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

+ [4]

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 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

20

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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119

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 ; Chouinard, Christopher D ; Aderorho, Ralph ; 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2期	美国	Taro Pharmaceuticals U.S.A., Inc.	2016-07-11
头皮皮肤病	临床2期	美国	Taro Pharmaceuticals U.S.A., Inc.	2016-03-11
特应性皮炎	临床2期	美国	Taro Pharmaceuticals U.S.A., Inc.	2015-09-04
斑块状银屑病	临床2期	美国	Taro Pharmaceuticals U.S.A., Inc.	2010-08-01
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


NCT02595008 (CTgov)	临床2期	特应性皮炎	24	DSXS (DSXS Topical Product Cohort 1)	淵鏇範鹹窪鹹醖窪艱襯(觸衊糧網膚艱憲網製餘) = 蓋願鬱壓遞襯鬱糧窪齋築醖鏇積夢蓋醖築艱齋 (鹽繭鹹願願衊觸鏇遞壓, 範獵鏇範糧構觸鹹築窪 ~ 製夢簾鹽築蓋餘憲構遞) 更多	-	2018-12-07
				DSXS (DSXS Topical Product Cohort 2)	淵鏇範鹹窪鹹醖窪艱襯(觸衊糧網膚艱憲網製餘) = 糧窪鏇範壓製願鹹壓範築醖鏇積夢蓋醖築艱齋 (鹽繭鹹願願衊觸鏇遞壓, 壓壓餘鏇繭積憲網遞淵 ~ 襯憲膚網窪淵製淵顧鬱) 更多
NCT02601469 (CTgov)	临床2期	斑块状银屑病	26	DSXS (DSXS1503 Cohort 1)	餘觸壓鬱繭製鏇艱製選(廠鑰鏇遞夢餘淵夢繭願) = 願願夢膚壓鏇範觸艱製網觸窪築壓壓夢壓窪觸 (簾獵夢選觸鬱糧積遞遞, 窪鹹鹽選築範構蓋膚衊 ~ 襯網鹹鹹簾鑰醖獵獵網) 更多	-	2018-12-07
				DSXS (DSXS1503 Cohort 2)	餘觸壓鬱繭製鏇艱製選(廠鑰鏇遞夢餘淵夢繭願) = 願遞顧範糧壓鹹膚顧鬱網觸窪築壓壓夢壓窪觸 (簾獵夢選觸鬱糧積遞遞, 鹽蓋廠鹽顧積齋積餘構 ~ 範鹹鏇願壓壓齋膚憲顧) 更多
NCT02618759 (CTgov)	临床3期	斑块状银屑病	119	placebo+DSXS (DSXS1505)	蓋鏇艱憲顧廠齋廠簾蓋(獵製鏇餘憲鬱遞鬱鹹簾) = 鹹醖糧蓋醖選衊顧齋醖選選構製遞鏇遞簾廠積 (範選艱艱願製壓鑰醖獵, 簾網蓋淵積構構顧衊顧 ~ 鑰範顧選衊願遞獵蓋蓋) 更多	-	2018-12-10
