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diflucortolone + isoconazole (Travocort)

✓ Approved

Johnson & Johnson Services, Inc. · NR3C1 · Small Molecule

What is diflucortolone + isoconazole?

diflucortolone + isoconazole is a small molecule developed by Johnson & Johnson Services, Inc.. It is approved for therapeutic indications via unknown.

Drug Profile

Brand NamesTravocort
CompanyJohnson & Johnson Services, Inc.
Drug ClassSmall Molecule
Molecular TargetNR3C1
RouteUnknown
StatusApproved

Mechanism of Action

Molecular Targets

diflucortolone + isoconazole acts on 1 molecular target:

NR3C1nuclear receptor subfamily 3 group C member 1 (GR, GCCR)
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Therapeutic Indications

diflucortolone + isoconazole is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Infections and infestationsWound infection fungal✓ Approved

Related Research Articles

PubMedMycoses2026-03-28

Diversity and Antifungal Susceptibility of Malassezia spp. Isolated From Brazilian Patients With Pityriasis Versicolor and Seborrheic Dermatitis.

de Pádua Oliveira Diogo Coelho DC, Possa Ana Paula AP, de Oliveira Santos Ana Raquel AR, Borges Ana Kleiber P AKP et al.

Malassezia spp. are part of the microbiota of many animals, including humans. However, under certain conditions, they can become pathogenic. Diseases associated with Malassezia include pityriasis versicolor (PV), seborrheic dermatitis (SD), Malassezia folliculitis, atopic dermatitis, psoriasis and fungemia. The present study aimed to describe the distribution of Malassezia species among Brazilian patients with PV and SD and to evaluate their susceptibility profiles to common antifungals. In this study, 102 clinical samples from patients with PV or SD were analysed. Clinical isolates of Malassezia were identified at the species level by sequencing the D1/D2 variable domains of the large subunit rRNA gene. Antifungal susceptibility was assessed using a modified microbroth dilution method adapted for the growth of Malassezia species. Among the 40 cultures obtained, six Malassezia species were identified. M. furfur was the most prevalent species (40.0%), followed by M. sympodialis (27.5%), M. globosa (15.0%), M. japonica (7.5%) and both M. yamatoensis and M. slooffiae (5.0% each). All isolates exhibited high MICs to caspofungin (> s16 μg/mL) and to isoconazole (MIC₅₀ = 8 μg/mL). Miconazole and clotrimazole showed MIC₅₀ values of 4 μg/mL, while itraconazole and ketoconazole were more active, with an MIC₅₀ of 0.125 μg/mL. This study showed the diversity of Malassezia species causing PV and SD in Brazil, including the rare species M. yamatoensis and M. japonica. These findings highlight the importance of antifungal susceptibility testing for these species to guide appropriate therapy.

PubMedArchiv der Pharmazie2026-02-19

Investigating the Telomerase Downregulatory Potential of Steroidal Drugs Following Pharmacophore-Based Rational; Computational and In Vitro Assessments.

Al-Karmalawy Ahmed A AA, Alabdali Aya Yaseen Mahmood AYM, Yousef Tarek A TA, Elmaaty Ayman Abo AA et al.

Inhibiting telomerase could lead to telomere shortening, chromosomal instability, and eventually cell death in cancer cells. The use of steroids in cancer treatment is significant; besides, drug repurposing can be a quicker and less expensive method of drug discovery than de novo drug development. Accordingly, diverse 280 steroidal drugs-following a pharmacophore-based rationale-were docked against telomerase receptor and compared to the co-crystallized inhibitor (BIBR1532) as a reference standard. Additionally, a molecular dynamics simulation for 200 ns was performed to confirm the docking results. Moreover, the six steroidal drugs (Betamethasone disproportionate, Beclomethasone disproportionate, Clobetasone butyrate, Desonide, diflucortolone valerate, and Hydrocortisone butyrate) were selected for further in vitro investigation. The antitumor activities of the six steroidal drugs against H1299, HuH7, HCT116, A549, MDA-MB-231, MCF7, PC3, MG63, and A375 cancer cell lines, besides OEC and HSF normal cell lines, were evaluated and compared to doxorubicin (Dox) as a reference positive standard. Especially, Clobetasone butyrate represented the better cytotoxicity against seven cancer cell lines (H1299, HuH7, HCT116, MDA-MB-231, PC3, MG63, and A375) with IC50 values of 12.56, 13.95, 12.00, 17.51, 11.69, 20.64, and 20.21 µg/mL, respectively. The outstanding antitumor six steroidal drugs were further investigated for their telomerase downregulatory potentials. All analogs recorded outstanding downregulatory results against telomerase, especially Clobetasone butyrate, Desonide, Diflucortolone valerate, and Hydrocortisone butyrate, where the protein expression for telomerase was downregulated up to 0.66-, 0.76-, 0.56-, and 0.73-fold change for clobetasone butyrate, desonide, diflucortolone valerate, and hydrocortisone butyrate, respectively, compared to the control.

PubMedPharmaceutics2025-12-31

Dermal Formulation Incorporating Isoconazole Nitrate Nanoparticles Offers High Absorption into Skin and Antimicrobial Effect Against Candida albicans.

Harada Ayako A, Tanaka Rie R, Otake Hiroko H, Yoshimura Masanori M et al.

