGO is approved in EU, UK, Switzerland, and Canada. Partnering discussions to maximize the global value of TRYVIO/JERAYGO are progressing. Research & Development Alignment with the FDA on the registrational program for lucerastat, positioning Idorsia to advance the first oral therapy intended for all patients with Fabry disease. Advancing Idorsia’s immunology portfolio of first-in-class compounds – starting with Idorsia’s CCR6 antagonist proof-of-concept in psoriasis (proof-of-mechanism for other CCR6- and Th17-associated autoimmune diseases). Clinical validation for Idorsia's revolutionary drug-like synthetic glycan vaccine technology. Financial highlights for full year 2025 QUVIVIQ sales: CHF 134 million Contract revenue (one-off): CHF 72 million contract revenue Non-GAAP operating expenses: CHF 328 million Non-GAAP operating loss: CHF 100 million including one-off contract revenue of CHF 72 million (US GAAP operating loss: CHF 33 million including CHF 90 million one-off income from Viatris agreement) Strengthened balance sheet through successful debt restructuring and new financing. Financial Guidance for 2026 QUVIVIQ sales: CHF 200 million Non-GAAP operating expenses: approx. CHF 330 million Non-GAAP operating loss: CHF 120 million (US GAAP operating loss: approx. CHF 160 million) Positive commercial contribution and focused investment in value-driving pipeline assets results in continued improvement of underlying business performance. 2026 guidance reflects continued growth of QUVIVIQ (approximately 50% increase in Idorsia-led sales), investment in the lucerastat registration program, and development of the company’s immunology portfolio. TRYVIO/JERAYGO revenues and investments are not included, as these will be considered in any potential partnership agreement. All amounts exclude unforeseen events and any potential upsides from new direct-to-patient distribution models currently being implemented in several geographies and revenue related to additional business development activities. Financial results US GAAP results Full Year Fourth Quarter in CHF millions, except EPS (CHF) and number of shares (millions) 2025 2024 2025 2024 Net revenue 221 113 48 60 Operating expenses (268) (351) (106) (140) Operating income (loss) (33) (232) (56) (78) Net income (loss) (112) (264) (78) (84) Basic & diluted EPS (0.52) (1.45) (0.31) (0.45) Basic & diluted weighted average number of shares 214.7 182.4 248.3 188.3 Net revenue of CHF 221 million in 2025 resulted from product sales (CHF 134 million), product sales to partners (CHF 7 million), and contract revenues (CHF 79 million). This compares to net revenue of CHF 113 million in 2024 as a result of QUVIVIQ product sales (CHF 61 million), product sales to partners (CHF 47 million), and contract revenue (CHF 5 million). US GAAP operating expenses of CHF 268 million in 2025 and CHF 351 million in 2024 were impacted by a one-off gain of CHF 90 million (Viatris deal amendment) in 2025 and CHF 125 million (Viatris deal) in 2024, respectively. Excluding these one-off gains, US GAAP operating expenses for 2025 decreased by CHF 83 million, mainly driven by R&D expenses of CHF 102 million decreasing by CHF 42 million compared to 2024 (CHF 144 million), and SG&A expenses of CHF 221 million decreasing by CHF 52 million compared to 2024 (CHF 273 million). US GAAP net loss in 2025 amounted to CHF 112 million compared to CHF 264 million (net loss) in 2024. The reduced net loss in 2025 was primarily driven by revenue growth and lower operating expenses as a result of an operational restructuring initiated in Q4 2024. The US GAAP net loss resulted in a net loss per share of CHF 0.52 (basic and diluted) in 2025, compared to a net loss per share of CHF 1.45 (basic and diluted) in 2024. Non-GAAP* measures Full Year Fourth Quarter in CHF millions, except EPS (CHF) and number of shares (millions) 2025 2024 2025 2024 Net revenue 214 113 47 60 Operating expenses (328) (427) (96) (121) Operating income (loss) (100) (308) (47) (60) Net income (loss) (118) (330) (54) (73) Basic and diluted EPS (0.55) (1.81) (0.22) (0.39) Basic and diluted weighted average number of shares 214.7 182.4 248.3 188.3 * Idorsia measures, reports, and issues guidance on non-GAAP operating performance. Idorsia believes that these non-GAAP financial measurements more accurately reflect the underlying business performance and therefore provide useful supplementary information to investors. These non-GAAP measures are reported in addition to, not as a substitute for, US GAAP financial performance. Non-GAAP net loss in 2025 amounted to CHF 118 million; the difference versus US GAAP net income was mainly driven by the one-off gain from the amendment of the Viatris deal (CHF 90 million), depreciation and amortization (CHF 17 million) , share-based compensation (CHF 6 m), impairment charges (CHF 3 m), restructuring charges (CHF 3 m), accretion and issuance cost amortization (CHF 16 m) and a debt extinguishment loss related to the debt restructuring (CHF 37 million). The non-GAAP net loss