A PHASE 3, EXTERNAL AND SYNTHETIC PLACEBO-CONTROLLED RANDOMIZED STUDY WITH DOSE-UP FOR NON-RESPONDERS TO INVESTIGATE SAFETY AND EFFICACY OF RITLECITINIB 50 MG AND 100 MG ONCE DAILY IN ADULT AND ADOLESCENT PARTICIPANTS 12 YEARS OF AGE AND OLDER WITH ALOPECIA AREATA

The purpose of the study is to learn about the safety and effects of the study medicine (called ritlecitinib) for the treatment of alopecia areata. Alopecia areata is a disease that causes hair loss on the scalp, face, and areas of the body.
Ritlecitinib is approved in many countries at a dose of 50 mg (milligram) taken by mouth once a day for the treatment of patients 12 years and older with severe alopecia areata. This study will look at both the 50 mg dose and a 100 mg dose.
This study is seeking participants who:
* Are 12 years of age or older
* Have a diagnosis of alopecia areata
* Have lost 50% or more of the hair on their scalp
* Do not have any other conditions that causes hair loss
* Are willing to stop all other treatments that they may be taking for alopecia areata
About 550 participants will take part in in this study.
Participants will be chosen by chance, like drawing names out of a hat, to receive 1 of 2 different amounts of ritlecitinib (50 mg and 100 mg) taken by mouth once daily.
The 2 doses of ritlecitinib in this study will be compared to each other and also to data from previous studies. This will help to see if the 100 mg dose of ritlecitinib is safe and effective.
People will be in this study for about 13 months. During the study, participants will need to visit the study site up to 9 times. Participants will undergo various tests and procedures such as:
* alopecia areata assessment,
* physical examinations,
* hearing tests,
* blood tests,
* x-ray,
* ECG (electrocardiogram),
* photographs of the scalp and eyes. Participants will also be asked to complete questionnaires about their alopecia areata.

开始日期2025-03-19

申办/合作机构

Pfizer Inc.

ChiCTR2500095989

/ Suspended临床4期IIT

Real-world study on the efficacy and safety of Ritlecitinib in Chinese patients with severe alopecia areata: A single-center, prospective, observational study

开始日期2025-02-01

申办/合作机构

中南大学湘雅医院

NCT06795373

/ Recruiting临床2期IIT

A Single-center, Single-arm, Open-label Phase IIA Clinical Trial to Investigate Efficacy and Safety of Ritlecitinib (PF-06651600) in Participants With Chronic Spontaneous Urticaria

The purpose of this research study is to see if a drug called ritlecitinib is safe and effective for treating chronic spontaneous urticaria (CSU). CSU is hives and itching lasting over six weeks. Ritlecitinib is approved by the Food and Drug Administration (FDA) to treat another condition, but it is not approved for treating CSU. Participation is expected to last 20 weeks and include 7 clinic visits. This study will involve physical examinations, blood tests, looking at and taking pictures of participant's skin and hives, optional skin biopsies, and hearing tests. Eligible participants for this study will take ritlecitinib for 12 weeks and complete a daily diary about their skin and hives. The main risks of being in this study are side effects from ritlecitinib. Less than 1 in 10 people taking ritlecitinib experience diarrhea, acne, hives, rash, inflammation of hair follicles, dizziness, and increased blood levels of creatine phosphokinase (a muscle protein). Participants could also experience a rare but serious side effect, such as shingles, unusual infection, cancer, or blood clot. Benefits of participating in this study include a potential improvement in participant's condition and quality of life. Participating in this study may also help researchers develop new ways of helping future patients.

开始日期2025-02-01

申办/合作机构

Icahn School of Medicine at Mount Sinai

100 项与甲苯磺酸利特昔替尼相关的临床结果

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100 项与甲苯磺酸利特昔替尼相关的转化医学

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100 项与甲苯磺酸利特昔替尼相关的专利（医药）

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154

项与甲苯磺酸利特昔替尼相关的文献（医药）

2025-04-01·JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY

Response to ritlecitinib with or without narrow-band ultraviolet B add-on therapy in patients with active nonsegmental vitiligo: Results from a phase 2b extension study

Article

作者: Adiri, Roni ; Napatalung, Lynne ; Shore, Ronald N ; Guttman-Yassky, Emma ; Pandya, Amit G ; Peeva, Elena ; Ezzedine, Khaled ; Hamzavi, Iltefat ; Ghosh, Pranab ; Yamaguchi, Yuji

BACKGROUND:

Ritlecitinib demonstrated efficacy in a phase 2b trial of nonsegmental vitiligo.

OBJECTIVE:

To evaluate the efficacy and tolerability of ritlecitinib with add-on narrow-band ultraviolet B (nbUVB) phototherapy in patients with nonsegmental vitiligo.

METHODS:

Following a 24-week, placebo-controlled, dose-ranging period, patients received ritlecitinib 200 mg for 4 weeks then 50 mg for 20 weeks, with or without nbUVB phototherapy 2x/week. Missing data were handled using last observation carried forward and observed case (OC).

