Delving into the Latest Updates on Amiloride Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-carboxamide, Amiloride, Amiloride hydrochloride (USP)

+ [9]

Target

ENaCα

Action

inhibitors

Mechanism

ENaCα inhibitors(sodium channel epithelial 1 subunit alpha inhibitors)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Heart FailureHypertension

Inactive Indication-

Originator Organization

Perrigo Co. Plc

Active Organization

Padagis US LLC

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

United States (05 Oct 1981),

Heart FailureHypertension

RegulationOrphan Drug (United States)

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Structure/Sequence

Molecular FormulaC6H8ClN7O

InChIKeyXSDQTOBWRPYKKA-UHFFFAOYSA-N

CAS Registry2609-46-3

View All Structures (2)

This phase II trial tests how well ARX788 works in treating patients diagnosed with HER2-low, locally advanced unresectable or metastatic breast cancer. ARX788 is an antibody-drug conjugate (ADC) that is given by infusion (diluted and injected slowly into veins). Antibodies are proteins which are naturally produced by the body's immune system to help fight infections. ARX788 consists of antibodies that have been attached to a toxin that has the potential to kill cancer cells. ARX788 sticks to a protein called human epidermal growth factor receptor (HER2), which is found on some breast cancer cells. Giving ARX788 may be safe and effective in treating patients with HER2-low locally advanced unresectable metastatic breast cancer.

Start Date28 Feb 2025

Sponsor / Collaborator

The University of California, San Francisco

[+1]

NCT05753059

/ RecruitingPhase 1IIT

Mechanisms of Diuretic Resistance in Heart Failure, Aim 2

Randomized placebo-controlled, double-blind, double-dummy, crossover design testing combinations placebo/placebo, bendroflumethiazide/placebo, amiloride/placebo, and bendroflumethiazide/amiloride added to bumetanide.

Start Date10 Aug 2023

Sponsor / Collaborator

Yale University

[+1]

NCT05125237

/ Active, not recruitingNot ApplicableIIT

Data Analysis for Drug Repurposing for Effective Alzheimer's Medicines (DREAM)- Amiloride vs Triamterene

This study aims to evaluate the comparative risk of dementia/Alzheimer's disease onset between patients treated with medications that target specific metabolic pathways and patients treated with alternative medications for the same indication.

Start Date01 Oct 2021

Sponsor / Collaborator

The Brigham & Women's Hospital, Inc.

[+3]

100 Clinical Results associated with Amiloride Hydrochloride

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100 Translational Medicine associated with Amiloride Hydrochloride

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100 Patents (Medical) associated with Amiloride Hydrochloride

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10,207

Literatures (Medical) associated with Amiloride Hydrochloride

01 May 2025·Antiviral Research

Assessment of repurposed compounds against coronaviruses highlights the antiviral broad-spectrum activity of host-targeting iminosugars and confirms the activity of potent directly acting antivirals

Article

Author: Makower, Laetitia L ; Zitzmann, Nicole ; Rangel, Victor ; Alonzi, Dominic S ; Hill, Michelle L ; Kiappes, J L ; Dwek, Raymond A ; von Delft, Annette ; Gileadi, Carina ; Brun, Juliane ; Arman, Benediktus Yohan ; Witt, Karolina D

The COVID-19 pandemic highlights the need for novel antiviral drug discovery approaches that could dramatically shorten timelines from compound discovery to clinical development. At the beginning of the pandemic, repurposing approaches were at the forefront of early research efforts to screen for antiviral activity against SARS-CoV-2 in over 2500 compounds. Here, we report cellular screening results of 100 FDA-approved and experimental compounds against SARS-CoV-2 in the human Calu-3 cell line. We observed 13 compounds showing antiviral activity against SARS-CoV-2, including seven FDA-approved compounds (remdesivir, boceprevir, amiloride, nafamostat, cisplatin, silmitasertib, and miglustat), and six compounds in pre-clinical and clinical development (tarloxotinib, lucerastat (NB-DGJ), MON-DNJ, NAP-DNJ, NN-DGJ and NN-DNJ). Further, we observed that our screening hits include several host-targeting antivirals, namely iminosugars, that are largely non-toxic and offer a large therapeutic window. The most-developed iminosugar MON-DNJ (UV-4B), which has been evaluated in a Phase 1 clinical trial, shows antiviral activity against SARS-CoV-2 wild type as well as alpha, beta, gamma, delta, and Omicron variants. Its activity also extended to another betacoronavirus HCoV OC43, but not alphacoronavirus HCoV 229E. Our cellular screening results add to the body of knowledge on antivirals against coronaviruses and confirm the antiviral efficacy of iminosugars in cellular assays using the human lung-cell line Calu-3.