Background: Isoconazole nitrate (ISN), an antifungal agent that inhibits ergosterol synthesis by blocking lanosterol 14α-demethylation, is widely used to treat candidiasis, and improving its skin retention and permeability can enhance its therapeutic efficacy. Therefore, we developed an ISN nanoparticle (ISN-NP) gel by wet-bead milling in the presence of methylcellulose (MC). Methods: These ISN nanoparticles were incorporated into a carboxypolymethylene hydrogel (Carbopol). The ISN concentration was measured using HPLC, and Wistar rats and Candida albicans were used to evaluate skin absorption and antifungal activity, respectively. Results: The ISN-NP gel exhibited a particle size distribution ranging from 60 to 220 nm, with the nanoparticles remaining stable. In addition, the ISN-NP gel demonstrated superior antifungal activity against Candida albicans. The Carbopol gel maintained appropriate viscosity and physical stability, and the ISN nanoparticles were released from the gel. Compared with microparticle-based gels (ISN-MP gels), the ISN-NP gel showed significantly enhanced drug release and transdermal permeation, with 1.54- and 1.7-fold increases, respectively. Conclusions: These findings indicate that incorporating ISN nanoparticles (nanocrystalline ISN) into a Carbopol-based gel matrix provides a promising strategy to enhance the topical delivery of this poorly water-soluble antifungal drug. Overall, this nanogel system represents a valuable platform for transdermal delivery in clinical applications.

PubMedPharmacoepidemiology and drug safety2025-12-06

Risk of Major Congenital Malformations Associated With First-Trimester Exposure to Topical Antifungal Medications: A Large Claims Database Study.

Kunitoki Tadaharu T, Sakai Takamasa T, Ishikawa Tomofumi T, Obara Ryo R et al.

Vulvovaginal candidiasis is highly prevalent among pregnant women, and its treatment is crucial. However, there is a lack of evidence regarding the risks on fetal outcomes associated with the use of antifungal medications during the first trimester of pregnancy in Japan. This study examined the association between topical antifungal use during the first trimester of pregnancy and the risk of major congenital malformations (MCMs) in infants using a Japanese database. We conducted a cohort study using a pregnancy cohort nested in the JMDC Claims Database from Japan. This dataset included 12 472 women who gave birth between 2010 and 2019 and were diagnosed with vulvovaginal candidiasis. Among the antifungal medications frequently dispensed or prescribed during the first trimester of pregnancy in this cohort, miconazole, oxiconazole, and isoconazole were assessed for the risk of MCMs, using clotrimazole, an antifungal medication with established safety during pregnancy, as a reference. Among 12 472 women, the overall prevalence of MCMs was 5.8% (n = 249) in women exposed to topical antifungals, while unexposed were 6.2% (n = 508). Using propensity score overlap weight (wOR), no increased risk of MCMs in infants was observed in pregnancies exposed to oxiconazole, isoconazole, and miconazole compared to clotrimazole (overlap weighted odds ratio [95% confidence interval]: 0.875 [0.599-1.277], 1.001 [0.611-1.640], and 0.887 [0.497-1.581], respectively). There was no significant association between topical antifungal use during the first trimester of pregnancy and the risk of MCMs in infants in Japan.

PubMedMethods in molecular biology (Clifton, N.J.)2025-11-22

Chiral Separation in Capillary Electrophoresis Using Cyclodextrins in Combination with Hydrophobic Deep Eutectic Solvents.

Zhang Qi Q, Xue Song S, Xu Yu Y

Hydrophobic deep eutectic solvents (HDESs) can serve as pseudostationary phases (PSPs) in capillary electrophoresis (CE). Their integration into conventional chiral CE methodologies, such as cyclodextrin-based electrokinetic chromatography, demonstrates a synergistic effect that notably enhances chiral separation efficiency. This chapter presents an example elucidating the enantioseparation of four azole antifungal drugs (tioconazole, isoconazole, miconazole, and econazole) employing carboxymethyl-β-cyclodextrin and the HDES methyltrioctylammonium chloride-octanoic acid.

PubMedChemico-biological interactions2025-06-21

Metallothioneins protect against isoconazole nitrate-induced antitumor activity through the maintenance of cellular redox homeostasis in hepatocellular carcinoma.

Mo Chun-Fen CF, Lei Ya-Ruo YR, Lin Jun J, Liu Yi Y et al.

Hepatocellular carcinoma (HCC) is the predominant histological subtype of primary liver cancer with high cancer-related mortality. Despite the development of clinical advances, the prognosis of HCC patients remains very poor, and beneficial therapeutic strategies are urgently needed. Isoconazole nitrate (ISN) is an azole derivative that exhibits potent and broad-spectrum fungistatic activities for the clinical therapy of dermatomycosis. However, the role and molecular mechanism underlying the anti-neoplastic activity of ISN against HCC remain unknown. Here, we provided the first evidence that ISN inhibited the proliferation and motility of HCC cells via the generation of excessive ROS. Transcriptome sequencing and subsequent Gene Ontology (GO) enrichment analysis revealed that the detoxification of inorganic compound (metallothionein (MT) family) was most enriched in response to ISN administration. Knockdown or inhibition of MTs synergistically improved the anti-HCC activity of ISN. Moreover, we confirmed that ISN facilitated the nuclear translocation of the nuclear factor erythroid 2-related factor 2 (NRF2) protein, which in turn increased the transcription of MT family genes by directly binding to the antioxidant response elements within the MT gene promoter. Taken together, our findings revealed a novel antitumor effect of ISN on HCC and delineated an important mechanism by which NRF2-mediated transcriptional activation of MTs protects HCC cells against ISN through the maintenance of cellular redox homeostasis and mitochondrial function. ISN combined with pharmacological inhibition of MTs may be a prospective and available therapeutic approach for the clinical treatment of HCC.

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