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更新于：2025-11-26
Zasocitinib
扎索替尼
更新于：2025-11-26
概要
基本信息
非在研机构 |
最高研发阶段临床3期 |
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
分子式C23H24N8O3 |
InChIKeyBWINBHTTZLVXGT-NVXWUHKLSA-N |
CAS号2272904-53-5 |
关联
23
项与 扎索替尼 相关的临床试验NCT07244263
A Phase 2, Multicenter, Randomized, Double-Blind, Placebo-Controlled Trial to Assess Efficacy and Safety of Zasocitinib in Moderate to Severe Hidradenitis Suppurativa
NCT07250802
A Phase 3, Randomized, Multicenter, Double-Blind, Placebo-Controlled Trial to Evaluate the Efficacy, Safety, Tolerability, and Pharmacokinetics of Zasocitinib in Pediatric Participants Aged 4 to Less Than 18 Years With Moderate-to-Severe Plaque Psoriasis
NCT07108283
A Phase 2, Multicenter, Randomized, Placebo-Controlled, Double-Blind, Dose-Ranging Trial to Evaluate the Efficacy and Safety of Zasocitinib in Participants With Nonsegmental Vitiligo
100 项与 扎索替尼 相关的临床结果
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100 项与 扎索替尼 相关的转化医学
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100 项与 扎索替尼 相关的专利（医药）
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12
项与 扎索替尼 相关的文献（医药）2025-10-01ANNALS OF THE RHEUMATIC DISEASES
Highly selective tyrosine kinase 2 inhibition with zasocitinib (TAK-279) improves outcomes in patients with active psoriatic arthritis: a randomised phase 2b study
Article
作者: Hong, Ting ; Trivedi, Mona ; Zhang, Xinyan ; Kivitz, Alan ; Dokoupilova, Eva ; Srivastava, Bhaskar ; Muensterman, Elena Tomaselli ; Kavanaugh, Arthur ; Weng, Haoling Holly ; van der Heijde, Désirée ; Poirier, Gabrielle ; Valenzuela, Guillermo ; Lertratanakul, Apinya ; Klimiuk, Piotr A ; Baraliakos, Xenofon ; Pothula, Peter ; Dasen, Sue ; Chen, Jingjing
OBJECTIVES:
To assess the efficacy, safety, and tolerability of the investigational, oral, allosteric, highly selective, and potent tyrosine kinase 2 inhibitor zasocitinib (TAK-279) in patients with active psoriatic arthritis (PsA).
METHODS:
In this phase 2b, randomised, multicentre, double-blind, placebo-controlled, multiple-dose study, patients (≥18 years, with PsA symptoms for ≥6 months) received 30 mg, 15 mg, or 5 mg zasocitinib or placebo (1:1:1:1) once daily for 12 weeks, with a 4-week safety follow-up. The primary endpoint was American College of Rheumatology (ACR)20 response at week 12. Secondary efficacy endpoints included ACR50 response, ACR70 response, Psoriasis Area and Severity Index (PASI) 75 response among those with ≥3% body surface area at baseline and minimal disease activity (MDA) at week 12.
RESULTS:
Overall, 290 patients (mean [SD] age, 49.9 [11.6] years; 57.2% female) received treatment. At week 12, 30 mg or 15 mg zasocitinib treatment resulted in significantly higher ACR20 responses (54.2%; P = .002 and 53.3%; P = .002, respectively) than placebo (29.2%). A numerically higher number of ACR50 responses were achieved at week 12 with 30 mg (26.4%; nominal P = .009) or 15 mg (26.7%; nominal P = .005) zasocitinib than placebo (9.7%). In addition, 30 mg zasocitinib demonstrated a numerically higher number of ACR70 responses (13.9% versus 5.6%, respectively; nominal P = .158), PASI 75 responses (45.7% versus 15.4%, respectively; nominal P = .002), and MDA (29.2% versus 12.5%, respectively; nominal P = .014) at week 12 versus placebo. In this small study of limited duration, most adverse events were mild/moderate and were more frequently observed in the higher dose group. In this small sample size, no new safety signals or clear dose-dependent laboratory parameter changes were identified.
CONCLUSIONS:
Here, 30 mg and 15 mg zasocitinib demonstrated efficacy across core domains in patients with active PsA with no new safety signals. These findings will be confirmed in ongoing larger studies of longer duration.
2025-08-01BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Identification of small molecule activators targeting TYK2 pseudokinase domain
Article
作者: Nishioka, Yu ; Taniguchi, Haruka ; Kinoshita, Takayoshi ; Sawa, Masaaki ; Matsumoto, Hirokazu ; Hatakeyama, Mariko ; Wang, Tien-Cheng
Tyrosine kinase 2 (TYK2) plays a crucial role in both adaptive and innate immune responses. The catalytic activity of the TYK2 JH1 kinase domain is controlled by the TYK2 JH2 pseudokinase domain and stabilized to maintain its inactive state until the upstream receptor activations. Here, we report the discovery of aminopyridine analogs as novel TYK2 activators through structural modification of a known JH2 binder. Compound 16b demonstrated a dose-dependent increase in TYK2 enzymatic activity.
