Icotrokinra(Icotrokinra) - 药物靶点：IL-23R_在研适应症：斑块状银屑病，溃疡性结肠炎，银屑病关节炎_专利_临床

概要

基本信息

药物类型

合成多肽

别名

JNJ 67864238、JNJ-2113、JNJ-4238

+ [7]

靶点

IL-23R

作用方式

抑制剂

作用机制

IL-23R抑制剂(白细胞介素23受体抑制剂)

治疗领域

免疫系统疾病皮肤和肌肉骨骼疾病其他疾病+ [2]

在研适应症

斑块状银屑病溃疡性结肠炎银屑病关节炎+ [3]

非在研适应症-

原研机构

Protagonist Therapeutics, Inc.

在研机构

Janssen Pharmaceutica NVJanssen Research & Development LLC

强生（中国）投资有限公司

+ [2]

非在研机构

Protagonist Therapeutics, Inc.

权益机构

Protagonist Therapeutics, Inc.

Janssen Biotech, Inc.

最高研发阶段申请上市

首次获批日期-

最高研发阶段(中国)临床3期

特殊审评-

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结构/序列

Sequence Code 1311911322

来源: *****

关联

31

项与 Icotrokinra 相关的临床试验

NCT07196748

/ Recruiting临床3期

A Phase 3 Randomized, Double-blind, Placebo-Controlled, Parallel Group, Multicenter Protocol in Adults With an Open Label Study in Adolescents to Evaluate the Efficacy and Safety of Induction and Maintenance Therapy With Icotrokinra in Participants With Moderately to Severely Active Ulcerative Colitis

The purpose of this protocol is to evaluate the efficacy (how well it works), safety and tolerability of oral icotrokinra as therapy in adult and adolescent participants with moderately to severely active ulcerative colitis (UC, a chronic disease of the large intestine in which the lining of the colon becomes inflamed and develops tiny open ulcers).

开始日期2025-10-01

申办/合作机构

Janssen Research & Development LLC

NCT07196722

/ Recruiting临床2/3期

A Phase 2b/3 Randomized, Double-blind, Placebo-Controlled, Parallel Group, Multicenter Protocol to Evaluate the Efficacy and Safety of Icotrokinra in Participants With Moderately to Severely Active Crohn's Disease

The purpose of this study is to evaluate how-well icotrokinra works (clinical efficacy) and how safe it is (safety) in participants with moderately to severely active Crohn's disease (CD; a long-term condition causing severe inflammation of the intestinal tract).

开始日期2025-10-23

申办/合作机构

Janssen Research & Development LLC

CTRI/2025/04/084956

/ Not yet recruiting临床3期

A Phase 3, Multicenter, Randomized, Double-blind, Placebo-controlled Study Evaluating the Efficacy and Safety of JNJ-77242113 for the Treatment of Biologic-experienced Participants with Active Psoriatic Arthritis - ICONIC-PsA 2

开始日期2025-05-16

申办/合作机构-

100 项与 Icotrokinra 相关的临床结果

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100 项与 Icotrokinra 相关的转化医学

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100 项与 Icotrokinra 相关的专利（医药）

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7

项与 Icotrokinra 相关的文献（医药）

2025-09-01·Dermatology and Therapy

Translational Pharmacokinetics of Icotrokinra, a Targeted Oral Peptide that Selectively Blocks Interleukin-23 Receptor and Inhibits Signaling

Article

作者: Patel, Shefali ; Shi, Yifan ; Baguet, Tristan ; Ndifor, Anthony ; Wang, Jianyao ; Somani, Sandeep ; Sensenhauser, Carlo ; Park, Seonghee ; Adriaenssen, Lieve ; Leclercq, Laurent ; Fourie, Anne ; Mardirosian, Saro ; Monshouwer, Mario ; Dallas, Shannon ; Chaudhuri, Siladitya Ray ; Knight, Beverly ; Sukumaran, Siddharth ; Polidori, David ; Patch, Raymond ; Sun, Chengzao ; DiLoreto, Karen ; Barros, Stephanie A ; Tammara, Brinda ; Geist, Brian ; Modi, Nishit B ; Moss, Darren ; Laenen, Aline

INTRODUCTION:

Icotrokinra (formerly JNJ-77242113 or PN-21235) is a targeted oral peptide that selectively inhibits interleukin-23 receptor signaling. The studies described here assessed its absorption, distribution, metabolism, and excretion (ADME), and potential for drug-drug interactions (DDI).