RESULTS:

Forty-three patients received ritlecitinib + nbUVB and 187 received ritlecitinib-monotherapy. Nine patients receiving ritlecitinib + nbUVB discontinued due to nbUVB group-specific efficacy criteria requiring >10% improvement in % change from baseline (% change from baseline) in Total-Vitiligo Area Scoring Index at week 12. At week 24, mean % change from baseline in Facial-VASI score was -57.0 vs -51.5 (last observation carried forward; P = .158) and -69.6 vs -55.1 (OC; P = .009), for ritlecitinib + nbUVB vs ritlecitinib-monotherapy, respectively. Mean % change from baseline in Total-Vitiligo Area Scoring Index at week 24 was -29.4 vs -21.2 (last observation carried forward; P = .043) and -46.8 vs -24.5 (OC; P < .001), respectively. nbUVB addition to ritlecitinib was well tolerated with no new safety signals.

LIMITATIONS:

Exploratory analysis; discontinuation criterion applied only to the ritlecitinib + nbUVB group; small sample size.

CONCLUSION:

Ritlecitinib alone and with nbUVB therapy improved facial and total body repigmentation and was well tolerated. Adding nbUVB may improve ritlecitinib efficacy.

2025-04-01·CLINICAL IMMUNOLOGY

Novel janus kinase 3 inhibitor ritlecitinib suppresses T and B cell responses to prevent acute cardiac allograft rejection in mice

Article

作者: Xu, Jian ; Hui, Jialiang ; Deng, Wenfeng ; Xia, Renfei ; Yan, Ziyan ; Wang, Yuchen ; Miao, Yun ; Zeng, Wenli ; Liu, Rumin ; Mo, Liqian ; Liao, Tao ; Shi, Xiaoyi

Acute rejection is the main contributor to early allograft failure. Current immunosuppressive regimens have shortcomings, such as toxicity and minimal inhibitory effects on B cells. Hence, developing novel, effective, and selective anti-acute rejection drugs is crucial. Therefore, this study aimed to investigate the inhibitory effect of ritlecitinib (PF-06651600), a new janus kinase 3 inhibitor, on T and B cells, as well its preventive effects on acute allograft rejection. A murine cardiac transplantation model coupled with cell culture- and immunohistochemistry-based techniques was used. In vitro assays demonstrated that ritlecitinib inhibits naïve CD4⁺ T cell differentiation into T helper (Th)1 and Th17 cells, reduces relative inflammatory cytokines, and suppresses CD4⁺ and CD8⁺ T cell proliferation. Furthermore, ritlecitinib inhibited B cell activation and differentiation and antibody production. In vivo experiments revealed that ritlecitinib significantly prolongs allograft survival, decreases serum donor-specific antibody immunoglobulin G levels, alleviats allograft damage, and reduces C4d deposition and T, B, and plasma cell infiltration in allografts. Moreover, B and plasma cell percentages and counts were significantly decreased in recipient spleen, lymph nodes, bone marrow, and blood. Overall, ritlecitinib prevented acute rejection in cardiac transplantation by inhibiting T and B cells, suggesting its potential as a novel clinical immunosuppressant.

2025-04-01·MOLECULAR DIVERSITY

Identification of novel covalent JAK3 inhibitors through consensus scoring virtual screening: integration of common feature pharmacophore and covalent docking

Article

作者: Qiu, Genhong ; Xu, Lei ; Jia, Lei ; Zhu, Jingyu ; Yu, Li ; Chen, Yun ; Jin, Jian ; Cai, Yanfei

Accumulated research strongly indicates that Janus kinase 3 (JAK3) is intricately involved in the initiation and advancement of a diverse range of human diseases, underscoring JAK3 as a promising target for therapeutic intervention. However, JAK3 shows significant homology with other JAK family isoforms, posing substantial challenges in the development of JAK3 inhibitors. To address these limitations, one strategy is to design selective covalent JAK3 inhibitors. Therefore, this study introduces a virtual screening approach that combines common feature pharmacophore modeling, covalent docking, and consensus scoring to identify novel inhibitors for JAK3. First, common feature pharmacophore models were constructed based on a selection of representative covalent JAK3 inhibitors. The optimal qualitative pharmacophore model proved highly effective in distinguishing active and inactive compounds. Second, 14 crystal structures of the JAK3-covalent inhibitor complex were chosen for the covalent docking studies. Following validation of the screening performance, 5TTU was identified as the most suitable candidate for screening potential JAK3 inhibitors due to its higher predictive accuracy. Finally, a virtual screening protocol based on consensus scoring was conducted, integrating pharmacophore mapping and covalent docking. This approach resulted in the discovery of multiple compounds with notable potential as effective JAK3 inhibitors. We hope that the developed virtual screening strategy will provide valuable guidance in the discovery of novel covalent JAK3 inhibitors.

