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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
Sources: ClinicalTrials.gov, Transdermal

Therapeutic Indications

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

Therapeutic AreaConditionPhase
InvestigationsDermatologic examination✓ Approved

Related Research Articles

PubMedACS medicinal chemistry letters2026-09-15

Discovery of Forvisirvat (DS-7830a/SP-624), a Brain-Penetrant Sirtuin 6 Activator Derived from Griseofulvin with Antidepressant-Like Effects.

Ogawa Yasuyuki Y, Saito Keiji K, Nakajima Katsuyoshi K, Iwamoto Osamu O et al.

We report the discovery of forvisirvat (DS-7830a/SP-624), a potent and selective brain-penetrant activator of sirtuin 6 (SIRT6) derived from natural product griseofulvin. Photoaffinity labeling combined with molecular docking identified an allosteric binding site that overlaps with the substrate myristoyl pocket. SAR studies focused on C-6 modification yielded forvisirvat with markedly improved pharmacokinetic properties and CNS exposure. Forvisirvat selectively activated SIRT6 over other sirtuin isoforms and exhibited robust antidepressant-like effects in mouse models, supporting the therapeutic potential of SIRT6 activation in depression.

PMID 42741293
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PubMedBiotechnic & histochemistry : official publication of the Biological Stain Commission2026-09-11

Efficiency of griseofulvin and plumbagin in mitigating N-nitrosodiethylamine-induced hepatocellular carcinoma.

Tyagi Ekta E, Bhuyan Rajabrata R, Prakash Anand A

Hepatocellular carcinoma (HCC) is a globally prevalent malignancy often triggered by oxidative stress and exposure to hepatotoxic agents such as N-nitrosodiethylamine (NDEA), which induces DNA adducts, inflammation, and liver dysfunction. Natural compounds like plumbagin (PL) and griseofulvin (GF) have demonstrated anticancer potential; however, their in vivo efficacy in NDEA-induced HCC models remains insufficiently explored. This study investigated the protective effects of PL and GF against NDEA-induced hepatocarcinogenesis in male Swiss albino mice. Animals were randomly assigned to seven groups, including normal control, NDEA control (200 mg/kg), and treatment groups receiving PL (2 mg/kg and 6 mg/kg, intraperitoneally), GF (225 mg/kg and 450 mg/kg, orally), or the reference drug sorafenib (30 mg/kg, orally) for 14 days. Biochemical, hematological, and oxidative stress markers were evaluated alongside histopathological analysis. NDEA exposure significantly elevated liver enzymes (ALT, AST, ALP), cholesterol, and malondialdehyde (MDA), while reducing antioxidant enzyme levels (SOD, CAT, GST, and GSH-Px), indicating marked hepatic damage. Treatment with PL and GF led to significant, dose-dependent restoration of these parameters, with notable reductions in MDA and improvements in antioxidant activity. Histopathological assessments further confirmed these findings, showing reduced fibrosis, enhanced hepatocyte regeneration, and improved liver architecture, particularly with high-dose PL, which demonstrated efficacy comparable to sorafenib. In conclusion, PL and GF exhibited substantial hepatoprotective and anticancer effects in the NDEA-induced HCC model, primarily by restoring liver function, reducing oxidative stress, and improving histological outcomes. These findings support their potential as complementary therapeutic agents in liver cancer management.

PMID 42725366
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PubMedInternational journal of pharmaceutics2026-09-10

A solid-state-dependent correlation between drug-polymer hot melt extrudate mechanical behavior and milled extrudate tablet tensile strength.

Kossor Christopher C, Bhat Roopal R, Tripathi Siddharth S, Majumder Sushmita S et al.

The mechanical behavior of drug-polymer hot melt extrudates, whether amorphous or partially crystalline, was found to predict the tensile strength of tablets directly compressed from the milled extrudates, with the most predictive test depending on the extrudate solid state. Griseofulvin (GF), a poorly water-soluble BCS class II drug prone to crystallization, was selected as the model drug. Two polymers were compared, Hydroxypropyl Cellulose SL (HPC) and Kollidon VA 64 (PVPVA), to uncover the influence of drug-polymer interactions and identify (anti)plasticization phenomena. Extrudates were prepared spanning fully amorphous to partially crystalline states, as defined by XRPD, by varying HME processing temperature and drug loading. Mechanical behavior was assessed by nanoindentation (modulus and hardness) and three-point bend testing (flexural modulus and breaking force). The milled extrudates were directly compressed without extragranular material to assess tabletability, compressibility, and compactability. Increasing GF concentration in HPC extrudates increased modulus and breaking force via antiplasticization until 20 wt% GF followed by plasticization, while PVPVA extrudates exhibited bulk plasticization. The most predictive test depended on solid state: flexural modulus correlated with tablet tensile strength for amorphous extrudates (R2 = 0.903), while nanoindentation modulus correlated for crystalline extrudates (R2 = 0.910), providing a material-sparing screening methodology. Notably, this work uncovers a thermodynamic-mechanical paradox: the marginally miscible GF/HPC system antiplasticized while the strongly miscible GF/PVPVA system plasticized in bulk, contrary to what the Flory-Huggins interaction parameter and Tg would predict. This paradox is explained by polymer chain architecture and free-volume (hole-filling) effects rather than thermodynamic interaction strength alone.