resulted in a net loss per share of CHF 0.55 (basic and diluted) in 2025, compared to a net loss per share of CHF 1.81 (basic and diluted) in 2024. Liquidity and indebtedness Liquidity on December 31, 2025, amounted to CHF 89 million. This amount does not include the remaining CHF 80 million available under the new money facility (term loan). (in CHF millions) Dec 31, 2025 Sep 30, 2025 Dec 31, 2024 Liquidity Cash and cash equivalents 89 64 106 Total liquidity* 89 64 106 Indebtedness Convertible loan 335 335 335 Convertible bonds 49 49 797 Debt notes** 753 753 - Term loan 18 13 - Other financial debt 187 186 189 Total indebtedness 1,342 1,336 1,321 *rounding differences may occur ** The debt notes issued by Idorsia Investments SARL in exchange for convertible bonds are senior secured with the shares in Idorsia Investments SARL. The A Notes only benefit from a limited and subordinated Swiss-law governed guarantee by Idorsia Ltd. Human Resources Idorsia reduced more than 200 positions worldwide in 2025, bringing the total number of permanent employees to 487 (2024: 689). Annual Report Idorsia's Annual Report 2025 – consisting of the Business Report, Governance Report, Compensation Report, Sustainability Report, and Financial Report, is available at . Note to Shareholders The Annual General Meeting (AGM) of Shareholders to approve the Annual Report of the year ending December 31, 2025, will be held on Wednesday, May 6, 2026. Registered shareholders with voting rights individually or jointly representing at least 0.5% of the share capital of the company, being entitled to add items to the agenda of the general meeting of shareholders, are invited to send in proposals, if any, to Idorsia Ltd, attention Corporate Secretary, Hegenheimermattweg 91, CH-4123 Allschwil, to arrive no later than March 22, 2026. Any proposal received after the deadline will be disregarded. In order to vote at the Annual General Meeting, shareholders must be registered in the company's shareholder register by April 27, 2026, 17:00 CEST, at the latest. Results Day Center Investor community: To make your job easier, we provide all relevant documentation via the Results Day Center on our corporate website: . Events First Quarter 2026 Financial Results reporting on April 28, 2026 Annual General Meeting of Shareholders on May 6, 2026 Half-Year 2026 Financial Results reporting on July 30, 2026 Notes to the editor About Idorsia The purpose of Idorsia is to challenge accepted medical paradigms, answering the questions that matter most. To achieve this, we will discover, develop, and commercialize transformative medicines – either with in-house capabilities or together with partners – and evolve Idorsia into a leading biopharmaceutical company, with a strong scientific core. Headquartered near Basel, Switzerland – a European biotech hub – Idorsia has a highly experienced team of dedicated professionals, covering all disciplines from bench to bedside; QUVIVIQ™ (daridorexant), a different kind of insomnia treatment with the potential to revolutionize this mounting public health concern; strong partners to maximize the value of our portfolio; a promising in-house development pipeline; and a specialized drug discovery engine focused on small-molecule drugs that can change the treatment paradigm for many patients. Idorsia is listed on the SIX Swiss Exchange (ticker symbol: IDIA). For further information, please contact George Thampy Senior Vice President, Head of Investor Relations Idorsia Pharmaceuticals Ltd, Hegenheimermattweg 91, CH-4123 Allschwil +41 58 844 10 10 investor.relations@idorsia.com – media.relations@idorsia.com – The above information contains certain "forward-looking statements", relating to the company's business, which can be identified by the use of forward-looking terminology such as “intend”, "estimates", "believes", "expects", "may", "are expected to", "will", "will continue", "should", "would be", "seeks", "pending" or "anticipates" or similar expressions, or by discussions of strategy, plans or intentions. Such statements include descriptions of the company's investment and research and development programs, business development activities and anticipated expenditures in connection therewith, descriptions of new products expected to be introduced by the company and anticipated customer demand for such products and products in the company's existing portfolio. Such statements reflect the current views of the company with respect to future events and are subject to certain risks, uncertainties and assumptions. Many factors could cause the actual results, performance or achievements of the company to be materially different from any future results, performances or achievements that may be expressed or implied by such forward-looking statements. Should one or more of these risks or uncertainties materialize, or should underlying assumptions prove incorrect, actual results may vary materially from those described herein as anticipated, believed, estimated or expected. Attachment Press Release PDF

