rosiglitazone / Generic mfg. - LARVOL DELTA

Rosiglitazone alleviates white matter injury by inhibiting NLRP3/capspase-1 mediated microglial pyroptosis via downregulating KLF4. (PubMed, Exp Brain Res) - "Notably, ROSI downregulated KLF4 in microglia isolated from WMI rats, further supporting its role in inhibiting pyroptosis. Collectively, these findings demonstrated that ROSI alleviated WMI by inhibiting NLRP3/caspase-1-mediated microglial pyroptosis through downregulation of KLF4, highlighting its potential as a therapeutic strategy for WMI."

Journal • CNS Disorders • Inflammation • Solid Tumor • IL18 • IL1B • KLF4 • NLRP3

Association Between Thiazolidinedione Therapy and Tuberculosis-Related Events in Type 2 Diabetes: A Population-Based Cohort Study. (PubMed, Microorganisms) - "Rosiglitazone use was associated with lower risks of TB-related outcomes in the primary Cox analyses; however, these associations were attenuated in time-dependent analyses and were no longer statistically significant after accounting for death as a competing event. These observational findings should therefore be considered hypothesis-generating rather than evidence of a causal or protective effect and require confirmation using more robust causal-inference approaches."

Journal • Diabetes • Infectious Disease • Metabolic Disorders • Pulmonary Disease • Respiratory Diseases • Tuberculosis • Type 2 Diabetes Mellitus

CXCL10 Is Inhibited by PPARβ/δ-Selective Activation in Human Monocyte-Derived Dendritic Cells, T Lymphocytes and Monocytes In Vitro: Insights into Autoimmune Rheumatic Diseases. (PubMed, Biomolecules) - "This study aims to investigate CXCL10 in human monocyte-derived mDCs, CD4+ T cells, and monocytes exposed to PPARβ/δ agonist carbaprostacylin (cPGI2) or PPARγ agonist rosiglitazone (RGZ), to verify drug-class-related effects...cPGI2-induced CXCL10 downregulation, with TNFα and IFNγ decrease, might be relevant, given its early activity in ARD development. Scenarios on PPARβ/δ agonist re-positioning aimed at modulating CXCL10 might open opportunities to support ARD management and targeted therapy development."

Journal • Preclinical • Immunology • Oncology • Rheumatology • CD14 • CXCL10 • IFNG • IL10 • TNFA

Concurrent Thiazolidinediones and GLP-1 Receptor Agonists Therapy in MASH Cirrhosis Patients: A Propensity-Score-Matched Retrospective Cohort Study (ACG 2026) - "Introduction: Metabolic dysfunction-associated steatohepatitis (MASH) cirrhosis carries a significant clinical burden with unmet therapeutic needs... Our retrospective cohort study utilized the TriNetX US Collaborative Network to identify patients with MASH-related cirrhosis (ICD-10: K75.81/K76.0 plus K74.6/K74.69) receiving GLP-1RA/GIP (semaglutide, tirzepatide, liraglutide, exenatide, dulaglutide, or albiglutide) alone or with TZD (pioglitazone or rosiglitazone)... After matching, cohorts were well balanced (mean age 58.5 years; 81% White; 78% T2DM; 10% esophageal varices) except for higher BMI and HbA1c in combination cohort, reflecting TZD use as add-on therapy for refractory hyperglycemia. The combination group demonstrated a 37% relative reduction in all-cause mortality (3.7% vs. 5.1%; risk difference â1.4%, 95% CI â2.4% to â0.4%; p=0.007; HR 0.63, 95% CI 0.50â0.80; log-rank p0.001)."

