Delving into the Latest Updates on Nitrofurantoin with Synapse

Overview

Basic Info

SummaryNitrofurantoin, an antibiotic medication approved in 1953 by Procter & Gamble, is used to treat uncomplicated lower urinary tract infections.Nitrofurantoin works by using multiple mechanisms to achieve an antimicrobial effect, including uptake by bacterial intracellular flavoproteins and reduction to reactive intermediates that bind to bacterial ribosomes and inhibit DNA and RNA synthesis, cell wall protein synthesis, and other metabolic enzymes. Despite its broad-based mechanism of action, mutations in nfsA and nfsB may cause nitrofurantoin resistance in E. coli. Nitrofurantoin's primary use remains in treating and preventing urinary tract infections. However, common side effects such as nausea, loss of appetite, diarrhea, and headaches may occur. It is important to complete the full course of treatment as prescribed by a healthcare provider to ensure the infection is fully cleared.

Drug Type

Small molecule drug

Synonyms

1-((5-nitro-2-furanyl)methylene)amino-2,4-imidazolidenedione, 1-((5-nitrofurfurylidene)amino)hydantoin, 5-Nitrofurantoin

+ [18]

Target

DNA

Action

inhibitors

Mechanism

DNA inhibitors(DNA inhibitors)

Therapeutic Areas

Infectious DiseasesUrogenital Diseases

Active Indication

CystitisProstatitisPyelitis+ [1]

Inactive Indication

Acute cystitis

Originator Organization

Procter & Gamble Co.

Active Organization

Nova Pharmaceuticals Australasia Pty Ltd.

Almatica Pharma LLC

Casper Pharma LLC

+ [1]

Inactive Organization

Procter & Gamble, Inc.Procter & Gamble Pharmaceuticals, Inc.

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (06 Feb 1953),

Urinary Tract Infections

Regulation-

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Structure/Sequence

Molecular FormulaC8H6N4O5

InChIKeyNXFQHRVNIOXGAQ-UHFFFAOYSA-N

CAS Registry67-20-9

The escalating threat of antibiotic resistance, fueled by drug misuse, coupled with the health risks posed by vitamin deficiencies, underscores a critical demand for efficient detection technologies. Herein, a novel V-shaped organic compound containing 2,1,3-benzothiadiazole (BTD) group, 4,4'-(benzo[c][1,2,5]thiadiazol-5,6-diyl)dibenzoic acid (H₂BTDA), has been designed and synthesized. Further, a Cd(II) metal-organic framework (MOF) has been successfully prepared with the formula {[Cd(BTDA)]∙0.5DMF}_n, (JXUST-61, where JXUST denotes Jiangxi University of Science and Technology). Interestingly, JXUST-61 exhibits a three-dimensional (4,8)-connected with alb-4,8-Fddd topological structure, which shows solvent-stability after soaking in organic solvents for at least 24 h. JXUST-61 is capable of rapidly detecting nitrofuran antibiotics (furacilin, nitrofurantoin, and furazolidone) via a fluorescence quenching effect with remarkably low detection limits (0.208, 0.265, and 0.168 μM, respectively). Simultaneously, it demonstrates outstanding fluorescence recognition for VB1 and VB9, achieving the detection limits of 0.189 and 0.291 μM, respectively. More importantly, it has good biocompatibility and low cytotoxicity to sense VB1 and VB9 in living cells. Therefore, JXUST-61 functions as a highly efficient multi-functional fluorescent probe, offering a novel strategy for the real-time monitoring of antibiotic residues and the diagnosis of vitamin deficiency-related health conditions.