228

项与甲苯磺酸利特昔替尼相关的新闻（医药）

2025-03-22

·微信

头等大事！国产斑秃药来了！

400万患者的“头等大事”亟待解决斑秃是仅次于雄激素性脱发的第二大脱发类型，全球患者约1.47亿，我国患者达400万，其中30%为难治性重度斑秃（头皮脱发≥50%）。此类患者脱发面积广、病程长，传统疗法（如糖皮质激素、免疫抑制剂）存在复发率高、副作用显著等问题，患者对创新药物需求迫切。近年来，JAK抑制剂通过阻断炎症信号通路，成为斑秃治疗的核心突破方向。全球上市的共三款JAK抑制剂获批斑秃适应症，分别是礼来的巴瑞替尼、辉瑞的利特昔替尼，和太阳制药（印度）Deuruxolitinib。在中国，2023年巴瑞替尼片在中国批准第二个适应症，用于成人重度斑秃的系统性治疗，这是国内首个系统性治疗重度斑秃的创新靶向药物。也是首个获批治疗重症斑秃的JAK抑制剂。销量不俗，2023年在中国公立医疗机构终端的销售额超过了3亿元人民币‌。但近期巴瑞替尼在中国市场遭遇了专利问题。其核心专利面临仿制药竞争（如南京力博维的“首仿”获批）等。男女脱发国际分级图来源：网络中国药企亮剑AAD：Ⅲ期数据揭秘艾玛昔替尼如何实现毛发再生恒瑞医药自主研发的高选择性JAK1抑制剂艾玛昔替尼（Ivarmacitinib，SHR0302）于2025年3月AAD年会（第83届美国皮肤病学会）公布Ⅲ期临床数据。艾玛昔替尼对JAK1的选择性是JAK2的9倍、JAK3的77倍、TYK2的420倍，通过精准抑制IL-4、IL-13、IFN-γ等炎症因子，减少对JAK2相关通路（如造血功能）的干扰，从而降低贫血、中性粒细胞减少等风险。这一特性在Ⅱ期临床中已得到验证（SALT评分降幅达30.5%-56.1% vs 安慰剂组19.9%），Ⅲ期数据进一步巩固其疗效与安全性平衡的优势。第24周主要终点：艾玛昔替尼4mg组和8mg组达到SALT≤20的患者比例分别为34.9%和40.6%，显著高于安慰剂组的9.0%（p<0.0001），效应值（OR）分别为5.2和6.9。具体实验数据可查看文末。艾玛昔替尼不仅针对斑秃，还在开发外用剂型（如碱凝胶），用于轻中度特应性皮炎和白癜风，可减少系统性副作用，提升患者依从性。同时，其适应症覆盖类风湿关节炎、强直性脊柱炎等自身免疫疾病，具备更广泛的市场潜力。同时期，礼来也在AAD年会上也公布关于巴瑞替尼（Baricitinib）在青少年斑秃治疗领域取得III期突破性进展的消息。结果显示，青少年人群的36周数据与成人人群的52周数据相当。将在未来几个月内提交巴瑞替尼治疗青少年斑秃的补充新药申请。百亿赛道烽烟起，首个国产JAK抑制剂花落谁家？在中国JAK抑制剂市场尚未实现国产化突破的背景下，恒瑞医药与泽璟制药围绕"首款国产JAK抑制剂"的竞争已进入白热化阶段。从竞争格局看，恒瑞医药艾玛昔替尼布局强直性脊柱炎(As)、中重度特应性皮炎、类风湿性关节炎和成人重度斑秃领域，虽有跨国公司竞争但是凭借医保政策倾斜，将为国产替代创造机遇。而泽璟制药的吉卡昔替尼选择的骨髓纤维化赛道，凭借"孤儿药"资格认定和临床急需性，可享受优先审评等政策红利，形成天然的竞争壁垒。恒瑞医药艾玛昔替尼预计2025年下半年获批斑秃适应症，并布局特应性皮炎、类风湿关节炎等领域。作为第二代高选择性JAK1抑制剂，其核心优势在于对JAK1亚型的高度特异性（选择性较JAK2高出16倍）。这种设计通过精准抑制炎症相关信号通路，大幅降低了第一代泛JAK抑制剂常见的血小板减少、贫血等JAK2抑制相关风险。泽璟制药盐酸吉卡昔替尼片，已完成重症斑秃III期临床试验，达到主要疗效终点，正在推进上市进程。2024年6月12日，泽璟制药宣布，公司自主研发的1类新药盐酸吉卡昔替尼片（曾用名：盐酸杰克替尼片）治疗重症斑秃的III期临床主试验《盐酸杰克替尼片治疗重症斑秃患者的有效性和安全性的多中心、随机、双盲、安慰剂平行对照III期临床试验》（方案编号：ZGJAK018）达到了主要疗效终点，达到统计显著性（p<0.0001）。公司将加快推进盐酸吉卡昔替尼片治疗重症斑秃患者适应症的上市进程。