rosiglitazone / Generic mfg. - LARVOL DELTA

Reversing neuroinflammation in ischemic stroke through efferocytotic phenotype reprogramming with polymeric nanoparticles. (PubMed, Biomaterials) - "Specifically, we encapsulated rosiglitazone into mPEG-PLA nanoparticles and further coated them with platelet membranes, obtaining a targeted nanoplatform termed pmPELA@R...This dual modulation synergistically shifted the inflammatory microenvironment toward a reparative state, leading to enhanced neural tissue recovery. Our findings present a novel nanotherapeutic approach for precise immunomodulation in ischemic stroke."

Journal • Cardiovascular • Immunology • Inflammation • Ischemic stroke

Influence of heat-reinforcing Needling on the PPAR-γ/NF-κB signaling pathway in the synovial membrane of rats with rheumatoid arthritis. (PubMed, Histol Histopathol) - "Forty-eight male Sprague-Dawley rats were randomly assigned to four groups (control, model, rosiglitazone, and HRN groups)...In the RA cold syndrome model rats, HRN may reduce joint swelling and suppress inflammation of the synovial membrane, possibly via controlling the PPAR-γ/NF-κB signaling pathway. This method could provide a fresh therapeutic approach to RA symptom management."

Journal • Preclinical • Immunology • Inflammation • Inflammatory Arthritis • Rheumatoid Arthritis • Rheumatology • IL1B • IL4 • IL6 • PPARA • TNFA

METTL14 inhibits atherogenesis by epigenetically activating PPAR-α/γ transcription and fatty acid oxidation in VSMCs. (PubMed, Cardiovasc Res) - "We have unveiled that METTL14 promotes lipid metabolism and inhibits atherogenesis through activating PPAR-α/γ expression. These experiments highlight the therapeutic potential of the endogenous METTL14/PPAR-α/γ axis for treating atherosclerotic and metabolic diseases."

Journal • Atherosclerosis • Cardiovascular • Gene Therapies • Inflammation • Metabolic Disorders • APOE • METTL14 • METTL3 • PPARA • PPARG • SETD1A

FDA-approved drug library screen identifies antidepressants, antimicrobials, anti-COPD, and anti-CVD agents as blockers of NLRP3 inflammasome and sepsis in a sex-dependent manner. (PubMed, bioRxiv) - "Various classes of drugs, such as antidepressants (Fluoxetine, Duloxetine), antihypertensives (Irbesartan, amlodipine, nebivolol), antidiabetics (Rosiglitazone), β-adrenergic agonists (Salmeterol), antimalarials (Mefloquine), antifungals (Azoles, ciclopirox), and antivirals (Saquinavir, Remdesivir), were identified as potent blockers of either priming or assembly of NLRP3 inflammasome. Mice treated with LPS-priming blockers showed a sex-specific increase in survival rate in the mouse model of LPS-induced mortality, validating the in vitro screen. Further studies in primary human cells and in vivo disease models are needed to assess the repurposing and therapeutic relevance of identified drugs."

FDA event • Journal • Alzheimer's Disease • Asthma • Chronic Obstructive Pulmonary Disease • CNS Disorders • Diabetes • Genetic Disorders • Gout • Immunology • Infectious Disease • Inflammatory Arthritis • Metabolic Disorders • Metabolic Dysfunction-Associated Steatotic Liver Disease • Movement Disorders • Novel Coronavirus Disease • Obesity • Parkinson's Disease • Pulmonary Disease • Respiratory Diseases • Rheumatology • Septic Shock • NLRP3

PPAR-γ suppresses macrophage senescence and allergic airway inflammation through controlling lipid metabolic pathways. (PubMed, EBioMedicine) - "These findings identify macrophage senescence as a pathogenic driver of allergic airway inflammation and establish PPAR-γ as a critical regulator of macrophage senescence and homoeostasis, highlighting its potential as a therapeutic target for asthma."

Journal • Asthma • Immunology • Inflammation • Metabolic Disorders • Pulmonary Disease • Respiratory Diseases • CD36 • CDKN2A • FABP4 • ICAM1 • IL4 • IL5 • IL6 • ITGAX • PPARG • SCARB1 • TIMP1 • TNFA

Mutual solubilization of rosiglitazone and ibuprofen: Investigation and mechanistic insight. (PubMed, PLoS One) - "The observed mutual solubilization is attributed to specific intermolecular interactions and enhanced solvent compatibility. These findings offer a simple, formulation-free strategy for improving the dissolution of poorly water-soluble drugs."

