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 DiseaseUrogenital Diseases+ [1]

Active Indication

Heart FailureAcute Kidney InjuryDrug intoxication+ [6]

Inactive Indication

Autism Spectrum Disorder

Originator Organization

Daiichi Sankyo Co., Ltd.

Active Organization

Guilin Pharmaceutical Co., Ltd.

Knight Therapeutics, Inc.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-

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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

NCT07005414

/ RecruitingPhase 2IIT

Efficacy of Bumetanide in Children With Autism Spectrum Disorder Guided by Peripheral Blood Biomarkers and Machine Learning Models: A Randomized Controlled Trial

The objective of this study is to learn if bumetanide could alleviate the clinical symptoms in children with autism spectrum disorder (ASD), who has been predicted as high responders to bumetanide via a cytokine-based predictive model. The Eligible ASD participants identified as high responder to bumetanide will be randomly assigned to either the experimental group or the control group. Participants in the experimental group will receive bumetanide interventions, along with the behavioral interventions, for three months. Participants in the control group will only undergo behavioral interventions. The clinical symptoms and potential adverse effects will be closely monitored throughout the intervention period.

Start Date04 Jun 2025

Sponsor / Collaborator-

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.

100 Clinical Results associated with Bumetanide

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100 Translational Medicine associated with Bumetanide

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100 Patents (Medical) associated with Bumetanide

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3,815

Literatures (Medical) associated with Bumetanide

01 Jul 2025·Current drug discovery technologies

Potential Role of Benzoic Acid and its Synthetic Derivatives to Alleviate Cancer: An Up-to-Date Review

Article

Author: Singh, Mhaveer ; Kaushik, Niranjan ; Koya Kamal, Yoonus Kunju Thajuddin ; Mishra, Amrita ; Mishra, Arun K. ; Singh, Harpreet ; Kumar, Arvind

Unregulated cell division is one of the main causes of cancer. These cancerous cells negatively impact nearby healthy cells. Cancer can occur anywhere in the body. Normal cell division occurs when cells grow, reproduce, and divide as the body needs. As a normal cascade of cell growth and division, when the cells get damaged, they undergo death, and normal cells develop. However, sometimes, this process is not followed, and abnormal or damaged cells start to grow and multiply several times more than normal. This particular process may form the basis of cancer. There is a research gap in terms of identifying personalized synthetic anticancer therapy, which may be based on individual patient characteristics with an aim to optimize treatment efficacy and minimize adverse effects. While searching for new bioactive compounds, it has been observed that organic molecules with benzoic acid (BA) moiety possess significant anticancer potential. Several works of literature reported the use of BA from natural or synthetic sources to synthesize bioactive chemicals. It has been observed that several natural products also contain BA moiety, and the presence of this moiety is considered responsible for several important biological activities. Therefore, in order to chemically synthesize a wide variety of potent biologically active compounds, benzoic acid as a basic moiety in the form of a scaffold can be employed. Other synthetic compounds with BA scaffolds include furosemide, tetracaine, and bumetanide. The current article aims to focus on past and present work done on BA derivatives and to emphasize the molecular pathways involved in cancer treatment. The future prospects for research in this area are encouraging as researchers are striving to advance synthetic BA derivatives. This could possibly contribute to more efficient treatments and better results for cancer patients.

10 Jun 2025·Current Neuropharmacology

Mendelian Randomization Uncovers Potential Repurposable Medications for Neuropsychiatric Disorders

Article

Author: Liu, Shanling ; Li, Tingyu ; Gao, Linbo ; Xiao, Xiao ; Zhang, Lin ; Wang, Qiang

Background::

The growing prevalence of neuropsychiatric disorders is becoming a major health challenge. Traditional pharmacotherapies face limitations, making drug repurposing a valuable strategy. However, high-throughput screening approaches for these conditions are scarce.

Methods::

This study leveraged exposure data from the UK Biobank Neale Lab (N = 361,141) and outcome data from the FinnGen database (N = approximately 410,000) to employ Mendelian Randomization (MR) analyses and identify potential drug repurposing candidates for neuropsychiatric disorders. Sensitivity, Linkage Disequilibrium Score Correlation (LDSC), and Bayesian Colocalization (COLOC) analyses were conducted to ensure the robustness and reliability of our findings.

Results::

Using the IVW method, seven medications with negative causal associations with neuropsychiatric disorders were identified. Pregabalin, bumetanide, and prednisolone were associated with reduced anxiety (beta = -7.28, p = 4.00e-03; beta = -2.24, p = 6.00e-03; beta = -1.74, p = 2.84e-03). Vitamin B1 preparations showed an inverse association with dementia (beta = -2.47, p = 1.51e-03), Creon E/C granules with epilepsy (beta = -4.99, p = 3.91e-03), Pentasa SR 250 mg with multiple sclerosis (beta = -3.95, p = 3.83e-03), and zolmitriptan with stroke excluding subarachnoid hemorrhage (beta = -1.61, p = 6.00e-03). Sensitivity analyses confirmed these findings, whereas the LDSC and COLOC analyses provided additional support.

