Rizaben (tranilast) / Kissei, Nuon Therapeutics - LARVOL DELTA

Multilineage anti-fibrotic effects and MoA of N23Ps quantified by single-cell RNA-seq in 3D human lung slices (hPCLS) (ERS 2026) - "Human precision-cut lung slices (hPCLS) were treated with control or fibrotic cocktail and challenged with N23Ps (HLM1196), Nintedanib, or Tranilast. N23Ps proposes a shift toward dismantling cellular physical infrastructure. By disabling the machinery for stiffness sensing and secretion, HLM1196 arrests complex multicellular circuits of human lung fibrosis."

Fibrosis • Idiopathic Pulmonary Fibrosis • Immunology • Pulmonary Disease • Respiratory Diseases • CTHRC1 • KRT17 • NOX4 • RHOA • SPP1

Tranilast/roxithromycin with topical tacrolimus in refractory atopic facial eczema: Case report. (PubMed, Int J Clin Pharmacol Ther) - "Within 3 weeks, his eczematous lesions on the face, as well as the severe itching, were completely cured. Addition of this combination therapy may be a promising therapeutic strategy for treating uncontrollable atopic dermatitis, particularly for facial eczema and itching."

Journal • Atopic Dermatitis • Dermatitis • Dermatology • Immunology • Pediatrics

Characterization of TRPV2-associated pathology in Parkinson's disease and therapeutic modulation using Tranilast. (PubMed, Front Cell Neurosci) - "Also, it diminished the intracellular Ca2+ influx and reduced ROS levels in the 6-OHDA-treated SH-SY5Y cells. Overall, our results suggest that TRPV2 levels are elevated in PD, and targeting TRPV2 could be a potential therapeutic approach in the future."

Journal • CNS Disorders • Movement Disorders • Parkinson's Disease • TRPV2

Targeting NLRP3 inflammasome to mitigate chemotherapy-induced cardiotoxicity: advances in selective inhibitors and natural modulators. (PubMed, Mol Biol Rep) - "This broader perspective illustrates the wider impact of inflammasome-mediated pathophysiology in chemotherapy-induced cardiac failure and goes beyond traditional doxorubicin-centered treatments. The review also provides an overview of the therapeutic landscape of selective NLRP3 inhibition, including natural modulators such as oridonin, curcumin, resveratrol, honokiol, and flavonoids, as well as synthetic inhibitors such as MCC950, CY-09, OLT1177 (dapansutrile), and tranilast...Despite encouraging preclinical findings, translational challenges remain, including long-term safety assessment. Modulation of NLRP3 inflammasome activation has emerged as a potential intervention to limit chemotherapy-induced cardiac injury and dysfunction in cardio-oncology."

Journal • Review • Cardiovascular • Congestive Heart Failure • Heart Failure • Metabolic Disorders • Oncology • IL18 • IL1B • NLRP3 • TXNIP

Novel Oral Treatment of Anastomotic Stenosis After Salvage Extended Sleeve Lobectomy. (PubMed, Ann Thorac Surg Short Rep) - "The patient was treated with oral tranilast and clarithromycin, which resulted in significant improvement in the stenosis within 4 weeks. This case highlights the potential efficacy of antiinflammatory medications in managing anastomotic stenosis and preventing granulation tissue formation."

Journal • Lung Cancer • Oncology • Solid Tumor

Multimodal PET Imaging Reveals Stromal Remodeling–Driven Enhancement of Adoptive γδ T Cell Therapy in Fibrotic Triple-Negative Breast Cancer (SNMMI 2026) - "This study demonstrates that antifibrotic treatment with tranilast can sensitize fibrotic TNBC to adoptive γδ T cell therapy by relieving stromal barriers and enhancing immune cell infiltration. By integrating [68Ga]Ga-FAPI-04 and [68Ga] Ga-LLP2A-based PET imaging, we establish a noninvasive, imaging-guided framework to visualize stromal remodeling and γδ T cell trafficking in vivo. This approach provides mechanistic insight into fibrosis-driven resistance to adoptive cell therapy and offers a clinically translatable strategy for optimizing γδ T cell–based immunotherapy in desmoplastic solid tumors."

