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Enoxacin
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Since enoxacin has activity similar to or inferior to that of other fluoroquinolones, such as ciprofloxacin or norfloxacin, and has a relatively high incidence of side effects (especially if used in higher doses), there is little to recommend its use in preference to newer agents. Indeed, there have been no formal comparative studies of enoxacin efficacy in at least the past decade. Nevertheless, given its reasonable clinical activity against some infections and potentially lower cost in some geographical regions, enoxacin may be a suitable treatment choice in certain circumstances.
Emerging clinical investigational drugs for the treatment of amyotrophic lateral sclerosis
Published in Expert Opinion on Investigational Drugs, 2023
Loreto Martinez-Gonzalez, Ana Martinez
(NCT04840823) is an oral bactericidal fluoroquinolone agent present in the clinical setting for more than20 years that has been reported as the first small-molecule enhancer of microRNA (miRNA) maturation by increasing the activity of the key endoribonuclease DICER, essential for this process [24]. Downregulation of miRNA levels is a common molecular feature of ALS subjects [25]. Treatment with enoxacin improved miRNA maturation, mRNA metabolism and therefore protein homeostasis in ALS cellular models including the SOD1G93A mice [26]. On March 2015, enoxacin received an orphan designation by the EMA (EU/3/15/1459) for ALS treatment [27]. Currently, the trial REALS (Repurposed Enoxacion for the treatment of patients with ALS) will assess the safety of the drug enoxacin at specific dose levels in 36 adults with ALS.
Emerging therapeutic targets for osteoporosis
Published in Expert Opinion on Therapeutic Targets, 2020
Luigi Gennari, Daniela Merlotti, Alberto Falchetti, Cristina Eller Vainicher, Roberta Cosso, Iacopo Chiodini
The suppression of bone resorption by targeting the vacuolar H+-ATPases (V-ATPases) of the OC ruffled border might represent an alternative approach for the development of novel antiresorptive compounds. In fact, V-ATPases are essential for the acidification of resorption lacunae, mobilizing bone mineral content and allowing CK and other proteases to digest bone matrix proteins. However, since V-ATPases are ubiquitous proton pumps, there is the necessity to identify selective mechanisms directly targeting V-ATPases within the OC ruffled border, without affecting those that are required for everyday cell survival in other tissues. Some compounds targeting ruffled border V-ATPases as well as their OC-specific regulation or trafficking have been identified, but so far none of them has been translated to the clinic [63,64]. Enoxacin is a fluoroquinolone that is able to prevent V-ATPase insertion into the ruffled-border membrane, with potential advantages in terms of clinical development [64]. However, a long-term treatment with this agent (due to its antibiotic activity) might induce dysbacteriosis and gastrointestinal discomfort. Thus, a BP derivative of enoxacin (Bis-enoxacin) has been more recently developed, which targets more specifically the skeleton. In a preclinical study in ovariectomized (OVX) mice, bis-enoxacin prevented bone loss and improved the bone biomechanical properties better than zoledronate [65].