泽璟制药的杰克替尼虽属第一代泛JAK抑制剂，但通过差异化的适应症选择开辟了生存空间。该药物专注骨髓纤维化领域，其II期临床数据显示41.3%的有效率显著优于进口药芦可替尼的27%历史数据。更值得注意的是，杰克替尼展现出改善贫血的独特优势，可减少患者输血依赖，这一特性在目前全球仅芦可替尼获批的骨髓纤维化治疗领域形成差异化竞争力。科伦药业 KL130008胶囊，正在开展重度斑秃的II期临床试验。目前暂无消息。石药集团 SYHX1901片，正在开展非节段型白癜风和重度斑秃的II期临床试验。目前暂无消息。斑秃JAK抑制剂竞争格局（部分）数据来源：药智数据新疗法与新技术 ● S1P受体调节剂：如BMS的BMS-986165，通过调控免疫细胞迁移减少毛囊炎症。 ● Wnt通路激活剂：Samumed公司的SM04554通过激活毛囊干细胞促进再生，II期数据积极。 ● 基因疗法：RepliCel的RCH-01利用自体真皮鞘杯细胞修复毛囊，处于临床前阶段 ● 微针递送技术：如韩国CosmeRNA通过小核酸药物靶向抑制雄激素受体，已上市。结束语：市场尚未饱和，一片蓝海斑秃患者中，重度斑秃（如全秃、普秃）对生活质量影响极大，尤其是青少年患者，心理负担较重。现有治疗手段（如糖皮质激素、米诺地尔）疗效有限，患者对创新药物的需求极大。目前国内正在销售的巴瑞替尼挂网价每盒1064元（2mg*28片/盒），若按治疗斑秃需要每日服用4mg计算自费月费用为2千余元。南京力博维制药有限公司的“首仿”药品巴瑞替尼已于2023年10月13日获批，其价格为896元/2mg/28片，折合单片价格为32元，该仿制药已经上市销售。按照一些使用巴瑞替尼的案例，毛发完全生产需要9个月左右，总体价格对于患者来说价格仍然比较昂贵。未来，随着艾玛昔替尼预计2025年获批上市，吉卡昔替尼推进NDA进程，中国患者将首次拥有本土研发的高选择性靶向治疗方案，这不仅意味着治疗选择从“进口垄断”向“国产替代”的历史性跨越，更预示着中国药企在全球自免药物版图中从边缘走向核心的产业升级。当创新药的星辰大海照进现实，这场关于头顶生机的科技突围，终将转化为千万患者重拾尊严的生命曙光。补充内容：恒瑞医药艾玛昔替尼（Ivarmacitinib，SHR0302）Ⅲ期临床数据这项随机、双盲、安慰剂对照Ⅲ期研究（NCT05470413）纳入我国31家中心的330例重度斑秃患者（基线平均SALT评分≥78.6），随机分为艾玛昔替尼4mg组（n=109）、8mg组（n=111）和安慰剂组（n=110），核心治疗期24周后，安慰剂组患者转至艾玛昔替尼治疗，并延长观察至52周。主要终点为第24周时SALT评分≤20（头皮脱发≤20%）的患者比例，次要终点包括患者满意度、长期疗效及安全性。第24周主要终点：艾玛昔替尼4mg组和8mg组达到SALT≤20的患者比例分别为34.9%和40.6%，显著高于安慰剂组的9.0%（p<0.0001），效应值（OR）分别为5.2和6.9。早期应答：第8周时，两治疗组SALT≤20比例已显著优于安慰剂组（p值未披露），提示快速改善脱发症状。长期持续改善：至第52周，4mg和8mg组SALT≤20比例进一步提升至46.8%和63.1%，且SALT评分绝对值和百分比变化持续优化。安全性可控：治疗相关不良事件（AE）发生率与安慰剂组相当（4mg组77.1% vs 8mg组84.7% vs 安慰剂组75.5%），主要为轻中度感染（如COVID-19、上呼吸道感染），未报告死亡、血栓栓塞或重大心血管事件。仅2例严重感染（带状疱疹、复杂性阑尾炎）及2例恶性肿瘤（滤泡性淋巴瘤、甲状腺癌），均被判定与药物无关。喜欢我们文章的朋友点个“在看”和“赞”吧，不然微信推送规则改变，有可能每天都会错过我们哦~ 免责声明 “汇聚南药”公众号所转载文章来源于其他公众号平台，主要目的在于分享行业相关知识，传递当前最新资讯。图片、文章版权均属于原作者所有，如有侵权，请在留言栏及时告知，我们会在24小时内删除相关信息。信息来源：求实药社往期推荐本平台不对转载文章的观点负责，文章所包含内容的准确性、可靠性或完整性提供任何明示暗示的保证。

