Delving into the Latest Updates on Bumetanide with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

3-(aminosulfonyl)-5-(butylamino)-4-phenoxybenzoic acid, 3-butylamino-4-(phenoxy)-5-sulfamoylbenzoic acid, 3-butylamino-4-phenoxy-5-sulfamoyl-benzoic acid

+ [20]

Target

NKCC1 x NKCC2 x SLC12A4

Action

inhibitors

Mechanism

NKCC1 inhibitors(Solute carrier family 12 member 2 inhibitors), NKCC2 inhibitors(Sodium-(potassium)-chloride cotransporter 2 inhibitors), SLC12A4 inhibitors(solute carrier family 12 member 4 inhibitors)

Therapeutic Areas

Cardiovascular DiseasesEndocrinology and Metabolic DiseaseOther Diseases+ [1]

Active Indication

Heart FailureHypercalcemiaHyperkalemia+ [5]

Inactive Indication

Autism Spectrum Disorder

Originator Organization

Daiichi Sankyo Co., Ltd.

Active Organization

Knight Therapeutics, Inc.

Guilin Pharmaceutical Group Co., Ltd.Corstasis Therapeutics

+ [3]

Inactive Organization

Adir SRLInstitut de Recherches Intern Servier

License Organization

Les Laboratoires Servier SAS

Neurochlore

Drug Highest PhaseApproved

First Approval Date

Japan (08 Apr 1976),

Edema

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC17H20N2O5S

InChIKeyMAEIEVLCKWDQJH-UHFFFAOYSA-N

CAS Registry28395-03-1

Patients with cirrhosis are frequently hospitalized due to an acute decompensation of their liver disease including bleeding, jaundice, encephalopathy, and volume overload. Volume overload is associated with increased mortality from acute hypoxic respiratory failure, hemorrhage from esophageal varices, and spontaneous bacterial peritonitis.
Clinical practice guidelines describe sodium restriction and diuretics as first-line treatment, combined with regular body weight monitoring to assess response. In patients with suboptimal response to furosemide, alternative loop diuretics like torsemide or bumetanide may improve natriuresis. Bumetanide has a theoretic advantage over furosemide due to its more rapid and complete intestinal absorption, combined with a prolonged half-life in patients with hepatic dysfunction. In this pragmatic study, the aim is to compare the efficacy of diuresis with bumetanide versus furosemide among hospitalized patients with cirrhosis.

Start Date01 Jul 2025

Sponsor / Collaborator

University of Utah

CTR20240307

/ CompletedNot Applicable

中国健康受试者单次口服布美他尼片（1mg）的开放、随机、单剂量、两制剂、单次给药、交叉设计的生物等效性试验

[Translation] An open-label, randomized, single-dose, two-formulation, single-dose, crossover-design bioequivalence study of a single oral dose of bumetanide tablets (1 mg) in healthy Chinese subjects

主要研究目的研究空腹和餐后单次口服布美他尼片受试制剂（规格：1mg，新乡市常乐制药有限责任公司生产，浙江和沐康医药科技有限公司提供）与布美他尼片参比制剂（Burinex®，规格：1mg，Karo Pharma AB持证，浙江和沐康医药科技有限公司提供）在中国健康受试者体内的药代动力学行为，评价空腹及餐后口服两种制剂的生物等效性。次要研究目的评价中国健康受试者空腹和餐后单次口服受试制剂（T）布美他尼片和参比制剂（R）布美他尼片（Burinex®）后的安全性。

[Translation]

Main study objectives To study the pharmacokinetic behavior of the test formulation of bumetanide tablets (specification: 1 mg, produced by Xinxiang Changle Pharmaceutical Co., Ltd., provided by Zhejiang Hemukang Pharmaceutical Technology Co., Ltd.) and the reference formulation of bumetanide tablets (Burinex®, specification: 1 mg, licensed by Karo Pharma AB, provided by Zhejiang Hemukang Pharmaceutical Technology Co., Ltd.) in Chinese healthy subjects after single oral administration on an empty stomach and after a meal, and to evaluate the bioequivalence of the two formulations after oral administration on an empty stomach and after a meal. Secondary study objectives To evaluate the safety of the test formulation (T) bumetanide tablets and the reference formulation (R) bumetanide tablets (Burinex®) after single oral administration on an empty stomach and after a meal in Chinese healthy subjects.

