CPL-207-280(CPL-207-280) - 药物靶点：GPR40_在研适应症：2型糖尿病，糖尿病性神经病变_专利_临床

概要

基本信息

药物类型

小分子化药

别名

+ [2]

靶点

GPR40

作用方式

激动剂

作用机制

GPR40激动剂(游离脂肪酸受体-1激动剂)

治疗领域

神经系统疾病内分泌与代谢疾病

在研适应症

2型糖尿病糖尿病性神经病变

非在研适应症-

原研机构

Celon Pharma SA

在研机构

Celon Pharma SA

非在研机构-

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-

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关联

3

项与 CPL-207-280 相关的临床试验

NCT05248776

/ Recruiting临床2期

A Phase 2, Double-Blind, Randomized, Placebo-Controlled, Parallel-Group Study to Evaluate Efficacy, Safety and Pharmacokinetics After 2-weeks Administration of CPL207280 (GPR40 Agonist) in Subjects With Type 2 Diabetes (T2D)

The planned study is to evaluate the efficacy, safety and pharmacokinetic (PK) properties of CPL207280 after multiple (14 days) administration in patients with type 2 diabetes.

开始日期2022-01-21

申办/合作机构

Celon Pharma SA

[+1]

EUCTR2021-002947-32-PL

/ Not yet recruiting临床2期

A Phase 2, Double-Blind, Randomized, Placebo-Controlled, Parallel-Group Study to Evaluate Efficacy, Safety and Pharmacokinetics after 2-weeks Administration of CPL207280 (GPR40 agonist) in Subjects With Type 2 Diabetes (T2D)

开始日期2021-10-28

申办/合作机构

Celon Pharma SA

NCT04622111

/ Completed临床1期

One Centre, Single Ascending Dose and Double Blind Multiple Ascending Dose, Safety and Pharmacokinetics Phase I Study of CPL207280 Compound in Healthy Volunteers.

The planned study is to determine the safety and pharmacokinetic properties of CPL207280 compound after single and multiple (two weeks) administration in healthy volunteers.

开始日期2020-05-27

申办/合作机构

Celon Pharma SA

[+1]

100 项与 CPL-207-280 相关的临床结果

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100 项与 CPL-207-280 相关的转化医学

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100 项与 CPL-207-280 相关的专利（医药）

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6

项与 CPL-207-280 相关的文献（医药）

2025-06-01·Bioorganic & Medicinal Chemistry

Discovery of potent free fatty acid receptor 1 full agonists with a novel scaffold bearing conjugated double bond linker

Article

作者: Guo, Shimeng ; Yang, Ziwei ; Shen, Jianhua ; Fang, Jiahui ; Xie, Xin ; Wang, Yu ; Wang, Kai ; Sun, Jun ; Xu, Tifei

GPR40 full agonists can not only lower blood glucose via glucose-stimulated insulin secretion (GSIS) with a low risk of hypoglycemia, but also promote incretin release such as glucagon-like peptide-1 (GLP-1). Compared with partial agonists, full agonists are superior in the treatment of diabetes and obesity. Based on patent research, we combined the highly compatible linker with CPL207280, a GPR40 partial agonist that metabolized mainly through oxidation, to design a potent GPR40 full agonist with a novel scaffold. We explored the linker, tail and acid head and finally found compound H1-2 with excellent glucose-lowering ability.

2024-04-01·Diabetes, Obesity and Metabolism

First‐in‐human study of CPL207280, a novel G‐protein‐coupled receptor 40/free fatty acid receptor 1 agonist, in healthy volunteers after single and multiple administration

Article

作者: Jarus-Dziedzic, Katarzyna ; Buda, Paweł ; Tratkiewicz, Ewa ; Wieczorek, Maciej ; Gierczak-Pachulska, Agnieszka ; Bazydło-Guzenda, Katarzyna ; Juszczyk, Ewelina ; Buś-Kwaśnik, Katarzyna ; Segiet-Święcicka, Agnieszka ; Rudzki, Piotr J ; Rabczenko, Daniel

