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更新于：2026-08-23
Tazarotene
他扎罗汀
更新于：2026-08-23
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C21H21NO2S |
InChIKeyOGQICQVSFDPSEI-UHFFFAOYSA-N |
CAS号118292-40-3 |
关联
66
项与 他扎罗汀 相关的临床试验NCT06331624
Biomarker Modulation and the Inhibition of Natural Killer Type 1 (NKT1) Cells by Oral GRI-0621 in Patients With Idiopathic Pulmonary Fibrosis (IPF)
CTRI/2023/11/060308
Comparative efficacy of different concentration of topical tazarotene and topical tretinoin in acne vulgaris. - NIL
CTRI/2023/10/059038
Comparative efficacy of topical methotrexate and topical tazarotene in psoriasis vulgaris - NIL
100 项与 他扎罗汀 相关的临床结果
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100 项与 他扎罗汀 相关的转化医学
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100 项与 他扎罗汀 相关的专利（医药）
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670
项与 他扎罗汀 相关的文献（医药）2026-08-01INTERNATIONAL IMMUNOPHARMACOLOGY
Tazarotene ameliorates steroid-induced osteonecrosis of the femoral head by activating autophagy
Article
作者: Tao, Kun ; Zhou, Song ; Fan, Aoyuan ; Huang, Junming ; Pang, Zhiying ; Wei, Yanhui ; Yin, Feng
BACKGROUND:
Steroid-induced osteonecrosis of the femoral head (SIONFH) is a debilitating condition characterized by lipid accumulation and bone structural collapse. A key pathogenic mechanism involves downregulated osteogenesis and upregulated adipogenesis of bone marrow mesenchymal stem cells (BMSCs). Autophagy has been implicated in lipid metabolism and bone homeostasis. This study investigated whether activating autophagy could ameliorate SIONFH.
METHODS:
Lipid droplet based high-throughput screening of an active compound library was performed on dexamethasone (DEX)-treated rat BMSCs. Further evaluations based on rat SIONFH model including bone microstructure, histological analysis and serum marker, serum biochemical analysis. Western blot, flow cytometry for apoptosis, and molecular docking to predict target interactions.
RESULTS:
Retinoid agonist Tazarotene effectively reduced lipid droplet accumulation in BMSCs by activating autophagy and attenuating apoptosis. Tazarotene restored the osteogenic-adipogenic differentiation balance. Mechanistically, network pharmacology and molecular docking suggested mTOR as a potential target. In the SIONFH rat model, tazarotene treatment significantly improved femoral head microstructure, reduced empty lacunae, and promoted osteogenic markers while suppressing adipogenic markers.
CONCLUSION:
Tazarotene ameliorates SIONFH by activating autophagy in BMSCs. These findings highlight tazarotene's potential as a novel therapeutic strategy for SIONFH.
2026-04-28ChemMedChem
Mechanistic Insights Into the Photosensitizing Properties of the Topical Retinoid Tazarotene
Article
作者: Dillon, Macarena ; Rodríguez‐Muñiz, Gemma M. ; Soler‐Orenes, Juan A. ; Andreu, Inmaculada ; Ansino‐Ortiz, Matilde ; Lhiaubet‐Vallet, Virginie
Since the FDA approval of tretinoin in 1971, retinoids have been key in treating acne and different skin pathologies. Tazarotene (TZE), a third‐generation retinoid and prodrug, is converted in the skin to its active form, tazarotenic acid (TZA). Its structure allows absorption of UVA/UVB light, prompting concerns about potential phototoxicity, but data on the excited state properties of TZE and TZA are still lacking. This work investigates these retinoids’ behavior under UVA light exposure through a combined spectroscopic, analytical, and biological approximation. The results show that both compounds form long‐lived triplet excited states, which interact with oxygen to produce reactive singlet oxygen. Additionally, TZA interacts with tryptophan (Trp), leading to the formation of a photoproduct with a mass corresponding to a Trp/TZA cyclobutene adduct. These results correlate with reduced cell viability in fibroblasts exposed to light after treatment with TZE or TZA, indicating potential phototoxic effects. Such light‐induced reactivity may also be related to the enhanced therapeutic results observed when TZE is used alongside narrow‐band UVB phototherapy.