Conclusion::

MR-based drug repurposing is a promising approach for the treatment of neuropsychiatric disorders. Further validation is necessary to effectively integrate these medications into clinical practice.

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.

10

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

20 Nov 2024

·pharma.economictimes.indiatimes.com

Lupin Launches Bumetanide Injection in the U.S.

Mumbai: Generics drug maker Lupin Limited (Lupin) has announced the launch of its Bumetanide Injection in the United States. This generic medication is commonly prescribed to treat fluid retention and swelling associated with heart failure. The FDA-approved injection has been launched in two dosage forms: 1 mg/4 mL (0.25 mg/mL) Single-Dose Vials and 2.5 mg/10 mL (0.25 mg/mL) Multiple-Dose Vials. Bumetanide Injection USP is indicated for treating edema associated with congestive heart failure, hepatic and renal diseases, including nephrotic syndrome. It is a generic equivalent of Bumex Injection (0.25 mg/mL) by Validus Pharmaceuticals, LLC. According to Lupin, Bumetanide Injection had an estimated annual sale of $20 million in the U.S. as of September 2024. By Online Bureau ,

Drug Approval

100 Deals associated with Bumetanide

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External Link

KEGG	Wiki	ATC	Drug Bank
D00247	Bumetanide	C03CA02	DB00887

R&D Status

Approved

10 top approved records.

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

Developing

10 top R&D records.

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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	Adir SRL	24 Sep 2018
Autism Spectrum Disorder	Phase 3	Hungary	Institut de Recherches Intern Servier	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

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ATS2025	Not Applicable	Infant, Premature, Diseases	-	Furosemide	xmtwfnugzp(ugspwcciwr) = jleytxvyxp osotinoxzz (acseopbopd ) View more	-	16 May 2025
				Chlorothiazide	xmtwfnugzp(ugspwcciwr) = sqthpwrjyx osotinoxzz (acseopbopd ) View more
NCT03715153 (CTgov)	Phase 3	Autism Spectrum Disorder	211	S95008 (BUMETANIDE (S95008) Followed by Open-Label S95008)	ahkfmeuswz = xzdwgnvddo svkvhcdogf (cdplolnisi, qsubmybnht - kthgaepomw) View more	-	05 Jun 2023
				PLACEBO for week 0 - 26+S95008 (PLACEBO Followed by Open-Label S95008)	ahkfmeuswz = estjrsywxd svkvhcdogf (cdplolnisi, aydiptmqek - ookvcetyzl) View more
NCT03923933 (HEBE-CKD, Pubmed \| BMC Nephrol)	Phase 2	Chronic Kidney Diseases	34	Bumetanide plus chlorthalidone	gugilwcifb(unorzmidhh) = zuydyozdkb hayzxbaymv (iemuuxrgdd ) View more	-	20 Sep 2022
				Bumetanide plus placebo	gugilwcifb(unorzmidhh) = gxxuddagdo hayzxbaymv (iemuuxrgdd ) View more
EULAR2020	Not Applicable	Acute congestive heart failure	130	Intravenous Bumetanide	hskxvfbefi(ceaaeyjaml) = The use of IV bumetanide in patients hospitalized for AHF exacerbations is associated with a 7.17% yearly incidence of acute gout flares jfjfhwpflj (eifscsuums ) View more	-	03 Jun 2020
NCT03923933 (HEBE-CKD, CTgov)	Phase 2	Chronic Kidney Diseases	34	Bumetanide (Placebo)	sfnegwcnqv(exnfoadcng) = hmomsvlxnl okgtoownkz (pugqvrykye, 1.78) View more	-	10 Mar 2020
				Bumetanide+chlorthalidone (Treatment Grup)	sfnegwcnqv(exnfoadcng) = ulguuouist okgtoownkz (pugqvrykye, 3.29) View more
ANA2018	Not Applicable	Epilepsy, Benign Neonatal Add-on	-	Phenobarbital + Placebo	rqurpjblpq(bsxwezpjep) = p=0.02 njnrfiqbwj (kkwnbyonnj ) View more	Positive	05 Oct 2018
				Phenobarbital + Bumetanide 0.1mg/kg
ANA2015	Not Applicable	Seizures Adjuvant	-	Bumetanide 0.1mg/kg	hyvijggyck(mjwwfkzsrh) = comparable between subjects receiving bumetanide vs. phenobarbital alone ovgmicfnqy (nvwtcuwbyf ) View more	Positive	25 Sep 2015
				Bumetanide 0.2mg/kg
SFN2007	Not Applicable	Blood brain barrier defect	-	Bumetanide	pgpufeyxha(fcelgyxxjw) = vymybxrhre lovprjapwz (pcsqqbyqlf, 0.2)	-	04 Nov 2007
				Unlabeled bumetanide	pgpufeyxha(fcelgyxxjw) = wiltiydygn lovprjapwz (pcsqqbyqlf, 0.2)