AbstractAimTo assess the safety, tolerability and pharmacokinetic (PK) profile of single and multiple doses of CPL207280, a new G‐protein‐coupled receptor 40 agonist developed to treat type 2 diabetes (T2D).MethodsThe phase 1 study in healthy volunteers (White, age 18–55 years, body mass index 18.5–29.9 kg/m2) was performed after single (24 subjects, 5–480 mg) and multiple (32 subjects, 60–480 mg) once‐daily administration of CPL207280. The effect of food intake and interaction with metformin were evaluated in additional cohort (12 subjects, 120 mg). The primary objective was the safety and tolerability of CPL207280. Secondary objectives included PK and pharmacodynamic (PD) characteristics (glucose, insulin, C‐peptide, proinsulin, glucagon levels) observed during the 14‐day treatment period.ResultsNo deaths or serious adverse events (AEs) were reported. All reported AEs were classified as unrelated to the study product. No clinically significant differences in safety parameters were observed between cohorts and no food or metformin effect on safety parameters was identified. The ascending dose of CPL207280 caused an increase in the PK parameters maximum observed plasma concentration (Cmax) or area under the plasma concentration–time curve up to 24 h. However, dose‐normalized Cmax decreased with ascending dose. There was no relationship between the CPL207280 dose or prandial state and terminal elimination half‐life and terminal elimination rate constant. No clear relationship between CPL207280 dose and PD area under the effect curve values was observed.ConclusionsCPL207280 was found to be safe and well tolerated by healthy volunteers (with a low risk of hepatotoxicity) for up to 14 days of administration. The PK profile of CPL207280 supports single‐daily administration and justifies further development of this therapy for patients with T2D.

2021-12-01·European Journal of Medicinal Chemistry1区 · 医学

Discovery and development of CPL207280 as new GPR40/FFA1 agonist

1区 · 医学

Article

作者: Bazydło-Guzenda, Katarzyna ; Dubiel, Krzysztof ; Dawid, Urszula ; Dzida, Radosław ; Smuga, Damian ; Hołowińska, Dagmara ; Gurba-Bryśkiewicz, Lidia ; Stelmach, Filip ; Buda, Paweł ; Gałązka, Kinga ; Wiśniewski, Krzysztof ; Pieczykolan, Jerzy ; Mach, Mateusz ; Matłoka, Mikołaj ; Wieczorek, Maciej ; Wąsińska-Kałwa, Małgorzata

Due to a unique mechanism that limits the possibility of hypoglycemia, the free fatty acid receptor (FFA1) is an attractive target for the treatment of type 2 diabetes. So far, however, none of the promising agonists have been able to enter the market. The most advanced clinical candidate, TAK-875, was withdrawn from phase III clinical trials due to liver safety issues. In this article, we describe the key aspects leading to the discovery of CPL207280 (13), the design of which focused on long-term safety. The introduction of small, nature-inspired acyclic structural fragments resulted in compounds with retained high potency and a satisfactory pharmacokinetic profile. Optimized synthesis and upscaling provided a stable, solid form of CPL207280-51 (45) with the properties required for the toxicology studies and ongoing clinical trials.

100 项与 CPL-207-280 相关的药物交易

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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
2型糖尿病	临床2期	波兰	Celon Pharma SA	2022-01-21
糖尿病性神经病变	临床2期	-	Celon Pharma SA	-

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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


NCT04622111 (Phase 1, EASD2021)	临床1期	-	32	CPL207280 60 mg	遞製鏇築簾選觸製糧衊(鬱築鏇窪窪鏇選鹽鑰構) = The administration of CPL207280 was generally safe and well-tolerated with no serious AEs. All adverse events were classified as not related to the study product. No increase in the tested hepatic parameters (ALT, AST, ALP, bilirubin, creatinine) was observed. There were no hypoglycaemia episodes during the study. 築網願網鏇鹹顧顧憲鏇 (製憲鹽艱獵淵遞窪醖齋 )	积极	2021-10-01
				CPL207280 480 mg
NCT04622111 (CPL207280, Pubmed \| Mol Pharmacol)	临床1期	-	68	CPL207280	醖襯窪簾壓襯淵膚積鬱(選夢壓觸蓋窪鬱網餘糧) = 鹹夢糧製夢築壓憲鑰築鏇遞構蓋蓋鹹鬱憲鑰鏇 (製淵觸築醖淵構壓衊鹹 ) 更多	-	2021-08-04
EASD2018	N/A	糖尿病 Ca 2+	-	CPL207-280CA	憲餘蓋構窪衊壓餘膚鹽(選艱獵艱鏇築鹹鏇選獵) = 鹽簾鬱餘鏇襯夢蓋齋鬱製構範醖選範獵壓襯餘 (衊襯餘膚獵艱顧鑰製遞 )	积极	2018-10-03
				Fasiglifam	憲餘蓋構窪衊壓餘膚鹽(選艱獵艱鏇築鹹鏇選獵) = 獵積窪鬱築衊糧願醖襯製構範醖選範獵壓襯餘 (衊襯餘膚獵艱顧鑰製遞 )