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

+ [22]

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 DiseasesDigestive System DisordersEndocrinology and Metabolic Disease+ [3]

Active Indication

Edema, CardiacHepatic ascitesOedema due to renal disease+ [9]

Inactive Indication

Autism Spectrum Disorder

Originator Organization

Daiichi Sankyo Co., Ltd.

Active Organization

Corstasis Therapeutics

Neurochlore

Guilin Pharmaceutical Co., Ltd.

+ [4]

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 Oct 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-

CTR20251712

/ CompletedNot Applicable

布美他尼片在健康研究参与者中的单剂量、随机、开放、交叉、两制剂、两周期餐后人体生物等效性试验

[Translation] A single-dose, randomized, open-label, crossover, two-dose, two-period fed human bioequivalence study of bumetanide tablets in healthy study participants

主要目的：以成都新恒创药业有限公司的布美他尼片（规格：1mg）为受试制剂，以Karo Pharma AB的布美他尼片（规格：1mg）为参比制剂，按生物等效性试验的有关规定，考察两制剂在健康人体内的生物等效性。次要目的：观察受试制剂和参比制剂在健康人体中的安全性。

[Translation]

Primary objective: Using bumetanide tablets (specification: 1 mg) of Chengdu Xinhengchuang Pharmaceutical Co., Ltd. as the test preparation and bumetanide tablets (specification: 1 mg) of Karo Pharma AB as the reference preparation, the bioequivalence of the two preparations in healthy humans was investigated according to the relevant provisions of the bioequivalence test. Secondary objective: To observe the safety of the test preparation and the reference preparation in healthy humans.

Start Date02 Jun 2025

Sponsor / Collaborator

Chengdu Sino-Strong Pharmaceutical 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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3,492

Literatures (Medical) associated with Bumetanide

01 Nov 2025·NEUROCHEMISTRY INTERNATIONAL

Imbalance of NKCC1/KCC2 contributes to the pathogenesis of primary focal hyperhidrosis

Article

Author: Yu, Feng-Qiang ; Lin, Nan-Long ; Zheng, Ru-Jie ; Li, Xu ; Zhang, Meng-Long ; Lin, Jian-Bo ; Qiu, Rui-Qin

BACKGROUND:

Primary focal hyperhidrosis (PFH) is characterized by excessive sweating in localized regions, significantly impacting patients' quality of life. The imbalance between sodium-potassium-chloride cotransporter 1 (NKCC1) and potassium-chloride cotransporter 2 (KCC2) disrupts chloride ion homeostasis, potentially contributing to the pathogenesis of PFH.

METHODS:

Sweat gland tissues from 76 healthy controls and 76 PFH patients were collected. Expression levels of NKCC1 and KCC2 were assessed using quantitative real-time PCR and Western blotting. Primary sweat gland cells isolated from PFH patients (PFH-SG) and controls (NPFH-SG) were subjected to NKCC1 knockdown via lentiviral shRNA transfection. A hyperhidrosis mouse model was induced by intraperitoneal injection of pilocarpine hydrochloride, and mice were pretreated with the NKCC1 inhibitor bumetanide for one week. Sweat secretion, serum acetylcholine, and chloride ion concentrations were measured. Expression levels of aquaporin 5 (AQP5), brain-derived neurotrophic factor (BDNF), and neuregulin-1 (NRG-1) proteins were analyzed.

RESULTS:

PFH tissues showed significantly elevated NKCC1 and decreased KCC2 expression compared to controls, correlating with lower sweat chloride levels. NKCC1 knockdown in PFH-SG cells reduced elevated AQP5 expression. In vivo, bumetanide treatment markedly reduced sweat secretion, lowered serum acetylcholine, and restored chloride ion concentrations in hyperhidrosis mice. Furthermore, bumetanide treatment significantly decreased expressions of BDNF and NRG-1 in sympathetic ganglia axons, indicating attenuation of sympathetic hyperactivity associated with hyperhidrosis. NKCC1/KCC2 imbalance contributes significantly to PFH pathology.

CONCLUSIONS:

Bumetanide effectively improves this imbalance, reducing excessive sweating and modulating related neurotransmitter signaling, offering potential therapeutic avenues for PFH.

