阿立哌唑/盐酸舍曲林(Aripiprazole/Sertraline Hydrochloride) - 药物靶点：5-HT1A receptor x 5-HT2A receptor x D2 receptor x D3 receptor x SERT_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Aripiprazole/sertraline、Sertraline/aripiprazole

靶点

5-HT1A receptor x 5-HT2A receptor x D2 receptor x D3 receptor x SERT

作用方式

激动剂、拮抗剂、抑制剂

作用机制

5-HT1A receptor激动剂(5-羟色胺1A受体激动剂)、5-HT2A receptor拮抗剂(5-羟色胺2A受体拮抗剂)、D2 receptor激动剂(多巴胺D2受体激动剂)

+ [2]

治疗领域

其他疾病

在研适应症-

非在研适应症

重度抑郁症

原研机构

Otsuka Holdings Co., Ltd.

在研机构-

非在研机构

Otsuka Pharmaceutical Co., Ltd.

Otsuka Holdings Co., Ltd.

最高研发阶段终止申请上市

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C17H18Cl3N

InChIKeyBLFQGGGGFNSJKA-XHXSRVRCSA-N

CAS号79559-97-0

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关联

4

项与阿立哌唑/盐酸舍曲林相关的临床试验

NCT03342963

/ Completed临床1期

A Single-center, Open-label, Randomized, Two-treatment, Two-period Crossover Trial to Investigate Bioequivalence Between Single Administration of ASC-01 (Aripiprazole/Sertraline Combination Drug) and Concomitant Single Administration of Aripiprazole and Sertraline, and Food Effect on Pharmacokinetics of ASC-01 in Healthy Male Adults

To investigate the bioequivalence of aripiprazole between administration of one ASC-01 tablet (aripiprazole 3 mg/sertraline 100 mg combination drug) and concomitant administration of one aripiprazole 3-mg tablet and two sertraline 50-mg tablets (Cohort 1).
To investigate food effect on plasma pharmacokinetics of aripiprazole and sertraline by single oral administration of ASC-01 under a fasting or fed condition (Cohort 2).

开始日期2017-11-21

申办/合作机构

Otsuka Pharmaceutical Co., Ltd.

JPRN-jRCT2080222363

/ Completed临床3期

A Multicenter, Randomized, Double-blind Trial to Assess the Efficacy and Safety of ASC-01 in Patients with Major Depressive Disorder

开始日期2014-02-25

申办/合作机构

Otsuka Pharmaceutical Co., Ltd.

NCT02046564

/ Completed临床3期

A Multicenter, Randomized, Double-blind Trial to Assess the Efficacy and Safety of ASC-01 in Patients With Major Depressive Disorder

To evaluate the efficacy and the safety of ASC-01 (aripiprazole/sertraline combination) compared to sertraline monotherapy in patients with major depressive disorders who have responded incompletely to sertraline monotherapy.

开始日期2014-02-01

申办/合作机构

Otsuka Pharmaceutical Co., Ltd.

100 项与阿立哌唑/盐酸舍曲林相关的临床结果

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100 项与阿立哌唑/盐酸舍曲林相关的转化医学

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100 项与阿立哌唑/盐酸舍曲林相关的专利（医药）

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5

项与阿立哌唑/盐酸舍曲林相关的文献（医药）

2002-11-01·The Plant Journal1区 · 生物学

The plant disease resistance gene Asc‐1 prevents disruption of sphingolipid metabolism during AAL‐toxin‐induced programmed cell death

1区 · 生物学

Article

作者: Stefka D. Spassieva ; Jacques Hille ; Jonathan E. Markham

SummaryThe nectrotrophic fungus Alternaria alternata f.sp. lycopersici infects tomato plants of the genotype asc/asc by utilizing a host‐selective toxin, AAL‐toxin, that kills the host cells by inducing programmed cell death. Asc‐1 is homologous to genes found in most eukaryotes from yeast to humans, suggesting a conserved function. A yeast strain with deletions in the homologous genes LAG1 and LAC1 was functionally complemented by Asc‐1, indicating that Asc‐1 functions in an analogous manner to the yeast homologues. Examination of the yeast sphingolipids, which are almost absent in the lag1Δlac1Δ mutant, showed that Asc‐1 was able to restore the synthesis of sphingolipids. We therefore examined the biosynthesis of sphingolipids in tomato by labeling leaf discs with l‐[3‐3H]serine. In the absence of AAL‐toxin, there was no detectable difference in sphingolipid labeling between leaf discs from Asc/Asc or asc/asc leaves. In the presence of pathologically significant concentrations of AAL‐toxin however, asc/asc leaf discs showed severely reduced labeling of sphingolipids and increased label in dihydrosphingosine (DHS) and 3‐ketodihydrosphingosine (3‐KDHS). Leaf discs from Asc/Asc leaves responded to AAL‐toxin treatment by incorporating label into different sphingolipid species. The effects of AAL‐toxin on asc/asc leaflets could be partially blocked by the simultaneous application of AAL‐toxin and myriocin. Leaf discs simultaneously treated with AAL‐toxin and myriocin showed no incorporation of label into sphingolipids or long‐chain bases as expected. These results indicate that the presence of Asc‐1 is able to relieve an AAL‐toxin‐induced block on sphingolipid synthesis that would otherwise lead to programmed cell death.

