Delving into the Latest Updates on Naftifine Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Naftifine, Naftifine HCl, Naftifine Hydrochloride Cream

+ [13]

Target

SQLE

Mechanism

SQLE inhibitors(Squalene monooxygenase inhibitors)

Therapeutic Areas

Infectious DiseasesSkin and Musculoskeletal Diseases

Active Indication

Tinea corporistinea crurisTinea Pedis

Inactive Indication

Tinea Capitis

Originator Organization

Merz Pharma GmbH & Co. KGaA

Active Organization

Sebela Ireland Ltd.

Inactive Organization

GenZum Life Sciences LLC

Merz North America, Inc.Taro Pharmaceuticals U.S.A., Inc.

Drug Highest PhaseApproved

First Approval Date

US (29 Feb 1988),

Tinea corporistinea crurisTinea Pedis

Regulation-

Login to view timeline

Structure

Molecular FormulaC21H21N

InChIKeyOZGNYLLQHRPOBR-DHZHZOJOSA-N

CAS Registry65472-88-0

View All Structures (2)

In this study, An 8-mo-old female giant panda from the Chengdu Research Base of Giant Panda Breeding developed a hair loss area of 15 9 20 cm on the lumbosacral.Region for 4 days, accompanied with skin ulceration and pus discharging.It needed breastfeeding every night, but its mother and brother didn't reveal similar skin lesions.While the panda was under general anesthesia, veterinarians performed debridement, and collected secretion and hair samples from the lesions.The DNA was amplified by ITS1/4 primer-based PCR (ITS1:50-TCCGTAGGTGAACCTGCGG-30, ITS4: 50-TC CTCCGCTTATTGATATGC-30), the products were sequenced and BLASTed, and identified as Nannizzia gypsum (Accession Numbers: MN314834 and MN315461).Oral antifungal drug is not only convenient but also prevents pathogens from spreading from lesion site to other parts of the body.

01 Jul 2024·Nature Nanotechnology

Multimodal nanoimmunotherapy engages neutrophils to eliminate Staphylococcus aureus infections

Article

Author: Gao, Ruixuan ; Tong, Yao ; Xie, Ruosen ; Gong, Shaoqin ; Ye, Mingzhou ; Burger, Jacobus C ; Zhu, Min ; Yodsanit, Nisakorn ; Zhao, Yi ; Zhu, Jingcheng

The increasing prevalence of antimicrobial resistance in Staphylococcus aureus necessitates alternative therapeutic approaches. Neutrophils play a crucial role in the fight against S. aureus but suffer from deficiencies in function leading to increased infection. Here we report a nanoparticle-mediated immunotherapy aimed at potentiating neutrophils to eliminate S. aureus. The nanoparticles consist of naftifine, haemoglobin (Hb) and a red blood cell membrane coating. Naftifine disrupts staphyloxanthin biosynthesis, Hb reduces bacterial hydrogen sulfide levels and the red blood cell membrane modifies bacterial lipid composition. Collectively, the nanoparticles can sensitize S. aureus to host oxidant killing. Furthermore, in the infectious microenvironment, Hb triggers lipid peroxidation in S. aureus, promoting neutrophil chemotaxis. Oxygen supplied by Hb can also significantly enhance the bactericidal capability of the recruited neutrophils by restoring neutrophil respiratory burst via hypoxia relief. This multimodal nanoimmunotherapy demonstrates excellent therapeutic efficacy in treating antimicrobial-resistant S. aureus persisters, biofilms and S. aureus-induced infection in mice.

01 Jun 2024·Infectious Diseases and Therapy

Penetration Profiles of Four Topical Antifungals in Mycotic Human Toenails Quantified by Matrix-Assisted Laser Desorption Ionization–Fourier Transform Ion Cyclotron Resonance Imaging

Article

Author: Schaller, Martin ; Legouffe, Raphael ; Bonnel, David ; Tomezyk, Aurore ; Gumez, Clémence ; Joly-Tonetti, Nicolas ; Gaudin, Mathieu

