Netazepide(Netazepide) - 药物靶点：CCKB_在研适应症：巴雷特食管，Zollinger-Ellison综合征_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

CCKB

作用方式

拮抗剂

作用机制

CCKB拮抗剂(胆囊收缩素B受体拮抗剂)

治疗领域

肿瘤消化系统疾病内分泌与代谢疾病+ [1]

在研适应症

巴雷特食管Zollinger-Ellison综合征

非在研适应症

巴雷特食管高度不典型增生类癌消化不良+ [5]

原研机构

Ferring BV

在研机构

Ferring BV

非在研机构

Trio Medicines Ltd.

Ferring Pharmaceuticals A/S

权益机构-

最高研发阶段临床2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C28H30N6O3

InChIKeyYDZYKNJZCVIKPP-VWLOTQADSA-N

CAS号155488-25-8

关联

16

项与 Netazepide 相关的临床试验

PACTR202407466904092

/ Unknown status临床3期IIT

A Randomized, Double Blind, Single Centre, study to assess the efficacy, safety and tolerability of the Gastrin Receptor Antagonist (GRA), Netazepide administered for 90 days, in post-menopausal women (OSTEO-GRA)

开始日期2019-04-01

申办/合作机构

University of Cape Town

NCT02597712

/ Completed临床2期

Randomized, Placebo-controlled Trial of YF476, a Gastrin Receptor Antagonist, in Barrett's Esophagus

A phase 2, randomised, double-blind, out-patient trial to determine if YF476 is a safe and effective treatment in patients with Barrett's esophagus.

开始日期2013-05-15

申办/合作机构

Trio Medicines Ltd.

[+2]

EUCTR2012-002183-27-GB

/ Unknown statusN/A

Can netazepide eradicate the inflammatory response of the gastric mucosa to H. pylori infection? - Gastroscopy study of netazepide and H. pylori infection; version 1

开始日期2013-04-03

申办/合作机构

Hammersmith Medicines Research Ltd.

100 项与 Netazepide 相关的临床结果

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100 项与 Netazepide 相关的转化医学

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100 项与 Netazepide 相关的专利（医药）

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72

项与 Netazepide 相关的文献（医药）

2024-04-01·Journal of Gastrointestinal Surgery

Gastrin: a new branch of the gastropancreatic axis that can explain the effect of sleeve gastrectomy on glucose metabolism

Article

作者: Castro-Santiago, María-Jesús ; Valverde-Martínez, Amparo ; Casado-Maestre, María-Dolores ; Pérez-Arana, Gonzalo-Martín ; Almorza-Gomar, David ; Prada-Oliveira, José-Arturo ; Mayo-Ossorio, Maria-Angeles ; Bohórquez-Sierra, Juan Carlos ; Visiedo, Francisco ; Ramírez, Alonso Camacho

BACKGROUNDAmong bariatric techniques, sleeve gastrectomy (SG) stands out owing to its efficiency. The role of the stomach as a secretory organ of many substances, such as gastrin, related to insulin secretion is well known. Gastrin induces insulin release in isolated pancreatic islets, limiting somatostatin-14 intraislet release, and has been associated with blood glucose level improvement in diabetic models after SG. SG involves gastric resection along the greater curvature. This study aimed to determine the role of gastrin in glucose metabolism improvement after SG with the aid of the gastrin antagonist netazepide.METHODSIn 12 sham-operated, 12 SG-operated, and 12 SG-operated/netazepide-treated Wistar rats, we compared medium- and long-term plasma insulin, oral glucose tolerance test (OGTT) results, and plasma gastrin levels. In addition, gastrin expression was assessed in the gastric remnant, and the beta-cell mass was measured.RESULTSSG induced a medium-term elevation of the insulin response and plasma gastrin levels without modification of the OGTT results. However, long-term depletion of the insulin response with elevated OGTT areas under the curve and plasma gastrin levels appeared after SG. Netazepide prevented the SG effect on these parameters. Gastrin tissue expression was greater in SG animals than in SG/netazepide-treated or control animals. The beta-cell mass was lower in the SG group than in the control or SG/netazepide group.CONCLUSIONGastrin plays a central role in glucose improvement after SG. It stimulates a medium-term strong insulin response but also causes long-term beta-cell mass depletion and a loss of insulin response. These effects are prevented by gastrin antagonists such as netazepide.

