Urinary Concentrations and Antibacterial Activities of Nitroxoline at 250 Milligrams versus Trimethoprim at 200 Milligrams against Uropathogens in Healthy Volunteers

Wagenlehner, Florian M. E.; Münch, Fabian; Pilatz, Adrian; Bärmann, Birte; Weidner, W.; Wagenlehner, C.; Straubinger, Marion; Blenk, H.; Pfister, W.; Kresken, Michael; Naber, Kurt G.

doi:10.1128/aac.02147-13

Cited by 50 publications

(35 citation statements)

References 21 publications

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“…Nitroxoline possesses activity in vitro against a variety of microorganisms, including E. coli and other uropathogens (4,5). The mechanism of action is believed to be chelation of divalent cations required for bacterial RNA polymerase, leading to bacteriostatic activity in most cases (6,7).…”

mentioning

confidence: 99%

“…The standard daily dosage of nitroxoline is 250 mg administered every 8 h. The drug is heavily metabolized (Ͼ95%) into microbiologically active conjugated and nonconjugated derivatives. Urine recovery is Ͼ50% (30% microbiologically active) (7,8). At subinhibitory concentrations, the drug inhibits the adhesion of uropathogenic E. coli to uroepithelial cells and urinary catheters (9)(10)(11)).…”

mentioning

confidence: 99%

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In Vitro Activity of Nitroxoline against Escherichia coli Urine Isolates from Outpatient Departments in Germany

Kresken

Körber-Irrgang

2014

Antimicrob Agents Chemother

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confidence: 99%

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confidence: 99%

In Vitro Activity of Nitroxoline against Escherichia coli Urine Isolates from Outpatient Departments in Germany

Kresken

Körber-Irrgang

2014

Antimicrob Agents Chemother

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“…Due to its long time use in clinical practice, the pharmacokinetic and pharmacodynamic properties of nitroxoline are well established. It is administered orally, the standard dose of nitroxoline used in treatment of urinary tract infections being 250 mg per 8h (Mrhar et al, 1979;Wagenlehner et al, 2014;Naber et al, 2014;Wijma et al, 2018). After administration, complete and rapid adsorption of nitroxoline in the urinary tract was observed (Wijma et al, 2018;Mrhar et al, 1979).…”

Section: Nitroxoline In Clinical Practice -An Antimicrobial Agentmentioning

confidence: 99%

“…After administration, complete and rapid adsorption of nitroxoline in the urinary tract was observed (Wijma et al, 2018;Mrhar et al, 1979). Following adsorption, nitroxoline is excreted in the urine, either in unconjugated or, more commonly, in metabolized conjugated forms such as glucuronide or sulfate (Mrhar et al, 1979;Wagenlehner et al, 2014;Naber et al, 2014). The antibacterial urinary activity of nitroxoline can be observed soon after administration of a single dose.…”

Section: Nitroxoline In Clinical Practice -An Antimicrobial Agentmentioning

confidence: 99%

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Nitroxoline: repurposing its antimicrobial to antitumor application

Mitrović

Kos

2019

Acta Biochim Pol

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Cancer is a disease receiving an outstanding input of funds for basic and clinical research but is, nevertheless, still the second leading cause of death in the developed world and a great burden for health systems. New drugs are therefore needed to improve therapy, prolong survival of cancer patients and improve their quality of life. The high cost of development and clinical evaluation of new drugs limits the number that actually enter clinical use. To overcome this problem, repurposing of established drugs for new indications has gained a lot of interest, especially in the field of oncology. The well-established antimicrobial agent nitroxoline has been identified as a promising candidate to be repurposed for cancer treatment in several independent studies. Here we have reviewed a wide range of molecular mechanisms and tumor models involving nitroxoline in impairment of tumor progression. Furthermore, nitroxoline was used as a lead compound for structure-based chemical synthesis of new derivatives in order to improve its potency as well as selectivity for various targets. The potent antitumor activity of nitroxoline points strongly in the direction of its repurposing for cancer treatment and to the benefits of this strategy for patients and healthcare system.

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Synthesis of Novel Nitroxoline Analogs with Potent Cathepsin B Exopeptidase Inhibitory Activity

et al. 2020

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Nitroxoline, a well‐known antimicrobial agent, has been identified in several independent studies, and on different molecular targets, as a promising candidate to be repurposed for cancer treatment. One specific target of interest concerns cathepsin B, a lysosomal peptidase involved in the degradation of the extracellular matrix (ECM), leading to tumor invasion, metastasis and angiogenesis. However, dedicated optimization of the nitroxoline core is needed to actually deliver a nitroxoline‐based antitumor drug candidate. Within that context, 34 novel nitroxoline analogs were synthesized and evaluated for their relative cathepsin B inhibitory activity, their antiproliferative properties and their antimicrobial activity. More than twenty analogs were shown to exert a similar or even slightly higher cathepsin B inhibitory activity compared to nitroxoline. The implemented modifications of the nitroxoline scaffold and the resulting SAR information can form an eligible basis for further optimization toward more potent cathepsin B inhibitors in the quest for a clinical nitroxoline‐based antitumor agent.

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Urinary Concentrations and Antibacterial Activities of Nitroxoline at 250 Milligrams versus Trimethoprim at 200 Milligrams against Uropathogens in Healthy Volunteers

Cited by 50 publications

References 21 publications

In Vitro Activity of Nitroxoline against Escherichia coli Urine Isolates from Outpatient Departments in Germany

In Vitro Activity of Nitroxoline against Escherichia coli Urine Isolates from Outpatient Departments in Germany

Nitroxoline: repurposing its antimicrobial to antitumor application

Synthesis of Novel Nitroxoline Analogs with Potent Cathepsin B Exopeptidase Inhibitory Activity

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