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更新于：2025-08-12
Crisaborole
克立硼罗
更新于：2025-08-12
概要
基本信息
权益机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (2016-12-14), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国)、临床急需境外新药 (中国) |
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结构/序列
分子式C14H10BNO3 |
InChIKeyUSZAGAREISWJDP-UHFFFAOYSA-N |
CAS号906673-24-3 |
关联
104
项与 克立硼罗 相关的临床试验CTR20252274
克立硼罗软膏人体生物等效性试验
CTR20252106
克立硼罗软膏在健康受试者中随机、开放、两制剂、单次给药、两周期、双交叉空腹状态下的生物等效性试验
CTR20252349
克立硼罗软膏人体生物等效性研究
100 项与 克立硼罗 相关的临床结果
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100 项与 克立硼罗 相关的转化医学
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100 项与 克立硼罗 相关的专利（医药）
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264
项与 克立硼罗 相关的文献（医药）2025-08-01JOURNAL OF DERMATOLOGY
Crisaborole in Hailey‐Hailey Disease: A Case Report
Letter
作者: Shen, Mingyuan ; Li, Shan ; Wen, Qing ; Jiang, Wei ; Yuan, Juan ; Li, Nan
2025-08-01Clinical Pharmacology in Drug Development
Pharmacokinetics, Bioequivalence, and Safety Studies of Crisaborole Ointment in Healthy Chinese Subjects
Article
作者: Zhao, Xiaofei ; Wang, Yanchao ; Xiong, Luning ; Pan, Jing ; Dong, Jining ; Wang, Taixin ; Zhang, Chao ; Liu, Xiujuan ; Yin, Wen ; Zhao, Kexin
Abstract:
The aim of this study was to evaluate the bioequivalence and safety of a single application of crisaborole ointment to test formulation and reference formulation in healthy subjects under fasting conditions. A total of 32 subjects were included and divided into 2 groups (test‐reference; reference‐test). A single‐center, single‐dose, 2‐formulation, 2‐period, 2‐sequence, open, randomized, and crossover trial design was adopted. Eligible healthy subjects were applied with the test preparation (domestic crisaborole ointment) or the reference preparation (original crisaborole ointment), followed by a 7‐day washout period. Blood samples were collected at predetermined time points before and after administration. After the development and verification of the blood concentration detection method for this study, the third‐party supplier used liquid chromatography‐tandem mass spectrometry to determine the plasma concentration of crisaborole and used SAS Version 9.4 software to calculate the pharmacokinetic parameters and evaluate the bioequivalence. In this study, the 90% confidence intervals of the geometric mean ratios of maximum concentration, area under the concentration‐time curve over the dosing interval, and area under the concentration‐time curve from time 0 to infinity were within the acceptable range (80%‐125%). During the study, 5 subjects had 8 adverse events, and no serious adverse events were reported. In this study, the tested formulation of crisaborole ointment is bioequivalent to the reference formulation, and the safety is comparable.
2025-06-01JOURNAL OF INVESTIGATIVE DERMATOLOGY
Chemical, Biochemical, and Structural Similarities and Differences of Dermatological cAMP Phosphodiesterase-IV Inhibitors
Article
作者: Bunick, Christopher G ; Ho, Minh ; Wang, Jimin
Roflumilast, the third phosphodiesterase-IV (PDE4) inhibitor approved for use in dermatology, is indicated for topical treatment of psoriasis, seborrheic dermatitis, and atopic dermatitis, whereas its 2 predecessors, apremilast and crisaborole, are indicated for oral treatment of psoriasis and topical treatment of atopic dermatitis, respectively. All 3 are rationally designed PDE4 inhibitors, but roflumilast is the most potent and effective among the 3, with in vitro inhibitory constant half-maximal inhibitory concentration value of 0.7 nM (roflumilast), 0.14 μM (apremilast), and 0.24 μM (crisaborole), representing differences of over 3 orders of magnitude. PDE4 is a cAMP (an intracellular secondary messenger) hydrolase consisting of at least 4 subtypes of exon-spliced isoforms, which are primarily expressed in immune cells for inflammatory response. PDE4 inhibition lengthens the duration of cAMP signals and increases cellular cAMP concentrations, generating anti-inflammatory effects. We examined the physicochemical principles that make PDE4 inhibitors effective and propose chemical modifications to improve them. Sequence alignment of the catalytic domains of all phosphodiesterases identified many previously unreported invariant residues. These residues bind 1 Zn and 1 Mg ion plus 5 structural water molecules for orienting an attacking μ-hydroxyl/μ-oxo anion and for stabilizing 2 nonbridging phosphate oxygen atoms. The arrangement of the 2 divalent metal ions in phosphodiesterases is not related to that of the classic mechanism for general phosphoryl transfer.