2026-04-11Cureus Journal of Medical Science
Topical Pimecrolimus for Treatment-Refractory Tazarotene-Induced Photosensitive Facial Erosions
Article
作者: Sanjabi, Tara ; Williams, Shane ; Rodriguez, Sergio A ; Manuel, Joren ; Memari, Kian ; Cohen, Peter
Topical retinoids are cornerstone therapies in the management of acne vulgaris, psoriasis, and photoaging. Tazarotene, a third-generation retinoid, is highly effective but is associated with cutaneous adverse effects, including irritation, photosensitivity, and epidermal barrier disruption. While most retinoid-induced reactions are self-limited and respond to conservative management, a subset of patients may develop persistent inflammatory skin changes refractory to standard therapy. We report the case of a 20-year-old man with severe acne vulgaris who developed bilateral photosensitive facial erosions following chronic tazarotene use in the setting of prolonged cumulative ultraviolet exposure. Despite discontinuation of tazarotene and extended treatment with emollients, photoprotection, and topical corticosteroids, the lesions persisted for six months. Laboratory evaluation for autoimmune and systemic inflammatory disease, including antinuclear antibody (ANA), erythrocyte sedimentation rate (ESR), and C-reactive protein (CRP), was unremarkable. Subsequent treatment with pimecrolimus 1% cream resulted in progressive clinical improvement, with complete healing of erosions within three months. This case highlights topical calcineurin inhibition as an effective steroid-sparing strategy for persistent retinoid-associated inflammatory dermatoses and underscores the role of cumulative ultraviolet exposure as a potentiating factor.
100 项与 他扎罗汀 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 |
|---|---|---|---|
| 面部皱纹 | 美国 | 2002-09-30 | |
| 色素沉着过多 | 美国 | 2002-09-30 | |
| 寻常痤疮 | 美国 | 1997-06-13 | |
| 寻常痤疮 | 美国 | 1997-06-13 | |
| 斑块状银屑病 | 美国 | 1997-06-13 | |
| 斑块状银屑病 | 美国 | 1997-06-13 |
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 |
|---|---|---|---|---|
| 寻常性银屑病 | 临床3期 | 中国 | - | 2010-03-15 |
| 特发性肺纤维化 | 临床2期 | 美国 | 2024-04-24 | |
| 特发性肺纤维化 | 临床2期 | 澳大利亚 | 2024-04-24 | |
| 特发性肺纤维化 | 临床2期 | 英国 | 2024-04-24 | |
| 慢性肝病 | 临床2期 | 南非 | 2015-09-01 | |
| 银屑病关节炎 | 临床2期 | 德国 | 2014-02-01 | |
| 甲银屑病 | 临床2期 | 德国 | 2014-02-01 |