01 Sep 2026·TOXICOLOGY

Towards a novel toxicity prediction pipeline, combining PBPK models and mechanistic cellular adversity models

Article

Author: Beltman, Joost B ; Sharma, Raju P ; Zickgraf, Franziska M ; Burgers, Elsje J ; Leist, Marcel ; Vogel, Sem ; Schildknecht, Stefan ; Bouwman, Peter ; van de Water, Bob ; Wijaya, Lukas S ; Danilyuk, Tamara Y

There is a strong need for animal-free methods that properly predict drug adversity. Especially drug-induced liver injury (DILI) is a common adverse effect that is difficult to predict with current methodology. In this study, we developed a data-driven computational adversity model for predicting the relative number of apoptotic cells in vitro, based on stress pathway activity invoked by exposure of liver cells to nitrofurantoin, diclofenac, and ketoconazole. Next, we adapted this adversity model to represent an in vivo situation and developed physiologically-based pharmacokinetic (PBPK) models for all three drugs to simulate the concentration of the drugs in the liver of humans and rats. Coupling the PBPK, stress pathway and adversity models generated quantitative systems toxicology models for rats and humans at clinically-relevant doses. For all three drugs, low levels of toxicity were predicted in rats and humans, which is consistent with in vivo observations. A detailed analysis of modifying factors (sex, age) showed that the amount of apoptotic cells is expected to increase for females and elderly people compared to males. Coupling the different models generated a novel modelling pipeline that is an important step towards in silico DILI predictions.

01 Sep 2026·MICROBIOLOGICAL RESEARCH

Beyond dormancy: Active DNA repair and protein synthesis drive antibiotic tolerance and enable synergistic eradication

Article

Author: Heng, Heng ; Zheng, Jiaqi ; Tang, Yang ; Ye, Lianwei ; Wan, Yingkun ; Chen, Sheng ; Chan, Edward Wai-Chi

The unresponsiveness of bacterial tolerant cells to antibiotics has been attributed to physiological dormancy triggered by environmental stresses. Interestingly, after a 24 - hour treatment, the tolerant cells became susceptible to ciprofloxacin and nitrofurantoin, which target DNA, as well as gentamicin, which targets protein synthesis, with distinct combinational effects. However, they remained resistant to ampicillin, which targets the cell wall. The mechanism study revealed that the activities of protein synthesis and DNA repair in tolerant bacteria formed during nutrient starvation remained at a high level and only gradually decreased during six days of starvation. Meanwhile, the reduction in energy production (ATP level), antioxidant defense (ROS level), and efflux functions led to an increased susceptibility of the bacterial tolerant subpopulation to antibiotics. These findings confirm that bacterial tolerant cells remain physiologically active, and inhibiting protein synthesis and DNA repair presents promising opportunities for combating bacterial tolerance with existing antibiotics.

40

News (Medical) associated with Nitrofurantoin

12 Feb 2026

·hamletbiopharma.com

PRESS RELEASE – Lund, February 12th, 2026 – Nature Microbiology publishes the paper ‘’Targeted innate immune inhibition therapy compared with antibiotics for recurrent acute cystitis: a randomized, open-label phase 2 trial.’’