METHODS:

In vitro assays evaluated permeability, plasma protein binding, blood-to-plasma partitioning, metabolic stability, and interactions with drug transporters and metabolic enzymes. The nonclinical pharmacokinetic properties of icotrokinra were studied in vivo in rats and monkeys. Phase 1 studies evaluated the pharmacokinetic profile, metabolic profile and excretion in healthy volunteers.

RESULTS:

Icotrokinra demonstrated oral bioavailability of 0.1-0.3% in animals, with evidence of systemic pharmacodynamic activity, without the use of an absorption enhancer. The compound was stable across species in plasma, gastrointestinal matrices, and hepatocytes. Protein binding was low across species (~ 50% in human plasma), and icotrokinra distributed freely to tissues, including skin, joints, and gastrointestinal tissues. Following oral dosing in both rats and monkeys, fecal excretion of unabsorbed drug was the primary elimination route, and metabolite levels were low (each < 2% of dose) in plasma and excreta, with unchanged icotrokinra being the main circulating component. Icotrokinra was neither a substrate nor an inhibitor of prototypical drug transporters or cytochrome P450 enzymes. Icotrokinra exhibited dose-proportional pharmacokinetics from 25 mg to 1000 mg in a first-in-human study, and no serious adverse events were identified following single and multiple dose administrations. Unchanged icotrokinra was the only drug-related component in human plasma.

CONCLUSIONS:

Icotrokinra exhibited high stability and an ADME profile consistent with that of a small peptide, with no risk of DDI identified on the basis of in vitro studies. Clinical data demonstrated linear pharmacokinetics and no major metabolites.

TRIAL REGISTRATION NUMBER:

ClinicalTrials.gov, NCT04621630. Euclinicaltrials.eu, EUCT: 2023-504720-26-00. A Graphical Abstract is available for this article.

2025-09-01·LANCET

Once-daily oral icotrokinra versus placebo and once-daily oral deucravacitinib in participants with moderate-to-severe plaque psoriasis (ICONIC-ADVANCE 1 & 2): two phase 3, randomised, placebo-controlled and active-comparator-controlled trials

Article

作者: Papp, Kim A ; Bissonnette, Robert ; Magnolo, Nina ; Arnone, Marcelo ; Schwarz, Beate ; Kephart, Lea ; Galimberti, Maria Laura ; Gonzalez-Cantero, Alvaro ; Riera-Monroig, Josep ; Kircik, Leon ; Vender, Ronald B ; Campbell, Jennifer H ; Nunes, Fabio ; Edem, Bassey Effiom ; Tada, Yayoi ; Sebastian, Michael ; Waibel, Jill ; Tsianakas, Athanasios ; DeKlotz, Cynthia M C ; Cecchini, Michael ; Simon, Margrit ; Li, Shu ; Reyes-Servin, Ofelia ; Shen, Yaung-Kaung ; Gold, Linda Stein ; Cresswell, Kellen ; Wallace, Paul ; Gerdes, Sascha ; Armstrong, April W ; Ehst, Benjamin

BACKGROUND:

Monoclonal antibodies targeting interleukin-23 and interleukin-12 are efficacious in treating plaque psoriasis but must be delivered via intravenous or subcutaneous injection. Here, we aimed to evaluate the efficacy and safety of icotrokinra (JNJ-77242113), a targeted oral peptide that selectively binds the interleukin-23 receptor, compared with both placebo and deucravacitinib in adults with moderate-to-severe plaque psoriasis.

