Delving into the Latest Updates on Proglumide with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Proglumide (JP17/USAN/INN), 普格鲁胺, 242 DL

+ [6]

Target

CCK receptor x P2Y14

Action

antagonists

Mechanism

CCK receptor antagonists(Cholecystokinin receptors antagonists), P2Y14 antagonists(purinergic receptor P2Y14 antagonists)

Therapeutic Areas

Digestive System DisordersNeoplasms

Active Indication

Peptic UlcerPancreatitis, ChronicHepatocellular Carcinoma

Inactive Indication

Venous Thromboembolism

Originator Organization

Yichang Humanwell Pharmaceuticals Co., Ltd.

Active Organization

Yichang Humanwell Pharmaceuticals Co., Ltd.CCKr Therapeutics, Inc.

Inactive Organization

China Pharmaceutical University

License Organization-

Drug Highest PhaseApproved

First Approval Date

China (01 Jan 1981),

Peptic Ulcer

RegulationOrphan Drug (United States)

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Structure/Sequence

Molecular FormulaC18H26N2O4

InChIKeyDGMKFQYCZXERLX-UHFFFAOYSA-N

CAS Registry6620-60-6

This is a Phase 2 study with an open labelled lead-in study to approximately treat 30 patients [6 subjects for Lead-in and 24 for Phase 2] enrolled with metastatic pancreatic cancer with combination therapy using standard of care first line therapy with GEM-NAB-P (GEM 1000mg/m2 IV and NAB-P 125 mg/m2 given days 1, 8, and 15 every 28 days, and proglumide will be tested at the daily dose of 1200 mg orally given as 400 mg po TID. The lead-in study will determine the safety and tolerability of the 1200 mg daily dose of proglumide with standard of care GEM-NAB-P. If 0 or 1 of a total of 6 patients at 400mg experiences a DLT, then we will proceed to the Phase 2 randomized trial.

Start Date31 Jan 2024

Sponsor / Collaborator

Georgetown University

NCT05551858

/ Active, not recruitingPhase 1/2IIT

A Phase 1/2 Trial to Test the Safety of a CCK Receptor Antagonist, Proglumide, in Management of Chronic Pancreatitis Symptoms and Pain for 12 to 24 Months

Chronic pancreatitis is a rare but debilitating condition associated with chronic abdominal pain, diarrhea, diabetes, and an 8-fold increased risk for the development of pancreatic cancer. Unfortunately, there is no available treatment to prevent the progression of chronic pancreatitis, and most subjects require narcotic medications to control the pain. A receptor protein call the CCK-B receptor becomes activated in chronic pancreatitis and is in part responsible for the scar tissue or fibrosis that occurs and responsible for the cancer risk. In mice with chronic pancreatitis, the inflammation and damage was reversed with an old drug called proglumide that blocks the activation of the CCK-B receptor. Proglumide has also been shown to possibly reduce pain.
This protocol involved a 2-Part study to test the safety of oral proglumide in those with confirmed chronic pancreatitis and the second goal is to determine if proglumide improves pain and function of the pancreas. Part-1 is an open-labelled Lead-in Study of N=8 subjects over a 12-week treatment period. Part-2 is a randomized double blind pseudo cross over study where subjects will be treated in Arm A (placebo for 12 weeks followed by 12 weeks of proglumide) and Arm B ( proglumide for 24 weeks).

Start Date17 Nov 2022

Sponsor / Collaborator

Georgetown University

NCT04814602

/ CompletedEarly Phase 1IIT

Single-dose Pharmacokinetic (PK) Assessment of Oral Proglumide in Those With Hepatic Impairment

Proglumide is an oral cholecystokinin (CCK) receptor antagonist that has been shown in non-clinical studies to reverse hepatic fibrosis and decrease the incidence of hepatocellular carcinoma (HCC). Because of these potential beneficial properties, proglumide may be useful in decreasing the fibrosis and risk for HCC in those with cirrhosis. Although proglumide is safe in those with normal hepatic function, the pharmacokinetics have not been established in those that are hepatic impaired. The purpose of this study is to analyze proglumide blood levels and excretion in subjects with cirrhosis compared to health controls.

Start Date30 Mar 2021

Sponsor / Collaborator

Georgetown University

100 Clinical Results associated with Proglumide

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100 Translational Medicine associated with Proglumide

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100 Patents (Medical) associated with Proglumide

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539

Literatures (Medical) associated with Proglumide

15 Aug 2024·FASEB JOURNAL

Activation of the G protein‐coupled sulfakinin receptor inhibits blood meal intake in the mosquito Aedes aegypti

Article

Author: Xie, Xiao Bing ; Jiang, Linlong ; Zhu, Xiaojing ; Cui, Zong Jie ; Zhang, Lei ; Huang, Yuqi ; Han, Qian ; Hong, Yue ; Tang, Yu ; Hansson, Bill S.