This groundbreaking study introduces an entirely new approach to managing recurrent urinary tract infections. Instead of killing the bacteria, the treatment focuses on targeting and calming the disease response. Clinical efficacy of this approach is demonstrated in this study, showing effects comparable to standard antibiotic therapy. This discovery could also mark a major breakthrough in the fight against antibiotic resistance and the future treatment of infections. This non-antibiotic treatment approach is conceptually novel and the study is the first to demonstrate clinical effects comparable to antibiotics in this patient group, explaining why a leading international journal such as Nature Microbiology has agreed to publish https://www-nature-com.libproxy1.nus.edu.sg/articles/s41564-026-02262-1. Scientists collaborating with Hamlet BioPharma have also developed several new therapeutics agaist bacterial infections with potent effects. These new discoveries suggest a transformative shift in infectious disease management, built on the discovery of molecules that target the disease response of the host rather than the bacteria. These treatments are promising tools in the fight against antibiotic resistance and essential to innovate the treatment of bacterial infections. The study compared the treatment efficacy of the IL-1 receptor antagonist anakinra to the antibiotic nitrofurantoin, showing similar efficacy of both treatment approaches in patients with recurrent acute cystitis. Female patients with a documented history of recurrent cystitis and a current acute cystitis episode, were randomized to treatment with anakinra or nitrofurantoin for five days. Primary and secondary efficacy end points were reached, defined as the reduction in typical symptoms, measured by the acute cystitis symptom score (day 5), longitudinal symptom scores, recurrence rates, quality of life, and microbiology and gene expression analysis at follow-up on days 15, 30 and at six months. Symptom scores were decreased in the anakinra (P<0.001), and nitrofurantoin (P<0.001) arms after five days and remained low after 15, 30 days and 6 months. Recurrences were less frequent after 6 months in both treatment groups compared to the 6-month pre-enrolment history (P<0.001 for anakinra and P=0.004 for nitrofurantoin) and the quality of life was increased. Immune gene expression was inhibited in the anakinra treated patients but not in the nitrofurantoin group and the microbial burden was affected in both groups. The main goal of antibiotic therapy is to remove bacteria and end the disease process that they provoke. Since the discovery of antibiotics, bacterial infections have been treated with great success, and treatment still relies on antibiotics with clinical efficacy. The rise in antibiotic-resistance limits the therapeutic options, increasing mortality rates and the need for advanced medical care. Resistance to antibacterial drugs is particularly in common infections such as urinary tract infections (UTIs), highlighting the need for alternative therapeutic strategies. Hamlet BioPharma’s phase 2 clinical trial in patients with recurrent acute cystitis offers a new solution to addressing this problem. ‘’This study was based on extensive molecular studies and preclinial treatment data from infection models, confirming the potential of this approach. The extensive data sets and advanced technology are unique, internationally, says Ines Ambite, PhD, Lund University. ‘’These findings create optimism in times when antibitotic resistance is a very dark cloud above all of our heads. The new treatments are also effective against antibiotic resistant bacteria’’, says Catharina Svanborg, Professor at Lund Univeristy, Founder and chairman of Hamlet BioPharma. ‘’Clinical studies like this are essential to validate new treatment concepts and drive the development towards the market. This next generation translational trial design is very important to further develop the field of UTI research,’’ says Florian Wagenlehner, Professor at the University of Giessen, Germany. Links to the publication: https://www-nature-com.libproxy1.nus.edu.sg/articles/s41564-026-02262-1 https://doi-org.libproxy1.nus.edu.sg/10.1038/s41564-026-02262-1ture=share For more information, please contact: Ines Ambite, PhD, +46-762 08 89 58 Ines.Ambite@med.lu.se Catharina Svanborg, Chair of the Board, Hamlet BioPharma, +46-709 42 65 49 catharina.svanborg@hamletpharma.com

03 Sep 2025

·pmlive.com

UK’s first new type of antibiotic for UTIs in nearly 30 years approved by MHRA

Gepotidacin (Blujepa) has been approved by the Medicines and Healthcare products Regulatory Agency (MHRA) for use by women and girls from 12 years of age, with a weight of at least 40kg. The new antibiotic is an oral pill that can be used to treat uncomplicated urinary tract infections (UTIs). It is effective against many drug-resistant infections, including E. coli, using an active ingredient that targets and blocks two enzymes that bacteria need to replicate and multiply. This type of UTI affects around 50% of women in the UK and is the most common bacterial infection in women. With drug-resistant bacteria increasing, new treatment options are critical in preventing treatment failure and complications, including sepsis or permanent kidney damage. Julian Beach, MHRA Interim Executive Director, Healthcare Quality and Access, said: “As the first new type of oral antibiotic to treat uncomplicated UTIs to be approved in nearly three decades, gepotidacin provides a new treatment option for women facing urinary tract infections that can severely impact daily life. “The antibiotic’s targeted mechanism of action makes it more difficult for bacteria to develop treatment resistance – a crucial factor as drug-resistant bacteria are increasingly on the rise globally.” Results from two multicentre, randomised, active-controlled phase 3 trials were used as evidence to support the new drug approval. In the trials, 1,572 participants were given gepotidacin and 1,564 received nitrofurantoin, the current treatment for uncomplicated UTIs. In both trials, gepotidacin was shown to be at least as effective as nitrofurantoin, with consistent results across patient groups, including those with drug-resistant bacteria and recurrent infections.

