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griseofulvin (Grisol)

✓ Approved

Transdermal · 小分子 · 小分子

什么是 griseofulvin？

griseofulvin 是一种小分子，由Transdermal研发。该药已获批，用于治疗相关适应症，给药途径：Topical。

药物档案

商品名Grisol
公司Transdermal
药物类别小分子
给药途径Topical
状态Approved
来源： ClinicalTrials.gov, Transdermal

治疗适应症

griseofulvin 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
InvestigationsDermatologic examination✓ Approved

相关研究文献

PubMedPesticide biochemistry and physiology2026-06-10

Antifungal products and associated mechanisms of action in the fight against Didymella segeticola responsible for tea and tobacco leaf spot diseases.

Bailly Christian C

The fungus Didymella segeticola is a major plant pathogen which causes significant damages to cultures and important economic losses. It is chiefly responsible for leaf spots and leaf blights of tea and tobacco species, and at least seven other plants. Effective measures are taken to detect early the disease and to limit its propagation and its impact on plant culture. However, novel fungicidal and fungistatic agents are needed to combat D. segeticola-induced leaf spot disease. The present review provides an analysis of the top-10 natural and synthetic products active against D. segeticola and the associated molecular targets and/or mechanism of action. The products include (1) ergosterol synthesis inhibitor jiahuangxianjunzuo, (2) protein translation inhibitor zhongshengmycin, (3) succinate dehydrogenase inhibitor boscalid, (4) nitrate reductase inhibitor kasugamycin, (5) β-tubulin binder griseofulvin, (6) DNA-binding agent carvacrol, (7) pyruvate dehydrogenase inhibitor phenazine-1-carboxamide, (8) threonine dehydratase inhibitor wuyiencin, (9) glucose regulator erlvejunzuo, and (10) phosphoenolpyruvate carboxykinase inhibitor ningnanmycin. The potency of the compounds varies significantly, with EC50 values from 0.5 nM (boscalid) to 100 μM (kasugamycin). The diversity of products and their molecular targets underline the multiplicity of approaches currently investigated to tackle leaf spot disease. On this basis, novel products and combinations can be proposed and the battle is going again.

PMID 42264763
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PubMedRSC advances2026-06-04

Design, synthesis, and biological evaluation of novel imidazole-morpholinone hybrids as broad-spectrum antimicrobial agents: molecular docking, DFT, and ADMET studies.

Dave Amrish J AJ, Joshi Sweta S SS, Maheta Jay B JB, Bhola Yogesh O YO et al.

A novel series of five imidazole-morpholinone hybrid compounds (10a-e) was designed, synthesised, and evaluated as broad-spectrum antimicrobial agents. The target molecules integrate a 5-formyl-1-butylimidazole core, a (3-oxomorpholin-4-yl)phenyl pharmacophore, and variable C5-aryl groups introduced via late-stage Suzuki-Miyaura cross-coupling, assembled through a concise five-step convergent route. All compounds were characterised by 1H/13C NMR, IR, and HR-ESI-MS. In vitro antimicrobial evaluation against four bacterial (S. aureus, S. pyogenes, E. coli, P. aeruginosa) and two fungal (C. albicans, A. niger) strains revealed compound 10c as the most potent analogue, matching chloramphenicol (MIC 7.81 µg mL-1) and griseofulvin (MIC 15.62 µg mL-1) reference standards. Molecular docking against S. aureus DNA gyrase (2XCT) and E. coli GyrB24 (7P2M), corroborated by DFT analysis (B3LYP/6-311++G(d,p)) and ADMET profiling, confirmed DNA gyrase inhibition as the primary mechanism and established 10c as a promising drug-like lead for further development.

PMID 42239570
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PubMedSkin health and disease2026-06-01

Clinical description and management of two terbinafine-resistant cases of tinea caused by Trichophyton indotineae from Finland.

Kantola Niina N, Varpuluoma Outi O, Aho-Laukkanen Elina E, Sinikumpu Suvi-Päivikki SP et al.

The first reports of terbinafine-resistant Trichophyton indotineae emerged from India in late 2017. Since then, superficial fungal infections caused by terbinafine-resistant T. indotineae have been increasingly reported in European countries as well. Some cases originate from travelling abroad, but local transmission also occurs. Currently, there are no internationally accepted guidelines for dealing with these cases. In some reports, itraconazole has been suggested as a drug of choice to treat these cases. Here, we report two cases in which griseofulvin was used successfully.

PMID 42222699
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PubMedChemical & pharmaceutical bulletin2026-05-28

Mechanisms Underlying the Rheological Changes of Drug Nanosuspensions in Wet Media Milling.

Ito Hiromitsu H, Ueda Keisuke K, Tsuruta Yumi Y, Kanda Mayumi M et al.