临床3期

2025-03-13

·研发客

自免战歌起，强生口服多肽站上C位，多家中国公司闪亮登场｜2025 AAD

// • 强生口服多肽icotrokinra展现出重塑中重度斑块状银屑病治疗标准的潜力； • 多家中国公司也展示各自在研产品治疗中重度斑块状银屑病的研究成果； • BMS尝试突破突围，寻求氘可来昔替尼更广阔的适应症； • Q32 Bio治疗斑秃的核心产品被医生看好，但投资人并不买账； • 特应性皮炎治疗领域将迎来OX40抑制剂新生力军。随着自免领域的研发热度持续升温，一众参赛选手开始亮出阶段性研究成果。在刚刚落幕的2025年美国皮肤病学会（AAD）年会上，或许能窥见这个赛道未来将诞生哪些“重磅炸弹”。银屑病可能是今年大会最受关注的治疗领域之一。其中，强生的IL-23受体（IL-23R）靶向拮抗多肽icotrokinra站上舞台C位，不仅显著疗效，对比BMS的TYK2变构抑制剂氘可来昔替尼也不落下风，展现出重塑中重度斑块状银屑病治疗标准的潜力。来自诺诚健华、益方生物和翰森制药/荃信生物等中国公司的新药也纷纷闪亮登场。氘可来昔替尼四面受敌，不过BMS没有退缩，而是转战银屑病关节炎、红斑狼疮等其他疾病领域。此外，Q32 Bio、礼来、恒瑞医药等竞相布局斑秃市场，安进/协和麒麟和赛诺菲则在特应性皮炎上争夺“first-in-class”的宝座。大获全胜作为银屑病巨头，强生在该领域的新药研发经验毋庸置疑。与此前推出的英夫利西单抗、戈利木单抗、乌司奴单抗、古塞奇尤单抗等均为注射液不同，icotrokinra（JNJ-2113）采用更为便利的口服给药方式。早在去年11月，强生就宣布icotrokinra在关键性3期研究ICONIC-LEAD中取得积极结果。此次大会公布了该研究的完整结果，显示该产品每日一次在12岁及以上中重度斑块状银屑病患者中显著的皮肤清除率与良好安全性。数据显示，第16周时，icotrokinra组65%的患者达到IGA 0/1，即皮肤症状清除或几乎清除，50%患者达到PASI 90，即银屑病面积与严重程度指数改善至少90%。在第24周时，PASI 90应答率提升至65%，74%达到IGA 0/1，近半数患者实现皮肤完全清除（46%达IGA 0，40%达PASI 100）。另外，icotrokinra还在Ⅲ期ICONIC-ADVANCE 1/2研究中，在第16周达到IGA 0/1与PASI 90的共同主要终点，并在所有关键次要终点中显著优于氘可来昔替尼。氘可来昔替尼是过去10余年来首个获批治疗中重度斑块状银屑病的口服疗法，其他创新疗法以注射用的单抗为主。现在，这种治疗格局可能很快就要被打破。据悉，强生将启动首个斑块状银屑病头对头研究ICONIC-ASCEND，以证明口服给药的icotrokinra相较于注射用生物制剂乌司奴单抗的优效性。神仙打架在BMS和强生后面奋起直追的还有多家中国公司。其中，诺诚健华与益方生物都在本次大会亮出各自开发的口服TYK2抑制剂治疗中重度斑块状银屑病的Ⅱ期研究成果。其中，诺诚健华ICP-488经12周治疗后，每天一次6mg和9mg剂量组的PASI 75应答率分别为77.3%和78.6%，PASI 90应答率分别达到36.4%和50.0%，sPGA 0/1（即皮损完全清除或基本清除）应答率分别为70.5%和71.4%。益方生物D-2570经12周治疗后，18mg、27mg、36mg剂量组的PASI 75应答率分别为90.0%、85.4%和85.0%，PASI 90应答率分别为75.0%、70.7%和77.5%，PASI 100应答率分别为40.0%、39.0%和50.0%，sPGA 0/1应答率分别为82.5%、80.5%和87.5%。单从数值来看，ICP-488的PASI 90应答率在第12周时与icotrokinra第16周时旗鼓相当，而D-2570则更胜一筹。益方生物在新闻稿中表示，D-2570的疗效数据优于已上市的同类TYK2抑制剂，并且在效果上可与IL-17A、IL-23等抗体生物药相媲美。在注射疗法方面，翰森制药与荃信生物合作开发的长效疗法HS-20137也值得关注。这是一款靶向IL-23的人源化IgG1单抗，翰森制药于2024年4月获得其独家权益。 Ⅱ期临床数据显示，HS-20137在中重度斑块状银屑病患者中起效迅速，200mg每八周给药一次剂量组治疗16周后PASI 75、PASI 90应答率分别为92.3%和76.9%，该比例在第20、24和28周时分别达到84.6%、89.7%和87.2%。试验还设置了200mg每十二周给药一次剂量组，16周时PASI 100高达40%。 BMS的守与攻眼下，全球银屑病市场获批疗法众多，针对TNF-α、IL-12/23、IL-23、IL-17A、IL-36等靶点的新药层出不穷，生物类似药来势汹汹，新一代的口服、长效疗法也试图杀出重围。在这种背景下，氘可来昔替尼的处境可谓前有狼后有虎。不过BMS并未坐以待毙，而是在更广阔的适应症中找寻出路。本次大会上，BMS首度公布了氘可来昔替尼治疗活动性银屑病关节炎（PsA）成人患者的Ⅲ期POETYK PsA-2（IM011-055）试验结果，证实了其在改善关节及皮肤症状、提升患者报告生活质量方面的潜力。数据显示，治疗组在16周后ACR20（疾病体征和症状至少改善20%）应答比例达到54.2%，显著高于安慰剂组的39.4%。