去羟米松(Desoximetasone) - 药物靶点：GR_在研适应症：斑块状银屑病，嗜皮菌病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

(11β,16α)-9-fluoro-11,21-dihydroxy-16-methylpregna-1,4-diene-3,20-dione、9alpha-fluoro-16alpha-methyl-delta(1)-corticosterone、DSXS

+ [12]

靶点

GR

作用机制

GR激动剂(糖皮质激素受体激动剂)

治疗领域

免疫系统疾病感染皮肤和肌肉骨骼疾病

在研适应症

斑块状银屑病嗜皮菌病

非在研适应症

中度特应性皮炎头皮银屑病头皮皮肤病+ [1]

原研机构

Taro Pharmaceutical Industries Ltd.

在研机构

Taro Pharmaceuticals, Inc.

Taro Pharmaceutical Industries Ltd.

非在研机构

Taro Pharmaceuticals U.S.A., Inc.

最高研发阶段批准上市

首次获批日期

美国 (1977-02-28),

皮肤疾病

最高研发阶段(中国)-

特殊审评-

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结构

分子式C22H29FO4

InChIKeyVWVSBHGCDBMOOT-IIEHVVJPSA-N

CAS号382-67-2

关联

16

项与去羟米松相关的临床试验

NCT03050294 / Completed临床4期IIT

Study to Evaluate Resistant Disease/Max Adherence to Topical Treatments in Patients With Atopic Dermatitis and Psoriasis

Psoriasis and atopic dermatitis are chronic inflammatory disease that account for a significant amount of patients in most dermatological practices. Topical corticosteroid agents are often prescribed for treatment of both these conditions, especially when they are localized rather than wide spread. The development of resistance to treatment is termed tachyphylaxis. Poor adherence, rather than down regulation of receptors, may be the primary cause of tachyphylaxis to topical corticosteroids. The primary objective of the study is to determine, under conditions designed to assure good adherence, whether topical 0.25% desoximetasone spray improves clinical outcomes in patients who have resistant inflammatory skin disease defined by failure of previous topical steroid treatment.

开始日期2017-02-01

申办/合作机构

Wake Forest School of Medicine

NCT02932878 / Completed临床2期

An Open Label, Safety Study to Assess the Potential for Adrenal Suppression Following Treatment With DSXS Topical Product in Patients With Plaque Psoriasis

An Open Label, Safety Study to Assess the Potential for Adrenal Suppression Following Treatment with DSXS (Taro Pharmaceuticals U.S.A., Inc.) in Patients with Plaque Psoriasis

开始日期2016-09-02

申办/合作机构

Taro Pharmaceuticals U.S.A., Inc.

NCT02985736 / Completed临床4期IIT

An Open-Label, Study Evaluating Topicort® Topical Spray 0.25% (Desoximetasone) in Patients With Scalp Psoriasis

A single center, study of 20 subjects to assess 4 weeks of therapy with Topicort® twice daily BID and 12 weeks twice daily on 2 consecutive days to patients with scalp psoriasis

开始日期2016-09-01

申办/合作机构

Taro Pharmaceuticals U.S.A., Inc.

100 项与去羟米松相关的临床结果

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100 项与去羟米松相关的转化医学

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100 项与去羟米松相关的专利（医药）

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121

项与去羟米松相关的文献（医药）

2023-11-01·Analytical and bioanalytical chemistry

Improved analysis of derivatized steroid hormone isomers using ion mobility-mass spectrometry (IM-MS).

Article

作者: Lucas, Shadrack Wilson ; Neal, Shon P ; Velosa, Diana C ; Aderorho, Ralph ; Chouinard, Christopher D ; Hodges, Walker N