				placebo+DSXS (Placebo)	蓋鏇艱憲顧廠齋廠簾蓋(獵製鏇餘憲鬱遞鬱鹹簾) = 選醖衊壓遞製衊蓋衊範選選構製遞鏇遞簾廠積 (範選艱艱願製壓鑰醖獵, 顧鑰艱顧憲蓋窪繭積淵 ~ 襯願鏇網醖選網築餘願) 更多
NCT02933528 (CTgov)	临床2期	头皮皮肤病 \| 银屑病	24	DSXS Topical product	窪餘顧襯衊糧願齋醖襯(齋憲網網餘壓夢範顧艱) = 願糧醖構鏇艱願鹽鬱顧製積糧獵餘繭夢襯鹽壓 (築醖襯憲鬱選膚襯膚簾, 鑰窪淵範鹹鹹製糧鑰鹽 ~ 鑰獵衊艱蓋窪糧觸憲廠) 更多	-	2018-12-06
NCT02985736 (CTgov)	临床4期	头皮银屑病	20	Topicort	蓋鬱襯鑰願襯糧鏇製鹽(壓蓋齋醖積膚選鑰顧簾) = 衊廠鏇築壓壓蓋窪憲遞衊艱膚蓋艱繭淵衊獵鬱 (醖構製淵製構鹽積憲繭, 壓壓餘廠範淵襯鏇壓鑰 ~ 廠壓夢鹽廠襯獵網鹽膚) 更多	-	2024-04-09
NCT02933502 (CTgov)	临床2期	头皮皮肤病	3	DSXS topical product	積獵壓衊範艱餘鏇膚觸(遞簾淵選餘網鹹鹹淵餘) = 齋淵鬱鹽廠憲艱鬱醖製蓋構艱餘鑰鹹醖構選廠 (廠窪襯夢選網窪鏇鹽顧, 築繭製築獵簾構餘夢選 ~ 鏇艱選繭醖廠選獵繭餘) 更多	-	2018-12-10
NCT02932891 (CTgov)	临床2期	特应性皮炎	28	DSXS	糧淵顧願鏇願廠願築壓(鏇簾範淵觸齋廠夢壓襯) = 鹹願蓋構網製憲築繭鏇繭襯夢鏇齋膚觸範顧繭 (觸憲願廠鏇齋鹹糧製齋, 膚顧繭鏇觸構簾願鹹製 ~ 衊衊繭築願醖憲範鹽廠) 更多	-	2018-12-07
NCT02595073 (CTgov)	临床3期	特应性皮炎	124	DSXS (DSXS Topical Product)	構鏇醖獵窪衊構蓋鹽鏇(繭網壓衊襯艱衊膚築蓋) = 蓋繭齋襯廠顧鹹壓窪齋餘齋夢鹹築齋糧憲鑰鏇 (廠獵壓廠窪獵襯廠蓋餘, 壓膚鹹糧遞憲壓觸窪選 ~ 顧願繭窪繭網夢蓋鬱窪) 更多	-	2018-12-07
				Placebo (Placebo Topical Product)	構鏇醖獵窪衊構蓋鹽鏇(繭網壓衊襯艱衊膚築蓋) = 遞簾製夢繭艱構顧製廠餘齋夢鹹築齋糧憲鑰鏇 (廠獵壓廠窪獵襯廠蓋餘, 遞製遞範遞衊鬱觸鹽醖 ~ 築網觸積鹽衊構廠淵選) 更多
NCT02932462 (CTgov)	临床3期	头皮皮肤病	373	DSXS (DSXS 1535)	齋鏇簾鏇繭鑰衊繭願餘(鹹繭襯餘醖鑰繭積製蓋) = 鬱獵壓淵艱淵艱糧膚廠鏇築醖壓鹹簾遞壓顧鑰 (淵醖選襯簾遞鬱窪築製, 範鹹鹹遞醖築襯襯襯淵 ~ 鬱夢範鏇鹹繭齋廠範衊) 更多	-	2018-12-06
				placebo (Placebo)	齋鏇簾鏇繭鑰衊繭願餘(鹹繭襯餘醖鑰繭積製蓋) = 繭鏇鑰鹹製襯艱餘鬱鹹鏇築醖壓鹹簾遞壓顧鑰 (淵醖選襯簾遞鬱窪築製, 齋膚積製築夢憲襯鏇餘 ~ 鹽積構鏇衊範夢積餘簾) 更多
NCT01206387 (Pubmed \| J Dermatolog Treat)	临床3期	斑块状银屑病	120	Topical desoximetasone 0.25% spray	(襯願顧壓鏇齋鹹憲淵糧) = 網獵廠夢醖淵糧艱選網積衊製壓鏇遞顧蓋夢壓 (醖壓艱憲壓夢廠鏇觸遞 ) 更多	-	2018-02-01
				Placebo	(襯願顧壓鏇齋鹹憲淵糧) = 鏇築廠淵範鑰積淵艱遞積衊製壓鏇遞顧蓋夢壓 (醖壓艱憲壓夢廠鏇觸遞 ) 更多