此外，研究还达到了多个关键次要终点，并展现良好的耐受性和安全性特征。除了POETYK PsA-2，氘可来昔替尼另一项针对PsA的Ⅲ期研究POETYK PsA-1也在去年12月达到了主要终点和关键次要终点。这些研究结果均表明，口服氘可来昔替尼有可能成为PsA患者的首个TYK2抑制剂。此外，该药还在开展治疗红斑狼疮的全球Ⅱ期PAISLEY CLE研究，同样可能帮助这款口服TYK2抑制剂摆脱“银屑病专药”的标签。下一位斑秃克星作为仅次于雄激素性脱发的第二大脱发类疾病，斑秃市场潜力巨大。随着礼来的巴瑞替尼、辉瑞的利特昔替尼和太阳制药的deuruxolitinib等JAK抑制剂相继获批，这个领域的参与者也在加紧步伐。比如Q32 Bio。在今年2月经历大幅裁员、重组并砍掉肾脏管线后，这家Biotech正全力推进其核心资产bempikibart用于中重度斑秃的Ⅱ期研究。bempikibart是一款IL-7/TSLP双功能受体拮抗剂，通过阻断IL-7和TSLP信号重新调节适应性免疫功能。在本次AAD大会上，Q32 Bio公布了2a期斑秃试验SIGNAL-AA的结果，bempikibart用于重度及极重度斑秃患者，第24周SALT评分（头皮脱发）显著改善，且停药后疗效持续。尽管只有24周的给药，多名患者在36周的随访期间获得持续的反应，甚至超过55周。目前，bempikibart的开发计划进展顺利，开放标签扩展研究将于2025年上半年启动，SIGNAL-AA Part B研究预计于2025年上半年开始给药，关键数据2026年上半年公布。康涅狄格州皮肤病医生Brett King博士评论道：“重症患者在治疗24周后甚至停药数周仍显示疗效，这一现象非常引人注目。若bempikibart的活性（包括诱导长期缓解的潜力）及安全性在后续试验中得以验证，它有望改变斑秃的治疗范式。” 不过这一数据并未说服投资人，消息公布后，Q32 Bio股价已连续两日下跌7%以上。部分分析师认为bempikibart在斑秃中的疗效可能不及现有疗法。礼来的JAK1/2抑制剂巴瑞替尼则瞄准了12岁至18岁的严重斑秃青少年这一群体。大约40%的斑秃患者在20岁前首次发病。在AAD上公布的3期BRAVE-AA-PEDS研究结果显示，在第36周接受每日一次口服巴瑞替尼 4mg和2mg治疗后，患者头皮、眉毛和睫毛的头发再生得到了临床意义上的改善。42.4%的患者接受巴瑞替尼4mg治疗后，第36周头皮头发覆盖率达到80%以上。如果巴瑞替尼在这一年轻群体中获批，将直接对垒辉瑞的JAK3/TEC抑制剂利特昔替尼，这是全球首款获批同时用于治疗12岁及以上青少年及成人重度斑秃患者的创新药物。此外，恒瑞医药也携其JAK1抑制剂硫酸艾玛昔替尼片的Ⅲ期成果加入斑秃战场。数据显示，该药在第8周即可改善成人重度斑秃患者症状，4mg和8mg剂量组24周时分别有34.9%和40.6%的患者达到SALT评分≤20，显著优于安慰剂组。在治疗核心期和延长期间，达到SALT评分≤20的患者比例持续增加。 OX40抑制剂在AD中的突破目前，全球范围内尚未有OX40抑制剂获批上市，而安进/协和麒麟的rocatinlimab及赛诺菲的amlitelimab，是自免领域临床进度较快的两个选手。在本次AAD大会上公布的Ⅲ期IGNITE试验的最新数据显示，rocatinlimab有望争夺特应性皮炎（AD）领域“first-in-class”的宝座。在为期24周的研究中，rocatinlimab达到了共同主要终点和所有关键次要终点，两种剂量均显示具有统计学意义的疾病活动性降低。高剂量组中42.3%的患者湿疹面积和严重程度指数评分较基线降低≥75%（EASI 75），低剂量组中36.3%的患者达到EASI 75。这支持了rocatinlimab作为特应性皮炎一种新治疗选择的潜力。安进计划在ASCEND试验中进一步探索该药超过24周的效果，并在ASTRO和ORBIT试验中评估其在青少年患者中的作用。尽管取得了积极的成果，专家和分析人士预计，rocantinlimab的应用将被降至二线治疗领域，而且它可能必须面对来自赛诺菲OX40L单抗amlitelimab的竞争。后者也在本次大会上海报展示了针对中重度AD患者的STREAM-AD与RIVER-AD研究结果。 RIVER-AD是一项单臂长期扩展Ⅱ期研究。此次大会首次公布了该研究的中期分析结果，主要针对Ⅱb期STREAM-AD试验中第24周未达到EASI-75或IGA 0/1应答的患者，统一予以amlitelimab 250mg Q4W，并于治疗28周评估有效性和安全性。结果显示，试验组和安慰剂组患者进入这项扩展研究时的EASI评分与STREAM-AD研究基线时的EASI评分相比，平均降低了35.8%和18.3%；治疗第28周，EASI评分分别较基线下降了83.4%和85.2%；同时，治疗28周时的EASI-75、EASI-90、IGA 0/1应答率与STREAM-AD研究第24周的应答率相当。这一数据展现了amlitelimab在特应性皮炎中的潜力。它提供了一种独特的作用机制，可以帮助使过度活跃的免疫系统正常化，并在不消耗T细胞的情况下恢复免疫平衡。编辑 | 姚嘉 yao.jia@PharmaDJ.com 总第2360期访问研发客网站，深度报道和每日新闻抢鲜看 www.PharmaDJ.com