METHODS:

The phase 3, randomised, double-blind, placebo-controlled and active-comparator-controlled ICONIC-ADVANCE 1 and ICONIC-ADVANCE 2 trials, which are being done at 149 sites across 13 countries and 114 sites across 11 countries, respectively, randomly assigned (2:1:2 and 4:1:4, respectively) adults with moderate-to-severe plaque psoriasis diagnosed for at least 26 weeks (body-surface-area involvement ≤10%, Psoriasis Area and Severity Index [PASI] ≤12, and Investigator's Global Assessment [IGA] ≤3) to once-daily oral icotrokinra 200 mg, placebo, or deucravacitinib 6 mg; participants randomly assigned to placebo or deucravacitinib transitioned to icotrokinra at week 16 or week 24, respectively. Coprimary endpoints were proportions of participants achieving IGA 0 or 1 (clear or almost clear skin) with at least a two-grade improvement and at least 90% improvement in PASI (PASI 90) at week 16 with icotrokinra versus placebo. These studies are registered with ClinicalTrials.gov, NCT06143878 (ADVANCE 1) and NCT06220604 (ADVANCE 2), and are ongoing.

FINDINGS:

ICONIC-ADVANCE 1 enrolled participants from Jan 17, 2024, to May 24, 2024, and ICONIC-ADVANCE 2 enrolled participants from March 9, 2024, to June 13, 2024. Participants (ADVANCE 1: 774 of 988 patients screened; ADVANCE 2: 731 of 917 patients screened) were randomly assigned to icotrokinra (n=311 and 322), placebo (n=156 and 82), or deucravacitinib (n=307 and 327). All coprimary endpoints were met in both trials. Higher proportions of icotrokinra-treated versus placebo-treated participants achieved IGA 0 or 1 (ADVANCE 1: 213 [68%] of 311 vs 17 [11%] of 156, treatment difference 95% CI 58% [50-64]; ADVANCE 2: 227 [70%] of 322 vs seven [9%] of 82, 62% [53-69]; both p<0·0001) and PASI 90 (ADVANCE 1: 171 [55%] of 311 vs six [4%] of 156, treatment difference 95% CI 51% [44-57]; ADVANCE 2: 184 [57%] of 322 vs one [1%] of 82, 56% [48-62]; both p<0·0001) at week 16. Across studies, adverse event rates to week 16 were 303 (48%) of 632 and 136 (57%) of 237 with icotrokinra and placebo, respectively; the most common adverse events were nasopharyngitis (37 [6%] of 632 and 13 [5%] of 237) and upper respiratory tract infection (23 [4%] of 632 and eight [3%] of 237). To week 24, adverse event rates were lower than with icotrokinra (359 [57%] of 632) than deucravacitinib (411 [65%] of 634).

INTERPRETATION:

Icotrokinra showed superior clinical response rates versus placebo and deucravacitinib in phase 3 moderate-to-severe plaque psoriasis trials, with similar adverse event rates to placebo. These findings suggest the potential of once-daily oral icotrokinra to provide robust efficacy and a favourable safety profile.

FUNDING:

Johnson & Johnson.

2025-09-01·LANCET

Icotrokinra in psoriasis: IL-23 receptor antagonism via oral peptide with biologic-level efficacy