Retrospective data • CNS Disorders • Diabetes • Fibrosis • Gastroenterology • Hematological Disorders • Hepatic Encephalopathy • Hepatocellular Cancer • Hepatology • Immunology • Liver Failure • Metabolic Disorders • Metabolic Dysfunction-Associated Steatohepatitis • Nephrology • Renal Disease • Solid Tumor • Type 2 Diabetes Mellitus

Inducing adipocyte hyperplasia improves growth performance, alleviates hepatic steatosis and counteracts muscle quality deterioration in largemouth bass (Micropterus salmoides) fed with high-carbohydrate diet. (PubMed, Fish Physiol Biochem) - "In this study, we fed largemouth bass (Micropterus salmoides) with a control diet, an HCD, or HCD supplemented with 30, 60, or 90 mg/kg rosiglitazone, a PPARγ agonist that induces adipocyte hyperplasia, for 8 weeks...Ultimately, the improved carbohydrate tolerance restored growth performance and reversed muscle texture deterioration, as evidenced by increased chewiness and gumminess and normalized adhesiveness. These findings demonstrate that promoting adipocyte hyperplasia effectively counteracts HCD-induced growth suppression, hepatic steatosis and flesh quality deterioration in carnivorous largemouth bass, providing a promising strategy to improve carbohydrate utilization in carnivorous fish aquaculture."

Journal • Metabolic Disorders • CXCL8 • IL1B

Identification of multi-target lead compounds from iron-stressed Aspergillus species using LC-MS, in silico analysis, and pharmacokinetics profiling. (PubMed, Nat Prod Res) - "The metabolites exhibited notable binding affinities comparable to standard drugs, including Erlotinib and Rosiglitazone. Pharmacokinetic and toxicity predictions using SwissADME, pkCSM, and ProTox-3.0 indicated favourable drug-likeness, high intestinal absorption, and no predicted hepatotoxicity or immunotoxicity. Overall, these findings suggest that Aspergillus-derived metabolites may serve as promising candidates for future antimicrobial and therapeutic drug discovery studies."

Journal • PK/PD data • Oncology • EGFR

FABP1-Mediated Lipid Metabolic Reprogramming Buffers Lipotoxicity in Nephrolithiasis via Maintaining PPARγ Activity. (PubMed, FASEB J) - "Importantly, targeted pharmacological activation of PPARγ utilizing rosiglitazone circumvents FABP1 depletion, rewiring global lipid and energetic fluxes to rescue tubular cell injury. Our findings redefine FABP1 from a passive clinical biomarker to an active homeostatic buffer. This study delineates the Ca2+/calcineurin-TFEB-FABP1-PPARγ axis as a vital defense mechanism against lipotoxicity, providing a compelling translational rationale for PPARγ-targeted metabolic interventions to treat nephrolithiasis."

Journal • Nephrology • Renal Calculi • FABP1 • PPARG • TFEB

PPARγ-dependent and -independent regulation of genes involved in hepatic methionine cycle in fasted or diet-induced obese mice. (PubMed, PLoS One) - "We previously reported that diet-induced steatosis increased hepatocyte Pparg expression, and here we show that PPARγ-specific agonist rosiglitazone (RSG) reduced the expression of betaine homocysteine S-methyltransferase (Bhmt) and Cbs in diet-induced obese control mice. The PPARγ-dependent reduction of hepatic Bhmt and Cbs expression was confirmed in mouse primary hepatocytes. Interestingly, PpargΔHep increased the expression of Pemt in HFD-fed mice and that of key genes of the methionine cycle in RSG-treated obese mice, including Pemt, Bhmt and Cbs, suggesting that Pparg negatively regulates their expression in the liver."

Journal • Preclinical • Genetic Disorders • Hepatology • Metabolic Disorders • Metabolic Dysfunction-Associated Steatohepatitis • Obesity • PPARG

Ultrasmall Polymeric Micelles Enable Noninvasive Transdermal Rosiglitazone Delivery via Lipid Fluidization and Transcytosis. (PubMed, Biomacromolecules) - "In a T2DM model, transdermal RGT reduced blood glucose by 30% over 12 days without observable skin or organ toxicity. This nanoplatform enables noninvasive systemic delivery, offering a robust alternative to oral administration for sustained glycemic control."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Potential Role for the Ubiquitin Ligase SIAH2 in Modulating Bone Morphology and Adiposity. (PubMed, Calcif Tissue Int) - "Bone morphology and adiposity were assessed, in vivo, using WT and Siah2-/- mice in the context of dietary, high-fat diet, and pharmacological, rosiglitazone, PPARγ stimulation...Our results suggest SIAH2 moderates both osteogenic and adipogenic commitment as the absence of SIAH2 results in progenitor cells that will more readily commit to either outcome. These observations underscore SIAH2's context-specific modulatory effects on PPARγ activities determined by tissue, nutrients and pharmacological cues."