临床3期申请上市临床成功

2025-03-09

·Firstwordpharma

AAD25: Lilly, Incyte's Olumiant gains ground in severe adolescent alopecia with late-stage success

Eli Lilly and Incyte’s once-daily oral JAK1/2 inhibitor Olumiant (baricitinib) demonstrated notable improvements in hair regrowth on the scalp, eyebrows and eyelashes in a Phase III study of adolescents with severe alopecia areata (AA), moving the drug a step closer to taking on Pfizer’s JAK3/TEC kinase inhibitor Litfulo (ritlecitinib) — the first alopecia medication approved for the younger age group in the US and EU. The findings were presented over the weekend at the American Academy of Dermatology (AAD) annual meeting.Backed by the BRAVE-AA1 and BRAVE-AA2 trials, Olumiant secured FDA authorisation in 2022 for adults with severe AA, making it the first systemic treatment approved in the US for the condition.The BRAVE-AA-PEDS study randomised 257 participants aged 12 to under 18 to receive daily baricitinib 2 mg, 4 mg or placebo — the primary efficacy goal being Severity of Alopecia Tool (SALT) score ≤20 at 36 weeks. Results showed that at this timepoint, 42.4% of patients receiving the 4-mg dose achieved the main goal, compared with 4.5% in the placebo group. Moreover, Olumiant 4 mg led to at least a 50% disease improvement in 60% of patients, while the 2 mg dose achieved the same in 36.9%, and placebo in 5.7%.Specifically, Olumiant 4 mg achieved 90% scalp hair coverage in 36.5% of patients, significant eyebrow regrowth in 50.0%, and eyelash regrowth in 42.9%, while the 2 mg dose showed 21.4%, 24.1%, and 25.5% improvement, respectively. In contrast, placebo results were 2.3% for scalp, 0% for eyebrows and 14.0% for eyelashes. Notably, outcomes in adolescents achieved at 36 weeks were comparable to those seen in adult studies at 52 weeks, suggesting faster hair regrowth in the former. Meanwhile, the safety profile in adolescents was consistent with previous Olumiant trials in juvenile idiopathic arthritis and atopic dermatitis. "With these data, baricitinib is the most well-studied JAK inhibitor in severe alopecia areata," remarked Anabela Cardoso, senior vice president of immunology medical affairs at Lilly. The drugmaker plans to present additional data from BRAVE-AA-PEDS later this year, whilst also discussing the findings with global regulators.Following the footsteps of Olumiant and Litfulo, Sun Pharmaceutical’s oral JAK1/2 inhibitor Leqselvi (deuruxolitinib) entered the severe AA market last year, albeit only approved for adults. Also at AAD this year, Q32 Bio unveiled upbeat mid-stage data for its IL-7/TSLP bifunctional receptor antagonist, bempikibart, in severe to very severe disease. For more on the severe AA space, read: Spotlight On: AAD25 – Lilly's data puts Pfizer on notice while Q32 Bio plays long game in alopecia areata.

临床结果上市批准临床3期

100 项与甲苯磺酸利特昔替尼相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB14924

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10 条最早获批的记录,

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适应症	国家/地区	公司	日期
斑秃	美国	Pfizer Inc.	2023-06-23

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适应症	最高研发状态	国家/地区	公司	日期
非节段型白癜风	临床3期	美国	Pfizer Inc.	2022-12-01
非节段型白癜风	临床3期	中国	Pfizer Inc.	2022-12-01
非节段型白癜风	临床3期	日本	Pfizer Inc.	2022-12-01
非节段型白癜风	临床3期	澳大利亚	Pfizer Inc.	2022-12-01
非节段型白癜风	临床3期	保加利亚	Pfizer Inc.	2022-12-01
非节段型白癜风	临床3期	加拿大	Pfizer Inc.	2022-12-01
非节段型白癜风	临床3期	德国	Pfizer Inc.	2022-12-01
非节段型白癜风	临床3期	印度	Pfizer Inc.	2022-12-01
非节段型白癜风	临床3期	意大利	Pfizer Inc.	2022-12-01
非节段型白癜风	临床3期	墨西哥	Pfizer Inc.	2022-12-01

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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


