Delving into the Latest Updates on Terconazole with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Terconazole (USP/INN)

+ [4]

Target

fungal CYP51A1

Mechanism

fungal CYP51A1 inhibitors(Fungal CYP51A1 inhibitors)

Therapeutic Areas

Infectious DiseasesUrogenital Diseases

Active Indication

Candidiasis, Vulvovaginal

Inactive Indication

Infective vaginitis

Originator Organization

Johnson & Johnson

Active Organization

Shanghai Shyndec Pharmaceutical Co., Ltd.

Fougera Pharmaceuticals, Inc.Taro Pharmaceuticals U.S.A., Inc.

Inactive Organization

Curatek Pharmaceuticals, LLCJanssen-Cilag SA

Janssen Pharmaceuticals, Inc.

Drug Highest PhaseApproved

First Approval Date

US (31 Dec 1987),

Candidiasis, Vulvovaginal

Regulation-

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Structure

Molecular FormulaC26H31Cl2N5O3

InChIKeyBLSQLHNBWJLIBQ-OZXSUGGESA-N

CAS Registry67915-31-5

A Prospective, Open-Label, Comparative, Parallel Double-Arm, Multicentric Clinical Study to Evaluate the Efficacy of an Ovule With Triple Active Agents (Terconazole, Clindamycin, Fluocinolone) Administered Once Per Day for Three Days Versus an Ovule With Triple Active Agents (Metronidazole, Nystatin, Fluocinolone) Administered Once Per Day for Ten Days to Treat Secondary Vulvar/Vaginal Symptoms of Vaginitis/Infectious Vaginosis (Bacterial and/or Mycotic and/or Parasitic)

The purpose of this comparative study is to evaluate the efficacy of an ovule with triple active agents (terconazole, clindamycin and fluocinolone) versus another ovule with triple active agents (nystatin, metronidazole and fluocinolone) in the treatment of symptoms caused by the presence of vaginitis (inflammation of the vagina) or bacterial vaginosis (polymicrobial, nonspecific vaginitis associated with positive cultures of Gardnerella vaginalis and other anaerobic organisms and a decrease in lactobacilli).

Start Date01 Dec 2007

Sponsor / Collaborator

Janssen-Cilag SA

100 Clinical Results associated with Terconazole

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100 Translational Medicine associated with Terconazole

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100 Patents (Medical) associated with Terconazole

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118

Literatures (Medical) associated with Terconazole

01 Aug 2024·International Journal of Food Microbiology

Nobiletin enhances the antifungal activity of eugenol nanoemulsion against Penicillium italicum in both in vitro and in vivo settings

Article

Author: Guo, Long ; Liu, Yanchi ; Ye, Zimao ; Chen, Hongyang ; Zhou, Zhiqin ; Zhao, Lintao

The study prepared and used eugenol nanoemulsion loaded with nobiletin as fungistat to study its antifungal activity and potential mechanism of Penicillium italicum (P. italicum). The results showed that the minimum inhibitory concentration (MIC) of eugenol nanoemulsion loaded with nobiletin (EGN) was lower than that of pure eugenol nanoemulsion (EG), which were 160 μg/mL and 320 μg/mL, respectively. At the same time, the mycelial growth inhibition rate of EGN nanoemulsion (54.68 %) was also higher than that of EG nanoemulsion (9.92 %). This indicates that EGN nanoemulsion is more effective than EG nanoemulsion. Compared with EG nanoemulsion, the treatment of EGN nanoemulsion caused more serious damage to the cell structure of P. italicum. At the same time, in vitro inoculation experiments found that EGN nanoemulsion has better control and delay the growth and reproduction of P. italicum in citrus fruits. And the results reflected that EGN nanoemulsion may be considered as potential resouces of natural antiseptic to inhibit blue mold disease of citrus fruits, because it has good antifungal activity.

