Delving into the Latest Updates on Ciclopirox olamine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Ciclopirox Olamine Cream, Ciclopirox Olamine Gream, Ciclopirox Olamine Vaginal Suppositories

+ [13]

Target-

Mechanism-

Therapeutic Areas

Infectious DiseasesSkin and Musculoskeletal DiseasesUrogenital Diseases+ [1]

Active Indication

Candidiasis, VulvovaginalDermatitis, SeborrheicNeoplasms

Inactive Indication

Tinea Pedis

Originator Organization

Medimetriks Pharmaceuticals, Inc.

Active Organization

Hubei Ke Tian Pharmaceutical Co. Ltd.

Louisiana State University Health Shreveport

Hubei Keyi Pharmaceutical Co., Ltd.

Inactive Organization

Perrigo Co. Plc

Drug Highest PhaseApproved

First Approval Date

CA (01 Jan 1985)

Regulation-

Login to view timeline

Structure

Molecular FormulaC14H24N2O3

InChIKeyMBRHNTMUYWQHMR-UHFFFAOYSA-N

CAS Registry41621-49-2

View All Structures (2)

AbstractThe emerging pathogen Trichophyton indotineae, often resistant to terbinafine (TRB), is known to cause severe dermatophytoses such as tinea corporis and tinea cruris. In order to achieve successful treatment for these infections, insight in the resistance profile of T. indotineae strains and rapid, reliable identification is necessary. In this research, a screening medium was tested on T. indotineae strains (n = 20) as an indication tool of TRB resistance. The obtained results were confirmed by antifungal susceptibility testing (AST) for TRB following the in vitro broth microdilution reference method. Additionally, AST was performed for eight other antifungal drugs: fluconazole, itraconazole, voriconazole, ketoconazole, griseofulvin, ciclopirox olamine, naftifine and amorolfine. Forty-five percent of the strains were confirmed to be resistant to terbinafine. The TRB resistant strains showed elevated minimal inhibitory concentration values for naftifine and amorolfine as well. DNA sequencing of the squalene epoxidase-encoding gene showed that TRB resistance was a consequence of missense point mutations in this gene, which led to amino acid substitutions F397L or L393F. MALDI-TOF MS was used as a quick, accurate identification tool for T. indotineae, as it can be challenging to distinguish it from closely related species such as Trichophyton mentagrophytes or Trichophyton interdigitale using morphological characteristics. While MALDI-TOF MS could reliably identify ≥ 95% of the T. indotineae strains (depending on the spectral library), it could not be used to successfully distinguish TRB susceptible from TRB resistant strains.

01 Mar 2024·European Journal of Pharmacology

Hydroxypyridone anti-fungals selectively induce myofibroblast apoptosis in an in vitro model of hypertrophic scars

Article

Author: Lapthorn, Alice Ruth ; Cellek, Selim ; Ilg, Marcus Maximillian ; Dziewulski, Peter

Hypertrophic scars are a common complication of burn injuries, yet there are no medications to prevent their formation. During scar formation, resident fibroblasts are transformed to myofibroblasts which become resistant to apoptosis. Previously, we have shown that hydroxypyridone anti-fungals can inhibit transformation of fibroblasts, isolated from hypertrophic scars, to myofibroblasts. This study aimed to investigate if these drugs can also target myofibroblast persistence. Primary human dermal fibroblasts, derived from burn scar tissue, were exposed to transforming growth factor beta-1 (TGF-β1) for 72 h to induce myofibroblast transformation. The cells were then incubated with three hydroxypyridone anti-fungals (ciclopirox, ciclopirox ethanolamine and piroctone olamine; 0.03-300 μM) for a further 72 h. The In-Cell ELISA method was utilised to quantify myofibroblast transformation by measuring alpha-smooth muscle actin (α-SMA) expression and DRAQ5 staining, to measure cell viability. TUNEL staining was utilised to assess if the drugs could induce apoptosis. When given to established myofibroblasts, the three hydroxypyridones did not reverse myofibroblast transformation, but instead elicited a concentration-dependent decrease in cell viability. TUNEL staining confirmed that the hydroxypyridone anti-fungals induced apoptosis in established myofibroblasts. This is the first study to show that hydroxypyridone anti-fungals are capable of inducing apoptosis in established myofibroblasts. Together with our previous results, we suggest that hydroxypyridone anti-fungals can prevent scar formation by preventing the formation of new myofibroblasts and by reducing the number of existing myofibroblasts.

100 Deals associated with Ciclopirox olamine

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D01364	Ciclopirox olamine	D01AE14 G01AX12	DBSALT001147

R&D Status

Approved

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Candidiasis, Vulvovaginal	CN	Hubei Ke Tian Pharmaceutical Co. Ltd.	01 Jan 1989
Dermatitis, Seborrheic	CN	Hubei Keyi Pharmaceutical Co., Ltd.	01 Jan 1989

Developing

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Neoplasms	Discovery	US	Louisiana State University Health Shreveport	15 Apr 2012
Tinea Pedis	Discovery	-	Perrigo Co. Plc	01 Dec 2003

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASN2019	Not Applicable	Polycystic Kidney Diseases	-	Ciclopirox-Olamine	gcfymgcyen(zlgrcteefx) = tcssvordha jqtcslatba (chkhsmxxpu ) View more	Positive	05 Nov 2019
NCT00804193 (CTgov)	Not Applicable	Tinea Pedis	553	Ciclopirox Olamine Topical Suspension (Test Product)	hvdubkrmvr(mirbvlfpbn) = kiuuskzqfv aqgzcdxfom (sazbqsfxtf, rrhyznjylr - qmufvtpwks) View more	-	17 Dec 2012
				Ciclopirox Topical Suspension 0.77%-Reference Product (Reference Product)	hvdubkrmvr(mirbvlfpbn) = yvrwvagkls aqgzcdxfom (sazbqsfxtf, zhohdixngf - dtddkgocvp) View more
NCT00802672 (CTgov)	Phase 3	Tinea Pedis	561	Ciclopirox Olamine Cream (Test Product)	frrjcrzjab(uzrmfjtxoo) = lupjpbbxfp xlpmtdnshc (ftemmaplxu, mffkqoeoqo - xrmwnhqvsn) View more	-	19 Jun 2012
				Loprox Cream 0.77% (Reference Product)	frrjcrzjab(uzrmfjtxoo) = dcnvteiyfs xlpmtdnshc (ftemmaplxu, cuptcxlkxy - yhjidrpbmi) View more