PMID 42722216
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PubMedCancer treatment and research communications2026-09-08

Griseofulvin as a dual-action agent against glioblastoma: anti-tumor effect and enhancement of 5-ALA photodynamic diagnosis in stem-like cells.

Nishiwaki Takayuki T, Yamada Takumi T, Kudo Urara U, Nakamura Shinsuke S et al.

5-aminolevulinic acid (5-ALA)-mediated photodynamic diagnosis (PDD), a standard surgical adjunct for glioblastoma (GBM), is limited in its efficacy by heterogeneous protoporphyrin IX (PpIX) accumulation. We investigated the drug repurposing potential of griseofulvin (GF), an antifungal agent, as a dual-action agent that directly inhibits tumor growth through cell cycle arrest and enhances 5-ALA-induced fluorescence by regulating ferrochelatase (FECH). The antitumor effects of GF on glioma stem-like cells (NCH644) and other differentiated GBM cell lines were evaluated using cell viability, colony formation, and cell cycle assays. PpIX accumulation and its enhancement by GF were quantified using a time-course analysis. The mechanisms were investigated using western blotting, RT-qPCR, and confocal visualization. An orthotopic GBM mouse model was used to assess in vivo antitumor activity using preliminary ex vivo fluorescence imaging. GF first exerted direct antitumor effects via G2/M arrest, characterized by cyclin D1 downregulation and cyclin B1 transient upregulation. Second, GF attenuated the 5-ALA-induced increase in FECH mRNA levels and enhanced PpIX accumulation. In vivo, oral administration of GF significantly inhibited tumor growth in vivo In a preliminary ex vivo assessment, tumors from GF-treated mice showed a higher tumor-to-normal PpIX fluorescence ratio than those receiving 5-ALA monotherapy, enabling superior tumor visualization. These preclinical findings identify GF as a candidate dual-action agent for GBM treatment. Whether the fluorescence enhancement translates into improved intraoperative detection, extent of resection, or patient survival remains to be determined through future in vivo and clinical studies.

PMID 42710153
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PubMedMolecular pharmaceutics2026-09-07

Pure but Not Simple: Supersaturation from Excipient-Free, Vapor-Generated, Amorphous Griseofulvin Nanoparticles.

Huang Chao C, Ogunwale Samuel S, Pontrelli Eva K EK, Machado Tatiane C TC et al.

Rapid crystallization of an active pharmaceutical ingredient can suppress its observable supersaturation and negate this potential advantage of the amorphous form. Excipients added to formulations can prolong supersaturation, but reduce drug loading and obscure the intrinsic dissolution behavior of the drug in testing. Here, we describe spring-and-parachute dissolution behavior in fasted-state simulated intestinal fluid of an archetypal poorly soluble and strongly crystallizing drug, griseofulvin (GSF), in the form of excipient-free, pure, amorphous nanopowders generated using a novel, single-step, solvent-free technique of organic vapor jet desublimation. Using experiments and modeling, we establish how initial dissolution rate, peak concentration, and area under the concentration-time curve scale with dose, distinguishing between dose regimes in which supersaturation behavior is monotonic and nonmonotonic. The roles of local surface crystallization, particle aggregation, and nonequilibrium crystallization at high supersaturation are elucidated, providing a framework for attaining excipient-free supersaturation and guiding the development of improved dissolution models.

PMID 42704141
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PubMedCureus2026-08-31

Severe Adult Kerion Celsi With Rapid Improvement During Systemic Antifungal and Adjunctive Secretome Therapy: A Case Report.

Dewi Dian Andriani Ratna DAR, Tasya Khufitha K, Firdaus Juliandra J, Maulida Sausan S et al.

Kerion celsi is a severe inflammatory form of tinea capitis that is uncommon in adults and may mimic bacterial furunculosis, abscess, or cellulitis, resulting in delayed diagnosis and antibiotic-only treatment. We report a 48-year-old woman with a one-month history of a painful, purulent, crusted lesion on the left temporal and retroauricular scalp, localized alopecia, and ipsilateral periorbital edema. She reported close exposure to 10 cats daily and did not improve after treatment for presumed furunculosis. Potassium hydroxide examination demonstrated fungal elements. Fungal culture and lactophenol cotton blue morphology were consistent with Microsporum canis. Histopathology demonstrated dense suppurative follicular and perifollicular inflammation, follicular destruction, and granulomatous inflammation; fungal organisms were not identified on hematoxylin and eosin staining. The patient received oral griseofulvin, topical miconazole, structured wound care, empirical ciprofloxacin for clinically suspected secondary bacterial infection, and adjunctive intramuscular administration of a human umbilical cord-derived mesenchymal stromal cell conditioned-medium secretome preparation. Periorbital edema markedly decreased by day 2. By day 14, lesion dimensions remained approximately 8 × 5 cm, while pain and pruritus had decreased from 6/10 to 0/10 and exudation, pustulation, crusting, erythema, and scalp edema were substantially reduced. This improvement was temporally associated with the combined regimen. Because several interventions were initiated concurrently, the specific contribution of secretome could not be determined. Systemic antifungal therapy remains the cornerstone of treatment, and the safety and efficacy of secretome in active inflammatory dermatophyte infection require further study.

PMID 42670489
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