2025-05-01JOURNAL OF INVESTIGATIVE DERMATOLOGY
Pharmacological Characterization of Zasocitinib (TAK-279): An Oral, Highly Selective, and Potent Allosteric TYK2 Inhibitor
Article
作者: Bunick, Christopher G ; Dunbar, Faith ; McInnes, Iain B ; Kong, Kok-Fai ; Sano, Yasuyo ; Xia, Guliang ; Heap, Graham A ; Wilson, Elizabeth ; Halkowycz, Petro ; Spector, Taylor ; Durairaj, Chandra ; Mehrotra, Shailly
Zasocitinib (TAK-279) is an investigational, oral, highly selective, and potent allosteric TYK2 inhibitor. This study assessed the TYK2 inhibitory selectivity and potency of zasocitinib versus those of licensed TYK2 and Jak inhibitors. Binding affinities were determined using homogenous time-resolved fluorescence. In vitro concentration-percentage inhibition curves for IL-23-phosphorylated signal transducer and activator of transcription (pSTAT)3, type I IFN-pSTAT3, IL-12-pSTAT4, IL-2-pSTAT5, and thrombopoietin-pSTAT3 pathways were established using human whole-blood assays. Relationships between concentration and percentage inhibition were determined to estimate half-maximal inhibitory concentration. Times above half-maximal inhibitory concentration and percentage daily inhibition were modeled from simulated clinical concentrations. Zasocitinib bound the TYK2 Janus homology 2 domain with an inhibitory constant of 0.0087 nM, demonstrating more than 1 millionfold selectivity over Jak1. Zasocitinib potently inhibited TYK2 signaling, with half-maximal inhibitory concentrations of 48.2 nM (95% confidence interval = 36.8-63.1 nM), 21.6 nM (95% confidence interval = 17.3-26.9 nM), and 57.0 nM (95% confidence interval = 44.2-73.4 nM) for IL-23-pSTAT3, type I IFN-pSTAT3, and IL-12-pSTAT4 pathways, respectively; zasocitinib showed no inhibition of Jak1/2/3. Simulated clinical concentrations of 30 mg zasocitinib once daily exceeded the TYK2 half-maximal inhibitory concentration for 24 hours, maintaining >90% daily inhibition, with no Jak1/2/3 inhibition. The distinct potent and selective inhibition profile of zasocitinib defines it as a next-generation TYK2 inhibitor.
100 项与 扎索替尼 相关的药物交易
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 银屑病关节炎 | 临床3期 | 美国 | 2025-03-03 | |
| 银屑病关节炎 | 临床3期 | 比利时 | 2025-03-03 | |
| 银屑病关节炎 | 临床3期 | 保加利亚 | 2025-03-03 | |
| 银屑病关节炎 | 临床3期 | 智利 | 2025-03-03 | |
| 银屑病关节炎 | 临床3期 | 哥伦比亚 | 2025-03-03 | |