Phase 3Clinical ResultDrug ApprovalQualified Infectious Disease Product

27 Mar 2025

·pmlive.com

GSK’s antibiotic Blujepa granted FDA approval to treat urinary tract infections

GSK’s oral antibiotic Blujepa (gepotidacin) has been approved by the US Food and Drug Administration (FDA) to treat uncomplicated urinary tract infections (uUTIs). The drug, which is the first in a new class of oral antibiotics for uUTIs in nearly 30 years, has been specifically authorised to treat female adults and adolescents aged 12 years and older and weighing at least 40kg with uUTIs caused by E. coli, Klebsiella pneumoniae, Citrobacter freundii complex, Staphylococcus saprophyticus and Enterococcus faecalis. More than half of women are affected by UTIs, common infections that affect the urinary tract, in their lifetime, and approximately 30% experience at least one recurrent episode. Most uUTIs respond well to treatment. However, the number of uUTIs caused by drug-resistant bacteria is increasing, underscoring the need for new treatment options. “For many, uUTIs can be a burden that severely impacts daily life,” said Thomas Hooton, professor of clinical medicine, University of Miami School of Medicine. “With an increasing number of patients experiencing recurrent infections, there remains a clear need for continued research of antimicrobials to help address ongoing patient challenges and the strain on healthcare systems.” The FDA’s decision on Blujepa was supported by positive results from the late-stage EAGLE-2 and EAGLE-3 trials, which evaluated the drug against standard-of-care nitrofurantoin in female adults and adolescents with a confirmed uUTI for five days. In EAGLE-2, Blujepa demonstrated non-inferiority to nitrofurantoin, with therapeutic success occurring in 50.6% and 47% of patients, respectively. Meanwhile, in EAGLE-3, Blujepa showed statistically significant superiority versus nitrofurantoin, with therapeutics success occurring in 58.5% of patients receiving GSK’s drug, compared to 43.6% of those being treated with standard-of-care. The safety and tolerability profile of Blujepa in both trials was also shown to be consistent with previous trials of the drug. GSK’s chief scientific officer, Tony Wood, described the approval as “a crucial milestone with uUTIs among the most common infections in women”. “We are proud to have developed Blujepa, the first in a new class of oral antibiotics for uUTIs in nearly three decades, and to bring another option to patients given recurrent infections and rising rates of resistance to existing treatments,” he said.

Drug ApprovalClinical ResultPhase 3Qualified Infectious Disease Product

100 Deals associated with Nitrofurantoin

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External Link

KEGG	Wiki	ATC	Drug Bank
D00439	Nitrofurantoin	J01XE01	DB00698

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Cystitis	Australia	Nova Pharmaceuticals Australasia Pty Ltd.	09 Apr 2026
Prostatitis	Australia	Nova Pharmaceuticals Australasia Pty Ltd.	09 Apr 2026
Pyelitis	Australia	Nova Pharmaceuticals Australasia Pty Ltd.	09 Apr 2026
Urinary Tract Infections	United States	Procter & Gamble Pharmaceuticals, Inc.	06 Feb 1953

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acute cystitis	Phase 2	United States	Procter & Gamble, Inc.	01 Jan 2002