IO biomarker • Stroma • Breast Cancer • Fibrosis • Immunology • Oncology • Solid Tumor • Triple Negative Breast Cancer • CAFs • CD31 • PECAM1 • TGFB1

Sustainable Synthesis of Novel Hydroxylated Tranilast Analogues and Their Bioactivities. (PubMed, Molecules) - "Furthermore, some derivatives significantly reduced nitric oxide production in LPS-stimulated HaCaT cells, confirming their anti-inflammatory potential. Overall, hydroxylation proves to be an effective strategy for improving the biological profile of Tranilast, yielding promising candidates for further pharmacological development."

Journal • Genito-urinary Cancer • Infectious Disease • Oncology • Pneumonia • Prostate Cancer • Solid Tumor

Structural Modification of Tranilast against Poxvirus Based on α, β-Unsaturated Acrylamide Covalent Warhead and Confirmation of the Targets and Mode of Action. (PubMed, J Med Chem) - "The acrylamide warhead in 8l forms covalent adducts with serine residues of both targets via Michael addition. This work provides a promising covalent lead and identifies potential targets for the development of broad-spectrum anti-orthopoxvirus agents."

Journal • Infectious Disease

Fast-Dissolving Sodium Alginate-Based Microneedle Patch Integrating Tranilast and Glabridin-Loaded Nanoparticles for Dual-Action Hypertrophic Scar Therapy. (PubMed, Biomater Res) - "In vivo studies in a rabbit ear HS model demonstrate accelerated HS healing, reduced HS thickness, epidermal thickness index (ETI), scar elevation index (SEI), and collagen deposition, along with decreased profibrotic markers, inflammatory cytokines, and angiogenic factors. Overall, the TS+GLNPs@sMN patch offers a minimally invasive, self-administrable, dual-action therapeutic strategy for enhanced HS management, with safety and efficacy in preclinical models."

Journal • Dermatology • Fibrosis • Pain • Pruritus

Tranilast ameliorates experimental abdominal aortic aneurysm by inhibiting the NLRP3 inflammasome pathway. (PubMed, J Pharm Anal) - "Additionally, tranilast treatment reduced caspase 1 cleavage by the NLRP3 inflammasome and consequently interleukin-1β secretion in peritoneal macrophages in vitro. These findings indicate that the protective effect of tranilast on AAA may be partially mediated by the inhibition of the NLRP3 inflammasome pathway and may represent a potential drug for the treatment of AAA in the clinic."

Journal • Cardiovascular • Inflammation • ELANE • IL1B • NLRC5 • NLRP3

Heat and Heal: Microwave-Responsive Gelling Hydrogel Nanocomposites for Postablation Extracellular Matrix Normalization and Chemotherapy Sensitization. (PubMed, ACS Appl Mater Interfaces) - "The nanocomposite was prepared by dispersing polymeric nanoparticles, comprising a CaCl2-rich core and a tranilast-loaded shell, into alginate solution...By integrating microwave sensitization with postablation microenvironment regulation, this strategy simultaneously resolves insufficient heating and aberrant ECM remodeling, enabling improved chemotherapeutic efficacy. This simple and biocompatible platform provides a rational approach for improving local tumor MWA and reducing postablation recurrence."

Journal • Oncology

Prospects for solving difficulties in steroid withdrawal and management supplementing tranilast and roxithromycin in corticosteroid-dependent atopic dermatitis. (PubMed, Int J Clin Pharmacol Ther) - "One approach involves combining the anti-allergic drug tranilast, which inhibits mast cell degranulation, with the unique macrolide antibiotic roxithromycin, known for its T helper type 2 (Th2) suppressive effect. Moreover, we examine the methods for managing steroid-dependent atopic dermatitis, a condition that poses significant challenges in terms of withdrawal."