2023-10-01·Molecular Diversity

Identification of small molecules as potential inhibitors of interleukin 6: a multi-computational investigation

Article

作者: Thai, Khac-Minh ; Le, Minh-Tri ; Tran, Viet-Hung ; Nguyen, Quoc-Thai ; Tran, Que-Huong ; Trinh, Dieu-Thuong Thi ; Tran, Thanh-Dao ; Tran, Van-Thanh ; Tran, Thi-Thuy Nga

IL(interleukin)-6 is a multifunctional cytokine crucial for immunological, hematopoiesis, inflammation, and bone metabolism. Strikingly, IL-6 has been shown to significantly contribute to the initiation of cytokine storm-an acute systemic inflammatory syndrome in Covid-19 patients. Recent study has showed that blocking the IL-6 signaling pathway with an anti-IL-6 receptor monoclonal antibody (mAb) can reduce the severity of COVID-19 symptoms and enhance patient survival. However, the mAb has several drawbacks, such as high cost, potential immunogenicity, and invasive administration due to the large-molecule protein product. Instead, these issues could be mitigated using small molecule IL-6 inhibitors, but none are currently available. This study aimed to discover IL-6 inhibitors based on the PPI with a novel camelid Fab fragment, namely 68F2, in a crystal protein complex structure (PDB ID: 4ZS7). The pharmacophore models and molecular docking were used to screen compounds from DrugBank databases. The oral bioavailability of the top 24 ligands from the screening was predicted by the SwissAMDE tool. Subsequently, the selected molecules from docking and MD simulation illustrated a promising binding affinity in the formation of stable complexes at the active binding pocket of IL-6. Binding energies using the MM-PBSA technique were applied to the top 4 hit compounds. The result indicated that DB08402 and DB12903 could form strong interactions and build stable protein-ligand complexes with IL-6. These potential compounds may serve as a basis for further developing small molecule IL-6 inhibitors in the future.

2021-09-26·World Journal of Clinical Cases4区 · 医学

Gastric neuroendocrine neoplasms: A review

4区 · 医学

Review

作者: Sezikli, Mesut ; Köseoğlu, Hüseyin ; Duzenli, Tolga

Gastric neuroendocrine neoplasms (g-NENs) or neuroendocrine tumors are generally slow-growing tumors with increasing incidence. They arise from enterochromaffin like cells and are divided into four types according to clinical characteristic features. Type 1 and 2 are gastrin dependent, whereas type 3 and 4 are sporadic. The reason for hypergastrinemia is atrophic gastritis in type 1, and gastrin releasing tumor (gastrinoma) in type 2 g-NEN. The diagnosis of g-NENs needs histopathological investigation taken by upper gastrointestinal endoscopy. g-NENs are positively stained with chomogranin A and synaptophysin. Grading is made with mitotic index and ki-67 proliferation index on histopathological analysis. It is crucial to discriminate between types of g-NENs, because the management, treatment and prognosis differ significantly between subtypes. Treatment options for g-NENs include endoscopic resection, surgical resection with or without antrectomy, medical treatment with somatostatin analogues, netazepide or chemotherapy regimens. Follow-up without excision is another option in appropriate cases. The prognosis of type 1 and 2 g-NENs are good, whereas the prognosis of type 3 and 4 g-NENs are close to the prognosis of gastric adenocancer.

