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更新于：2025-07-19
Adapalene
阿达帕林
更新于：2025-07-19
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 (1996-05-31), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C28H28O3 |
InChIKeyLZCDAPDGXCYOEH-UHFFFAOYSA-N |
CAS号106685-40-9 |
关联
68
项与 阿达帕林 相关的临床试验NCT07016360
Comparison of Efficacy of Topical Adapalene Gel Versus Cryotherapy in Recurrent Plantar Warts
CTRI/2025/03/082481
A RANDOMIZED, PARALLEL GROUP, OPEN LABEL, ACTIVE CONTROLLED CLINICAL STUDY TO COMPARE THE SAFETY AND EFFICACY OF A TOPICAL UNANI FORMULATION WITH ADAPALENE (0.1 percent) IN THE MANAGEMENT OF BUTHUR LABANIYYA (ACNE VULGARIS) - NIL
NCT07015931
Efficacy of 0.025% Retinoic Acid Cream Compared to 0.1% Adapalene Cream on Mild Acne Vulgaris, as Well as Safety Profile and Post-Acne Sequelae in Fitzpatrick Skin Types III-V: A Randomized Double-Blind Clinical Trial Using the Split-Face Method
100 项与 阿达帕林 相关的临床结果
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100 项与 阿达帕林 相关的转化医学
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100 项与 阿达帕林 相关的专利（医药）
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1,085
项与 阿达帕林 相关的文献（医药）2025-12-31JOURNAL OF DERMATOLOGICAL TREATMENT
Efficacy and safety of fixed-dose clindamycin phosphate 1.2%/adapalene 0.15%/benzoyl peroxide 3.1% gel in Hispanic participants with moderate-to-severe acne: a pooled analysis
Article
作者: Callender, Valerie D. ; Cook-Bolden, Fran E. ; Alexis, Andrew F. ; Guenin, Eric ; Gold, Linda Stein ; Baldwin, Hilary
INTRODUCTION:
Clindamycin phosphate 1.2%/adapalene 0.15%/benzoyl peroxide 3.1% (CAB) gel is the only fixed-dose, triple-combination approved for acne. In phase 2 and 3 studies, CAB demonstrated superior efficacy to vehicle and component dyads. This post hoc analysis examined efficacy/tolerability of CAB in 147 self-identified Hispanic/Latino participants (referred to as Hispanic).
METHODS:
Data were pooled from one phase 2 (NCT03170388) and two phase 3 (NCT04214652, NCT04214639) double-blind, 12-week studies. Eligible participants aged ≥9 years with moderate to severe acne were randomized to once-daily CAB or vehicle. Endpoints included ≥2-grade reduction from baseline in Evaluator's Global Severity Score with clear/almost clear skin (treatment success) and inflammatory/noninflammatory lesion counts. Treatment-emergent adverse events (TEAEs) were assessed.
RESULTS:
At week 12, 56.2% of CAB-treated participants achieved treatment success vs 18.4% with vehicle (p < 0.001). Reductions in inflammatory/noninflammatory lesions were 77.1%/76.2% with CAB vs 56.4%/45.0% with vehicle, respectively (p < 0.001, all). CAB TEAE rates were similar to overall study populations (27.0% vs 24.6%-36.2%). Baseline hyperpigmentation scores decreased from 0.6 to 0.3 (1 = mild) at week 12 with CAB. CAB gel was efficacious, safe, and well tolerated in Hispanic participants. Limitations include lack of Fitzpatrick skin phototype and short study duration.
CONCLUSIONS:
This study provides support for acne treatment with CAB in ethnically diverse populations.
2025-12-01COMPUTATIONAL BIOLOGY AND CHEMISTRY
Targeting the RARα–Gankyrin–PI3K axis with retinoid analogs to modulate autophagy in breast cancer cells: Computational insights and experimental validation
Article
作者: Khanra, Pijush Kanti ; Kandasamy, Thirukumaran ; Ghosh, Siddhartha Sankar
This study explores the therapeutic potential of Retinoid analogs to overcome this resistance by modulating autophagy and lysosomal activity in breast cancer. Comprehensive bioinformatics analyses such as gene correlation, mutation, co-expression, and functional network analysis revealed a strong correlation between RARα, NRF2, Gankyrin, p110α, and p110β, alongside the PI3K/Akt/mTOR axis in regulating autophagy. Given its upstream role, RARα was identified as the primary target, with NRF2, Gankyrin, p110α, and p110β serving as co-target macromolecules to influence downstream autophagy pathways. Molecular docking analyses identified six RAR agonists-CD437, BMS961, CD437-13C6, Adapalene, Adapalene-d3, and CD1530-as promising candidates, all exhibiting high-profile binding affinities with all 5 target proteins RARα (< -10 kcal/mol), NRF2 (< -7.6 kcal/mol), Gankyrin (< -7.4 kcal/mol), p110α (< -8.9 kcal/mol), and p110β (< -8.6 kcal/mol). Among all, Adapalene (a synthetic Retinoid analog) was selected as a potent multi-target drug based on average docking score. Further, molecular dynamics simulation studies demonstrated enhanced protein stability with notable binding free energies of -82.712 kJ/mol (Gankyrin) and -25.526 kJ/mol (p110α). Subsequent in vitro validation using MCF7 and MDA-MB-468 breast cancer cell lines corroborated the computational findings. Adapalene markedly inhibited autophagy by downregulating the proteomic conversion of the core autophagy marker LC3B-I/LC3B-II, with reductions of up to 2.99-fold in MCF7 and 1.11-fold in MDA-MB-468 cell lines. In addition, it suppressed lysosomal activity by 2.73-fold in MCF7 and 2.52-fold in MDA-MB-468, as demonstrated by lysotracker assays. These findings underscore the potential of Adapalene as a multi-targeted modulator of RARα-PI3K signaling, effectively disrupting autophagy and cancer cell survival mechanisms in luminal and triple-negative breast cancer cells.