01 Apr 2025·Food Chemistry

Enhanced bioaccessibility of cyclolinopeptides via zein-cyclodextrin nanoparticles: Simulated gastrointestinal digestion and cellular uptake study

Article

Author: Wang, Yong ; Lu, Xuanxuan ; Chen, Peifang ; Cai, Zizhe

Cyclolinopeptides (CLS) are hydrophobic cyclic peptides in flaxseed with multiple bioactive activities. This study developed zein (Z)-cyclodextrin (CD) binary nanoparticles (NPs) as an oral delivery system for CLS. Z-CD NP had a smaller diameter (D_h) and better encapsulation effect on CLS. Formation of CLS-loaded NPs was driven by hydrogen bonds and electrostatic interactions. Presence of CD improved the thermal, pH and storage stabilities of NPs. Besides, CD prevented premature release of CLS in the stomach and enhanced the bioaccessibility of CLS to a maximum of 86.71 % ± 2.20 %. Lipid-raft-mediated endocytosis was involved in the cell uptake of NPs, where the addition of CD significantly facilitated the uptake of NPs. Z-CD NPs also enhanced absorption and reduced secretion of CLS after digestion. Overall, this study provides a simple approach to enhance the oral delivery efficiency of CLS by modulating Z-based NPs with CD.

03 Mar 2025·Molecular Pharmaceutics

Correction to “Tumor Cell Lysate-Based Multifunctional Nanoparticles Facilitate Enhanced mRNA Delivery and Immune Stimulation for Melanoma Gene Therapy”

Author: Wu, Jieping ; Wang, Kaiyu ; Zhang, Jin ; Huang, Jing ; Wu, Shan ; Men, Ke ; Lei, Sibei ; Duan, Xingmei ; Chen, Xiayu

MRNA (mRNA)-based gene therapy has great potential for cancer gene therapy.However, the effectiveness of mRNA in cancer therapy needs to be further improved, and the delivery efficiency and instability of mRNA limit the application of mRNA-based products.Both the delivery efficiency can be elevated by cell-penetrating peptide modification, and the immune response can be enhanced by tumor cell lysate stimulation, representing an advantageous strategy to expand the effectiveness of mRNA gene therapy.Therefore, it is vital to exploit a vector that can deliver high-efficiency mRNA with codelivery of tumor cell lysate to induce specific immune responses.We previously reported that DMP cationic nanoparticles, formed by the self-assembly of DOTAP and mPEG-PCL, can deliver different types of nucleic acids.DMP has been successfully applied in gene therapy research for various tumor types.Here, we encapsulated tumor cell lysates with DMP nanoparticles and then modified them with a fused cell-penetrating peptide (TAT-iRGD) to form an MLSV system.The MLSV system was loaded with encoded Bim mRNA, forming the MLSV/Bim complex.The average size of the synthesized MLSV was 191.4 nm, with a potential of 47.8 mV.The MLSV/mRNA complex promotes mRNA absorption through caveolin-mediated endocytosis with a transfection rate of up to 68.6% in B16 cells.The MLSV system could also induce the maturation and activation of dendritic cells, obviously promoting the expression of CD80, CD86, and MHC-II both in vitro and in vivo.By loading of the encoding Bim mRNA, the MLSV/Bim complex can inhibit cell proliferation and tumor growth, with inhibition rates of up to 87.3% in vitro.Similarly, the MLSV/Bim complex can inhibit tumor growth in vivo, with inhibition rates of up to 78.7% in the B16 s.c. tumor model and 63.3% in the B16 pulmonary metastatic tumor model.Our results suggest that the MLSV system is an advanced candidate for mRNA-based immunogene therapy.