100 项与 Netazepide 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB12355

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
巴雷特食管	临床2期	-	Ferring BV	-
Zollinger-Ellison综合征	临床2期	-	Ferring BV	-
类癌	临床前	英国	Trio Medicines Ltd.	2011-01-04
萎缩性胃炎	临床前	英国	Trio Medicines Ltd.	2011-01-04
胃泌素分泌增加	临床前	英国	Trio Medicines Ltd.	2011-01-04
巴雷特食管高度不典型增生	临床前	英国	Trio Medicines Ltd.	2010-06-01
巴雷特食管高度不典型增生	临床前	美国	Trio Medicines Ltd.	2010-06-01
类癌	药物发现	英国	Trio Medicines Ltd.	2011-01-04
萎缩性胃炎	药物发现	英国	Trio Medicines Ltd.	2011-01-04
胃泌素分泌增加	药物发现	英国	Trio Medicines Ltd.	2011-01-04

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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


NCT01298999 (CTgov)	临床2期	巴雷特食管 \| 巴雷特食管高度不典型增生	27	YF476 (YF476)	衊淵選齋淵廠顧齋繭鏇(艱窪簾遞糧積鬱選顧顧) = 製鏇淵餘齋夢鹽醖顧糧夢憲鏇顧醖簾膚淵窪築 (簾襯鹹夢網膚膚衊選鬱, 觸觸廠鏇顧糧鬱範夢艱 ~ 窪鹽餘鹹齋繭廠餘選醖) 更多	-	2021-11-23
				Placebo (Placebo)	衊淵選齋淵廠顧齋繭鏇(艱窪簾遞糧積鬱選顧顧) = 醖網壓餘蓋築築醖廠艱夢憲鏇顧醖簾膚淵窪築 (簾襯鹹夢網膚膚衊選鬱, 積齋壓築夢遞餘糧製壓 ~ 鏇艱襯夢蓋廠鑰鏇顧壓) 更多
NCT02597712 (CTgov)	临床2期	巴雷特食管	27	YF476 (Treatment)	憲範鬱衊範壓衊範壓憲(鑰憲鑰願餘夢艱積簾遞) = 衊觸壓範遞選鏇鏇衊醖鬱淵簾糧簾製夢築蓋繭 (獵築範糧觸網積鏇製艱, 艱衊簾鑰壓蓋構鹹鏇鑰 ~ 蓋衊齋鬱簾膚範遞夢襯) 更多	-	2021-04-12
				YF476 placebo (YF476 Placebo)	憲範鬱衊範壓衊範壓憲(鑰憲鑰願餘夢艱積簾遞) = 壓壓鬱襯廠齋築襯獵醖鬱淵簾糧簾製夢築蓋繭 (獵築範糧觸網積鏇製艱, 憲簾艱範餘艱願醖齋顧 ~ 獵簾選襯艱構蓋艱夢餘) 更多
NCT01298999 (Pubmed \| Cancer Prev Res (Phila))	临床2期	巴雷特食管	20	Netazepide	範築選遞鬱膚構餘遞餘(獵醖憲積願積窪夢鹽餘) = 糧製壓夢餘淵簾獵觸築網獵糧蓋廠遞鏇鏇鬱鹽 (選鬱窪衊襯餘齋觸齋膚, 620.7)	-	2021-03-29
				Placebo	範築選遞鬱膚構餘遞餘(獵醖憲積願積窪夢鹽餘) = 範鹹壓鹹範遞鬱膚廠餘網獵糧蓋廠遞鏇鏇鬱鹽 (選鬱窪衊襯餘齋觸齋膚, 640.3)
NCT02454075 (CTgov)	临床2期	Zollinger-Ellison综合征 \| 胃神经内分泌肿瘤 G1	3	YF476	襯構積齋鬱範構壓鑰構(築構壓壓憲範齋願淵範) = 壓襯鏇簾襯鑰鹽構鬱構廠壓範網衊選繭鏇醖鏇 (蓋壓襯衊鏇窪範齋顧顧, 醖憲構願蓋獵憲襯憲觸 ~ 窪廠鏇醖糧壓簾餘觸鏇) 更多	-	2021-01-29