Journal

Transient SUMOylation inhibition in human pre-adipocytes stably imprints a transcriptional beiging fate. (PubMed, Nucleic Acids Res) - "Here, we show that brief pharmacologic inhibition of SUMOylation in human pre-adipocytes using TAK-981 primes stable de novo beige differentiation in the presence of the PPARG agonist rosiglitazone. We propose that transient relief of SUMO-mediated repression unlocks dominant regulatory units, notably the UCP1 enhancer cluster, producing a monomorphic reprogramming toward adaptive thermogenesis. These findings identify SUMOylation as a reversible epigenetic barrier to adipocyte beiging and suggest that temporally controlled SUMO pathway inhibition combined with PPARG activation could be exploited to modulate adipose tissue thermogenic capacity."

Journal • CEBPA

Activation of PPARγ redirects fibro-adipogenic progenitors to replace ectopic bone with fat in models of fibrodysplasia ossificans progressiva and trauma-induced heterotopic ossification. (PubMed, bioRxiv) - "Our findings were corroborated by a single case report from 2010 showing positive results with rosiglitazone in a non-diabetic patient with FOP, with no subsequent studies. Overall, our findings suggest that a previously FDA-approved therapeutic is likely to be a successful therapeutic agent for both FOP and trauma-induced HO, both conditions for which current therapeutic options remain inadequate."

Journal • Metabolic Disorders • Mood Disorders • ACVR1 • BMP2 • PPARG

PPARγ Activation Protects against Hydrogen Peroxide-Induced Oxidative Stress and Apoptosis in Human Liver Cells. (PubMed, Biochemistry (Mosc)) - "Inhibition of the Nrf2 pathway by ML385 partially abolished the rosiglitazone-induced amelioration of oxidative stress and apoptosis. We conclude that activation of PPARγ protects liver cells against oxidative stress and apoptosis through the Nrf2 pathway."

Journal • BCL2 • CASP3 • CAT • PPARG

Assessing safety trends of withdrawn medications: A data-driven pharmacovigilance approach using growth models. (PubMed, Explor Res Clin Soc Pharm) - "For comparative safety assessment, 15 commonly used cancer medications (including Tamoxifen, Avastin, Bleomycin, Paclitaxel, Vincristine, Methotrexate, Cisplatin, Doxorubicin, Imatinib, Docetaxel, Rituximab, Trastuzumab, Revlimid, Lenalidomide, and Pembrolizumab) were analyzed...The examples presented in this investigation demonstrated that the drugs Benoxaprofen, Rosiglitazone, Temazepam, and Rofecoxib exhibited a robust correspondence with diverse modeling approaches...It also provides a foundation for future research. This research could help support safer clinical decisions and regulatory evaluations for both pharmaceuticals that are no longer on the market and those that are still available."

Adverse events • Journal • Oncology

Ag/ZnFe2O4-Au NPs-Based SERS Detection of Rosiglitazone in Seawater. (PubMed, Talanta) - "In addition, the high stability and the excellent selectivity against the coexisting objects offer potential for real samples measurement. The developed Ag-doped magnetic semiconductor-metal composite-based SERS strategy provides a potential for PPCPs monitoring in real environmental samples."

Journal

Design, synthesis, and biological evaluation of small-molecule HMGB1 inhibitors for the alleviation of radiation-induced skin injury. (PubMed, Bioorg Med Chem) - "Two novel classes of compounds were designed and synthesized based on molecular docking analysis of Methotrexate (MTX) and rosiglitazone (RSG) binding to HMGB1. Mechanistic studies suggest that 30 may exert its protective effects through the HMGB1-TLR4-NF-κB signaling pathway, while molecular dynamics simulations predicted stable binding of 30 to HMGB1. In conclusion, 30 represents a novel small-molecule HMGB1 inhibitor with significant therapeutic efficacy against RSI, validating HMGB1 as a viable target for the development of radioprotective agents."

Journal • Inflammation • HMGB1 • IL6 • TLR4

PPARγ contributes to cardioprotection against heat stroke through ABCC5-dependent lipid metabolism. (PubMed, Redox Biol) - "Importantly, we demonstrated that treatment with either rosiglitazone (a PPARγ agonist) or atorvastatin (a lipid-lowering drug) holds promising therapeutic potential for ameliorating HS-induced myocardial dysfunction. These findings indicate that PPARγ protects against HS-induced myocardial pathological manifestations through ABCC5-dependent regulation of lipid metabolism."

Journal • Cardiovascular • Metabolic Disorders • ABCC5 • PPARG

Identification of pharmaceuticals and environmental contaminants as obesogens inducing a locomotion-independent thrifty phenotype. (PubMed, Commun Biol) - "Using the zebrafish obesogenic test, our study demonstrates that amiodarone, dibutyl phthalate, rosiglitazone, tributyltin, and triclosan induce a thrifty phenotype under short-term fasting conditions. Diazepam significantly reduces locomotion without exhibiting any obesogenic effect, whereas tributyltin, which has the highest obesogenic potential among the tested compounds, has no effect on locomotion. The obesogen-induced resistance to fat loss is not correlated to inhibition of physical activity and a corresponding reduction in energy expenditure, nor to food consumption. Primary prevention measures to fight against the obesity pandemic may include reducing exposure to obesogens that can induce a thrifty phenotype."