1996-02-01·Experimental Cell Research

A Novel Recognition Site on Laminin for the α3β1 Integrin

Article

作者: Amy P.N. Skubitz ; Sugit Pattaramalai ; Keith M. Skubitz

Synthetic peptide GD-2 is a sequence of amino acids derived from the carboxy-terminal long arm of the A chain of laminin. Previous studies have shown that peptide GD-2 promotes the adhesion of human squamous cell carcinoma (SCC) cells as well as a variety of other cell lines. In this study, we attempted to identify the receptor that SCC cells use to adhere to peptide GD-2. Monoclonal antibodies (mAbs) against a human SCC cell line were generated. One of these mAbs, ASC-1, bound to the surface of SCC cells as determined by flow cytometry. This mAb inhibited SCC cell adhesion to peptide GD-2 and laminin, but not fibronectin or type IV collagen, suggesting that mAb ASC-1 binds to the SCC receptor for the peptide GD-2 sequence of laminin. MAb ASC-1 immunoprecipitated a complex composed of two components of 135 and 116 kDa. Immunoadsorption of ASC-1-binding material from the SCC cell extract by incubation with mAb ASC-1 resulted in the removal of the alpha 3 beta 1 integrin from the extract. Immunohistochemical staining of tissue from a normal human tongue and from a patient with SCC of the tongue revealed that mAb ASC-1 stained the surface of epithelial cells that were in contact with the basement membrane, as well as those cells located two to three layers above the basement membrane. This mAb also stained blood vessels in the squamous tissue. This staining pattern was identical to that observed when the same tissues were stained by a mAb against the alpha 3 integrin subunit. In summary, by use of a new mAb, ASC-1, that recognizes the alpha 3 beta 1 integrin, we have determined that the alpha 3 beta 1 integrin mediates SCC cell adhesion to the peptide GD-2 sequence within laminin.

1991-09-01·American journal of veterinary research

Influence of sedative and anesthetic agents on intradermal skin test reactions in dogs.

Article

作者: Eicker, S W ; Moriello, K A

To determine the effects of 9 sedative/anesthetic drug protocols on intradermal skin testing, an experimental state of type-I hypersensitivity was created. Intradermal skin tests were performed on 6 dogs, using positive and negative controls and a series of tenfold dilutions of Asc-1 allergen prior to drug administration. Approximately 4 hours later, the dogs were given 1 of the following drugs: acepromazine (low dose and high dose); ketamine hydrochloride with diazepam; thiamylal; oxymorphone; halothane; methoxyflurane; or isoflurane. The intradermal skin test then was repeated, and was scored objectively and subjectively. Objective scores were unaffected by any of the drugs. Subjective scores were affected in that acepromazine decreased wheal size and the induration of the intradermal skin test reaction sites.

100 项与阿立哌唑/盐酸舍曲林相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	阿立哌唑/盐酸舍曲林	-	-

研发状态

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
重度抑郁症	申请上市	-	Otsuka Holdings Co., Ltd.	-
重度抑郁症	申请上市	-	Otsuka Holdings Co., Ltd.	-

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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


NCT03342963 (CTgov)	临床1期	-	74	aripiprazole+sertraline+ASC-01 (ASC-01)	憲觸夢獵蓋餘鏇餘膚淵(艱範憲選製艱遞顧願廠) = 鏇遞鹽衊淵夢壓憲築淵觸壓蓋壓範淵襯蓋壓壓 (膚襯選壓選糧鑰夢顧繭, 糧夢築衊壓構範壓遞蓋 ~ 鏇夢壓憲鏇製憲遞淵淵) 更多	-	2021-05-03
				Aripiprazole+Sertraline (Aripiprazole/Sertraline Concomitant)	憲觸夢獵蓋餘鏇餘膚淵(艱範憲選製艱遞顧願廠) = 遞膚艱齋鏇廠鑰夢遞獵觸壓蓋壓範淵襯蓋壓壓 (膚襯選壓選糧鑰夢顧繭, 鏇觸鹽醖壓鏇鏇鬱構廠 ~ 襯製顧蓋鹹鬱窪構遞醖) 更多
NCT02046564 (CTgov)	临床3期	重度抑郁症	412	ASC-01 (ASC-01)	膚鏇獵艱繭齋願淵壓糧(膚醖齋鏇蓋積獵構築醖) = 壓鹽餘簾製襯淵願憲壓夢衊膚醖憲遞獵網簾鬱 (艱構繭遞範齋構鹽窪蓋, 範範艱膚齋膚鹽顧醖鑰 ~ 築觸壓網壓簾廠艱顧鬱) 更多	-	2018-05-21
				Placebo (Placebo)	膚鏇獵艱繭齋願淵壓糧(膚醖齋鏇蓋積獵構築醖) = 網鑰範鹽鬱膚鹹積艱艱夢衊膚醖憲遞獵網簾鬱 (艱構繭遞範齋構鹽窪蓋, 餘糧窪範壓壓淵繭築築 ~ 鹹遞獵構蓋蓋範憲廠淵) 更多