Start Date27 Feb 2024

Sponsor / Collaborator

Zhejiang Hemukang Pharmaceutical Technology Co. Ltd.

NCT06036914

/ CompletedPhase 2IIT

Ultra High Dose Diuretic Strategy for Management of Acute Decompensated Heart Failure - A Randomized, Double-Blind Pilot Trial

The purpose of this study is to determine the safety and effectiveness of ultrahigh dose diuretics compared to standard dose diuretics over 24 hours in patients with decompensated heart failure.

Start Date27 Nov 2023

Sponsor / Collaborator

Mayo Clinic

100 Clinical Results associated with Bumetanide

Login to view more data

100 Translational Medicine associated with Bumetanide

Login to view more data

100 Patents (Medical) associated with Bumetanide

Login to view more data

3,798

Literatures (Medical) associated with Bumetanide

01 Jun 2025·JOURNAL OF HAZARDOUS MATERIALS

Broad-spectrum antibody against thiazides and degraded salamide and immunoassay establishment for simultaneous detection

Article

Author: Li, Yunlong ; Wen, Jiaxin ; Pan, Liangwen ; Zhang, Shiwei ; Lei, Hongtao ; Huang, Xin-An ; Luo, Hewen ; Tang, Yu ; Liu, Zhiwei ; Chen, Jiahong

The illegal additive thiazides and degraded salamide in food supplements poses significant health risks and regulatory challenges. However, the structural differences between thiazides and salamide complicate the hapten design for immunoassay detection. In this study, we first outlined the common skeleton of thiazides and their shared epitopes with salamide through molecular overlap and atomic charge distribution analysis. Several haptens were rationally designed based on the private epitope of salamide and the shared epitopes with thiazides, assisted by computer-aided chemical analysis. Subsequently, the resultant monoclonal antibody exhibited broad specificity for thiazides (IC₅₀ value = 21.43-405.40 ng/mL) and salamide (IC₅₀ value = 0.76 ng/mL). The immunoassay affinities of 5 of these thiazides are reported for the first time. Further elucidation of the intrinsic recognition mechanism was achieved through homology modeling and molecular docking, clarifying the antibody's diverse recognition spectrum. Finally, we established a rapid, reliable colloidal gold-based immunochromatography strip for simultaneous detecting total thiazides and degraded salamide in food supplements and surface water sample for the first time. The cut-off value was as low as 7.5 ng/mL, which was 32 times more sensitive than that of established immunoassays for thiazides.

01 Apr 2025·TRENDS IN PHARMACOLOGICAL SCIENCES

Emerging autism and Fragile X syndrome treatments

Review

Author: Salmaso, Natalina ; D'Angiulli, Amedeo ; Parkhill, Michael ; Lee, Vivian ; Aguilar-Valles, Argel

The limitations of current symptom-focused treatments drive the urgent need for effective therapies for autism and Fragile X syndrome (FXS). Currently, no approved pharmacological interventions target the core symptoms of these disorders. Advances in understanding the underlying biology of autism and FXS make this an important time to explore novel options. Indeed, several treatments have recently been tested in clinical trials, with promising results in treating core symptoms of autism and FXS. We focus on emerging interventions, such as gut microbiome therapies, anti-inflammatory approaches, bumetanide, phosphodiesterase 4D inhibitors, and endocannabinoid modulators. We also discuss factors, such as disorder heterogeneity, which may have contributed to poor efficacy in previously failed late-phase trials and impact recent trials, emphasizing the need for personalized treatment approaches.