Journal • Genetic Disorders • Obesity

Cartilage Autophagy Dysregulation During OA Progression in Hip Femoroacetabular Impingement (AAOS 2026) - "Subsequently, we cultured the explants in untreated conditions, under catabolic stimulus with interleukin-1 β (IL1β) with or without PPARγ agonist (Rosiglitazone) or inhibitor (T0070907) for 48 hours... This study demonstrates that PPARγ receptor activation in human hip cartilage suppresses catabolic activity and promotes autophagy-related gene expression. PPARγ agonist treatment reduced MMP-13 levels and reversed IL1β- induced catabolic changes. These findings support the role of PPARγ in maintaining cartilage homeostasis via autophagy modulation."

Immunology • Orthopedics • Osteoarthritis • GAPDH • IL1B • MMP13 • PPARA

Ulcerative colitis, pathophysiological mechanisms and drug repurposing: a new therapeutic dawn-narrative review. (PubMed, Inflammopharmacology) - "Several medications, including rosiglitazone, amlodipine, felodipine, atorvastatin, metformin, pentoxifylline, nitazoxanide, nifuroxazide, carbocisteine, levetiracetam, topiramate, nicodamid, and vildagliptin, have been shown to have positive effects on multiple organs through their anti-inflammatory properties. Using the findings of in vitro, in vivo, and clinical investigations, the positive effects of these medications on UC are thoroughly outlined and examined in the present research. Having a better knowledge of these protective benefits and the basic mechanisms may make it possible for UC patients to take these medications effectively."

Journal • Review • Crohn's disease • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Ulcerative Colitis • AMPK • IL6 • mTOR • STAT3

A Novel PPARG R212W Variant Causes Familial Partial Lipodystrophy Type 3: Clinical Presentation and Functional Characterization. (PubMed, Int J Mol Sci) - "The partial rescue by rosiglitazone suggests a potential therapeutic avenue. This study underscores the importance of integrating clinical phenotyping with deep functional analysis to diagnose and understand rare monogenic lipodystrophies."

Journal • Dyslipidemia • Hypertriglyceridemia • Lipodystrophy • Metabolic Disorders • Pancreatitis • FABP4 • LPL • PPARG • SLC2A4

The Analgesic Effects of Nrf2 Activators in Chemotherapy-Induced Neuropathic Pain: Evidence from Animal Studies and Consequences for Translation into Clinical Trials. (PubMed, Int J Mol Sci) - "Chemotherapy-induced neuropathic pain (CINP) can be caused by several chemotherapeutic drugs, including paclitaxel, oxaliplatin, and vincristine, which is difficult to treat with several drugs, including antidepressants and anticonvulsants...Several Nrf2 activators, including tempol, oltipraz, rosiglitazone, pristimerin, cannabidiol, daidzein, bardoxolone methyl, curcumin, resveratrol, and mitoquinone, demonstrated analgesic effects in CINP animal models. Furthermore, in clinical studies, curcumin demonstrated significant efficacy in reducing vincristine-induced neuropathy in pediatric leukemia patients, while the combined administration of alpha-lipoic acid with ipidacrin hydrochloride prevented paclitaxel-induced motor neuropathy and improved axonal function in breast cancer patients. Thus, the purposes of our review article were to summarize the analgesic effects of Nrf2 activators and the patho-mechanisms of Nrf2 in CINP animal, and then the consequences for clinical..."

Journal • Review • Breast Cancer • Hematological Malignancies • Leukemia • Neuralgia • Oncology • Pain • Pediatrics • Solid Tumor

PPAR-γ Activation Alleviates Intestinal Dysfunction and Lactose Malabsorption in Experimental Food Allergy Rats. (PubMed, Nutrients) - "PPAR-γ signaling maintains intestinal lactose digestive capacity of rats during allergic inflammation by sustaining lactase production and monosaccharide transporter expression. Our findings verify an immunometabolism mechanism linking nuclear receptor activation to enhanced nutrient absorption and highlight PPAR-γ agonism as a promising therapeutic strategy to alleviate food allergy-associated lactose malabsorption."

Journal • Preclinical • Allergy • Food Hypersensitivity • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • PPARA

Lauric acid attenuates hepatic lipid metabolism by modulating the AMPK-SREBP pathway in high-fat diet-induced obese mice. (PubMed, Toxicol Mech Methods) - "Three experimental groups were co-treated with HFD and lauric acid (12 and 24 mg/kg orally), or HFD and rosiglitazone (20 mg/kg orally) for another eight consecutive weeks...Histological examination revealed that lauric acid-fed mice showed similar hepatic morphology compared to the HFD control. Finally, the data suggest that lauric acid is a potential nutraceutical intervention for lipid-lowering and insulin resistance in obese individuals."