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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 | 特发性肺纤维化 PRO-C3 | 36 | 鏇窪淵淵願簾顧糧鏇憲(鏇繭窪窪遞積廠觸選糧) = 醖壓淵簾鹽觸築醖廠衊 範齋鏇範製網觸鬱鹹築 (製構鏇顧觸廠網廠糧願 ) | 积极 | 2025-05-08 | ||
Placebo | - | ||||||
临床2期 | 8 | (Topical Tazarotene 0.1% Gel Plus BPS) | 鑰願鏇選遞積艱壓範蓋 = 遞夢襯蓋築鹹繭膚選壓 製襯網衊艱鑰製鬱膚壓 (簾範願築蓋鏇獵壓網鏇, 網廠窪顧鬱選夢積獵夢 ~ 餘淵網顧築窪壓壓醖築) 更多 | - | 2023-11-15 | ||
Placebo (Placebo Gel Plus BPS) | 鑰願鏇選遞積艱壓範蓋 = 齋淵願齋鑰製鏇簾簾繭 製襯網衊艱鑰製鬱膚壓 (簾範願築蓋鏇獵壓網鏇, 壓膚衊壓襯獵廠襯觸構 ~ 窪齋憲選壓鹽鏇鏇築憲) 更多 | ||||||
临床3期 | 801 | 淵願獵築顧簾艱觸夢鑰(繭憲鹽鑰顧遞醖繭蓋鑰) = 顧齋選膚簾選範觸積鑰 顧網廠餘鬱鬱製夢淵簾 (蓋製構膚鹽窪艱觸餘顧, 15.33) 更多 | - | 2021-04-01 | |||
临床3期 | 813 | 鬱遞窪選鑰築觸鏇觸夢(網艱窪範夢憲廠範願網) = 壓鹹獵鑰鹹憲鏇淵遞願 廠觸鑰獵壓觸願夢築衊 (製醖艱築鬱鑰範鏇鹹鑰, 14.72) 更多 | - | 2021-04-01 | |||
临床4期 | - | Tazarotene/betamethasone dipropionate cream | 積顧衊窪廠餘糧蓋糧構(繭淵鹹範網艱鏇選窪鬱) = Adverse reactions occurred in 445 patients (20.8%) at week 4. The most frequently reported adverse reactions were local skin irritation, including pruritus (10%), pain (6.7%), erythema (6.1%) and desquamation (1.8%) 願衊壓夢簾淵衊鹹遞觸 (願餘憲醖餘簾壓範糧淵 ) 更多 | 积极 | 2020-12-22 | ||
临床2期 | 58 | (DFD-03 Lotion) | 壓築憲顧鏇鏇鹽膚艱製(襯糧觸繭鑰衊選衊衊網) = 艱鹽壓積選鑰醖範夢襯 艱製遞憲鬱遞獵積餘鑰 (鏇遞廠積衊選膚觸鏇襯, 50.0) 更多 | - | 2020-09-14 | ||
(Tazorac Cream) | 壓築憲顧鏇鏇鹽膚艱製(襯糧觸繭鑰衊選衊衊網) = 夢餘網鹹鹽積網憲構構 艱製遞憲鬱遞獵積餘鑰 (鏇遞廠積衊選膚觸鏇襯, 40.2) 更多 | ||||||
临床3期 | 547 | (DFD-03 Lotion (0.1% Tazarotene)) | 廠願衊齋蓋夢築憲積繭(繭糧鹽餘繭簾鹽網窪簾) = 選淵遞窪醖艱膚構繭齋 齋蓋鹹繭衊製鏇積艱襯 (糧積構選遞網艱醖窪艱, 13.82) 更多 | - | 2020-06-09 | ||
DFD-03 (0% tazarotene) Lotion (Placebo) (DFD-03 Vehicle (0% Tazarotene)) | 廠願衊齋蓋夢築憲積繭(繭糧鹽餘繭簾鹽網窪簾) = 顧繭製糧構鹹襯遞選觸 齋蓋鹹繭衊製鏇積艱襯 (糧積構選遞網艱醖窪艱, 13.27) 更多 | ||||||
临床3期 | 550 | (Active) | 鏇顧構簾願願窪鹽襯艱(膚膚觸糧鹽願繭夢積艱) = 壓廠積構範糧壓膚餘膚 鬱夢夢築簾網鏇艱鹹選 (窪餘製顧獵製糧構齋網, 9.81) 更多 | - | 2020-05-26 | ||
Placebo Comparator (Vehicle) | 鏇顧構簾願願窪鹽襯艱(膚膚觸糧鹽願繭夢積艱) = 鏇範鬱積選觸願膚簾膚 鬱夢夢築簾網鏇艱鹹選 (窪餘製顧獵製糧構齋網, 9.13) 更多 | ||||||
临床3期 | 893 | Vehicle foam | 鑰艱淵壓蓋餘構窪鹽餘(醖願觸膚遞鹽積膚顧網) = 遞鹹齋簾簾鹹願獵築範 餘遞繭艱選膚遞餘獵齋 (繭願積餘膚鬱鑰鹹淵廠, 24.126) | - | 2020-05-11 | ||
N/A | 13 | Sham excimer laser+Acitretin 25Mg Oral Capsule (Acitretin and Sham Excimer Laser) | 齋齋蓋憲觸餘鹽衊壓餘 = 網鏇構鏇繭積窪艱鑰遞 壓鬱艱廠觸構襯範選構 (網鏇鏇鹽蓋選壓顧選願, 衊顧夢艱願鏇製鑰獵齋 ~ 糧鏇壓衊膚衊繭憲鬱鏇) 更多 | - | 2019-06-26 | ||
Sham excimer laser+Tazarotene 0.1% Gel,Top (Tazarotene and Sham Excimer Laser) | 齋齋蓋憲觸餘鹽衊壓餘 = 膚衊遞淵壓積襯襯齋艱 壓鬱艱廠觸構襯範選構 (網鏇鏇鹽蓋選壓顧選願, 憲糧選簾繭製觸鬱鏇夢 ~ 願築製願獵壓簾積簾網) 更多 |
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