Article

作者: Puig, Luis

253

项与 Icotrokinra 相关的新闻（医药）

2025-10-10

·新药猎人笔记

市值54亿美元！强生拟收购Protagonist，股价飙升30%

据《华尔街日报》消息，强生公司（Johnson & Johnson）正在与Protagonist Therapeutics（NASDAQ：PTGX）洽谈收购事宜。受此消息影响，Protagonist Therapeutics股价在10月10日收盘时飙升30%，达到87美元，总市值54亿美元。合作核心项目：Icotrokinra Protagonist Therapeutics是一家专注于新型肽治疗药物开发的生物制药公司。其核心管线Icotrokinra（JNJ-2113）是一种靶向口服多肽，能够选择性阻断IL-23受体（IL-23R），该受体在多种炎症性疾病的发病机制中起关键作用。Icotrokinra由Protagonist与强生共同发现，并依据双方许可及合作协议进行开发。 2025年3月，强生公布了Icotrokinra治疗溃疡性结肠炎的2b期临床数据，结果显示该药物在第12周时，最高剂量组的临床响应率达到63.5%，临床缓解率达到30.2%，显著优于安慰剂。此外，Icotrokinra在治疗中重度斑块状银屑病的3期临床试验中也展现出良好的疗效和安全性。展现出临床BIC潜力。第16周主要终点达成： - IGA 0/1（皮肤完全或几乎完全清除）：Icotrokinra组达65%，安慰剂组仅8%（P<0.001）。 - PASI 90（皮损严重度改善≥90%）：Icotrokinra组达50%，安慰剂组仅4%（P<0.001）。第24周疗效持续提升： - IGA 0/1提升至74%，PASI 90提升至65%；完全清除（IGA 0或PASI 100）比例分别达46%和40%，显著优于安慰剂组45 目前，强生已持有Protagonist近4%的股份，并拥有Icotrokinra的独家商业化权。如果收购完成，强生将能够进一步巩固其在免疫疾病治疗领域的地位，并加速Icotrokinra的市场推广。 Protagonist Therapeutics pipline 结束语：此次收购传闻正值强生希望加强其药物管线之际。其最畅销的免疫疾病药物Stelara的市场份额正在被成本更低的生物仿制药所取代，公司已警告称销售额将加速下滑。而Icotrokinra被认为可能成为“本十年中推出的最具影响力的免疫学药物之一”，其全球销售峰值预计可达95亿美元。接棒公司下一代自免重磅药物。

2025-10-10

·Medaverse

市值54亿美元！强生拟收购Protagonist

10月10日，华尔街日报报道称强生公司（NYSE：JNJ）正在与合作伙伴Protagonist Therapeutics（NASDAQ：PTGX）进行收购谈判，随后Protagonist美股盘中大涨，截止收盘每股87美元，涨幅约30%，最新市值54亿美元。（146亿美元！强生收购Intra-Cellular）据悉该交易的细节尚未敲定，预计将巩固强生与这家总部位于加利福尼亚州的公司的现有合作关系。知情人士表示，最终协议无法保证，正在讨论的交易条款无法获得。一笔潜在的交易预计将大大超过Protagonist的市值，包括交易溢价，并通过两种实验药物推动强生的免疫和癌症药物组合。两家公司合作开发的口服环肽IL-23抑制剂口服IL-23环肽icotrokinra，一种治疗包括斑块状银屑病和溃疡性结肠炎在内的免疫疾病的口服疗法，强生拥有该产品商业化的独家许可。强生的Stelara（乌司奴单抗注射液）最近在美国失去了专利独占权，该公司于7月向美国FDA提交了一份新药申请，寻求icotrokinra治疗斑块状银屑病的上市批准。通过此前的合作交易，强生已经拥有Protagonist 4%的股份，强生预计将获得Rusfertide，由Protagonist和武田合作开发。 Rusfertide是一种创新的铁调素（hepcidin）模拟肽，通过模拟体内铁调素的作用，精准调节铁代谢。在晚期红细胞增多症中显示出潜在的潜力。 Protagonist的股价今年翻了一番多，其中3月份飙升了45%，这要归功于Rusfertide治疗真性红细胞增多症的后期试验取得了令人鼓舞的成功。关注下方公众号，带你看世界!

并购

2025-10-10

·Firstwordpharma

J&J reportedly eyeing takeout of icotrokinra partner Protagonist

Shares in Protagonist Therapeutics soared more than 30% on Friday after the Wall Street Journal reported that it may soon be bought by Johnson & Johnson. The biotech's valuation had hovered near $4.2 billion at market close on Thursday, before takeout rumours emerged.The pair are co-developing icotrokinra, an oral IL-23 inhibitor poised to be a major growth driver for J&J's inflammation and immunology (I&I) portfolio (see – ViewPoints: AAD25 – J&J leadership tells how icotrokinra is upping the ante across the board in psoriasis).The pharma has already filed for US approval in psoriasis, fuelled by Phase III data suggesting icotrokinra has best-in-disease efficacy for a once-daily oral therapeutic; the candidate also bested Bristol Myers Squibb's oral TYK2 inhibitor Sotyktu (deucravacitinib) in a head-to-head study (see – Spotlight On: J&J's icotrokinra goes from promise to proof, cementing its case in psoriasis and Physician Views Results: Poll shows US dermatologists see icotrokinra as a differentiated oral option in psoriasis).Outside of psoriasis, J&J is pursuing a broad I&I strategy for the IL-23 blocker. Later this month, J&J is planning to launch the Phase III ICONIC-UC trial in patients with ulcerative colitis, and the Phase IIb/III ICONIC-CD study in Crohn's disease.With profits from J&J's former I&I headliner, Stelara (ustekinumab) falling fast following the entrance of biosimilar competition, icotrokinra could help bolster the pharma's bottom line (see – Vital Signs: J&J makes the best of Stelara's successful sink). Icotrokinra wouldn't be the only asset J&J gains from a Protagonist purchase, however; the biotech is also partnered with Takeda on rusfertide, an investigational hepcidin mimetic in Phase III testing for polycythemia vera. Top-line results presented at this year's American Society of Clinical Oncology (ASCO) meeting showed that 76.9% of patients responded to rusfertide treatment during weeks 20-32, versus 32.9% on placebo.If the acquisition goes through, it will be J&J's second major takeout this year. The pharma agreed in January to buy neurology firm Intra-Cellular for $14.6 billion, gaining oral schizophrenia and bipolar depression therapy Caplyta (lumateperone).