Journal • Preclinical • Diabetes • Genetic Disorders • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus • AMPK • APOA2 • ARG1 • PPARG • SREBF2

Effects of tea polyphenols on brain structure and function of hippocampus in aged type 2 diabetes mellitus rats with anxiety and depression-like behavior. (PubMed, Brain Res) - "TP intervention mitigated alterations in brain structure and function as well as anxiety and depression-like behaviors in aged T2DM rats."

Journal • Preclinical • CNS Disorders • Depression • Diabetes • Metabolic Disorders • Mood Disorders • Psychiatry • Solid Tumor • Type 2 Diabetes Mellitus • BDNF • IL1B • IL6 • TNFA

System biology and network-based approach to identify the therapeutic signatures and potential inhibitors against polycystic lipomembranous osteodysplasia with Sclerosing Leukoencephalopathy. (PubMed, PLoS One) - "Furthermore, Molecular docking of target PPARG gene with AMG-131 and Elafibranor drugs, having the chemical formulas 2-[2,6-dimethyl-4-[(E)-3-(4-methylsulfanylphenyl)-3-oxoprop-1-enyl]phenoxy], and 3,5-dichloro-4-quinolin-3-yloxyphenyl) benzenesulfonamide, along control (Rosiglitazone (S) shows binding affinities of -7.2 kcal/mol, -7.4 kcal/mol, and -7.6 kcal/mol respectively. Arg76 and Leu28leu Leu118 were shown to be essential enzyme residues for binding, anchoring, and bridging strong hydrogen and hydrophobic interactions between the enzyme and the inhibitor, according to the Radial Distribution Function (RDF). These results broadened our knowledge of putative biomarkers for PLOSL diseases, and an experimental strategy will improve our results even more in the future."

Journal • Alzheimer's Disease • CNS Disorders • Dementia • AIF1 • C1QA • PPARG • SIGLEC1

PPAR-gamma regulates PFAS-mediated proinflammatory cytokines in lung epithelial cells. (PubMed, Front Pharmacol) - "Primary human bronchial epithelial (NHBE) cells were exposed to 15 µM binary PFAS mixture (PFOS + PFOA) or quaternary mixture (PFOS, PFOA, PFHxS, GenX) with or without the PPARγ antagonist (15 µM) and/or the PPARγ agonists rosiglitazone (10 µM) or pioglitazone (10 µM) for 24 h. PFOS exposure in mice caused a reduction in lung PPARγ protein levels, while PPARα expression remained unchanged. These findings demonstrate that PFAS-induced pro-inflammatory cytokines is mediated, at least in part, through PPARγ signaling, and that pharmacological activation of PPARγ signaling can attenuate PFAS-triggered pro-inflammatory cytokine responses in lung epithelial cells."

Journal • Inflammation • Pneumonia • CXCL8 • IL6 • PPARA • PPARG

Polycystic Ovarian Syndrome - exploring the therapeutic and biomedical insights into the role of Silver nanoparticles. (PubMed, J Steroid Biochem Mol Biol) - "Conventional medicines, such as metformin, clomiphene citrate, letrozole, flutamide, and rosiglitazone, can regulate menstrual irregularities, improve ovulation, reduce insulin resistance, and decrease androgen levels, but may also cause various side effects. The review includes evidence from insulin, inflammation, oxidative processes, neuroendocrine factors and cystogenic pathways to combine and provide an overview. The review also discusses how to approach toxicity, especially dose-dependent, and the reproductive safety of AgNPs and their translational limitations to define the boundaries of AgNPs in the treatment of PCOS."

Journal • Review • Endocrine Disorders • Inflammation • Polycystic Ovary Syndrome • Women's Health

Heat Stress Induces Cognitive Impairment Through ACSL4-Mediated Lipid Peroxidation and Subsequent Ferroptosis. (PubMed, Mol Neurobiol) - "Pharmacological inhibition of ACSL4, the key enzyme incorporating peroxidation-susceptible PUFAs into membranes, using rosiglitazone, similarly suppressed ferroptosis markers, lipid peroxidation, ROS, and cell death in HT22 neurons, while restoring GPX4 expression. These findings establish that HS induces cognitive impairment via an ACSL4-driven lipid peroxidation-ferroptosis axis in hippocampal neurons, identifying ACSL4 as a potential therapeutic target for mitigating heat-related neurodegeneration."

Journal • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Metabolic Disorders • ACSL4 • CHAC1 • GPX4 • MT-CO2 • RGS4 • SLC7A11 • TFRC