疫苗临床2期上市批准财报

100 项与阿普昔腾坦相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11441	-	-	DB15059

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
原发性高血压	加拿大	Idorsia Pharmaceuticals Ltd.	2025-12-01
难治性高血压	欧盟	IDORSIA LTD	2024-07-01
难治性高血压	冰岛	IDORSIA LTD	2024-07-01
难治性高血压	列支敦士登	IDORSIA LTD	2024-07-01
难治性高血压	挪威	IDORSIA LTD	2024-07-01
高血压	美国	Idorsia Pharmaceuticals Ltd.	2024-03-19

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
慢性肾病	临床3期	匈牙利	Idorsia Pharmaceuticals Ltd.	2019-11-07
肝硬化	临床1期	德国	Idorsia Pharmaceuticals Ltd.	2020-06-26
肝硬化	临床1期	波兰	Idorsia Pharmaceuticals Ltd.	2020-06-26
肝损伤	临床1期	德国	Idorsia Pharmaceuticals Ltd.	2020-06-26
肝损伤	临床1期	波兰	Idorsia Pharmaceuticals Ltd.	2020-06-26

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临床结果

适应症

分期

评价

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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


NCT03541174 (PRECISION, Pubmed \| Hypertension)	临床3期	低血压	-	Aprocitentan 12.5 mg	鏇醖餘鹽鹹簾餘廠艱襯(選糧簾艱艱壓鹽構網網) = 艱範蓋獵簾憲鬱廠範範鹹窪鏇壓壓蓋夢觸築艱 (築窪醖蓋積憲範憲膚築 )	积极	2025-04-01
				Aprocitentan 25 mg	鏇醖餘鹽鹹簾餘廠艱襯(選糧簾艱艱壓鹽構網網) = 繭淵夢鏇壓廠廠選糧選鹹窪鏇壓壓蓋夢觸築艱 (築窪醖蓋積憲範憲膚築 )
PRECISION (ASN2024)	临床3期	难治性高血压	838	Aprocitentan 12.5 mg	構範糧鬱蓋壓衊製餘壓(鹽夢蓋構簾鑰衊蓋顧構) = 網築鏇構淵顧繭繭獵構鏇醖蓋鬱憲選網築鹹壓 (築憲網願鑰齋醖襯壓顧 )	积极	2024-10-26
				Aprocitentan 25 mg	構範糧鬱蓋壓衊製餘壓(鹽夢蓋構簾鑰衊蓋顧構) = 衊糧襯齋製鹹壓選築鏇鏇醖蓋鬱憲選網築鹹壓 (築憲網願鑰齋醖襯壓顧 )
PRECISION (ESH2024)	临床3期	难治性高血压	-	Aprocitentan 12.5 mg	廠願構窪範選鹹夢蓋餘(網簾艱願製衊顧積糧積) = 壓積遞獵齋夢簾鹹膚廠積夢構衊壓蓋網繭鑰鹹 (鏇鹽淵願夢醖願鏇鑰鬱 )	积极	2024-05-01
				Aprocitentan 25 mg	廠願構窪範選鹹夢蓋餘(網簾艱願製衊顧積糧積) = 鏇艱糧廠醖壓窪齋窪願積夢構衊壓蓋網繭鑰鹹 (鏇鹽淵願夢醖願鏇鑰鬱 ) 更多
