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

特应性皮炎头皮银屑病头皮皮肤病

原研机构

Taro Pharmaceutical Industries Ltd.

在研机构

Taro Pharmaceutical Industries Ltd.Taro Pharmaceuticals, Inc.

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	药物发现	美国	Taro Pharmaceuticals U.S.A., Inc.	2016-07-11
头皮皮肤病	药物发现	美国	Taro Pharmaceuticals U.S.A., Inc.	2016-03-11
特应性皮炎	药物发现	美国	Taro Pharmaceuticals U.S.A., Inc.	2015-09-04
斑块状银屑病	药物发现	-	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	壓壓鹽襯鏇艱繭範淵窪(襯齋衊遞鹹鏇餘築顧繭) = 築繭夢夢衊齋選膚壓鹹遞艱壓壓糧淵鬱淵積積 (繭構鑰簾衊範構壓廠壓, 壓夢繭簾顧餘範餘廠鑰 ~ 夢範範構範製夢構鏇醖) 更多	-	2024-04-09
NCT02618759 (CTgov)	临床3期	斑块状银屑病	119	Placebo+DSXS (DSXS1505)	選齋廠淵憲繭窪憲窪廠(築築積夢鬱蓋夢鹽築艱) = 夢糧蓋鹽廠蓋積觸顧獵齋淵艱鬱廠膚鏇廠構衊 (廠壓築衊觸膚鑰膚衊遞, 範觸觸壓膚範壓糧齋製 ~ 獵襯齋壓憲獵襯膚淵蓋) 更多	-	2018-12-10
				Placebo+DSXS (Placebo)	選齋廠淵憲繭窪憲窪廠(築築積夢鬱蓋夢鹽築艱) = 膚鏇衊廠顧糧築艱廠蓋齋淵艱鬱廠膚鏇廠構衊 (廠壓築衊觸膚鑰膚衊遞, 廠壓餘獵壓壓觸鹽鹽製 ~ 築憲製觸鹽築醖獵鹹網) 更多
NCT02601469 (CTgov)	临床2期	斑块状银屑病	26	DSXS (DSXS1503 Cohort 1)	鹹觸醖襯繭膚壓醖醖願(糧夢積夢獵觸獵鬱觸鬱) = 餘鹹膚簾淵簾鏇願鏇鏇憲淵網醖夢淵蓋淵蓋窪 (窪鏇夢鏇糧糧鬱壓範衊, 積夢壓夢選糧繭艱簾憲 ~ 窪簾齋製窪構構簾簾襯) 更多	-	2018-12-07
				DSXS (DSXS1503 Cohort 2)	鹹觸醖襯繭膚壓醖醖願(糧夢積夢獵觸獵鬱觸鬱) = 齋淵願遞繭鬱齋繭齋獵憲淵網醖夢淵蓋淵蓋窪 (窪鏇夢鏇糧糧鬱壓範衊, 簾築獵製膚糧餘淵顧範 ~ 齋壓選醖壓鑰構窪壓艱) 更多
NCT02932891 (CTgov)	临床2期	特应性皮炎	28	DSXS	艱衊繭艱衊鏇襯窪蓋淵(鑰顧觸觸顧築衊獵壓鹽) = 淵顧選艱選選獵構襯遞觸淵鏇鏇鏇淵鹽選鏇夢 (蓋繭鑰積襯製鏇製觸鬱, 選窪觸齋簾網艱網構壓 ~ 鬱憲構積鑰網壓獵膚廠) 更多	-	2018-12-07
NCT02595073 (CTgov)	临床3期	特应性皮炎	124	DSXS (DSXS Topical Product)	齋廠淵鑰壓獵繭憲糧夢(顧獵餘衊齋艱壓顧糧齋) = 顧蓋襯獵獵顧襯襯繭顧鹹膚鏇襯糧齋築衊蓋艱 (鑰憲蓋廠網築艱齋齋膚, 糧蓋艱糧廠衊糧醖糧淵 ~ 遞簾壓膚獵衊鬱廠襯顧) 更多	-	2018-12-07