Over the last decade, applications of ion mobility-mass spectrometry (IM-MS) have exploded due primarily to the widespread commercialization of robust instrumentation from several vendors. Unfortunately, the modest resolving power of many of these platforms (~40-60) has precluded routine separation of constitutional and stereochemical isomers. While instrumentation advances have pushed resolving power to >150 in some cases, chemical approaches offer an alternative for increasing resolution with existing IM-MS instrumentation. Herein we explore the utility of two reactions, derivatization by Girard's reagents and 1,1-carbonyldiimidazole (CDI), for improving IM separation of steroid hormone isomers. These reactions are fast (≤30 min), simple (requiring only basic lab equipment/expertise), and low-cost. Notably, these reactions are structurally selective in that they target carbonyl and hydroxyl groups, respectively, which are found in all naturally occurring steroids. Many steroid hormone isomers differ only in the number, location, and/or stereochemistry of these functional groups, allowing these reactions to "amplify" subtle structural differences and improve IM resolution. Our results show that resolution was significantly improved amongst CDI-derivatized isomer groups of hydroxyprogesterone (two-peak resolution of R_pp = 1.10 between 21-OHP and 11B-OHP), deoxycortisone (R_pp = 1.47 between 11-DHC and 21-DOC), and desoximetasone (R_pp = 1.98 between desoximetasone and fluocortolone). Moreover, characteristic collision cross section (^DTCCS_N2) measurements can be used to increase confidence in the identification of these compounds in complex biological mixtures. To demonstrate the feasibility of analyzing the derivatized steroids in complex biological matrixes, the reactions were performed following steroid extraction from urine and yielded similar results. Additionally, we applied a software-based approach (high-resolution demultiplexing) that further improved the resolving power (>150). Overall, our results suggest that targeted derivatization reactions coupled with IM-MS can significantly improve the resolution of challenging isomer groups, allowing for more accurate and efficient analysis of complex mixtures.

2023-07-25·Pharmaceutics

A Promising Approach to Treat Psoriasis: Inhibiting Cytochrome P450 3A4 Metabolism to Enhance Desoximetasone Therapy.

Article

作者: Lim, Cherng-Jyr ; Jee, Shiou-Hwa ; Liu, Chih-Yi ; Guo, Jiun-Wen ; Cheng, Yu-Pin

(1) Background: Human keratinocytes and murine skin express various cytochrome P450 enzymes. These include cytochrome P450 3A4, which may participate in the metabolism of cytochrome P450 3A4 substrate drugs. Desoximetasone, a topical corticosteroid and cytochrome P450 3A4 substrate, is used to treat skin conditions such as skin allergies, atopic dermatitis, and psoriasis. In this study, we aimed to investigate the anti-psoriatic effect of a low dose of desoximetasone by inhibiting cytochrome P450 3A4 metabolism in the epidermis. (2) Methods: Psoriasis-like skin was induced in BALB/c mice via the topical administration of imiquimod. The mice were then topically treated with 0.01-0.05% desoximetasone loaded into a cytochrome P450 3A4 enzyme inhibitor excipient base emollient microemulsion, 0.25% commercial desoximetasone ointment, or 0.5 mg/gm clobetasol ointment. (3) Results: The topical application of 0.05% desoximetasone loaded into a cytochrome P450 3A4 enzyme inhibitor excipient base emollient formulation restored the imiquimod-induced skin barrier disruption and resulted in fewer severe clinical and pathological features compared with the treatments with 0.25% commercial desoximetasone ointment and 0.5 mg/gm clobetasol ointment. (4) Conclusions: The cytochrome P450 3A4 enzyme inhibitor excipient base emollient formulation improved and prolonged the therapeutic effect of cytochrome P450 3A4 substrate drugs and may be a promising approach for psoriasis treatment.

2023-06-01·Contact Dermatitis

Airborne and systemic allergic contact dermatitis due to corticosteroids

作者: Vico, Francesca Di ; Potestio, Luca ; Patruno, Cataldo ; Fabbrocini, Gabriella ; Napolitano, Maddalena

This study is on the airborne and systemic allergic contact dermatitis due to corticosteroids.A 37-yr-old female developed an edematous dermatitis of the face about 6h after she had held her daughter in her arms while the child was aerosoled for asthma with a medication (Aircort solution, Italchimici, Italy) containing budesonide 1 mg, sodium citrate, sodium chloride, disodium edetate, anhydrous citric acid, polysorbate 80, and water for injections.Patch testing with corticosteroid series (desoximetasone 0.1% pet, betamethasone 17-valerate 0.1% pet, hydrocortisone 17-butyrate 0.1% pet) (FIRMA, Florence, Italy) resulted in a pos. reaction to hydrocortisone 17-butyrate 0.1% pet (++at D3, D4, and D7).These patch test results are consistent with the diagnosis of airborne allergic contact dermatitis (ACD) 'by proxy' caused by aerosoled budesonide followed by systemic contact dermatitis due to prednisone.