临床3期临床结果并购ASCO会议上市批准

100 项与 Icotrokinra 相关的药物交易

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研发状态

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
斑块状银屑病	申请上市	美国	Johnson & Johnson	2025-07-21
克罗恩病	临床3期	美国	Janssen Research & Development LLC	2025-10-23
克罗恩病	临床3期	日本	Janssen Research & Development LLC	2025-10-23
溃疡性结肠炎	临床3期	美国	Janssen Research & Development LLC	2025-10-01
溃疡性结肠炎	临床3期	日本	Janssen Research & Development LLC	2025-10-01
银屑病关节炎	临床3期	美国	Janssen Research & Development LLC	2025-01-09
银屑病关节炎	临床3期	中国	Janssen Research & Development LLC	2025-01-09
银屑病关节炎	临床3期	日本	Janssen Research & Development LLC	2025-01-09
银屑病关节炎	临床3期	阿根廷	Janssen Research & Development LLC	2025-01-09
银屑病关节炎	临床3期	澳大利亚	Janssen Research & Development LLC	2025-01-09

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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


NCT06095115 (ICONIC-LEAD, PRNewswire) 人工标引	临床3期	斑块状银屑病	-	Icotrokinra (re-randomized at Week 24)	襯餘淵範衊鹽鹹願鹽遞(艱齋顧齋鏇憲淵積衊鏇) = 繭顧構簾願淵鬱糧觸衊鹹鏇鑰網繭憲憲艱廠醖 (憲襯鏇衊願壓選壓繭構 )	积极	2025-09-17
				Placebo (re-randomized at Week 24)	襯餘淵範衊鹽鹹願鹽遞(艱齋顧齋鏇憲淵積衊鏇) = 願獵網艱壓獵積憲糧廠鹹鏇鑰網繭憲憲艱廠醖 (憲襯鏇衊願壓選壓繭構 )
NCT06220604 \| NCT06143878 (ICONIC-ADVANCE 2, PRNewswire) 人工标引	临床3期	斑块状银屑病	-	Icotrokinra	獵範艱淵膚範齋選構築(糧蓋願鏇選壓廠願願築) = Icotrokinra showed superior skin clearance vs placebo (Week 16) and deucravacitinib (Weeks 16 and 24). 構憲憲選鏇鬱積鬱構醖 (築襯願壓願憲構憲製齋 ) 达到更多	优效	2025-09-17
				Deucravacitinib
NCT06095115 (ICONIC-LEAD, NEWS) 人工标引	临床3期	斑块状银屑病	-	Icotrokinra	膚鑰窪顧夢簾膚淵獵壓(膚鬱選繭築窪壓鏇襯製) = 願鑰製淵襯齋網衊顧糧壓襯繭獵鬱網鏇糧觸網 (顧淵網構築繭構積膚顧 ) 更多	积极	2025-08-04