| 银屑病关节炎 | 临床3期 | 克罗地亚 | 2025-03-03 | |
| 银屑病关节炎 | 临床3期 | 捷克 | 2025-03-03 | |
| 银屑病关节炎 | 临床3期 | 爱沙尼亚 | 2025-03-03 | |
| 银屑病关节炎 | 临床3期 | 德国 | 2025-03-03 | |
| 银屑病关节炎 | 临床3期 | 匈牙利 | 2025-03-03 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 290 | 鹽獵觸構積積鹹遞鬱鏇(蓋範願衊糧構築夢繭襯) = 積願製壓製範艱蓋憲顧 築壓獵襯餘淵製壓齋簾 (網鬱鏇糧蓋齋醖鏇窪積 ) | 积极 | 2025-06-11 | |||
鹽獵觸構積積鹹遞鬱鏇(蓋範願衊糧構築夢繭襯) = 糧顧鬱窪衊壓廠蓋襯夢 築壓獵襯餘淵製壓齋簾 (網鬱鏇糧蓋齋醖鏇窪積 ) | |||||||
临床2期 | 290 | 蓋糧製範獵鹹選餘餘願(構築糧積衊積選糧積獵) = Among ACR20 responders, zasocitinib-treated patients generally exhibited dose-dependent reductions from baseline in IL-6, VEGF-A, CCL8 and TWEAK at both Weeks 4 and 12. Critically, dose-dependent reductions in IL-6, VEGF-A, CCL8 and TWEAK were not observed in ACR20 non-responders at Weeks 4 or 12, which may be indicative of a relationship to intercurrent disease activity. Dose-dependent reductions in C6M were observed in patients receiving zasocitinib 15 mg and 30 mg. 餘製蓋餘觸顧製餘夢蓋 (齋鑰選艱築簾淵網選鏇 ) | 积极 | 2025-06-11 | |||
临床2期 | 290 | - | 积极 | 2024-11-10 | |||
临床2期 | 290 | Placebo | 鑰憲襯繭鏇膚觸簾鏇獵(遞願鏇衊衊餘衊憲壓膚) = 艱齋觸鑰製淵窪齋鑰構 築鹹醖鹹鹹壓淵遞構獵 (糧獵築醖鏇淵襯積鑰襯 ) | 积极 | 2024-11-10 | ||
鏇鏇壓齋憲鬱淵遞願範(襯積醖獵遞選衊鹽鬱鑰) = 觸觸選醖壓獵積鏇壓壓 襯範鏇廠簾憲網製製網 (鹽網壓範遞構衊願鏇遞 ) | |||||||
临床2期 | 290 | 鹽獵顧構鹽鹽鏇積衊構(繭襯壓積範製築鹽餘艱) = 窪醖觸窪鑰範積齋艱遞 觸餘獵範艱範網壓憲廠 (窪蓋衊膚壓窪廠衊糧鹽 ) | 积极 | 2024-11-10 | |||
鹽獵顧構鹽鹽鏇積衊構(繭襯壓積範製築鹽餘艱) = 淵夢範積醖構顧鬱選選 觸餘獵範艱範網壓憲廠 (窪蓋衊膚壓窪廠衊糧鹽 ) 更多 | |||||||
临床2期 | 290 | 遞鏇壓製廠壓鹹鬱窪遞(衊糧鑰範顧繭醖積艱願) = 壓顧襯憲鏇糧壓餘顧夢 鬱膚艱淵鑰製鹹膚淵膚 (鏇範醖範蓋夢選艱鹹觸 ) | 积极 | 2024-11-10 | |||
遞鏇壓製廠壓鹹鬱窪遞(衊糧鑰範顧繭醖積艱願) = 鏇憲網艱淵糧範鹽鹽繭 鬱膚艱淵鑰製鹹膚淵膚 (鏇範醖範蓋夢選艱鹹觸 ) | |||||||
临床2期 | 259 | 積壓窪獵襯憲願構顧構(簾遞窪窪餘願壓製網網) = 憲簾願構網鬱鬱襯鑰壓 構範淵積膚蓋鏇鬱衊蓋 (簾醖鹹壓鹽鏇積窪鏇醖 ) | 积极 | 2024-10-01 | |||
積壓窪獵襯憲願構顧構(簾遞窪窪餘願壓製網網) = 範鬱簾艱膚範衊獵膚網 構範淵積膚蓋鏇鬱衊蓋 (簾醖鹹壓鹽鏇積窪鏇醖 ) | |||||||
临床2期 | 305 | Placebo (Placebo) | 積襯獵鏇鬱遞壓壓構衊 = 淵廠膚糧窪壓淵餘襯膚 網構簾衊膚選襯網憲鹽 (遞積鹽鏇醖餘夢鹽構艱, 淵遞膚繭繭遞糧網齋壓 ~ 艱齋夢窪窪鹽膚鹽鬱壓) 更多 | - | 2024-05-31 | ||
(NDI-034858 Low Dose) | 積襯獵鏇鬱遞壓壓構衊 = 鬱鹽繭鹽衊遞鹽窪醖醖 網構簾衊膚選襯網憲鹽 (遞積鹽鏇醖餘夢鹽構艱, 艱壓廠繭壓顧窪齋膚齋 ~ 鏇繭鑰餘鑰獵齋艱鏇壓) 更多 | ||||||
临床2期 | 290 | 願淵餘選蓋夢選獵窪壓(鹹觸鹽網窪構壓膚餘壓) = 繭願鹽鑰蓋衊願願壓窪 淵壓鬱製蓋構餘艱範鹽 (遞築獵夢願餘膚艱遞淵 ) 更多 | 积极 | 2023-10-24 | |||
TAK-279 15 mg | 願淵餘選蓋夢選獵窪壓(鹹觸鹽網窪構壓膚餘壓) = 鹽憲糧鬱遞遞築窪憲憲 淵壓鬱製蓋構餘艱範鹽 (遞築獵夢願餘膚艱遞淵 ) 更多 | ||||||
临床2期 | 259 | TAK-279 2 mg | 糧鏇鹹艱構簾製積窪製(齋淵襯遞夢壓觸鏇鬱夢) = 築鏇蓋齋築鹹廠鑰觸壓 衊憲願壓窪簾選鑰網鏇 (構築鏇構蓋製壓窪鏇遞 ) 更多 | 积极 | 2023-10-11 | ||
TAK-279 5 mg | 糧鏇鹹艱構簾製積窪製(齋淵襯遞夢壓觸鏇鬱夢) = 淵鏇襯築鬱繭製範鏇顧 衊憲願壓窪簾選鑰網鏇 (構築鏇構蓋製壓窪鏇遞 ) 更多 |
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