Journal • Atopic Dermatitis • CNS Disorders • Dermatitis • Dermatology • Immunology • Psychiatry

TRPV2 is essential for calcium signalling in the early stages of myogenesis. (PubMed, Biochem Biophys Res Commun) - "The effect of TRPV2 on Ca2+ signalling during early myogenesis is unknown; however, here, we demonstrate that tranilast, an inhibitor of TRPV2, suppressed IP3R-derived Ca2+ oscillations in early myogenesis. The addition of adenovirus (Ad)-TRPV2 or Ad-Cre recombinase to floxed-TRPV2 cells modulated TRPV2 expression, and demonstrated the TRPV2 dependence of IP3R and MEF2c expression, nuclear translocation of MEF2c, and Ca2+ oscillations. These findings indicate that TRPV2 regulates intracellular Ca2+ signalling during early myogenesis and highlight its potential as a target for the prevention and treatment of muscle disorders."

Journal • MEF2C • TRPV2

Development and in vivo evaluation of a self-polymerizable tranilast-loaded silicone gel for scar modulation. (PubMed, J Biomater Appl) - "Hydroxyproline content was significantly reduced in the tranilast group compared to both control and silicone-only groups (p < 0.01), accompanied by decreased α-SMA expression (27-30%), indicating suppression of myofibroblast activity. These findings demonstrate that the self-polymerizable silicone gel provides an effective delivery platform for tranilast, offering synergistic benefits in scar modulation and supporting its potential for advanced topical scar management."

Journal • Preclinical • Fibrosis

Anti-Inflammatory Lindolin Alkaloids Repress the Transcription of the Microsomal Prostaglandin E2 Synthase-1 Gene in Macrophages. (PubMed, J Nat Prod) - "Structure-activity relationship studies revealed that four lindolin analogs with enhanced anti-inflammatory activity possess an ortho-substituted carboxyl group, a structural feature shared with the clinically used antiallergic drug tranilast. Due to their high selectivity toward the mPGES-1 gene expression, lindolins represent promising lead structures for the development of selective mPGES-1 inhibitors with a novel mode of action. Moreover, these findings highlight early-diverging fungi as underestimated source of compounds with pharmaceutical potential."

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Tranilast Does Not Inhibit TRPV2. (PubMed, Cells) - "Instead, tranilast seems to indirectly suppress channel activation by reducing reactive oxygen species (ROS). This refined understanding of how tranilast modulates TRPV2 has important implications for the interpretation of prior and future pharmacological studies targeting TRPV2."

Journal • Hematological Malignancies • Leukemia • Oncology • TRPA1 • TRPV2

Study on the Effectiveness of Tranilast in the Treatment of Medium to Large Volume Benign Prostatic Hyperplasia (clinicaltrials.gov) - P1 | N=30 | Recruiting | Sponsor: Yifeng Jing | Not yet recruiting ➔ Recruiting | Trial completion date: Dec 2025 ➔ Dec 2026 | Trial primary completion date: Dec 2025 ➔ Dec 2026

Enrollment open • Trial completion date • Trial primary completion date • Benign Prostatic Hyperplasia

Efficacy and safety of tranilast combined with minocycline in the treatment of moderate-to-severe rosacea: a prospective, randomized controlled study. (PubMed, J Dermatolog Treat) - P4 | "In our study, patients with moderate to severe rosacea treated with tranilast showed a favorable clinical response and experienced no serious adverse events. The combination therapy yielded better outcomes than minocycline monotherapy, especially in improving facial erythema."

Clinical • Journal • Dermatology • Inflammation • Rosacea

Tranilast inhibits cell proliferation, migration and invasion of human hypertrophic scar fibroblasts by NOP2-mediated m5C methylation on COL1A1. (PubMed, Tissue Cell) - "Tranilast downregulates NOP2 to inhibit m5C modification of COL1A1, thereby suppressing COL1A1 expression and impairing HSFB proliferation, invasion, and migration. This study may provide a novel theoretical basis the mechanism of tranilast regulation of HS."