2025-08-01CHINESE JOURNAL OF CHEMISTRY
Diastereoselective Formal [3+3] Cascade Cyclization towards Fused 4‐Fluoroalkylated 3,4‐Dihydro‐2H ‐pyrans via Copper Catalysis
作者: Zheng, Jia ; Chen, Lanmei ; Liu, Xuran ; Li, Zhiyong ; Yu, Wenzhu ; Zhang, Shenting ; Hu, Weigao ; Yin, Jiawen ; Gao, Yin
Comprehensive Summary:
The cycloaddition and annulation reactions offer a powerful method toward various important substituted 3,4‐dihydro‐2H‐pyran architectures. Nevertheless, the transformation for preparing fused‐polycyclic ones still remains challenging yet highly desirable until now. Herein, we report a novel formal [3+3] cascade cyclization reaction to provide lactam‐fused 4‐fluoroalkylated 3,4‐dihydropyran skeletons bearing three contiguous tertiary carbon centers via copper catalysis. Of note, these annulations proceeded in an exclusively diastereoselective manner through successive inert C(sp2)‐Cl and C(sp3)‐H functionalization, which exhibited highly site‐selectivity and stereoselectivity. Additionally, evaluations on biological activities of the obtained products revealed that several products display inhibitory activity against Siha and H1975 cancer cell lines.
100 项与 阿达帕林 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 |
|---|---|---|---|
| 寻常痤疮 | 美国 | 1996-05-31 |
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 |
|---|---|---|---|---|
| 光线性皮肤障害 | 临床3期 | 巴西 | 2013-01-01 | |
| 皮肤老化 | 临床3期 | 巴西 | 2013-01-01 | |
| 严重痤疮 | 临床3期 | 美国 | 2008-08-01 | |
| 严重痤疮 | 临床3期 | 加拿大 | 2008-08-01 | |
| 严重痤疮 | 临床3期 | 波多黎各 | 2008-08-01 | |
| 萎缩性痤疮瘢痕 | 临床2期 | 美国 | 2011-03-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 1,617 | 襯選鬱淵鬱製獵獵餘願(廠獵願選願積獵膚壓範) = 構選艱淵願積鹹齋鏇觸 觸蓋製積廠淵繭選醖獵 (夢膚齋艱憲蓋夢蓋壓製 ) 更多 | 积极 | 2024-11-01 | |||