01 Jul 2025·Current drug discovery technologies

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

Review

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

11

News (Medical) associated with Bumetanide

23 Jul 2025

·www.businesswire.com

Corstasis Therapeutics Announces Appointment of Sanjeev Narula to its Strategic Advisory Board

HENDERSON, Nev.--(BUSINESS WIRE)--Corstasis Therapeutics Inc. (www.corstasis.com), a late clinical-stage innovator of therapies that enhance options for the treatment of fluid overload in patients with cardiorenal and hepatic diseases, with the intent of lowering the overall cost of care, today announced that life science executive Sanjeev Narula has joined the company’s Strategic Advisory Board. Corstasis Therapeutics Announces Appointment of Sanjeev Narula to its Strategic Advisory Board “Sanjeev’s extensive strategic, financial and operational experience in large commercial-stage pharmaceutical companies make him a tremendous addition to our strategic advisory board,” said Benjamin Esque, Chairman and Chief Executive Officer of Corstasis Therapeutics Inc. “We expect Corstasis will benefit greatly from Sanjeev’s advice as we prepare our commercial strategy and pre-launch activities for Enbumyst™ ahead of its potential approval in September.” Mr. Narula most recently served as the Chief Financial Officer of Intra-Cellular Therapies, Inc., which he joined in 2024. During his tenure, he played a crucial role in expanding the commercial and operational capabilities of the company , which culminated in the successful acquisition of Intra-Cellular Therapies by Johnson & Johnson for $14.6 billion less than a year later. Before Intra-Cellular, Mr. Narula served as the first Chief Financial Officer of Viatris, which he joined in 2020 when the company was formed through the combination of Mylan and Upjohn, a division of Pfizer Inc. Prior to Viatris, he served as Chief Financial Officer at Upjohn, overseeing finance, procurement and business technology for all functions of the business, and held several other financial leadership positions during his 16 years at Pfizer. “I am excited to join Corstasis as a strategic advisor at this critical inflection point in the company’s journey, and look forward to contributing to its growth and capital strategy as it prepares for the potential launch of Enbumyst™,” said Mr. Narula. About Corstasis Therapeutics Corstasis Therapeutics is a late clinical-stage biopharmaceutical company whose mission is to develop and commercialize enhanced outpatient treatment options for patients with cardiorenal and hepatic diseases, with the intent of improving outcomes and reducing overall healthcare costs. Our lead product, Enbumyst™ bumetanide nasal spray, has been developed for the short-term treatment of edema associated with congestive heart failure, liver and kidney disease, with an anticipated PDUFA action date of September 14, 2025. For more information, please visit www.corstasis.com.

Executive ChangeAcquisition

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

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
Edema, Cardiac	United States	Corstasis Therapeutics	12 Sep 2025
Hepatic ascites	United States	Corstasis Therapeutics	12 Sep 2025
Oedema due to renal disease	United States	Corstasis Therapeutics	12 Sep 2025
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	Adir SRL	24 Sep 2018
Autism Spectrum Disorder	Phase 3	Italy	Institut de Recherches Intern Servier	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


NCT03715153 (CTgov)	Phase 3	Autism Spectrum Disorder	211	S95008 (BUMETANIDE (S95008) Followed by Open-Label S95008)	cectwxgygg = xwqkjgfaki tifbcfbqkz (lxxvitjyin, qsnvzjhiqq - zytunfkiyz) View more	-	05 Jun 2023
				PLACEBO for week 0 - 26+S95008 (PLACEBO Followed by Open-Label S95008)	cectwxgygg = nfupbzuzzs tifbcfbqkz (lxxvitjyin, bgynawvcdy - qxfecmltru) View more
NCT03923933 (HEBE-CKD, Pubmed \| BMC Nephrol)	Phase 2	Chronic Kidney Diseases	34	Bumetanide plus chlorthalidone	lxboualahj(mzzwlakquj) = sbvtvacemq rgjetosgfn (obgrdngxhq ) View more	-	20 Sep 2022
				Bumetanide plus placebo	lxboualahj(mzzwlakquj) = qwieactubc rgjetosgfn (obgrdngxhq ) View more
NCT03923933 (HEBE-CKD, CTgov)	Phase 2	Chronic Kidney Diseases	34	Bumetanide (Placebo)	jaoddjzakf(uxptlrnqkq) = eagykrdwmj mpszphzdkj (iqenmwnqxs, 1.78) View more	-	10 Mar 2020
				Bumetanide+chlorthalidone (Treatment Grup)	jaoddjzakf(uxptlrnqkq) = hwduwaowvc mpszphzdkj (iqenmwnqxs, 3.29) View more