01 Apr 2025·NEUROBIOLOGY OF DISEASE

Neurodevelopmental defects in Dravet syndrome Scn1a+/− mice: Targeting GABA-switch rescues behavioral dysfunctions but not seizures and mortality

Article

Author: Menna, Elisabetta ; Capitano, Fabrizio ; Léna, Isabelle ; Mantegazza, Massimo ; Fossati, Giuliana ; Antonucci, Flavia ; Rusina, Evgeniia ; Pizzamiglio, Lara

Dravet syndrome (DS) is a developmental and epileptic encephalopathy (DEE) caused by mutations of the SCN1A gene (Na_V1.1 sodium channel) and characterized by seizures, motor disabilities and cognitive/behavioral deficits, including autistic traits. The relative role of seizures and neurodevelopmental defects in disease progression, as well as the role of the mutation in inducing early neurodevelopmental defects before symptoms' onset, are not clear yet. A delayed switch of GABAergic transmission from excitatory to inhibitory (GABA-switch) was reported in models of DS, but its effects on the phenotype have not been investigated. Using a multi-scale approach, here we show that targeting GABA-switch with the drugs KU55933 (KU) or bumetanide (which upregulate KCC2 or inhibits NKCC1 chloride transporters, respectively) rescues social interaction deficits and reduces hyperactivity observed in P21 Scn1a^+/- DS mouse model. Bumetanide also improves spatial working memory defects. Importantly, neither KU nor bumetanide have effect on seizures or mortality rate. Also, we disclose early behavioral defects and delayed neurodevelopmental milestones well before seizure onset, at the beginning of Na_V1.1 expression. We thus reveal that neurodevelopmental components in DS, in particular GABA switch, underlie some cognitive/behavioral defects, but not seizures. Our work provides further evidence that seizures and neuropsychiatric dysfunctions in DEEs can be uncoupled and can have differential pathological mechanisms. They could be treated separately with targeted pharmacological strategies.

9

News (Medical) associated with Bumetanide

25 Nov 2024

·www.drugs.com

AHA: Bumetanide Nasal Spray Statistically Bioequivalent to Oral Bumetanide

MONDAY, Nov. 25, 2024 -- Bumetanide nasal spray (BNS) has statistical bioequivalence to oral bumetanide, according to a research letter published online Nov. 18 in Circulation to coincide with the American Heart Association Scientific Sessions 2024, held from Nov. 16 to 18 in Chicago. Andrew P. Ambrosy, M.D., from the Kaiser Permanente San Francisco Medical Center, and colleagues conducted an open-label, randomized controlled trial in healthy volunteers to compare the bioavailability of BNS to that of an oral tablet and intravenous (IV) bumetanide. Sixty-eight participants were assigned to one of four treatment sequences across five treatment periods, with a 48-hour washout period between treatments. The researchers found that BNS achieved its primary end point, demonstrating statistical bioequivalence to oral bumetanide for maximum concentration, area under the concentration-time curve 0-t, and area under the concentration-time curve 0-inf. BNS was absorbed more rapidly, with a median time to maximum concentration of 1.0 and 1.5 hours for BNS and the oral formulation, respectively. Twenty-seven percent variability in absorption was seen for the nasal and IV forms compared with >40 percent for the oral form. BNS had comparable pharmacodynamic effects of diuresis and natriuresis to IV and oral bumetanide. Fewer individuals experienced treatment-emergent adverse events after BNS treatment compared with the IV and oral forms (8.8 percent versus 9.1 and 17.9 percent, respectively). "We were surprised by how fast the nasal spray worked and by how variable the absorption of the oral drug was even in healthy subjects," coauthor Daniel Bensimhon, M.D., of Cone Health in Greensboro, North Carolina, said in a statement. Several authors disclosed ties to pharmaceutical companies, including Corstasis Therapeutics, which developed and manufactured the BNS tested in the study and funded the study. Abstract/Full Text More Information Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