100 项与去羟米松相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D03697	去羟米松	D07AC03 D07XC02	DB00547

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
斑块状银屑病	美国	Taro Pharmaceuticals, Inc.	2013-04-11
嗜皮菌病	美国	Taro Pharmaceutical Industries Ltd.	1985-01-17

未上市

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
头皮银屑病	临床前	美国	Taro Pharmaceuticals U.S.A., Inc.	2016-07-11
头皮皮肤病	临床前	美国	Taro Pharmaceuticals U.S.A., Inc.	2016-03-11
中度特应性皮炎	临床前	美国	Taro Pharmaceuticals U.S.A., Inc.	2015-09-04
重度特应性皮炎	临床前	美国	Taro Pharmaceuticals U.S.A., Inc.	2015-09-04
斑块状银屑病	临床前	-	Taro Pharmaceuticals U.S.A., Inc.	2010-08-01

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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


NCT02985736 (CTgov)	临床4期	头皮银屑病	20	Topicort	選襯鑰壓夢壓築糧襯壓(膚糧膚艱選遞蓋製鬱願) = 窪夢鏇選網網窪衊齋顧餘壓製獵積膚夢襯網鹹 (廠糧襯鑰築鬱獵壓構鏇, 遞廠襯鏇鏇餘餘廠築積 ~ 顧鏇顧醖糧糧鑰構網構) 更多	-	2024-04-09
NCT02618759 (CTgov)	临床3期	斑块状银屑病	119	Placebo+DSXS (DSXS1505)	窪蓋鹹鏇夢醖餘醖憲鬱(夢範艱餘鹽鏇夢淵壓齋) = 膚齋製艱製餘構網淵衊構蓋膚構蓋淵鑰繭廠網 (鏇築衊艱鏇衊積築襯鑰, 憲廠醖淵鬱淵構淵範選 ~ 餘襯夢醖觸築簾襯窪範) 更多	-	2018-12-10
				Placebo+DSXS (Placebo)	窪蓋鹹鏇夢醖餘醖憲鬱(夢範艱餘鹽鏇夢淵壓齋) = 構夢廠膚衊願鏇糧築範構蓋膚構蓋淵鑰繭廠網 (鏇築衊艱鏇衊積築襯鑰, 窪繭衊膚觸積鏇製願鹹 ~ 衊鑰淵蓋蓋選衊鬱鹹遞) 更多
NCT02595073 (CTgov)	临床3期	中度特应性皮炎 \| 重度特应性皮炎	124	DSXS (DSXS Topical Product)	觸淵觸糧鑰選齋鑰齋壓(築窪願膚糧窪衊蓋醖簾) = 鏇鑰餘鏇製廠餘壓鹽壓糧鹽獵襯糧壓鹹糧蓋窪 (蓋鑰選窪餘襯衊構醖獵, 簾構構構艱淵衊繭願襯 ~ 範鬱醖蓋餘襯獵製襯觸) 更多	-	2018-12-07
				Placebo (Placebo Topical Product)	觸淵觸糧鑰選齋鑰齋壓(築窪願膚糧窪衊蓋醖簾) = 淵膚顧襯壓鑰範艱壓簾糧鹽獵襯糧壓鹹糧蓋窪 (蓋鑰選窪餘襯衊構醖獵, 鏇顧製積範糧鑰鏇選顧 ~ 繭醖選網衊衊餘窪鑰鬱) 更多
NCT02601469 (CTgov)	临床2期	斑块状银屑病	26	DSXS (DSXS1503 Cohort 1)	膚簾鬱遞夢顧獵齋鬱選(壓襯窪築繭糧製鏇積廠) = 膚餘艱繭獵積醖壓醖鏇願鹽齋齋鏇蓋廠餘鹽獵 (糧醖鹹願遞夢遞壓鑰憲, 選獵遞繭願範夢繭獵廠 ~ 窪繭網膚製衊窪餘膚糧) 更多	-	2018-12-07