This study investigated the rheological behavior of nanosuspensions prepared by a wet media milling technique using various model drugs and hydroxypropyl methylcellulose (HPMC) as a dispersing agent. These nanosuspensions were classified into two groups based on their apparent fluidity: the first included fenofibrate, glimepiride, and phenytoin nanosuspensions, which maintained high fluidity and exhibited Newtonian-like behavior (yield stress <0.09 Pa in the Herschel-Bulkley model); and the second comprised griseofulvin, ketoconazole, and nevirapine nanosuspensions, which showed markedly reduced fluidity and non-Newtonian characteristics (yield stress >1.7 Pa in the Herschel-Bulkley model). Quantitative analysis of HPMC adsorption showed a tendency for drugs with high HPMC adsorption (11.2-12.4 wt%) to demonstrate high fluidity, while drugs with low HPMC adsorption (8.14-8.86 wt%) generally showed reduced fluidity. Notably, fenofibrate remained flowable despite relatively low HPMC adsorption, underscoring that the adsorption amount alone is not sufficient to explain fluidity and that adsorption mode and coverage may also contribute. Rheological analysis under heating conditions revealed that all nanosuspensions exhibited a temperature-dependent rheological transition at temperatures lower than those typically reported for pure HPMC solutions. A reduction in fluidity was observed when this transition occurred below room temperature. Together, these results indicate that drug-dependent fluidity loss in wet-milled nanosuspensions is associated with differences in interfacial HPMC association and temperature-dependent structuring, involving both hydrophobic nanoparticle network formation and HPMC molecular assembly.

PMID 42203449
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PubMedAmerican journal of clinical dermatology2026-05-28

Trichophyton indotineae: Rise, Diagnosis, Treatment, and Future Directions.

Cox Victoria R V VRV, Zuluaga Tatiana T, Gupta Aditya K AK, Lipner Shari R SR et al.

Dermatophytoses (synonymous with tinea) are superficial fungal infections of the skin, hair, and nails, typically caused by dermatophytes in the genera of Trichophyton and Microsporum. Dermatophyte infections are common and are estimated to affect roughly 20-25% of the global population. Historically, tinea infections have been treated with short courses of topical and/or oral antifungal therapies, however, the last decade has seen increasing antifungal treatment failure. Trichophyton (T.) indotineae (previously termed Trichophyton mentagrophytes-genotype VIII) has emerged as the primary species driving antifungal treatment failure worldwide. Clinically, T. indotineae infection may present as a typical dermatophyte infection, or atypically may mimic eczema, psoriasis, or other inflammatory dermatoses. Patients are often strikingly itchy and may be using topical steroid creams inappropriately in combination with antifungal and antibiotic agents. Terbinafine, once considered a first-line oral agent for tinea infections, often fails against T. indotineae, for which prolonged courses of itraconazole (often at higher than typical dermatophyte dosing) are now regarded as the treatment of choice. Fluconazole and griseofulvin demonstrate limited efficacy. Antifungal susceptibility testing may guide treatment choices but is not well established for dermatophytoses. Dermatologists should be aware of an approach to evaluating and treating refractory dermatophyte infections. Increased awareness among clinicians, including in infectious diseases, primary care, and the emergency room, is also important to facilitate early recognition, appropriate management, and timely referral. Dermatologists may play a key role in promoting antifungal stewardship and educating other clinician groups about emerging dermatophyte infections. In this review, we detail T. indotineae with a focus on clinical presentation, diagnostic confirmation, and treatment.

PMID 42207393
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PubMedJournal of pharmaceutical sciences2026-05-09

Predicting surfactant effects on drug permeation across hollow fiber membrane.

Patel Roshni P RP, Murray Jack D JD, Griffin Brendan T BT, Polli James E JE

The hollow fiber membrane (HFM) system is a potential combined dissolution/permeation in vitro tool to predict oral solid dosage form performance. However, drug permeability interpretation in the presence of surfactants remains mechanistically challenging, particularly when surfactants are present in both the donor and receiver compartments. A model denoted the reduced resistance model was recently employed to explain enhanced drug permeability when surfactant was present in the receiver. The objective was to re-examine previously published HFM flux of griseofulvin and meloxicam to consider the reduced resistance model as an additional contributing mechanism impacting drug flux. Published HFM data under all four surfactant experimental scenarios (i.e., no surfactant, surfactant in the receiver only, surfactant in the donor only, and surfactant in both donor and receiver) were re-analyzed. For the latter two most complex scenarios, there were six competing permeation models. For these two scenarios, the best predictive model for griseofulvin was the reduced resistance model for total donor drug concentration; meanwhile, for meloxicam, which was much less micelle incorporated, the best predictive model was the simple free drug permeation model. Overall, these findings demonstrate that drug permeation across HFM in surfactant-containing systems is governed by the interplay between donor-side micellar sequestration and receiver-side resistance reduction.

PMID 42102964
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