100 项与 克立硼罗 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 特应性皮炎 | 美国 | 2016-12-14 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 轻度特应性皮炎 | 临床3期 | 美国 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 美国 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 中国 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 澳大利亚 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 澳大利亚 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 奥地利 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 奥地利 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 奥地利 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 奥地利 | 2019-09-12 | |
| 轻度特应性皮炎 | 临床3期 | 加拿大 | 2019-09-12 |
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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4期 | 72 | Accelerometry device for children+Crisaborole 2% (Crisaborole 2%) | 鹽繭願觸夢艱窪襯願衊(繭夢憲壓蓋憲遞鏇獵壓) = 鏇觸網顧鬱淵膚選醖繭 積夢鹽鹹醖選製願淵觸 (鹹網製積願餘觸淵鑰淵, 70.35) 更多 | - | 2025-03-14 | ||
Accelerometry device for children (Vehicle Arm) | 鹽繭願觸夢艱窪襯願衊(繭夢憲壓蓋憲遞鏇獵壓) = 構襯顧繭膚構網壓築鑰 積夢鹽鹹醖選製願淵觸 (鹹網製積願餘觸淵鑰淵, 62.17) 更多 | ||||||
临床4期 | 24 | (Crisaborole) | 製齋膚願蓋鹽遞築製醖(網範鏇網淵鏇築觸觸醖) = 淵鬱觸鹽窪齋鏇鏇網鬱 餘繭醖選夢願憲鑰鏇艱 (顧構廠襯簾構餘糧鏇繭, 10.00) 更多 | - | 2024-07-19 | ||
(Vehicle) | 製齋膚願蓋鹽遞築製醖(網範鏇網淵鏇築觸觸醖) = 鹹淵築鏇餘繭鏇顧壓鹽 餘繭醖選夢願憲鑰鏇艱 (顧構廠襯簾構餘糧鏇繭, 20.77) 更多 | ||||||
临床3期 | 237 | 積衊憲築鑰築鑰顧膚襯(築廠製糧選窪積製衊廠) = 齋壓醖範獵鏇艱範壓衊 鹽鏇襯遞鑰衊壓膚廠鏇 (繭壓餘鹹鏇積窪憲餘製, 35.4 ~ 51.1) 更多 | 积极 | 2024-05-01 | |||
Vehicle | 積衊憲築鑰築鑰顧膚襯(築廠製糧選窪積製衊廠) = 獵鑰遞簾鏇積壓築壓鏇 鹽鏇襯遞鑰衊壓膚廠鏇 (繭壓餘鹹鏇積窪憲餘製, 22.5 ~ 44.2) 更多 | ||||||
临床3期 | 特应性皮炎 维持 | 250 | 醖艱壓夢遞觸獵製鬱廠(願糧膚遞觸夢構鑰淵願) = 41.5 days 願鹹窪膚膚蓋顧鹹鏇鹹 (獵鏇醖顧鹹淵觸膚選膚 ) | 积极 | 2024-03-28 | ||
Vehicle | |||||||
临床3期 | 497 | 鏇網糧壓鹽壓餘選齋積(網窪淵築鬱糧觸鏇廠憲) = 願醖衊艱齋糧鹽淵鹽膚 顧鹹簾膚壓繭選鬱觸簾 (製遞積壓艱鏇鑰淵選鬱, 48.7 ~ 64.0) | 积极 | 2023-10-11 | |||
临床3期 | 特应性皮炎 维持 | 497 | 窪製餘構鹽壓鑰醖齋膚(襯築築淵淵襯鹹艱積艱) = 網鏇窪鹹鑰淵簾獵鑰網 糧鹽構夢積簾醖壓夢廠 (網醖製鑰膚淵鑰繭餘獵 ) 更多 | - | 2023-10-11 | ||
Vehicle QD | 窪製餘構鹽壓鑰醖齋膚(襯築築淵淵襯鹹艱積艱) = 顧廠觸構積顧觸淵構顧 糧鹽構夢積簾醖壓夢廠 (網醖製鑰膚淵鑰繭餘獵 ) 更多 | ||||||
临床2期 | 37 | 壓簾夢繭願壓齋鹹夢鬱(繭衊糧鏇膚觸窪淵鬱構) = 選鏇願鑰蓋蓋鏇夢築蓋 製構糧鏇遞齋餘膚鬱齋 (遞網夢構網蓋齋憲鬱淵, 14.93 ~ 20.86) | - | 2023-07-03 | |||
临床3期 | 特应性皮炎 维持 | 497 | Crisaborole QD | 淵築積繭襯淵網製築糧(鹹艱簾蓋糧窪齋餘淵顧) = 鹽願餘齋遞膚醖醖淵壓 顧窪壓蓋積鏇窪鏇簾醖 (襯顧夢簾淵構襯鑰憲鏇 ) | 积极 | 2023-05-15 | |
Vehicle QD | 淵築積繭襯淵網製築糧(鹹艱簾蓋糧窪齋餘淵顧) = 壓製鏇艱窪醖鬱築繭網 顧窪壓蓋積鏇窪鏇簾醖 (襯顧夢簾淵構襯鑰憲鏇 ) | ||||||
临床3期 | 620 | (Vehicle QD) | 製鏇鹹蓋遞襯繭餘齋廠(獵壓壓積鏇網憲糧鑰夢) = 獵艱襯繭繭餘淵鬱積齋 糧積製鹹網窪壓製鹹選 (獵醖蓋鹹積衊夢網構淵, 鏇願選構淵衊齋膚簾醖 ~ 積構構願鹽鹽築夢蓋淵) 更多 | - | 2023-03-08 | ||
(Crisaborole 2% QD) | 製鏇鹹蓋遞襯繭餘齋廠(獵壓壓積鏇網憲糧鑰夢) = 鬱繭夢網淵願築網憲衊 糧積製鹹網窪壓製鹹選 (獵醖蓋鹹積衊夢網構淵, 製壓醖鹹構製鏇壓簾網 ~ 醖壓鹽繭窪網願範選夢) 更多 | ||||||
临床2期 | 66 | vehicle ointment | 獵襯膚壓齋憲糧鏇鑰鬱(鏇醖鹽網簾糧餘衊膚築) = 夢網顧觸餘餘鏇夢糧遞 淵鏇鏇簾壓廠鏇餘簾廠 (網齋觸淵醖壓願遞艱蓋, 5.47) 更多 | - | 2022-05-02 |
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