AHAClinical StudyClinical Result

21 Nov 2024

·www.pharmaindustrial-india.com

Lupin Introduces Bumetanide Injection in US

Lupin has developed Bumetanide Injection USP, 1 mg/4 mL (0.25 mg/mL) Single-Dose Vials and 2.5 mg/10 mL (0.25 mg/mL) Multiple-Dose Vials in the United States, after having received approval from the United Food and Drug Administration (US FDA). Bumetanide Injection USP, is a generic equivalent of Bumex Injection, 0.25 mg/mL of Validus Pharmaceuticals, LLC., indicated for the treatment of edema associated with congestive heart failure, hepatic and renal disease, including the nephrotic syndrome. Bumetanide Injection USP (RLD Bumex) had an estimated annual sale of USD 20 million in the US. Lupin Limited is a global pharmaceutical leader headquartered in Mumbai, India, with products distributed in over 100 markets. Lupin specializes in pharmaceutical products, including branded and generic formulations, complex generics, biotechnology products, and active pharmaceutical ingredients. Trusted by healthcare professionals and consumers globally, the company enjoys a strong position in India and the US across multiple therapy areas, including respiratory, cardiovascular, anti-diabetic, anti-infective, gastrointestinal, central nervous system, and women’s health. Lupin has 15 state-of-the-art manufacturing sites and 7 research centers globally, along with a dedicated workforce of over 22,000 professionals. Lupin is committed to improving patient health outcomes through its subsidiaries – Lupin Diagnostics, Lupin Digital Health, and Lupin Manufacturing Solutions.

Drug Approval

19 Sep 2024

·www.pharmaindustrial-india.com

Lupin Gets FDA Approval for Bumetanide Injection

Lupin has secured approval from the United States Food and Drug Administration (US FDA) for its Abbreviated New Drug Application (ANDA) for Bumetanide Injection USP, 1 mg/4 mL (0.25 mg/mL) Single-Dose Vials and 2.5 mg/10 mL (0.25 mg/mL) Multiple-Dose Vials to market a generic equivalent of Bumex Injection, 0.25 mg/mL of Validus Pharmaceuticals, LLC. The product will be manufactured at Lupin’s Nagpur facility in India. Bumetanide Injection USP, 1 mg/4 mL (0.25 mg/mL) Single-Dose Vials and 2.5 mg/10 mL (0.25 mg/mL) Multiple-Dose Vials are indicated for the treatment of edema associated with congestive heart failure, hepatic and renal disease, including the nephrotic syndrome. Bumetanide Injection USP (RLD Bumex) had estimated annual sales of USD 20 million in the US. Lupin is a global pharmaceutical leader headquartered in Mumbai, India, with products distributed in over 100 markets. Lupin specializes in pharmaceutical products, including branded and generic formulations, complex generics, biotechnology products, and active pharmaceutical ingredients. Trusted by healthcare professionals and consumers globally, the company enjoys a strong position in India and the US across multiple therapy areas, including respiratory, cardiovascular, anti-diabetic, anti-infective, gastrointestinal, central nervous system, and women’s health.

Drug Approval

100 Deals associated with Bumetanide

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D00247	Bumetanide	C03CA02	DB00887

R&D Status

Approved

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Heart Failure	Canada	Knight Therapeutics, Inc.	31 Dec 1993
Hypercalcemia	China	Guilin Pharmaceutical Group Co., Ltd.	01 Jan 1982
Hyperkalemia	China	Guilin Pharmaceutical Group Co., Ltd.	01 Jan 1982
Hypertension	China	Guilin Pharmaceutical Group Co., Ltd.	01 Jan 1982
Hyponatremia	China	Guilin Pharmaceutical Group Co., Ltd.	01 Jan 1982
Poisoning	China	Guilin Pharmaceutical Group Co., Ltd.	01 Jan 1982
Edema	Japan	Daiichi Sankyo Co., Ltd.	08 Apr 1976

Developing

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Autism Spectrum Disorder	Phase 3	Brazil	Institut de Recherches Intern Servier	24 Sep 2018
Autism Spectrum Disorder	Phase 3	Brazil	Adir SRL	24 Sep 2018
Autism Spectrum Disorder	Phase 3	France	Adir SRL	24 Sep 2018
Autism Spectrum Disorder	Phase 3	France	Institut de Recherches Intern Servier	24 Sep 2018
Autism Spectrum Disorder	Phase 3	Germany	Adir SRL	24 Sep 2018
Autism Spectrum Disorder	Phase 3	Germany	Institut de Recherches Intern Servier	24 Sep 2018
Autism Spectrum Disorder	Phase 3	Hungary	Institut de Recherches Intern Servier	24 Sep 2018
Autism Spectrum Disorder	Phase 3	Hungary	Adir SRL	24 Sep 2018
Autism Spectrum Disorder	Phase 3	Italy	Institut de Recherches Intern Servier	24 Sep 2018
Autism Spectrum Disorder	Phase 3	Italy	Adir SRL	24 Sep 2018

