Emodepside(Emodepside) - 药物靶点：GPCR_在研适应症：蛔虫病，钩虫感染，鞭虫病_专利_临床

概要

基本信息

药物类型

合成多肽

别名

Macrofilaricide

+ [1]

靶点

GPCR

作用方式

调节剂

作用机制

GPCR调节剂(G蛋白偶联受体调节剂)

治疗领域

感染其他疾病眼部疾病+ [1]

在研适应症

蛔虫病钩虫感染鞭虫病+ [2]

非在研适应症-

原研机构

Astellas Pharma, Inc.

在研机构

Bayer AG

Drugs for Neglected Diseases initiative

Astellas Pharma, Inc.

非在研机构-

权益机构-

最高研发阶段临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评孤儿药 (美国)

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结构/序列

分子式C60H90N6O14

InChIKeyZMQMTKVVAMWKNY-YSXLEBCMSA-N

CAS号155030-63-0

Sequence Code 526155818

关联

10

项与 Emodepside 相关的临床试验

NCT06800248

/ Not yet recruiting临床3期IIT

A Phase III Single-center, Randomized, Double-Blinded, Parallel-group, Active Controlled Study to Evaluate the Efficacy and Safety of a Single Dose of Emodepside Compared to Multiple Doses of Mebendazole in Adolescent and Adult Participants With Soil-transmitted Helminthiasis

This study aims to assess the efficacy and safety of emodepside compared to mebendazole in adults and adolescents infected with T. trichiura, either as single infection or co-infections with hookworm and/or A. lumbricoides.

开始日期2025-08-01

申办/合作机构

Swiss Tropical & Public Health Institute

[+3]

NCT06736691

/ Not yet recruiting临床3期IIT

A Phase III Single-center, Randomized, Double-blinded, Parallel-group, Active-controlled Study to Evaluate the Efficacy and Safety of a Single Dose of Emodepside Compared to Multiple Doses of Mebendazole in Adolescent and Adult Participants With Soil-transmitted Helminthiasis

This study aims to assess the efficacy and safety of emodepside compared to mebendazole in adults and adolescents infected with T. trichiura, either as single infection or co-infections with hookworm and/or A. lumbricoides.

开始日期2025-05-01

申办/合作机构

Swiss Tropical & Public Health Institute

[+3]

NCT06373835

/ Completed临床2期IIT

Efficacy, Safety and Pharmacokinetics of Ascending Dosages of Emodepside and in Comparison to Ivermectin Against Strongyloidiasis Stercoralis in Adults: Randomized Stage II Seamless Adaptive Controlled Trials

Efficacy, safety and pharmacokinetics of ascending dosages of emodepside and in comparison to ivermectin against Strongyloidiasis stercoralis in adults: randomized stage II seamless adaptive controlled trials

开始日期2024-05-20

申办/合作机构

Swiss Tropical & Public Health Institute

100 项与 Emodepside 相关的临床结果

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100 项与 Emodepside 相关的转化医学

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100 项与 Emodepside 相关的专利（医药）

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204

项与 Emodepside 相关的文献（医药）

2025-04-04·American Journal of Veterinary Research

Topical and oral emodepside formulations for last-line treatment of multianthelmintic drug-resistant hookworms when given orally to dogs are not bioequivalent

Article

作者: Jugan, Maria C. ; Quintana, Theresa A. ; Karwath, Greta N. ; Martinez, Stephanie E. ; Jesudoss Chelladurai, Jeba R. J. ; Mayhue, Erin J.

AbstractObjectiveTo evaluate the pharmacokinetics of emodepside in dogs following single-dose administration of the FDA-approved feline topical solution orally and topically and the European Medicines Agency–approved canine modified-release tablet orally and to assess the bioequivalence of the feline topical solution administered orally compared to the canine modified-release tablet.MethodsThis study was conducted in 3 phases, during which dogs received single doses of emodepside as the feline topical solution (1 mg/kg) orally, the canine modified-release tablet (1 mg/kg) orally, and the topical feline solution (3 mg/kg) topically. Plasma pharmacokinetic profiles were determined for 21 days postdose. Bioequivalence testing was conducted for orally administered emodepside.Results7 healthy client-owned dogs (4 female and 3 male) were prospectively enrolled in this crossover study from May through August 2023. Oral administration of the feline topical solution resulted in markedly greater emodepside absorption than the modified-release tablet and was not bioequivalent. Emodepside plasma concentrations following topical administration of the FDA formulation were 36- to 122-fold lower than after oral administration.ConclusionsThe feline topical solution administered orally at 1 mg/kg is not bioequivalent to the canine modified-release tablet. Markedly higher absorption of the feline topical solution administered orally raises potential safety concerns for extralabel use in dogs to treat multianthelmintic drug-resistant hookworm infections. Poor absorption following topical administration suggests it may be unsuitable for treating multianthelmintic drug-resistant hookworm infections.Clinical RelevanceThese findings highlight potential emodepside toxicity risks with extralabel use of the FDA-approved topical feline product and help inform safe off-label use in dogs.