Journal • Genetic Disorders • Musculoskeletal Diseases • Obesity • Orthopedics • Targeted Protein Degradation • PPARG

A novel rosiglitazone-phosphatidylserine composite nanoparticle mediated targeted drug delivery to macrophages for treatment of ulcerative colitis. (PubMed, Nanomedicine (Lond)) - "PLN-PSR showed good stability and biocompatibility, targeted macrophages in inflamed colon, alleviated dextran sulfate sodium (DSS)-induced colitis, and promoted M1-to-M2 macrophage polarization. PLN-PSR enables targeted anti-inflammatory delivery via macrophage phagocytosis and modulates macrophage function, representing a promising UC therapy."

Journal • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Ulcerative Colitis

Insight Into the Recent Advancements in Thiazolidinedione Derivatives as PPAR-γ Agonists for the Treatment of Type 2 Diabetes. (PubMed, Mini Rev Med Chem) - "The potential of thiazolidinediones, regarding their chemical development and interaction with PPAR-γ receptors, is well known. Newer TZD analogues that offer enhanced safety and tolerability are anticipated to become widely accessible soon."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

New insights into diagnostic values and mechanisms of ferroptosis associated with immune infiltration in diabetic kidney disease. (PubMed, Exp Ther Med) - "Notably, both LTF and CCL5 showed a significant positive correlation with gamma delta T cells (γδT). Quantitative PCR results confirmed differential expression of the three hub genes in the DKD group, with elevated expression observed in DKD mice following intervention with rosiglitazone and hyperoside."

Journal • Diabetic Nephropathy • Inflammation • Nephrology • Renal Disease • FOXC1 • LTF

Dihydrocapsiate from Capsicum annuum inhibits adipogenesis and enhances glucose uptake via activation of PPARα and NRF2. (PubMed, Fitoterapia) - "In adipocytes, DHC effectively antagonized rosiglitazone-induced adipogenic differentiation without modulating basal adipogenesis...Owing to its enhanced metabolic stability and unique nuclear receptors' signature, DHC represents a promising natural alternative for the improved glucose uptake and selective adipogenesis. Hence it may play a significant role in management of metabolic syndrome and type2 diabetes."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus • AMPK • PPARA • PPARG

BAZ1B is a key regulator of mitochondrial thermogenesis and adipose tissue plasticity (EASD 2026) - "Thermogenic activation was induced with rosiglitazone... Together, these findings identify BAZ1B as a critical regulator of mitochondrial thermogenesis, required for both PPARƔ- driven activation of brown adipocytes in vitro and cold-induced browning of iWAT in vivo . Loss of BAZ1B reveals tissue-specific adaptation, with BAT engaging compensatory pathways to maintain mitochondrial function and body temperature, while beige fat recruitment is impaired. Ongoing RNA-seq & ATAC-seq and CUT&TAG studies will define direct BAZ1B targets and underlying gene regulatory mechanisms."