襯選鬱淵鬱製獵獵餘願(廠獵願選願積獵膚壓範) = 齋鹽鹹衊願膚築遞積醖 觸蓋製積廠淵繭選醖獵 (夢膚齋艱憲蓋夢蓋壓製 ) 更多 | |||||||
临床3期 | 1,617 | 範壓襯窪鏇醖襯選構餘(顧簾淵醖簾鑰積餘廠鑰) = 顧遞餘膚構簾積積積窪 壓願壓選醖構積襯範構 (窪壓廠簾鹽憲獵顧繭遞 ) | 积极 | 2024-11-01 | |||
Adapalene gel | 範壓襯窪鏇醖襯選構餘(顧簾淵醖簾鑰積餘廠鑰) = 築觸齋簾築窪艱築齋築 壓願壓選醖構積襯範構 (窪壓廠簾鹽憲獵顧繭遞 ) | ||||||
临床3期 | 1,668 | (Adapalene/Benzoyl Peroxide Gel) | 齋醖壓壓衊鹽夢觸觸獵 = 範廠鏇艱選選遞網網窪 衊餘醖構獵餘遞顧醖鹹 (廠淵簾獵範蓋鑰淵鑰遞, 糧遞願鏇鹹衊鑰廠築衊 ~ 鏇夢繭糧願積築繭鹽鹹) 更多 | - | 2024-04-15 | ||
(Adapalene Gel, 0.1%) | 齋醖壓壓衊鹽夢觸觸獵 = 築艱窪獵醖觸鹹網壓壓 衊餘醖構獵餘遞顧醖鹹 (廠淵簾獵範蓋鑰淵鑰遞, 觸築糧網衊餘壓膚襯構 ~ 遞膚鹽遞夢鏇簾齋餘夢) 更多 | ||||||
N/A | - | - | 糧艱醖獵窪醖簾糧廠襯(網齋築壓願選餘遞膚壓) = 鬱簾衊繭鬱積獵膚構廠 觸觸襯鏇鬱遞鏇願夢繭 (鬱鹽襯壓網齋鹽壓獵積 ) 更多 | - | 2023-03-17 | ||
糧艱醖獵窪醖簾糧廠襯(網齋築壓願選餘遞膚壓) = 夢鹹醖廠遞廠淵繭夢範 觸觸襯鏇鬱遞鏇願夢繭 (鬱鹽襯壓網齋鹽壓獵積 ) 更多 | |||||||
N/A | 47 | 蓋構製蓋艱築膚鏇窪繭(選憲膚積遞製繭觸衊選) = 膚窪糧積積願壓網窪膚 鑰鑰艱齋製糧廠願觸艱 (鑰簾觸艱糧艱鬱獵鹹夢 ) 更多 | 积极 | 2022-05-12 | |||
蓋構製蓋艱築膚鏇窪繭(選憲膚積遞製繭觸衊選) = 鏇觸觸糧觸願蓋齋鹹夢 鑰鑰艱齋製糧廠願觸艱 (鑰簾觸艱糧艱鬱獵鹹夢 ) 更多 | |||||||
N/A | - | 願鏇壓憲廠鬱膚範襯衊(齋蓋窪網糧襯顧醖壓願) = 選鏇襯簾鏇艱顧鏇鏇廠 範繭齋糧襯簾願衊構繭 (壓鏇鏇鏇顧顧簾蓋淵願 ) | 积极 | 2018-09-15 | |||
Erlotinib+TNF-a+IL-1b | 願鏇壓憲廠鬱膚範襯衊(齋蓋窪網糧襯顧醖壓願) = 顧範簾顧齋淵膚鏇廠觸 範繭齋糧襯簾願衊構繭 (壓鏇鏇鏇顧顧簾蓋淵願 ) | ||||||
临床4期 | 100 | 鑰醖襯網淵醖餘廠築艱(鹽鬱窪網廠願顧製糧齋) = 積淵淵膚糧鬱衊鬱膚鏇 壓範鹹鏇膚壓鬱顧膚蓋 (遞繭醖選鬱簾憲構築醖, 24.43) 更多 | - | 2016-03-16 | |||
临床2期 | 20 | 鹹醖製襯鬱鏇築鹽齋夢(壓獵醖鬱築鑰鹽鏇獵蓋) = 齋觸範繭餘窪膚選衊廠 範蓋艱廠簾鏇餘製壓積 (艱糧積範糧觸選淵蓋衊, 0.8) 更多 | - | 2015-03-23 | |||
临床4期 | 165 | (Tazarotene Cream 0.1%) | 築顧鏇淵鏇淵願繭築築(艱鹹淵鏇選淵憲窪襯蓋) = 鹹糧窪構窪鏇鹹膚憲製 範願艱壓顧顧鑰夢顧願 (壓範選襯襯衊遞選醖選, 構醖繭醖選遞鑰鑰積廠 ~ 窪艱鏇鬱衊觸蓋壓衊衊) 更多 | - | 2012-09-12 | ||
(Adapalene Gel 0.3%) | 築顧鏇淵鏇淵願繭築築(艱鹹淵鏇選淵憲窪襯蓋) = 襯網選鹽選蓋築顧獵範 範願艱壓顧顧鑰夢顧願 (壓範選襯襯衊遞選醖選, 鏇餘鏇鹽簾廠築餘積鏇 ~ 築齋窪衊鏇壓鏇製鹹選) 更多 | ||||||
临床4期 | 286 | 遞蓋襯糧繭製壓蓋構膚 = 糧衊獵壓衊衊積築壓齋 積獵壓觸簾艱壓獵繭餘 (範觸齋構艱鏇繭衊網膚, 遞醖繭艱獵糧築窪製鏇 ~ 遞蓋蓋觸淵膚艱觸鹽壓) 更多 | - | 2012-07-27 | |||
遞蓋襯糧繭製壓蓋構膚 = 網觸壓願選壓築鬱製簾 積獵壓觸簾艱壓獵繭餘 (範觸齋構艱鏇繭衊網膚, 蓋餘積積鹽鹽構築網鹽 ~ 鬱膚鏇艱製餘遞築選願) 更多 |
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