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03287089 (Pubmed \| Female Pelvic Med Reconstr Surg)	Phase 4	-	164	Nitrofurantoin	sbaqpyqkhv(fiqmmqltgh) = tzqhluqnmq tyccjpoqwr (fncnkikabe )	Negative	01 Mar 2021
				Placebo	sbaqpyqkhv(fiqmmqltgh) = xjmlfljadz tyccjpoqwr (fncnkikabe )
NCT03287089 (NAUTICA, CTgov)	Phase 4	Catheter-Related Infections	164	Nitrofurantoin 100 MG (Nitrofurantoin)	zsehymdijk = nnwesuljny qnzkopnqoq (zmhdzkpmxt, ayprhahiyz - khtegclwux) View more	-	09 Jun 2020
				Placebo Oral Tablet (Placebo)	zsehymdijk = tvffgkgmxo qnzkopnqoq (zmhdzkpmxt, iacpfuaipp - cnlklqbagp) View more
NCT02384200 (CTgov)	Phase 4	Kidney Calculi \| Urinary Tract Infections	86	nitrofurantoin monohydrate+gentamicin+ceftriaxone+ampicillin+Vancomycin (Antibiotic)	pafuvvckfv = exahngpugc ceesqlecly (qkxqbgelrr, lgxopfkbvr - jlujeuenzj) View more	-	22 Aug 2019
				gentamicin+ceftriaxone+ampicillin+Vancomycin (No Preoperative Oral Antibiotics)	pafuvvckfv = utaptjrvxz ceesqlecly (qkxqbgelrr, ybkskfqgpl - fcskhnybys) View more
NCT02727322 (CTgov)	Phase 4	Pelvic Organ Prolapse \| Acute retention of urine	154	Nitrofurantoin (Nitrofurantoin)	ogczbbyaew = cyltnzjlow boxapwpjgb (nxncgdrtep, hlsovskwpy - fncgbxdqke) View more	-	20 May 2019
				Placebo (Placebo)	ogczbbyaew = sdieogkffb boxapwpjgb (nxncgdrtep, zfaletewtb - vaeymyuboo) View more
NCT01749605 (CTgov)	Phase 4	Cystitis	35	Nitrofurantoin monohydrate (Nitrofurantoin 100 mg)	miqmymfmqu = ddffshaeoc yxmmsbbiwe (jqhofjbdoq, csganlrysn - dorprbyakr) View more	-	27 Apr 2017
				ciprofloxacin (Ciprofloxacin 250 mg)	miqmymfmqu = yeceutwbcr yxmmsbbiwe (jqhofjbdoq, lunfrjiptt - huggwwgmph) View more
NCT00734968 (CTgov)	Phase 4	Urinary Tract Infections \| Urinary Incontinence, Stress	161	Nitrofurantoin (Treatment)	zazaluekzp = zzidkwvnvo awlrrpihzb (afjucnhulj, sychwazbuv - oyhfmzybqn) View more	-	11 Oct 2016
				Placebo (Placebo)	zazaluekzp = qxqjzygjwh awlrrpihzb (afjucnhulj, tmsrnuazjn - ecrflxlvku) View more
NCT00678041 (APPIC, CTgov)	Not Applicable	Urinary Incontinence \| Urinary Tract Infections \| Pelvic Organ Prolapse	10	Nitrofurantoin (Arm 1: Nitrofurantoin Group)	ccwdumaqyu(tsqointrqg) = imqfhzfzed cwoesgcylh (lmdxrnddby, dcfkgqkpyf - sytwsowfds) View more	-	02 Aug 2016
				Placebo (Arm 2: Placebo Group)	ccwdumaqyu(tsqointrqg) = yjbnhmgail cwoesgcylh (lmdxrnddby, ywvqvngvwz - izazfmjmnd) View more
NCT00734968 (Pubmed \| Female Pelvic Med Reconstr Surg)	Phase 4	Urinary Tract Infections \| Urinary Incontinence, Stress	149	Placebo	oqutzpoecx(ffhaapycyn) = fazlvslzgi fbjfvmlmma (qdekpfhpal )	Positive	01 May 2013
				Nitrofurantoin	oqutzpoecx(ffhaapycyn) = tjtjrseyxb fbjfvmlmma (qdekpfhpal )
Pubmed \| Urol Res	Not Applicable	Urosepsis	205	Nitrofurantoin 100 mg bid for 7 days	iskdufcmwq(hpeeuntbpv) = wsontmxwhn lznjywgceo (xofywnxmjd ) View more	-	01 Feb 2012
Pubmed \| Urology	Early Phase 1	Respiratory Tract Infections \| Urosepsis	101	Nitrofurantoin prophylaxis	ghleddmtas(zrqwpfojvk) = ujdpqlgoii ltkphdwgeg (zoikuchqio ) View more	Positive	01 Jan 2011