Metabolic Disorders • Obesity • FABP4 • PPARGC1A

Anti-inflammatory Mechanisms of Human Resistin Through Activation of Peroxisome Proliferator-Activated Receptor γ (PubMed, Sichuan Da Xue Xue Bao Yi Xue Ban) - "Using resistin-treated RAW264.7 cells and C57BL/6J mice administered intraperitoneal injections as models, real-time quantitative PCR, Western blot, and ELISA were used to assess the mRNA and protein expression of PPARγ, total p65, phosphorylated p65, inhibitor of NF-κB alpha (IκBα), IL-1β, and TNF-α in LPS-induced RAW264.7 cells under conditions of resistin pretreatment or combined intervention with the PPARγ activator rosiglitazone or the inhibitor GW9662...Compared with the LPS-only treatment group, pretreatment with 25 μg/kg resistin reduced mouse serum IL-1β levels from (1616.66 ± 96.68) pg/mL to (1277.04 ± 27.73) pg/mL, TNF-α from (617.80 ± 145.54) pg/mL to (322.91 ± 129.50) pg/mL and IFN-γ from (12944.50 ± 90.69) pg/mL to (9222.84 ± 268.30) pg/mL, with all differences being statistically significant (P < 0.05); meanwhile, the 7-day survival rate of mice increased from 20% to 80%, which was statistically significant compared with..."

Journal • Oncology • IFNG • IL1B • NFKBIA • PPARG • RELA • RETN • TNFA

Di(2-ethylhexyl) phthalate and Mono(2-ethylhexyl) phthalate upregulate PPARG and induce metabolic reprogramming in hepatocellular carcinoma cells: a pan-cancer and metabolomics study. (PubMed, Food Chem Toxicol) - "Rosiglitazone promoted lipid accumulation and upregulated the lipid-storage genes DGAT2 and PLIN2, whereas GW9662 attenuated DEHP/MEHP-induced lipid accumulation and related transcriptional responses. Untargeted LC-MS metabolomics revealed relative alterations in phosphatidylcholine and phosphatidylethanolamine features and suggested perturbations in fatty acid-, bile acid-, arachidonic acid-, and nucleotide-related pathways. Collectively, these findings support a functional contribution of PPARG to DEHP/MEHP-associated lipid accumulation, potentially involving a DGAT2/PLIN2-related lipid-storage program, and provide mechanistic clues to phthalate-associated metabolic dysregulation in liver cancer cells."

Journal • Hepatocellular Cancer • Liver Cancer • Metabolic Disorders • Oncology • Solid Tumor • PLIN2 • PPARG

Sunitinib induces macrophage dysfunction and impaired tissue regeneration through suppression of PPARγ. (PubMed, Front Immunol) - "Treatment with rosiglitazone, a PPARγ agonist, effectively rescued the regeneration defects induced by sunitinib, restored macrophage infiltration, and recovered oxidative phosphorylation. Our results demonstrate that sunitinib impairs tissue regeneration by suppressing PPARγ signaling and oxidative phosphorylation in macrophages. Targeting the PPARγ pathway represents a promising therapeutic strategy to reverse sunitinib-associated deficits in tissue repair."

Journal • PPARG

Mesenchymal Stromal Cell-Based Cell-Drug Conjugates for the Treatment of Acute Liver Failure. (PubMed, Adv Sci (Weinh)) - "In a mouse model of ALF, rosiglitazone nanoparticle-modified MSCs exhibited enhanced accumulation and prolonged retention in the injured liver, more effectively inhibited hepatocyte apoptosis and promoted hepatocyte proliferation, thereby achieving superior therapeutic efficacy. Thus, our study provides a promising strategy for enhancing MSC-based therapy in ALF."

Journal • Hepatology • Liver Failure

Increasing local adipogenic signaling through cutaneous delivery of rosiglitazone decreases fibrosis in secondary lymphedema. (PubMed, Plast Reconstr Surg) - "Fibrosis is the most challenging aspect of lymphedema, as it permanently alters tissue quality and limits patient quality of life. Our topical rosiglitazone formulation reduces fibrosis and enhances adipose tissue, offering a novel strategy to improve tissue quality and surgical outcomes."

Journal • Fibrosis • Immunology • Obesity • CD4

The role and mechanism of rosiglitazone in endothelial-to-mesenchymal transition in pulmonary hypertension. (PubMed, Eur J Pharmacol) - "These findings reveal that RSG inhibits EndMT through regulating the noncoding RNA/PRKACB axis, suggesting that RSG can serve as a promising drug repurposing candidate for PH treatment."

