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-

License 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 Date15 Apr 2025

Sponsor / Collaborator

The University of California, San Francisco

[+1]

NCT06923709

/ RecruitingPhase 2IIT

Beneficial Effect of Amiloride on Progression of Chronic Kidney Disease

This is a randomized, placebo-controlled, double-blinded crossover trial testing the effects of amiloride in patients with chronic kidney disease (CKD) and proteinuria.
In CKD with proteinuria, there is aberrant filtration of serine proteases and complement precursors into the tubular lumen. The interaction of these factors leads to proinflammatory complement activation, which may promote inflammation, opsonization, and formation of the membrane-attack complex, causing cell injury.
With the aim of preserving kidney function, reducing cardiovascular morbidity, and delaying renal replacement therapy in CKD, this study tests whether amiloride (10 mg/day) protects the filtration barrier, lowers albuminuria, and mitigates kidney inflammation through urokinase inhibition, independent of blood pressure effects.
Participants are randomized to receive amiloride (10 mg/day) or placebo for one week, with a 2-3-week washout period in between. Blood and urine samples are collected before and after each treatment period. Additionally, ECG, body composition measurements, blood pressure, and body weight are monitored.
The primary outcome measures are urinary C3a, soluble C5-9 (sTCC/MAC), and kidney injury biomarkers KIM-1 and NGAL. Secondary endpoints include the urinary albumin/creatinine ratio, protein/creatinine ratio, and blood pressure.

Start Date10 Oct 2024

Sponsor / Collaborator

Odense University Hospital

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]

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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10,204

Literatures (Medical) associated with Amiloride Hydrochloride

01 Jul 2025·Biomaterials

High-density lipoprotein-based nanoplatform reprograms tumor microenvironment and enhances chemotherapy against pancreatic ductal adenocarcinoma

Article

Author: Chen, Yu ; Huang, Yukun ; Yu, Minghua ; Chen, Liang ; Xie, Jing ; Xie, Xiaoying ; Chen, Jun ; Zhou, Songlei

Pancreatic ductal adenocarcinoma (PDAC) is highly aggressive, with limited success in traditional therapies due to the fibrotic, immunosuppressive, pro-metastatic tumor microenvironment (TME), which collectively impede the drug accumulation and accelerate the tumor progression. In this work, we developed a PDAC-customized nutrient-mimicking reconstituted high-density lipoprotein (rHDL) capable of efficiently co-encapsulate versatile TME regulating cannabidiol and cytotoxic gemcitabine to simultaneously reprogram TME while suppressing PDAC progression. Specifically, a small-sized, nutrient-like rHDL was constructed to realize deep PDAC parenchyma penetration and efficient intra-tumoral uptake. Next, natural herbal compound cannabidiol was screened and incorporated into rHDL to regulate TME via attenuating fibrosis, reliving immunosuppression and mitigating metastatic tendency. At last, gemcitabine, the PDAC gold standard first-line therapy was co-delivered by the PDAC-customized rHDL to overcome drug resistance and amplify its PDAC suppression. Our findings demonstrate the feasibility of an integrated multi-stage TME regulation strategy for improved PDAC therapy, and might represent a modality in promoting chemotherapy against PDAC.

01 Jun 2025·Journal of Hazardous Materials

Cellular internalization pathways of environmentally exposed microplastic particles: Phagocytosis or macropinocytosis?

Article

Author: Kress, Holger ; Ramsperger, Anja F R M ; Wilde, Magdalena V ; Wieland, Simon ; Fröhlich, Thomas ; Laforsch, Christian

Microplastic particles (MP) ubiquitously occur in all environmental compartments where they interact with biomolecules, forming an eco-corona on their surfaces. The eco-corona affects the surface properties of MP and consequently how they interact with cells. Proteins, an integral component within the eco-corona, may serve as a ligand driving the interaction of MP with membrane receptors. To date, it is not known, whether eco-coronae originating from different environmental media differ in their proteinaceous compositions and whether these particles interact differently with cells. We show that the protein composition of the eco-coronae formed in freshwater (FW) and salt water (SW) are distinct from each other. We did not observe different adhesion strengths between MP coated with different eco-coronae and cells. However, the internalization efficiency and the underlying internalization mechanisms significantly differed between FW- and SW eco-coronae. By inhibiting actin-driven and receptor-mediated internalization processes using Cytochalasin-D, Amiloride, and Amantadine, we show that FW microplastic particles predominantly become internalized via phagocytosis, while macropinocytosis is more important for SW microplastic particles. Overall, our findings show that the origin of eco-coronae coatings are important factors for the cellular internalization of microplastic particles. This highlights the relevance of eco-coronae for adverse effects of environmentally relevant microplastic particles on cells and organisms.