2025-04-01·Parasitology Research

Implementation of real-time PCR assays for diagnosing intestinal protozoa infections

Article

作者: Lotz, Christian N ; Schneeberger, Pierre H H ; Keiser, Jennifer ; Mrimi, Emmanuel C ; Ali, Said M ; Concu, Maura

AbstractIntestinal protozoa infections present a major public health challenge, particularly in areas with poor sanitation and limited access to clean water. Effective diagnostic methods are critical, yet traditional microscopy, though widely used for its simplicity, lacks the sensitivity and specificity of modern techniques like real-time Polymerase Chain Reaction (qPCR), making the latter a more effective tool for monitoring and assessing the burden of intestinal protozoa diseases. In this study, we implemented two duplex qPCR assays to detect Entamoeba dispar + Entamoeba histolytica and Cryptosporidium spp. + Chilomastix mesnili, along with singleplex assays for Giardia duodenalis and Blastocystis spp., using a 10 µL reaction volume. This marks the first molecular detection of Chilomastix mesnili by qPCR, enhancing diagnostic precision. Using these, we analyzed stool samples from 70 patients on Pemba Island, Tanzania, before and 54 samples after treatment with 20, 25, or 30 mg of emodepside or placebo, aiming to assess protozoa prevalence for this region and emodepside’s potential antiprotozoal effects. Our qPCR reliably detected protozoa in 74.4% of samples, with Entamoeba histolytica and Entamoeba dispar in 31.4% of cases. Notably, one-third of these infections were caused by Entamoeba histolytica. No significant reduction in protozoa was observed after emodepside treatment compared to placebo. The study highlights the utility of qPCR in providing species-level differentiation and improving the speed and cost-effectiveness of testing. The high prevalence of protozoa in this region underscores the need for continued monitoring and control efforts, though emodepside was not effective against protozoa infections.

2024-10-30·Journal of Computational Chemistry

Monovalent cation binding to model systems and the macrocyclic depsipeptide, emodepside

Article

作者: Subramanian, Govindan ; Sathe, Rohit Y. ; Mo, Yirong ; Manchanda, Kanika ; Bharatam, Prasad V.

AbstractThis study focuses on the systematic exploration of the emodepside conformations bound to monovalent K+ ion using quantum mechanical density functional theory (DFT) calculations at the M06‐2X/6‐31+G(d,p) level of theory. Nine conformers of emodepside and their complexes with K+ ion were characterized as stationary points on the potential energy surface. The conformational isomers were examined for their 3D structures, bonding, energetics, and interactions with the cation. A cavitand‐like structure (CC) is identified to be the energetically most stable arrangement. To arrive at a better understanding of the K+ ion binding, calculations were initially performed on complexes formed by the K+ and Na+ ions with model ligands (methyl ester and N,N‐dimethyl acetamide). Both the natural bond orbital (NBO) method and the block‐localized wavefunction (BLW) energy decomposition approach was employed to assess the bonding and energetic contributions stabilizing the ion‐bound model complexes. Finally, the solvent effect was evaluated through complete geometry optimizations and energy minimizations for the model ion‐ligand complexes and the emodepside‐K+ bound complexes using an implicit solvent model mimicking water and DMSO.

100 项与 Emodepside 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	Emodepside	-	DB11403

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
蛔虫病	临床3期	坦桑尼亚	Bayer AG	2025-05-01
钩虫感染	临床3期	坦桑尼亚	Bayer AG	2025-05-01
鞭虫病	临床3期	坦桑尼亚	Bayer AG	2025-05-01
盘尾丝虫病	临床2期	刚果共和国	Bayer AG	2021-08-30
盘尾丝虫病	临床2期	加纳	Drugs for Neglected Diseases initiative	2021-08-30
盘尾丝虫病	临床2期	加纳	Bayer AG	2021-08-30
盘尾丝虫病	临床2期	刚果共和国	Drugs for Neglected Diseases initiative	2021-08-30
眼盘尾丝虫病	临床1期	德国	Bayer AG	2024-05-07
丝虫病	临床1期	英国	Bayer AG	2017-10-26
丝虫病	临床1期	英国	Drugs for Neglected Diseases initiative	2017-10-26

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临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05017194 (Pubmed)	临床2期	鞭虫病 \| 钩虫感染	442	Emodepside 5 mg	積鏇鹹鏇範夢襯齋鏇憲(構窪獵鏇醖積範獵顧願) = 衊積獵廠築願憲蓋築淵觸鬱願願鏇網繭積鏇艱 (觸餘齋繭鏇顧簾觸憲觸, 69 ~ 93)	-	2023-05-18
				Albendazole 400 mg	積鏇鹹鏇範夢襯齋鏇憲(構窪獵鏇醖積範獵顧願) = 選衊壓齋鏇淵餘鏇鹽鹽觸鬱願願鏇網繭積鏇艱 (觸餘齋繭鏇顧簾觸憲觸, 6 ~ 35)
NCT03383523 (CTgov)	临床1期	丝虫病	77	Emodepside (BAY 44-4400) (Part 1a - Treatment A)	壓醖製壓選遞遞鏇範鑰(窪製顧衊膚鹹窪襯繭製) = 觸壓鹽淵鑰鑰鏇鹹糧築顧憲衊窪遞築衊積壓獵 (醖積窪願鹹鑰醖製積膚, 廠襯糧窪膚憲艱範顧窪 ~ 蓋衊遞蓋鹽壓鏇淵鏇鹽) 更多	-	2020-03-09
				Emodepside (BAY 44-4400) (Part 1a - Treatment B)	壓醖製壓選遞遞鏇範鑰(窪製顧衊膚鹹窪襯繭製) = 醖選齋憲蓋觸窪鹽積鏇顧憲衊窪遞築衊積壓獵 (醖積窪願鹹鑰醖製積膚, 遞鑰衊鬱獵夢範鏇艱選 ~ 築觸夢淵壓糧淵築網製) 更多