01 Aug 2024·International Journal for Parasitology: Drugs and Drug Resistance

Exploring therapeutic approaches against Naegleria fowleri infections through the COVID box

Article

Author: Lorenzo-Morales, Jacob ; Piñero, José E ; Chao-Pellicer, Javier ; Arberas-Jiménez, Iñigo ; Sifaoui, Ines

Naegleria fowleri, known as the brain-eating amoeba, is the pathogen that causes the primary amoebic meningoencephalitis (PAM), a severe neurodegenerative disease with a fatality rate exceeding 95%. Moreover, PAM cases commonly involved previous activities in warm freshwater bodies that allow amoebae-containing water through the nasal passages. Hence, awareness among healthcare professionals and the general public are the key to contribute to a higher and faster number of diagnoses worldwide. Current treatment options for PAM, such as amphotericin B and miltefosine, are limited by potential cytotoxic effects. In this context, the repurposing of existing compounds has emerged as a promising strategy. In this study, the evaluation of the COVID Box which contains 160 compounds demonstrated significant in vitro amoebicidal activity against two type strains of N. fowleri. From these compounds, terconazole, clemastine, ABT-239 and PD-144418 showed a higher selectivity against the parasite compared to the remaining products. In addition, programmed cell death assays were conducted with these four compounds, unveiling compatible metabolic events in treated amoebae. These compounds exhibited chromatin condensation and alterations in cell membrane permeability, indicating their potential to induce programmed cell death. Assessment of mitochondrial membrane potential disruption and a significant reduction in ATP production emphasized the impact of these compounds on the mitochondria, with the identification of increased ROS production underscoring their potential as effective treatment options. This study emphasizes the potential of the mentioned COVID Box compounds against N. fowleri, providing a path for enhanced PAM therapies.

26 Sep 2023·ACS omega

Expired Antifungal Drugs as Effective Corrosion Inhibitors for Carbon Steel in 1 M HCl Solution: Practical and Theoretical Approaches.

Article

Author: Motawea, Mohamed S ; Abdallah, Metwally ; Al-Bonayan, Ameena Mohsen ; Soliman, Kamal A ; Alfakeer, Majda ; Al-Juaid, Salih S ; Hawsawi, Hanaa ; Abd El Wanees, Salah

The anticorrosion potency of two expired antifungal drugs, namely, bifonazole (BIF) and terconazole (TER), for X65 carbon steel (X65CS) in a 1.0 M HCl solution was estimated using practical and computational measurements. The results of all methods applied showed that the percentage of anticorrosive efficacy (% AE) increased for expired BIF and TER and reduced at elevated temperatures. The % AE values of expired BIF and TER (375 mg L^-1) reached 92.08 and 94.19%, respectively, using polarization methods. The anticorrosion activities of the two expired drugs were interpreted based on their adsorption on the X65CS surface. The adsorption occurred according to the Langmuir isotherm model. The polarization results indicated that the expired drugs BIF and TER were mixed inhibitors. The impedance results showed a single capacitive loop, confirming that the charge transfer process controlled the corrosion of X65CS. Expired BIF and TER served as good pitting inhibitors by shifting the pitting potential to positive values. The thermodynamic functions of activation and adsorption were defined and explained. Density functional theory and Monte Carlo simulations were used to investigate the BIF and TER inhibitors. The theoretical parameters were consistent with the experimental results. The anticorrosion efficiencies determined using the various methods were in complete agreement.

1

News (Medical) associated with Terconazole

22 Mar 2006

·www.biospace.com

Perrigo Company Announces Approval For Terconazole Suppositories

ALLEGAN, Mich., March 21 /PRNewswire-FirstCall/ -- The Perrigo Company announced today that it has received approval from the U.S. Food and Drug Administration (FDA) to manufacture and market terconazole vaginal suppositories, 80 mg. The product is the AB-rated equivalent to Ortho-McNeil Pharmaceutical's Terazol(R) 3 Vaginal Suppositories, 80 mg, an anti-fungal medication indicated for the treatment of vaginal candida (yeast) infections. Perrigo is currently the only approved generic for this product. Shipments will begin immediately. According to NDC data, annual U.S. sales are approximately $8.5 million. The Perrigo Company is a leading global healthcare supplier and the world's largest manufacturer of over-the-counter (OTC) pharmaceutical and nutritional products for the store brand market. Store brand products are sold by food, drug, mass merchandise, dollar store and club store retailers under their own labels. The Company also develops, manufactures and markets prescription generic drugs, active pharmaceutical ingredients and consumer products, and operates manufacturing facilities in the United States, Israel, United Kingdom, Mexico and Germany. Visit Perrigo on the Internet ( ). Note: Certain statements in this press release are forward-looking statements within the meaning of Section 21E of the Securities Exchange Act of 1934, as amended, and are subject to the safe harbor created thereby. These statements relate to future events or the Company's future financial performance and involve known and unknown risks, uncertainties and other factors that may cause the actual results, levels of activity, performance or achievements of the Company or its industry to be materially different from those expressed or implied by any forward-looking statements. In some cases, forward-looking statements can be identified by terminology such as "may," "will," "could," "would," "should," "expect," "plan," "anticipate," "intend," "believe," "estimate," "predict," "potential" or other comparable terminology. Please see the "Cautionary Note Regarding Forward-Looking Statements" on pages 33 - 41 of the Company's Form 10-K for the year ended June 25, 2005, as well as the Company's subsequent filings with the Securities and Exchange Commission, for a discussion of certain important factors that relate to forward-looking statements contained in this press release. Although the Company believes that the expectations reflected in these forward-looking statements are reasonable, it can give no assurance that such expectations will prove to be correct. Unless otherwise required by applicable securities laws, the Company disclaims any intention or obligation to update or revise any forward-looking statements, whether as a result of new information, future events or otherwise. Perrigo Company CONTACT: Ernest J. Schenk, Manager, Investor Relations and Communicationof Perrigo Company, +1-269-673-9212, E-mail: eschenk@perrigo.com Web site:

