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GR

griseofulvin (Grisol)

✓ Approved

Transdermal · Small Molecule · Small Molecule

What is griseofulvin?

griseofulvin is a small molecule developed by Transdermal. It is approved for therapeutic indications via topical.

Drug Profile

Brand NamesGrisol
CompanyTransdermal
Drug ClassSmall Molecule
RouteTopical
StatusApproved

Therapeutic Indications

griseofulvin is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
InvestigationsDermatologic examination✓ Approved

Related Research Articles

PubMedJournal der Deutschen Dermatologischen Gesellschaft = Journal of the German Society of Dermatology : JDDG2026-07-14

Consensus-based Guideline on tinea capitis.

Mayser Peter P, Abeck Dietrich D, Bosshard Philipp P PP, Brasch Jochen J et al.

The consensus-based guideline developed under the auspices of the German Dermatological Society (DDG) is intended to provide physicians with a structured framework for clinical decision-making in the management of patients with tinea capitis and to contribute to improved diagnostic accuracy, treatment adherence, and prevention. Tinea capitis is a dermatophyte-induced infection of the scalp that predominantly affects children and represents a common dermatological condition worldwide. In recent years, a marked shift in the epidemiology of causative dermatophytes has been observed in Europe, driven by migration, tourism, and socioeconomic factors, with an increasing prevalence of anthropophilic species, particularly Trichophyton tonsurans and Trichophyton violaceum. From a therapeutic perspective, a combination of systemic and topical antifungal treatment is recommended, as topical monotherapy is generally insufficient. In pediatric patients, the choice of systemic antifungal therapy is primarily guided by the identified pathogen, with Trichophyton infections preferably treated with terbinafine (off-label) and Microsporum/Nannizzia infections with itraconazole (off-label) or griseofulvin. In adult patients, terbinafine is recommended as first-line therapy irrespective of the causative species. In addition, the guideline addresses measures to interrupt chains of infection, including the treatment of asymptomatic carriers, implementation of hygiene measures, and management of outbreak situations in community settings.

PubMedACS omega2026-07-10

Experimentally Derived Hansen Solubility Parameters as a Screening Tool for the Formulation of Amorphous Solid Dispersions.

Osakwe Adaeze R AR, Le Mira T N MTN, Bramhall Jessica A JA, Klepov Vladislav V VV et al.

A major challenge in pharmaceutical development is the poor aqueous solubility of crystalline active pharmaceutical ingredients (APIs) generated during the API discovery. Amorphous solid dispersions (ASDs) improve solubility by molecularly dispersing amorphous APIs within a glassy polymer matrix; however, their utility is often constrained by limited API loading capacity and incomplete API release. To address these challenges, this study employs experimentally derived Hansen solubility parameters (HSP) as a predictive tool to assess polymer/API compatibility early in formulation development, rather than relying on conventional trial-and-error approaches. HSP values for ten commercially relevant ASD polymers and three APIs were determined using an experimental solubility screening method in conjunction with HSPiP software. Guided by these miscibility predictions, ASDs were prepared by materials-sparing hot-melt extrusion using only 2-7 g of API. A linear relationship was observed between the relative energy difference (RED) and the maximum amorphous API soluble (MADS), where lower RED values led to higher API loadings, up to 45%. Polymer/API interactions characterized using FTIR and DSC revealed that specific intermolecular interactions significantly influence dissolution behavior. Notably, the release of amorphous griseofulvin increased by up to 235% in ASD formulations exhibiting minimal intermolecular interactions compared to the crystalline API. Collectively, these results demonstrate the reliability of experimentally derived HSP for predicting ASD miscibility and API loading capacity, while complementary physicochemical characterization provides mechanistic insight into dissolution behavior. This integrated framework enables the rational design of high API-loaded, high-performance ASD formulations.

PubMedJournal of fungi (Basel, Switzerland)2026-06-25

Genomic Basis of Zoonotic Transmission and Antifungal Resistance in Microsporum canis.

Du Zebin Z, Zhang Yuling Y, Meng Xinting X, Lv Zexun Z et al.

Microsporum canis is a globally prevalent zoonotic dermatophyte and the major causative agent of dermatophytosis in both pets and humans. The widespread clinical use of antifungal drugs has led to the frequent emergence of decreased susceptibility, while its molecular features and the genomic basis of cross-host transmission remain incompletely elucidated. In this study, 38 clinical M. canis isolates were collected from dogs and cats in Beijing (2025). We determined the minimum inhibitory concentrations (MICs) of six common antifungal agents via microbroth dilution, and performed whole-genome sequencing and comparative genomic analysis. All isolates showed high clonal homogeneity, with ANI >99.9% to the reference. A local human-derived strain was nested within the pet-derived clade, supporting zoonotic cross-host transmission. Terbinafine exhibited the highest activity, while itraconazole, voriconazole, posaconazole, griseofulvin, and ciclopirox olamine showed higher MICs; 11 isolates showed a multidrug high-MIC phenotype. Notably, copy number variation in the ABC transporter gene CDR1 was positively correlated with MICs of multiple antifungal agents (p<0.05). This study provides a genomic basis for optimized antifungal therapy, resistance surveillance and transmission control of zoonotic M. canis.

PubMedBioorganic chemistry2026-06-22

Norlichexanthone, a shunt product of Griseofulvin, disrupts spindle assembly checkpoint and nucleocytoplasmic transport by targeting TPR in the nuclear pore complex.

Pham Huong T HT, Kim Seul S, Hong Jihee J, Gwon Dasom D et al.

Griseofulvin, a known antifungal, exhibits anticancer activity by disrupting centrosome clustering; however, its molecular target remains elusive. Here we report that griseofulvin impairs the Spindle Assembly Checkpoint (SAC) by binding directly to Mad1 and BubR1, interrupting the Mad1-Mad2 interaction and inducing mitotic cell death via multipolar spindle formation. Through chemical re-investigation of halogen substrate promiscuity of griseofulvin biosynthesis, we discovered that the shunt product norlichexanthone demonstrates significantly higher cytotoxicity than griseofulvin. Unlike griseofulvin, norlichexanthone induces both mitotic multipolar spindles and interphase nuclear membrane abnormalities. We found that norlichexanthone directly binds TPR, a scaffold protein essential for Mad1-Mad2 assembly at the nuclear pore complex (NPC). This novel dual mechanism-disrupting SAC assembly and nucleocytoplasmic transport-renders norlichexanthone a superior cytotoxic agent. Our findings position norlichexanthone as a promising chemotherapeutic candidate that promotes cancer cell death by targeting TPR-mediated pathways across both interphase and mitosis.

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.

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.

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