INTRODUCTIONOnychomycosis is a fungal infection of the nails that can be challenging to treat. Here, matrix-assisted laser desorption ionization-Fourier transform ion cyclotron resonance (MALDI-FTICR) imaging was applied to the quantitative analysis of the penetration profile of the antifungal compound, amorolfine, in human mycotic toenails. The amorolfine profile was compared with those of three other antifungals, ciclopirox, naftifine, and tioconazole.METHODSAntifungal compounds (amorolfine 5% lacquer, ciclopirox 8% lacquer, naftifine 1% solution, and tioconazole 28% solution) were applied to mycotic nails (n = 42). Nail sections were prepared, and MALDI-FTICR analysis was performed on the sections at a spatial resolution of 70 μm to compare the distribution profiles. Based on the minimum inhibitory concentrations of the four test compounds needed to kill 90% (MIC₉₀) of the fungal organism, Trichophyton rubrum, the fold differences between the MIC₉₀ and the antifungal concentrations in the nails (termed the multiplicity of the MIC₉₀) were calculated for each.RESULTSThe penetration profiles indicated higher concentrations of amorolfine and ciclopirox in the deeper layers of the nails 3 h after treatment, compared with naftifine and tioconazole. The mean concentrations across the entire nail sections at 3 h were significantly different among the four antifungals: amorolfine, 2.46 mM; ciclopirox, 0.95 mM; naftifine, 0.63 mM; and tioconazole, 1.36 mM (p = 0.016; n = 8 per compound). The median multiplicity of the MIC₉₀ at 3 h was 191-fold for amorolfine, tenfold for ciclopirox, 52-fold for naftifine, and 208-fold for tioconazole.CONCLUSIONIn this study, MALDI-FTICR was successfully applied to the quantitative analysis of antifungal distribution in human mycotic nails. The findings suggest that amorolfine penetrates deeper layers of the nail and accumulates at concentrations far exceeding the MIC needed to exert antimycotic activity.

100 Deals associated with Naftifine Hydrochloride

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D00883	Naftifine Hydrochloride	D01AE22	DB00735

R&D Status

Approved

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Tinea corporis	US	Sebela Ireland Ltd.	29 Feb 1988
tinea cruris	US	Sebela Ireland Ltd.	29 Feb 1988
Tinea Pedis	US	Sebela Ireland Ltd.	29 Feb 1988

Developing

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
tinea cruris	Phase 1	PR	Merz North America, Inc.	01 Sep 2008
tinea cruris	Phase 1	US	Merz North America, Inc.	01 Sep 2008
Tinea Pedis	Phase 1	US	Merz North America, Inc.	01 Aug 2008
Tinea Capitis	Preclinical	-	Merz North America, Inc.	18 Jan 2016

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01289015 (NAFT-600, CTgov)	Phase 3	Tinea Pedis	855	Placebo	ewgujvjghl(wzsswbzxop) = mhpokgsxbf adrnfuloij (brswrlumwt, ywqoaecryr - unpqedetep) View more	-	26 Sep 2013
NCT00750139 (CTgov)	Phase 3	Tinea Pedis	707	Naftin (NAFT-500)	xssgtqupde(wpjpfgyfcd) = eusxkyhptu yfjhqixpqv (hdwerzccvl, emuzmkeqnp - dydjlxzppg) View more	-	29 Jan 2013
				Placebo (Placebo 2-weeks)	xssgtqupde(wpjpfgyfcd) = exwpbrvnze yfjhqixpqv (hdwerzccvl, sgmbdlkvqw - cmakromgyf)
NCT00750152 (CTgov)	Phase 3	tinea cruris	334	Naftin (NAFT-500)	xokcddrolg(szoqidqxqp) = utoesddqqz jpsdgrbweq (cvsbtnsnjo, xfzlyrefjb - iqhnvcxdzb) View more	-	13 Mar 2012
				Placebo (Placebo-2wks)	xokcddrolg(szoqidqxqp) = jjhpboeeqn jpsdgrbweq (cvsbtnsnjo, qgkkkdmbtf - subfjhvwax) View more
NCT00750139 (Pubmed)	Phase 3	Tinea Pedis	709	Naftifine HCl 2% cream (NAFT-2)	(tepaymqtkq) = pvgetebznb gxdhctaszg (hupclirarl ) View more	Positive	01 Nov 2011
				naftifine 2% cream (Two-week vehicle)	(tepaymqtkq) = racqesuyau gxdhctaszg (hupclirarl ) View more
NCT00750152 (Pubmed)	Phase 3	tinea cruris	334	Naftifine HCl 2% cream	(wpcqgfrery) = 1 per group lmmxxisnog (xalvjgnfqq ) View more	-	01 Oct 2011
				Vehicle