Generic Drug

100 Deals associated with Terconazole

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External Link

KEGG	Wiki	ATC	Drug Bank
D00888	Terconazole	G01AG02	DB00251

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Candidiasis, Vulvovaginal	US	Taro Pharmaceuticals U.S.A., Inc.	06 Apr 2004

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Vaginal Diseases	Preclinical	US	Curatek Pharmaceuticals, LLC	01 Jun 2015
Infective vaginitis	Preclinical	MX	Janssen-Cilag SA	01 Dec 2007
Vaginitis	Preclinical	MX	Janssen-Cilag SA	01 Dec 2007

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02308007 (SMART GIVES, CTgov)	Phase 3	Infective vaginitis	475	Terconazole (Terconazole Vaginal Gel)	pwgewhqlxj(saznfteqxf) = ljhcsjshop yvopfsztlh (azgqfjomeu, jbsgsjkvia - fffwknuufu) View more	-	04 Aug 2020
				Metronidazole (Metronidazole Vaginal Gel)	pwgewhqlxj(saznfteqxf) = ngabljbdzd yvopfsztlh (azgqfjomeu, ikrminqaiv - zlgiojgbsb) View more
NCT02308046 (SMART GIVES, CTgov)	Phase 3	Infective vaginitis	212	Terconazole (Terconazole Vaginal Gel)	khjylqdyqf(ixawywvfbb) = ziisgqyvor qbvryxrwgy (ltajoqouxl, wlerucajmx - kaplsgjril) View more	-	27 Jul 2020
				Placebo (Gel Vehicle)	khjylqdyqf(ixawywvfbb) = eawvlobxri qbvryxrwgy (ltajoqouxl, bqojzualgs - yxmdnnbuix) View more
NCT01867164 (CTgov)	Phase 3	Infective vaginitis \| Vaginitis	160	Terconazole+Fluocinolone Acetonide+Gynoclin V (Gynoclin V (Terconazole+Clindamycin+Fluocinolone Acetonide))	gpocscqtfz(fxnntnqpqk) = bzodxfrhwa ugjwbhmfiq (qmmjlsfyfb, ovrgjvwdna - zsbmkmsoim) View more	-	24 Dec 2013
				Fluocinolone Acetonide+Nystatin+Metronidazole (Vagitrol V (Metronidazole+Fluocinolone Acetonide+Nystatin))	gpocscqtfz(fxnntnqpqk) = rvkjbwgnlr ugjwbhmfiq (qmmjlsfyfb, xipguewhfa - dqrdxpopam) View more
NCT00803738 (CTgov)	Not Applicable	Candidiasis, Vulvovaginal	572	Terconazole (Terconazole Vaginal Suppositories, 80 mg - Perrigo)	qrzyluxuda(coksilpebp) = ffcsjqwwpi ohqhjcqgnl (jebiddulgu, nxuwawplvo - hwyxlyezzy) View more	-	20 Feb 2013
				Terazol 3 - Terconazole (Terazol 3 - Terconazole Vaginal Suppositories 80 mg)	qrzyluxuda(coksilpebp) = dqntyizsjo ohqhjcqgnl (jebiddulgu, vlvugfuwkr - gvenriwzaw) View more