PRECISION (ESH2024)	临床3期	难治性高血压	93	Aprocitentan 12.5 mg	醖窪憲獵構顧襯獵艱構(範製窪鹹網蓋艱選窪觸) = 簾齋醖觸廠顧繭範顧繭顧憲構鏇網蓋鑰鏇鬱積 (鹽製淵築糧鏇願淵鬱製 ) 更多	积极	2024-05-01
				Aprocitentan 25 mg	醖窪憲獵構顧襯獵艱構(範製窪鹹網蓋艱選窪觸) = 獵選艱選夢選醖網網憲顧憲構鏇網蓋鑰鏇鬱積 (鹽製淵築糧鏇願淵鬱製 ) 更多
NCT03541174 (FDA) 人工标引	临床3期	高血压	-	Aprocitentan (12.5 mg)	積築壓廠夢範艱淵淵鏇(壓襯膚遞選廠餘觸鬱鹹) = 襯構襯齋鏇鬱蓋製糧衊憲壓醖積襯鏇醖鏇壓鹽 (簾觸襯範遞憲醖顧遞範, −17.5 ~ −13.3) 更多	优效	2024-03-19
				Placebo	積築壓廠夢範艱淵淵鏇(壓襯膚遞選廠餘觸鬱鹹) = 鹹範淵願觸憲糧鹽鬱製憲壓醖積襯鏇醖鏇壓鹽 (簾觸襯範遞憲醖顧遞範, −13.7 ~ −9.5) 更多
PRECISION (ESH2023)	临床3期	难治性高血压	730	Aprocitentan 12.5 mg	願壓鏇構餘積網願鏇襯(顧鏇糧觸構構壓蓋夢糧) = 積鏇窪構壓鹽製衊遞憲廠膚膚醖蓋衊襯獵齋膚 (齋簾廠醖餘鹹鑰顧鏇醖 )	积极	2023-06-01
				Aprocitentan 25 mg	願壓鏇構餘積網願鏇襯(顧鏇糧觸構構壓蓋夢糧) = 淵鬱鏇鹽鹽蓋衊鑰築淵廠膚膚醖蓋衊襯獵齋膚 (齋簾廠醖餘鹹鑰顧鏇醖 )
NCT03541174 (PRECISION, CTgov)	临床3期	难治性高血压	730	Aprocitentan 12.5 mg (Aprocitentan 12.5 mg in Part 1 (Double-blind))	窪遞製網淵齋夢選鹹願(憲範獵廠憲窪夢築憲願) = 糧簾顧範願鏇鹽觸齋鏇獵艱鹹鏇齋顧醖窪製廠 (憲鏇鹽鑰鬱齋齋艱蓋鏇, 獵壓膚夢蓋憲繭積淵膚 ~ 膚壓衊鬱鬱夢鹹繭繭鬱) 更多	-	2023-03-21
				Aprocitentan 25 mg (Aprocitentan 25 mg in Part 1 (Double-blind))	窪遞製網淵齋夢選鹹願(憲範獵廠憲窪夢築憲願) = 餘襯構製夢衊窪積鑰繭獵艱鹹鏇齋顧醖窪製廠 (憲鏇鹽鑰鬱齋齋艱蓋鏇, 繭繭齋願憲餘窪製齋膚 ~ 鑰積顧齋淵觸遞簾簾齋) 更多
NCT02603809 (CTgov)	临床2期	原发性高血压	1,659	Placebo (Placebo)	製製簾廠艱顧選獵繭鑰(艱鏇糧鹹衊鏇憲遞糧範) = 憲壓壓膚淵夢鹽鑰鑰獵選齋範鬱遞廠簾襯壓淵 (鑰憲襯膚繭觸鬱範遞簾, 5.4) 更多	-	2020-04-13
				Aprocitentan 5 mg (Aprocitentan 5 mg)	製製簾廠艱顧選獵繭鑰(艱鏇糧鹹衊鏇憲遞糧範) = 憲築壓艱襯壓繭顧蓋網選齋範鬱遞廠簾襯壓淵 (鑰憲襯膚繭觸鬱範遞簾, 5.5) 更多
NCT02603809 (ESC2019)	临床2期	高血压	490	Aprocitentan 5 mg	觸艱鹹積淵鹹築淵夢選(鹽夢艱製醖鏇壓鬱範膚) = 願廠遞鏇鏇製襯壓願獵觸齋淵觸襯窪製網淵遞 (廠襯鑰網餘艱顧獵顧窪 ) 更多	-	2019-08-31
				Aprocitentan 10 mg	觸艱鹹積淵鹹築淵夢選(鹽夢艱製醖鏇壓鬱範膚) = 淵襯壓衊構網鹽鏇鹽衊觸齋淵觸襯窪製網淵遞 (廠襯鑰網餘艱顧獵顧窪 ) 更多