100 Deals associated with Amiloride Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D00649	Amiloride Hydrochloride	C03DB01	DB00594

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Heart Failure	United States	Padagis US LLC	05 Oct 1981
Hypertension	United States	Padagis US LLC	05 Oct 1981

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05079789 (AMILOR, CTgov)	Phase 3	Hypernatremia \| Edema \| Nephrotic Syndrome	20	Amiloride (Amiloride)	gbhbzvpvdo(qbozhhacse) = vmakciwqtz xmpbecjafb (rwozphitcp, cqkdkrqhug - hwgrqyiksd) View more	-	14 Jan 2025
				Furosemide (Furosemide)	gbhbzvpvdo(qbozhhacse) = yayvbxoiot xmpbecjafb (rwozphitcp, baalqxdugl - nzkxqagcbd) View more
PMON89 (ENDO2022)	Not Applicable	Diabetes Insipidus, Nephrogenic	-	Temozolomide	vuudwswtbk(sheerhqffw) = govesgaweq tybzibgzhj (tfjapglrak, 280 - 295) View more	-	01 Nov 2022
				Pantoprazole	bfxkacktnf(yfjzbxjoyu) = agjonpoqlo bgpvjszzwn (cfxejurlpa )
NCT02522650 (Pubmed \| Am J Nephrol)	Phase 4	Kidney Diseases	12	Amiloride 5 mg	wxrujafvst(ypbiwdaoal) = grljknxovm hfqygpfwaw (mkdqehyaea )	-	06 May 2021
				Triamterene 50 mg	wxrujafvst(ypbiwdaoal) = zrmyxclxbt hfqygpfwaw (mkdqehyaea )
ESH2021	Not Applicable	Acute Kidney Injury plasmin activity	-	Amiloride (Normal salt diet (NS))	(ncxiixfkbr) = vrdcvonogf pyjysvmpvf (jjrykdymlu ) View more	Positive	01 Apr 2021
				Amiloride (Aldosterone + high salt diet (Ald+HS))	(ncxiixfkbr) = qiicyqdqis pyjysvmpvf (jjrykdymlu ) View more
ASN2020	Not Applicable	Urolithiasis	31	Amiloride	(ifxpgfbzzd) = Three (20%) patients stopped due to delayed intolerance and 2 (13%) due to elevated urinary calcium auwviwutav (vucttccpgd ) View more	Negative	19 Oct 2020
				Thiazide
ASN2020	Not Applicable	Kidney Diseases	12	Amiloride 5 mg	(hipptrozhv) = Three patients exited the study due to hyperkalemia utnnkbehct (lfqibyxrfq )	Positive	19 Oct 2020
				Triamterene 50 mg
NCT01733680 (CTgov)	Early Phase 1	Attention Deficit Disorder With Hyperactivity	3	Behavioral+amiloride (Amiloride)	musxiuxbsl(asyldptpgq) = rtynmyfbpt pzwwlekzkf (lhrkkfqnui, bkfuixbjco - mjkrzpyvde) View more	-	20 Jul 2018
				Behavioral (Placebo)	musxiuxbsl(asyldptpgq) = gbhsrcvhzc pzwwlekzkf (lhrkkfqnui, pklqucehau - npoedezjwv) View more
ESC2016	Not Applicable	Coronary Disease	-	Amiloride HCl Dihydrate	miltzeamcg(ahdzsxzyxm) = zenwpqikby xzvspphuhn (cduigjbnxd )	-	30 Aug 2016
ASN2015	Not Applicable	Hypokalemia \| Gitelman Syndrome SLC12A3 gene	-	Spironolactone	ubustellkv(yzjrahluzr) = xzhjvrcgzh cpzqqepfqf (ezttuxtgkb ) View more	Positive	03 Nov 2015
				Amiloride	ubustellkv(yzjrahluzr) = dojkcjrukw cpzqqepfqf (ezttuxtgkb ) View more
SP309 (ERA2015)	Not Applicable	Kidney Diseases urine albumin-to-creatinine ratio (ACR)	21	Spironolactone	besvoeykvr(hgmakpinrc) = bqxhckfpnz rotvitywft (gztimpguwo, -21% - -47.9%)	Positive	21 May 2015
				Hydrochlorothiazide	besvoeykvr(hgmakpinrc) = ugmjeewcqp rotvitywft (gztimpguwo, -28.1% - -56.9%)