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03715153 (CTgov)	Phase 3	Autism Spectrum Disorder	211	BUMETANIDE (S95008) for week 0 - 26 (BUMETANIDE (S95008) Followed by Open-Label S95008)	yucdsynplc = nyfnafdcwf czxfczdljy (vpiubfuwjc, nvthhxggsa - ivohvjokpj) View more	-	05 Jun 2023
				PLACEBO for week 0 - 26+Open-Label BUMETANIDE (S95008) for weeks 26 - 52 (PLACEBO Followed by Open-Label S95008)	yucdsynplc = knjrsrtyci czxfczdljy (vpiubfuwjc, qcpaympxao - zkbsiyfqjp) View more
NCT03923933 (HEBE-CKD, Pubmed \| BMC Nephrol)	Phase 2	Chronic Kidney Diseases	34	Bumetanide plus chlorthalidone	qyqmtktzqp(vvcahcffpi) = yqlumahesy nacywlvgsn (awyrroaxcd ) View more	-	20 Sep 2022
				Bumetanide plus placebo	qyqmtktzqp(vvcahcffpi) = exsqlphuzt nacywlvgsn (awyrroaxcd ) View more
EULAR2020	Not Applicable	Acute congestive heart failure	130	Intravenous Bumetanide	namfsgksqs(rwooutknhm) = The use of IV bumetanide in patients hospitalized for AHF exacerbations is associated with a 7.17% yearly incidence of acute gout flares ikaykeursi (dhtlljdfdr ) View more	-	03 Jun 2020
NCT03923933 (HEBE-CKD, CTgov)	Phase 2	Chronic Kidney Diseases	34	Bumetanide (Placebo)	swvesxexki(lxrvlbhfbv) = datwwkbnwz kgonrdipdp (toqkmdldce, 1.78) View more	-	10 Mar 2020
				Bumetanide+Chlorthalidone (Treatment Grup)	swvesxexki(lxrvlbhfbv) = cfqfxfoiwz kgonrdipdp (toqkmdldce, 3.29) View more
NCT01973335 (DIURESIS-CHF, CTgov)	Phase 4	Heart Failure	34	oral spironolactone+Combination therapy (Acetazolamide/Low-dose Loop Diuretics, Upfront Spironolactone)	wdbjpzyzjs(dzufxshjyx) = byipryonbt hqclwekglr (yudyijgtgr, 133) View more	-	21 Mar 2019
				Upfront therapy with oral spironolactone+High-dose loop diuretics (High-dose Loop Diuretics, Upfront Spironolactone)	wdbjpzyzjs(dzufxshjyx) = eytycacqep hqclwekglr (yudyijgtgr, 165) View more
ANA2018	Not Applicable	Epilepsy, Benign Neonatal Add-on	-	Phenobarbital + Placebo	rczawhwhbu(shxajxmayp) = p=0.02 dlrrzjwqgb (ibfebamkgk ) View more	Positive	05 Oct 2018
				Phenobarbital + Bumetanide 0.1mg/kg
ANA2015	Not Applicable	Seizures Adjuvant	-	Bumetanide 0.1mg/kg	bqvfjjrtax(nzpoitysex) = comparable between subjects receiving bumetanide vs. phenobarbital alone jidkpaxapf (mgsnrnphcw ) View more	Positive	25 Sep 2015
				Bumetanide 0.2mg/kg
SFN2007	Not Applicable	Blood brain barrier defect	-	Bumetanide	exisudxbbk(hdacoyokyx) = obwdseyzbz fbinhzvbzx (ovwauevzth, 0.2)	-	04 Nov 2007
				Unlabeled bumetanide	exisudxbbk(hdacoyokyx) = trqxwdhfji fbinhzvbzx (ovwauevzth, 0.2)