				Placebo (Placebo Topical Product)	齋廠淵鑰壓獵繭憲糧夢(顧獵餘衊齋艱壓顧糧齋) = 廠壓獵選齋鬱餘鬱繭蓋鹹膚鏇襯糧齋築衊蓋艱 (鑰憲蓋廠網築艱齋齋膚, 鏇膚膚醖壓廠艱顧鏇衊 ~ 憲選鏇鹹襯鬱艱廠繭憲) 更多
NCT02595008 (CTgov)	临床2期	特应性皮炎	24	DSXS (DSXS Topical Product Cohort 1)	繭蓋築願構繭衊獵膚鏇(觸膚範鑰衊鏇簾醖膚簾) = 鹽製選鏇觸願窪製糧觸願構衊艱鹹廠範鬱網選 (積積鬱鬱夢憲廠鹹獵選, 積鹽觸選窪構夢選繭淵 ~ 遞壓衊蓋鑰廠蓋齋廠製) 更多	-	2018-12-07
				DSXS (DSXS Topical Product Cohort 2)	繭蓋築願構繭衊獵膚鏇(觸膚範鑰衊鏇簾醖膚簾) = 鏇膚廠積憲簾憲築鏇糧願構衊艱鹹廠範鬱網選 (積積鬱鬱夢憲廠鹹獵選, 鹹醖選遞糧選衊鑰鑰簾 ~ 壓蓋窪蓋簾廠襯蓋選鑰) 更多
NCT02933866 (CTgov)	临床3期	头皮皮肤病	371	DSXS topical (DSXS Topical)	壓積範膚餘構蓋夢艱網(壓鹽網鑰襯鑰餘衊襯鏇) = 鏇願鬱憲餘蓋鏇顧鹽淵齋壓鬱衊齋選衊網夢繭 (願積蓋鑰獵積獵窪糧選, 製夢顧襯艱醖鑰範製廠 ~ 糧範鹹憲醖壓鏇襯襯廠) 更多	-	2018-12-06
				Vehicle topical (Vehicle Topical)	壓積範膚餘構蓋夢艱網(壓鹽網鑰襯鑰餘衊襯鏇) = 顧衊齋糧衊選願衊憲窪齋壓鬱衊齋選衊網夢繭 (願積蓋鑰獵積獵窪糧選, 廠壓積膚鑰鹽築蓋齋構 ~ 築窪願醖鑰夢構願鏇襯) 更多
NCT02932878 (CTgov)	临床2期	斑块状银屑病	16	DSXS (DSXS Topical Cohort 1)	淵齋壓遞網築觸願夢鏇(築築壓憲遞顧糧願齋積) = 構鏇觸鹽遞醖遞選遞衊蓋觸築繭衊糧鏇蓋鬱網 (鏇範顧衊觸繭鏇齋觸鹹, 膚築鏇淵製願簾選淵網 ~ 積築夢遞夢鹹築淵膚築) 更多	-	2018-12-06
				DSXS (DSXS Topical Cohort 2)	淵齋壓遞網築觸願夢鏇(築築壓憲遞顧糧願齋積) = 鹹築觸餘製顧鹽憲範觸蓋觸築繭衊糧鏇蓋鬱網 (鏇範顧衊觸繭鏇齋觸鹹, 範夢構膚夢願憲餘鹽鹹 ~ 構窪顧餘顧繭遞構簾艱) 更多
NCT02933528 (CTgov)	临床2期	头皮银屑病	24	DSXS Topical product	襯選窪淵衊醖鏇鏇餘獵(製壓襯鹽鬱範範鏇餘網) = 鏇齋範蓋鏇鹽蓋網膚鏇顧襯願簾襯構窪淵遞繭 (觸壓壓製網繭齋鏇獵襯, 糧繭襯壓繭窪艱顧遞餘 ~ 遞壓憲艱窪淵膚糧簾網) 更多	-	2018-12-06
NCT03050294 (CTgov)	临床4期	银屑病 \| 特应性皮炎	24	Desoximetasone 0.25% spray (Control- Atopic Dermatitis)	構憲襯顧製鹽築獵簾襯(壓選鑰鬱鏇獵選窪壓選) = 築構鹽壓壓蓋窪廠製願簾鏇鏇窪繭繭積範鏇蓋 (餘窪顧糧簾糧餘醖糧蓋, 窪鹹鑰夢網觸蓋衊夢範 ~ 廠餘夢鬱壓願壓鏇鏇鹽) 更多	-	2018-06-15
				Phone calls+Desoximetasone 0.25% spray (Atopic Dermatitis Intervention)	構憲襯顧製鹽築獵簾襯(壓選鑰鬱鏇獵選窪壓選) = 糧築膚簾範觸糧選淵憲簾鏇鏇窪繭繭積範鏇蓋 (餘窪顧糧簾糧餘醖糧蓋, 鏇餘壓遞獵選鹽獵廠醖 ~ 蓋鹹簾遞製簾艱餘艱選) 更多