Journal • Cardiovascular • Hypertension • Oncology • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases • Solid Tumor • Urothelial Cancer • MIR206 • PRKACB • UCA1

HMGB1/MYH9 suppresses PPARγ to induce lung injury in renal ischemia-reperfusion: protective effects of Rosiglitazone. (PubMed, Pediatr Res) - "HMGB1 released following renal ischemia-reperfusion binds MYH9 in lungs, suppressing PPARγ, driving inflammation and endothelial barrier dysfunction, thereby contributing to ALI pathogenesis. Rosiglitazone, a PPARγ agonist, restores PPARγ activity, strengthens barriers, reduces inflammation, and mitigates AKI-induced ALI in mouse models, with efficacy tied to serum CCL2 levels. Clinically, elevated urinary CCL2 in critically ill children associates with higher risk of concurrent AKI/ALI and poorer prognosis, indicating CCL2 as a biomarker for treatment response and prognosis. This work highlights a central pathogenic mechanism in AKI-ALI and proposes Rosiglitazone as a potential preventive/therapeutic strategy, with CCL2 guiding clinical monitoring."

Journal • Acute Kidney Injury • Acute Lung Injury • Cardiovascular • Inflammation • Nephrology • Pediatrics • Renal Disease • Reperfusion Injury • Respiratory Diseases • CCL2 • HMGB1 • MYH9 • PPARG

Synthesis, and biological evaluation of novel 4-thiazolidinone derivatives as promising antidiabetic agents: In silico and in vivo investigations. (PubMed, Biochem Biophys Res Commun) - "Remarkably, compound 3d (-8.67 kcal/mol) exhibited favorable binding interactions with the PPAR-γ receptor, surpassing the standard Rosiglitazone (-8.39 kcal/mol)...Furthermore, the compounds exhibited the ability to markedly decrease levels of HDL, LDL, VLDL, cholesterol, triglycerides, and protein, suggesting their promising antidiabetic efficacy. The synthetic strategy adopted in this study not only facilitated the creation of a novel set of thiazolidinone derivatives but also showed some good insights for the development of future agents with enhanced therapeutic potential and reduced side effects, based on the foundational thiazolidinone scaffold."

Journal • Preclinical • Diabetes

Mechanistic interplay between extracellular vesicles and neutrophil extracellular traps: unveiling the "sterile inflammation" cascade in obesity-induced diabetes progression. (PubMed, Front Immunol) - "Small vesicles from rosiglitazone-treated adipose tissue macrophages are enriched in microRNA-690 and exert similar effects...Among clinically deployed agents, metformin and sodium-glucose cotransporter 2 inhibitors already show anti-trap and anti-inflammasome activity...No completed randomized controlled trial in obesity-related type 2 diabetes has yet validated it. Translation requires multidisciplinary collaboration, methodological standardization, sex-stratified design, and adequately powered prospective human studies."

Journal • Review • Diabetes • Genetic Disorders • Hepatology • Inflammation • Liver Failure • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus • CGAS • NLRP3 • STING

Stigmasterol ameliorates obesity-associated insulin resistance by activating the PPARγ pathway and alleviating oxidative stress. (PubMed, Front Endocrinol (Lausanne)) - "In cell experiments, an insulin-resistant 3T3-L1 adipocyte model was treated with different concentrations of stigmasterol and rosiglitazone...Meanwhile, stigmasterol reduced hepatic ROS and MDA levels, restored antioxidant enzyme activities, and upregulated the protein expression of PPARγ, p-Akt/Akt, and GLUT4 in the liver (p < 0.05). Stigmasterol improved obesity-related glycolipid metabolic disorder and insulin resistance both in vitro and in vivo, and its mechanism involved activation of the PPARγ pathway and attenuation of oxidative stress."

Journal • Genetic Disorders • Metabolic Disorders • Obesity • PPARG • SLC2A4