Delving into the Latest Updates on Proglumide with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Proglumide (JP17/USAN/INN), 242 DL, CR-242

+ [5]

Target

CCK receptor

Mechanism

CCK receptor antagonists(Cholecystokinin receptors antagonists)

Therapeutic Areas

Digestive System DisordersNeoplasms

Active Indication

Peptic UlcerPancreatitis, ChronicHepatocellular Carcinoma

Inactive Indication-

Originator Organization

Yichang Humanwell Pharmaceuticals Co., Ltd.

Active Organization

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

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

CN (01 Jan 1981),

Peptic Ulcer

RegulationOrphan Drug (US)

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Structure

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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499

Literatures (Medical) associated with Proglumide

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.

18 May 2023·Cancers

Cholecystokinin Receptor Antagonist Induces Pancreatic Stellate Cell Plasticity Rendering the Tumor Microenvironment Less Oncogenic.

Article

Author: Bansal, Sunil ; Cheema, Amrita ; Jolly, Gurbani ; Shivapurkar, Narayan ; Chen, Wenqiang ; Smith, Jill P ; Duka, Tetyana

CCK receptors are expressed on pancreatic cancer epithelial cells, and blockade with receptor antagonists decreases tumor growth. Activated pancreatic stellate cells or myofibroblasts have also been described to express CCK receptors, but the contribution of this novel pathway in fibrosis of the pancreatic cancer microenvironment has not been studied. We examined the effects of the nonselective CCK receptor antagonist proglumide on the activation, proliferation, collagen deposition, differential expression of genes, and migration in both murine and human PSCs. CCK receptor expression was examined using western blot analysis. Collagen production using activated PSCs was analyzed by mass spectroscopy and western blot. Migration of activated PSCs was prevented in vitro by proglumide and the CCK-B receptor antagonist, L365,260, but not by the CCK-A receptor antagonist L365,718. Proglumide effectively decreased the expression of extracellular matrix-associated genes and collagen-associated proteins in both mouse and human PSCs. Components of fibrosis, including hydroxyproline and proline levels, were significantly reduced in PSC treated with proglumide compared to controls. CCK peptide stimulated mouse and human PSC proliferation, and this effect was blocked by proglumide. These investigations demonstrate that targeting the CCK-B receptor signaling pathway with proglumide may alter the plasticity of PSC, rendering them more quiescent and leading to a decrease in fibrosis in the pancreatic cancer microenvironment.

1

News (Medical) associated with Proglumide

19 Oct 2017

·www.bioportfolio.com

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100 Deals associated with Proglumide

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