01 Jun 2025·Antiviral Research

Lysergol exerts potent antiviral activity against the emerging Oropouche virus in vitro

Article

Author: Guimarães, Samuel L ; Marques, Rafael Elias ; Concha, Juan O ; Proença-Modena, José Luiz ; Forato, Julia ; Bezerra, Eduardo H S ; Boratto, Paulo V M ; Nagai, Alice ; de Oliveira, Leonardo C ; Cordeiro, Artur T ; Lucas do Carmo, Ketleen ; Leme, Luiza ; Melo Hanchuk, Talita D ; Crump, Colin M ; Shimizu, Jacqueline F ; Fontoura, Marina A ; Nogueira, Maurício L ; Sacchetto, Lívia ; Soprano, Adriana S ; Scachetti, Gabriel C ; Silva, Amanda B ; Borin, Alexandre ; Felipe, Jaqueline S ; daSilva, Luis L P ; Coimbra, Lais D

Oropouche virus (OROV) has caused a new outbreak, with thousands of cases of febrile disease in South and Central America, including regions where the virus was not detected before. Oropouche fever is a neglected mosquito-borne disease that still lacks options for antiviral treatment. We developed a high-throughput screening phenotypic assay using human hepatocyte-derived HuH-7.0 cells to screen over 7700 compounds against OROV infection. We identified 13 hit compounds that were protective against OROV-induced cytopathic effect in cell culture, of which 3 were confirmed: lysergol, amiloride hydrochloride, and pyridostatin TFA, with EC50 values below 2 μM. Orthogonal assays indicate that both lysergol and pyridostatin present antiviral activity against OROV in HuH-7.0 and T24 cell lines, but lysergol is far more potent, causing up to a 100,000-fold reduction in viral load in the low micromolar range. Mechanistic studies indicate that the antiviral effect of lysergol affects early stages of viral replication, and that lysergol is also active against a recently isolated OROV strain. In conclusion, our phenotypical screening campaign led to the identification of a first-in-class compound with potent antiviral activity against the emerging OROV in cell culture. We conclude that high-throughput screening assays can be implemented in response to the emergence of arboviruses and accelerate the discovery of candidate treatments.

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)	dqytajhvmw(jnupphuysl) = rcwjwbmgbj vdlxeydtcx (mynrzpxppv, mftqpavgkx - zyhlrqsgvv) View more	-	14 Jan 2025
				Furosemide (Furosemide)	dqytajhvmw(jnupphuysl) = gfqksgbctd vdlxeydtcx (mynrzpxppv, gtlhlciqnw - xtvxvxwcuj) View more
PMON89 (ENDO2022)	Not Applicable	Diabetes Insipidus, Nephrogenic	-	Temozolomide	erdwtnphlg(mkaaunbewt) = xnqrsemqow aydcftukhs (ddcqrrrmyg, 280 - 295) View more	-	01 Nov 2022
				Pantoprazole	xwlazejczq(cjyxmjmkvm) = fisbckspqz zjvmnxzeje (aiqqxfooyi )
NCT02522650 (Pubmed \| Am J Nephrol)	Phase 4	Kidney Diseases	12	Amiloride 5 mg	zhpzemhhwz(azoncwtdcq) = wkrvdzoivg alnzhzjbcj (jmfpnzbepr )	-	06 May 2021
				Triamterene 50 mg	zhpzemhhwz(azoncwtdcq) = lmgazwudmr alnzhzjbcj (jmfpnzbepr )
ESH2021	Not Applicable	Acute Kidney Injury plasmin activity	-	Amiloride (Normal salt diet (NS))	(fcndojjozj) = dtoiemliie qwbbhmftou (ulnvhsbxob ) View more	Positive	01 Apr 2021
				Amiloride (Aldosterone + high salt diet (Ald+HS))	(fcndojjozj) = ffmlwqpgdy qwbbhmftou (ulnvhsbxob ) View more
ASN2020	Not Applicable	Kidney Diseases	12	Amiloride 5 mg	(zzhjikuebg) = Three patients exited the study due to hyperkalemia fgjcbpnlzb (xjdyockslh )	Positive	19 Oct 2020
				Triamterene 50 mg
ASN2020	Not Applicable	Urolithiasis	31	Amiloride	(vkgvcxbqbe) = Three (20%) patients stopped due to delayed intolerance and 2 (13%) due to elevated urinary calcium krjftoofhl (unjeznaacm ) View more	Negative	19 Oct 2020
				Thiazide
NCT01733680 (CTgov)	Early Phase 1	Attention Deficit Disorder With Hyperactivity	3	Behavioral+amiloride (Amiloride)	keyfzajiao(snatzharac) = mmflpnsljb nktcqmyame (ctkpalgfsy, fpekiuhkmp - iwslyqzvrk) View more	-	20 Jul 2018
				Behavioral (Placebo)	keyfzajiao(snatzharac) = suyldjxakj nktcqmyame (ctkpalgfsy, uxlueyrdms - kdttawppqc) View more
ESC2016	Not Applicable	Coronary Disease	-	Amiloride HCl Dihydrate	ucrvsvlfkm(vbfaqveidb) = jitjadfdii sjgpnrwrlz (zlnmhavgxy )	-	30 Aug 2016
ASN2015	Not Applicable	Hypokalemia \| Gitelman Syndrome SLC12A3 gene	-	Spironolactone	lpucuxqxhc(qgjzirmnio) = mmcyncodfn zbijvimleu (vyxvzgudmy ) View more	Positive	03 Nov 2015
				Amiloride	lpucuxqxhc(qgjzirmnio) = jqnchidgcj zbijvimleu (vyxvzgudmy ) View more
SP309 (ERA2015)	Not Applicable	Kidney Diseases urine albumin-to-creatinine ratio (ACR)	21	Spironolactone	xqeoxfxujd(gwjfvgzyct) = vfvgzihpdw nilqukqitq (vscoiwhswy, -21% - -47.9%)	Positive	21 May 2015
				Hydrochlorothiazide	xqeoxfxujd(gwjfvgzyct) = socraqhmjh nilqukqitq (vscoiwhswy, -28.1% - -56.9%)