Abstract:

Little is known about the blood‐feeding physiology of arbovirus vector Aedes aegypti although this type of mosquito is known to transmit infectious diseases dengue, Zika, yellow fever, and chikungunya. Blood feeding in the female A. aegypti mosquito is essential for egg maturation and for transmission of disease agents between human subjects. Here, we identify the A. aegypti sulfakinin receptor gene SKR from the A. aegypti genome and show that SKR is expressed at different developmental stages and in varied anatomical localizations in the adult mosquito (at three days after eclosion), with particularly high expression in the CNS. Knockingdown sulfakinin and sulfakinin receptor gene expression in the female A. aegypti results in increased blood meal intake, but microinjection in the thorax of the sulfakinin peptide 1 and 2 both inhibits dose dependently blood meal intake (and delays the time course of blood intake), which is reversible with receptor antagonist. Sulfakinin receptor expressed ectopically in mammalian cells CHO‐K1 responds to sulfakinin stimulation with persistent calcium spikes, blockable with receptor antagonist. These data together suggest that activation of the Gq protein‐coupled (i.e., calcium‐mobilizing) sulfakinin receptor inhibits blood meal intake in female A. aegypti mosquitoes and could serve as a strategic node for the future control of A. aegypti mosquito reproduction/population and disease transmission.

01 Mar 2024·3 Biotech

Molecular authentication, metabolite profiling and in silico–in vitro cytotoxicity screening of endophytic Penicillium ramusculum from Withania somnifera for breast cancer therapeutics

Article

Author: Gajbhiye, Virendra ; Rajeshkumar, K C ; Jisha, M S ; Haldar, Niladri ; Shaikh, Aazam ; Varghese, Sherin

Supplementary Information:

The online version contains supplementary material available at 10.1007/s13205-023-03906-3.

01 Mar 2024·American journal of physiology. Gastrointestinal and liver physiology

Implicating the cholecystokinin B receptor in liver stem cell oncogenesis

Article

Author: Yassin, Amal A ; Huang, Yimeng ; Duka, Tetyana ; Drda, Jack C ; Chen, Wenqiang ; Gay, Martha D ; Shivapurkar, Narayan ; Fang, Hongbin ; Smith, Jill P

This investigation identified a novel pathway involving the activation of hepatic stem cells and liver oncogenesis. Receptor blockade or genetic disruption of the cholecystokinin-B receptor (CCK-BR) signaling pathway decreased the activation and proliferation of hepatic stem cells after liver injury without eliminating the regenerative capacity of healthy hepatocytes.

1

News (Medical) associated with Proglumide

19 Oct 2017

·www.bioportfolio.com

Global Proglumide Market Research Report Forecast 20172022 [Report Updated: 18092017] Prices from USD $2800

Delivery of the Report will take 4872 hours once order is placed. The Global Proglumide Market Research Report Forecast 20172022 is a valuable source of insightful data for business strategists. It provides the Proglumide industry overview with growth analysis and historical futuristic cost, revenue, demand and supply data as applicable. The research analysts provide an elaborate description of the value chain and its distributor analysis. This Proglumide market study provides comprehensive data which enhances the understanding, scope and application of this report. This report provides comprehensive analysis of Key market segments and subsegments Evolving market trends and dynamics Changing supply and demand scenarios Quantifying market opportunities through market sizing and market forecasting Tracking current trends/opportunities/challenges Competitive insights Opportunity mapping in terms of technological breakthroughs Global Proglumide Market: Regional Segment Analysis North America Europe China Japan Southeast Asia India The Major players reported in the market include: Tianyuan Pharmachemical Institute Hubei Prosoerity Galaxy Chemical Hubei Yikangyuan Chemical Hubei Yuancheng Saichuang Technology company 5 company 6 company 7 company 8 company 9 ... Global Proglumide Market: Product Segment Analysis Type 1 Type 2 Type 3 Global Proglumide Market: Application Segment Analysis Application 1 Application 2 Application 3 Reasons for Buying this Report This report provides pinpoint analysis for changing competitive dynamics It provides a forward looking perspective on different factors driving or restraining market growth It provides a sixyear forecast assessed on the basis of how the market is predicted to grow It helps in understanding the key product segments and their future It provides pin point analysis of changing competition dynamics and keeps you ahead of competitors It helps in making informed business decisions by having complete insights of market and by making indepth analysis of market segments

100 Deals associated with Proglumide

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External Link

KEGG	Wiki	ATC	Drug Bank
D01818	Proglumide	A02BX06	DB13431

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Peptic Ulcer	China	Yichang Humanwell Pharmaceuticals Co., Ltd.	01 Jan 1981

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Pancreatitis, Chronic	Preclinical	United States	CCKr Therapeutics, Inc.	01 Jul 2024
Hepatocellular Carcinoma	Preclinical	United States	CCKr Therapeutics, Inc.	13 Mar 2024
Venous Thromboembolism	Preclinical	China	China Pharmaceutical University	-