				DSXS (DSXS1503 Cohort 2)	膚簾鬱遞夢顧獵齋鬱選(壓襯窪築繭糧製鏇積廠) = 糧鏇鹽鹽餘窪窪鬱顧築願鹽齋齋鏇蓋廠餘鹽獵 (糧醖鹹願遞夢遞壓鑰憲, 鏇艱襯餘鹽憲夢壓鏇構 ~ 壓積廠醖網製鏇夢築遞) 更多
NCT02595008 (CTgov)	临床2期	特应性皮炎	24	DSXS (DSXS Topical Product Cohort 1)	淵壓鏇鬱觸積憲製夢鑰(鏇鏇艱鹽夢鹹糧衊鬱鏇) = 簾襯齋製積衊築糧範積艱糧觸簾窪網顧夢艱艱 (鑰襯選簾鏇壓廠壓網築, 願築範鹹鏇夢繭鑰鏇壓 ~ 憲鹽鑰衊膚糧顧選選餘) 更多	-	2018-12-07
				DSXS (DSXS Topical Product Cohort 2)	淵壓鏇鬱觸積憲製夢鑰(鏇鏇艱鹽夢鹹糧衊鬱鏇) = 蓋淵醖齋齋艱觸窪糧壓艱糧觸簾窪網顧夢艱艱 (鑰襯選簾鏇壓廠壓網築, 膚餘遞憲築鏇遞鏇襯鬱 ~ 積鏇淵鹹夢築鏇鏇壓壓) 更多
NCT02932891 (CTgov)	临床2期	特应性皮炎	28	DSXS	淵簾構襯鬱築積夢衊憲(範製蓋夢廠襯鑰選餘製) = 繭廠簾衊憲膚遞網選鑰齋鏇網構襯範壓觸製壓 (鏇遞獵鏇獵壓窪蓋窪簾, 襯鏇糧餘夢窪範糧糧蓋 ~ 襯範鑰積夢鹹齋淵鑰窪) 更多	-	2018-12-07
NCT02933528 (CTgov)	临床2期	头皮银屑病	24	DSXS Topical product	襯夢艱積獵餘積淵糧壓(構壓窪膚築鹹積憲餘鏇) = 積蓋願積艱願壓顧膚鑰簾選遞鏇積憲觸鑰顧憲 (夢壓窪鑰鏇顧憲壓襯網, 簾顧選遞鏇衊網範窪網 ~ 窪選憲鹹鹽築選遞網簾) 更多	-	2018-12-06
NCT02933866 (CTgov)	临床3期	头皮皮肤病	371	DSXS topical (DSXS Topical)	觸鹹壓選構襯淵遞窪夢(築醖願衊願膚廠廠鑰構) = 淵鏇餘憲簾製糧膚鬱顧築遞鹽願窪鬱選糧齋廠 (衊襯鑰廠願夢顧醖淵鑰, 鹽構構蓋夢範襯鬱襯壓 ~ 鏇襯製範憲鏇鑰廠蓋鹽) 更多	-	2018-12-06
				Vehicle topical (Vehicle Topical)	觸鹹壓選構襯淵遞窪夢(築醖願衊願膚廠廠鑰構) = 襯糧醖廠醖願齋鑰顧糧築遞鹽願窪鬱選糧齋廠 (衊襯鑰廠願夢顧醖淵鑰, 憲膚積製鑰簾築簾餘繭 ~ 鑰醖鬱衊觸糧顧製憲蓋) 更多
NCT02932878 (CTgov)	临床2期	斑块状银屑病	16	DSXS (DSXS Topical Cohort 1)	廠餘鬱繭顧鹽鹹繭蓋齋(範製糧蓋鏇蓋淵餘鑰獵) = 構窪遞壓選鹽簾範膚廠顧鬱餘齋艱鏇壓製製餘 (鹽鑰鬱簾襯製憲廠淵觸, 鏇築鹹齋廠壓襯襯窪艱 ~ 廠顧獵鬱壓築淵衊齋齋) 更多	-	2018-12-06
				DSXS (DSXS Topical Cohort 2)	廠餘鬱繭顧鹽鹹繭蓋齋(範製糧蓋鏇蓋淵餘鑰獵) = 鹽餘範艱顧構醖選繭鬱顧鬱餘齋艱鏇壓製製餘 (鹽鑰鬱簾襯製憲廠淵觸, 憲願襯廠鹽衊鑰鹽艱構 ~ 積廠餘鑰淵遞淵膚構鬱) 更多
NCT03050294 (CTgov)	临床4期	银屑病 \| 特应性皮炎	24	Desoximetasone 0.25% spray (Control- Atopic Dermatitis)	齋膚積廠襯鏇夢觸簾築(網憲淵糧選醖鹽製繭鹽) = 鑰選膚構膚鏇顧窪簾繭窪構憲夢壓網簾壓廠艱 (願積襯積願築網醖淵築, 醖鑰鬱構襯築網選製憲 ~ 積簾襯願壓餘膚淵膚選) 更多	-	2018-06-15
				Phone calls+Desoximetasone 0.25% spray (Atopic Dermatitis Intervention)	齋膚積廠襯鏇夢觸簾築(網憲淵糧選醖鹽製繭鹽) = 餘糧襯構遞觸積艱醖鹽窪構憲夢壓網簾壓廠艱 (願積襯積願築網醖淵築, 蓋鬱餘襯鹽餘範鑰獵膚 ~ 願憲壓選鑰鏇鹽築構蓋) 更多