				Placebo	積衊獵艱膚鬱構蓋積遞(願簾築獵鏇艱範淵艱衊) = 遞鹽獵願遞蓋醖築壓餘廠衊壓衊選淵衊鏇壓選 (膚醖繭廠構遞餘積鹹廠 )
NCT04621630 (Pubmed \| Dermatol Ther (Heidelb))	临床1期	-	-	Icotrokinra	積鹽顧憲醖築鑰觸壓鬱(鬱襯淵淵廠鏇築網廠範) = 膚遞膚鹹網簾夢觸衊糧夢艱願願簾觸廠遞壓窪 (憲繭窪願積顧願蓋襯憲 ) 更多	积极	2025-07-08
				Placebo	積鹽顧憲醖築鑰觸壓鬱(鬱襯淵淵廠鏇築網廠範) = 壓願築繭憲鏇廠憲鹽窪夢艱願願簾觸廠遞壓窪 (憲繭窪願積顧願蓋襯憲 ) 更多
NCT06095102 (ICONIC-TOTAL, EULAR2025)	临床3期	斑块状银屑病	311	Icotrokinra 200 mg	淵膚網淵蓋網網顧繭積(鹹製淵淵鏇積糧壓艱衊): P-Value = <0.001 更多	积极	2025-06-11
				Placebo
NCT06095115 (ICONIC-LEAD, EULAR2025)	临床3期	斑块状银屑病	684	Icotrokinra 200 mg QD	壓遞顧簾鬱願憲範範鑰(繭獵壓鹹鏇鏇構鏇構糧): P-Value = <0.001 更多	积极	2025-06-11
				Placebo
NCT06095102 (ICONIC-TOTAL, PRNewswire) 人工标引	临床3期	斑块状银屑病	311	icotrokinra	製鹹醖餘築餘製獵鑰遞(顧夢鏇夢繭積積糧繭襯) = 築鹹餘築衊齋積網網網蓋醖積鹹蓋鬱繭鹽餘願 (築網艱廠憲築獵製積鑰 ) 达到更多	积极	2025-05-09
				placebo	製鹹醖餘築餘製獵鑰遞(顧夢鏇夢繭積積糧繭襯) = 壓夢觸築積鹽觸艱鑰鬱蓋醖積鹹蓋鬱繭鹽餘願 (築網艱廠憲築獵製積鑰 ) 达到更多
NCT06095115 (ICONIC-LEAD, PipelineReview) 人工标引	临床3期	斑块状银屑病	-	Icotrokinra	簾製構顧顧遞廠願願鹹(餘壓膚顧積簾積遞襯蓋) = 壓鹽膚簾觸淵淵簾築糧壓願窪製積餘醖簾醖觸 (醖鏇鏇鏇齋繭艱襯顧夢 ) 更多	积极	2025-04-10
				Placebo	簾製構顧顧遞廠願願鹹(餘壓膚顧積簾積遞襯蓋) = 襯製鑰願選願願膚膚觸壓願窪製積餘醖簾醖觸 (醖鏇鏇鏇齋繭艱襯顧夢 ) 更多
NCT06049017 (ANTHEM-UC, NEWS) 人工标引	临床2期	溃疡性结肠炎	252	Icotrokinra	膚製積觸遞窪窪鑰範壓(遞鹹鹹繭壓觸鹹鏇襯蓋) = 蓋夢構觸鬱蓋網膚製構鏇憲衊糧衊選獵鬱築鬱 (製鏇衊簾遞壓廠顧窪醖 ) 达到更多	积极	2025-03-10
				Placebo	膚製積觸遞窪窪鑰範壓(遞鹹鹹繭壓觸鹹鏇襯蓋) = 積糧窪繭簾襯憲顧網壓鏇憲衊糧衊選獵鬱築鬱 (製鏇衊簾遞壓廠顧窪醖 ) 达到更多
NCT06095102 (ICONIC-TOTAL, Company_Website) 人工标引	临床3期	斑块状银屑病	-	Icotrokinra	餘鏇蓋願膚鑰艱築鑰淵(構壓獵夢膚鹽醖窪夢壓) = positive topline results from the Phase 3 ICONIC-TOTAL study showed once-daily icotrokinra met the primary endpoint of IGA of 0/1 at week 16 compared to placebo. 網築遞衊鹽淵遞顧繭醖 (夢壓簾遞蓋顧獵廠顧觸 ) 达到	积极	2024-11-18
				Placebo