NCT06172348 (CTgov)	临床1期	白癜风	12	Ritlecitinib (Ritlecitinib 100 mg Oral Solution (Fasted))	鹽繭願繭蓋選壓蓋範壓(窪淵築遞襯壓蓋廠選構) = 範製淵積蓋糧夢窪獵觸鬱鹹鹹簾窪糧艱範膚鑰 (構憲壓廠醖廠憲壓願鬱, 24) 更多	-	2025-04-10
				MR1+Ritlecitinib (Ritlecitinib 100 mg MR1 Capsule (Fasted))	鹽繭願繭蓋選壓蓋範壓(窪淵築遞襯壓蓋廠選構) = 遞蓋鑰獵獵衊網觸齋齋鬱鹹鹹簾窪糧艱範膚鑰 (構憲壓廠醖廠憲壓願鬱, 25) 更多
NCT04006457 (ALLEGRO-LT, Pubmed \| J Eur Acad Dermatol Venereol)	临床3期	斑秃	449	Ritlecitinib 200mg loading dose followed by 50mg daily	糧鏇膚窪鑰淵衊膚構廠(襯襯積鑰蓋網衊遞鹽築) = occurred in six patients 選製餘餘醖鑰醖壓鑰窪 (鹹範衊範淵願廠憲獵簾 ) 更多	积极	2025-01-23
NCT03395184 (CTgov)	临床2期	克罗恩病	244	Placebo (Induction Period: Placebo QD)	網簾淵鹹糧壓淵醖艱製 = 醖壓鑰鏇鏇廠顧鏇積願製範衊網艱廠網齋憲築 (簾繭糧鹹蓋製壓夢鑰顧, 繭膚鬱顧鹹襯夢製構艱 ~ 鹽鹽膚網簾壓網繭選鹹) 更多	-	2024-10-30
				Ritlecitinib (Induction Period: Ritlecitinib 200 mg/50 mg QD)	網簾淵鹹糧壓淵醖艱製 = 積糧鬱醖鏇憲鏇鹽積糧製範衊網艱廠網齋憲築 (簾繭糧鹹蓋製壓夢鑰顧, 糧願淵廠壓衊構餘淵鏇 ~ 製構範壓糧顧夢鬱觸簾) 更多
NCT03732807 (ALLEGRO, Pubmed \| Am J Clin Dermatol)	临床2/3期	斑秃	718	Ritlecitinib 50 mg	艱襯構壓獵選衊製夢顧(餘築廠鹹繭膚憲範鹽積) = 獵觸壓膚築衊齋築餘廠網網選願構選繭鹹蓋願 (願壓遞願製鹹襯顧蓋鑰 )	积极	2024-10-23
				Ritlecitinib 30 mg	艱襯構壓獵選衊製夢顧(餘築廠鹹繭膚憲範鹽積) = 齋夢製觸簾範鏇襯願網網網選願構選繭鹹蓋願 (願壓遞願製鹹襯顧蓋鑰 )
NCT03732807 \| NCT04006457 (ALLEGRO-2b/3 \| ALLEGRO Phase 2b/3 \| ALLEGRO phase 2b/3 study \| ALLEGRO, Pubmed \| Br J Dermatol) 人工标引	临床2/3期	斑秃	385	Ritlecitinib 50 mg	糧願餘鬱鹹獵鬱膚衊膚(衊鬱廠壓襯衊鬱獵構壓) = 構製願淵醖鹽憲觸製選獵獵鑰餘範夢壓遞積壓 (鬱夢壓艱繭獵遞淵鹹夢 ) 更多	积极	2024-10-21
				Ritlecitinib 200/50 mg	糧願餘鬱鹹獵鬱膚衊膚(衊鬱廠壓襯衊鬱獵構壓) = 獵膚醖壓製選製鏇鏇願獵獵鑰餘範夢壓遞積壓 (鬱夢壓艱繭獵遞淵鹹夢 ) 更多
NCT05650333 (Phase 1, CTgov)	临床1期	斑秃	15	Ritlecitinib 20 mg	壓選鑰獵醖餘顧餘艱鹽(鹽鹹觸醖襯繭製膚齋觸) = 膚糧繭選蓋簾艱製網積遞襯夢觸獵範構顧選憲 (餘鏇蓋窪積願膚鬱鹽醖, 30) 更多	-	2024-10-08
NCT03732807 (ALLEGRO phase 2b/3, Pubmed \| Dermatol Ther (Heidelb))	临床2/3期	斑秃	522	Ritlecitinib 30 mg	醖選糧獵築構淵衊遞醖(網網範鹽淵製窪範範艱): OR = 2.12 (95% CI, 1.23 ~ 3.65), P-Value = < 0.05	积极	2024-09-10
				Ritlecitinib 50 mg
NCT05128058 (CTgov)	临床1期	-	16	RITLECITINIB (RITLECITINIB 50 MG CAPSULE)	夢窪壓繭築壓壓齋築積(窪網積糧觸繭鬱膚膚網) = 顧鹽窪廠齋齋艱蓋鹽衊壓繭範淵簾選鏇遞鬱衊 (製糧鹽選製願餘衊鹽夢, 製壓網範製網鏇顧廠範 ~ 餘網糧艱製觸繭鹽廠繭) 更多	-	2023-11-13
				RITLECITINIB (RITLECITINIB 200 MG CAPSULE)	夢窪壓繭築壓壓齋築積(窪網積糧觸繭鬱膚膚網) = 觸構襯顧願蓋繭繭衊襯壓繭範淵簾選鏇遞鬱衊 (製糧鹽選製願餘衊鹽夢, 壓糧膚壓鹽繭鏇鹽觸鏇 ~ 構製淵觸構積範夢衊觸) 更多
NCT03732807 (ALLEGRO phase 2b/3, EADV2023)	临床2/3期	斑秃	191	Ritlecitinib 50mg QD	廠製夢觸顧選願淵築鹹(鹹淵艱鹹淵願糧淵獵糧) = 鏇膚鬱蓋願鏇範艱艱餘鬱鑰醖襯艱觸鏇鏇鬱蓋 (鬱膚鹹鬱廠選繭夢餘襯 ) 更多	-	2023-10-11
NCT04006457 (ALLEGRO-LT, EADV2023)	临床3期	斑秃	447	Ritlecitinib 200 mg	鬱艱艱襯願襯齋鏇窪憲(鏇顧艱觸餘廠鏇繭齋餘) = 構鑰膚衊積襯鑰齋蓋築憲壓範齋構廠願鏇繭簾 (構構製製餘築夢網醖醖 ) 更多	-	2023-10-11
				Ritlecitinib 50 mg	鬱艱艱襯願襯齋鏇窪憲(鏇顧艱觸餘廠鏇繭齋餘) = 淵鹽襯憲糧鹹壓鏇齋觸憲壓範齋構廠願鏇繭簾 (構構製製餘築夢網醖醖 ) 更多