Journal • Dermatology • COL1A1 • NOP2

Solid Tranilast Nanocrystal-Loaded Cationic Contact Lenses for Sustained Ocular Drug Delivery. (PubMed, Pharmaceutics) - "TRA-laden cationic CLs prepared using the hThP method achieved sustained and higher drug delivery into the lacrimal fluid and aqueous humor than those prepared using the conventional soaking method. Conclusions Our findings suggest that TRA-laden cationic CLs prepared using STNs and the hThP method can overcome the challenges associated with the conventional soaking method, including low drug uptake and high burst release."

Journal • Corneal Abrasion • Ophthalmology

A paradigm for sustainable analysis: QbD-driven HPLC-DAD for triple antiallergics in pharmaceutical, biological, and environmental samples. (PubMed, J Chromatogr B Analyt Technol Biomed Life Sci) - "This study introduces an innovative approach combining Quality by Design (QbD) principles with high-performance liquid chromatography and diode array detection (HPLC-DAD) for the simultaneous analysis of tranilast (TNL), pranoprofen (PPF), and chlorpheniramine maleate (CPM), a novel antiallergic combination therapy...A holistic sustainability assessment confirmed the method's environmental and economic viability, featuring low solvent use, minimal sample preparation, and long-term durability, in line with green analytical chemistry principles. This integrated strategy provides an efficient solution for the quality control of complex ophthalmic formulations, facilitating the development of safer and more effective antiallergic therapies."

Journal • Ophthalmology

Management and Clinical Outcomes of Scleredema Diabeticorum: A Scoping Review. (PubMed, Diseases) - "PUVA, UVA-1, and IVIG may offer benefit, while methotrexate alone is often ineffective. Evidence is predominantly from case reports and small series, which makes it difficult to generalize. Multicenter trials with standardized protocols are needed to develop evidence-based treatment recommendations."

Clinical data • Journal • Review • Diabetes • Metabolic Disorders

Complications of auricular cartilage harvest in rhinoplasty: Keloid and epidermal cyst formation. (PubMed, World J Clin Cases) - "In the few studies reporting this rare occurrence, various treatment protocols exist consisting of various combinations of surgical excision, intralesional corticosteroid injections, chemotherapeutic agents, laser therapy, radiotherapy, isotretinoin, and tranilast. As advancements in the comprehension and treatment of epidermoid cysts within keloid scars progress, customized therapeutic approaches provide promise for enhancing patient outcomes and quality of life."

Journal • Aesthetic Medicine • Fibrosis • Immunology • Oncology • Squamous Cell Carcinoma

Investigation of the Putative Relationship Between Copper Transport and the Anticancer Activity of Cisplatin in Ductal Pancreatic Adenocarcinoma. (PubMed, Cells) - "Two major strategies were pursued: (i) inhibiting copper transporters ATP7A and B with tranilast (TR) and omeprazole (OM) to block the cellular copper and, potentially, also cisplatin efflux, and (ii) using the chelator elesclomol (ES) to elevate intracellular copper and cisplatin levels. Moreover, all drugs contributed to the enhanced cellular anticancer activity of cisplatin, with ES being the most effective compound. The results suggest that the targeted modulation of copper transport mechanisms may offer novel adjuvant approaches for the treatment of PDAC."

Journal • Hepatocellular Cancer • Oncology • Pancreatic Adenocarcinoma • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • Solid Tumor • ATP7A

Ectomycorrhizal Fungi Associated with Pinus cembroides subsp. orizabensis, an Endemic Pine in the Arid Zones of the Oriental Basin, Puebla, Mexico. (PubMed, J Fungi (Basel)) - "This is the first report of EMF fungi associated with Pinus cembroides subsp. orizabensis, as well as the first record of G. arenicola in arid pine forests in Mexico."

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