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

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."

Journal

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."

Journal

HBx promotes podocyte-macrophage transdifferentiation by mediating NLRP3 expression in hepatitis B virus-associated glomerulonephritis. (PubMed, Virol J) - "These findings indicate that HBx triggers NLRP3 upregulation in podocytes and activates PMT. Thereafter, podocytes may function as antigen-presenting cells (APCs), consequently stimulating immune cell activation and resulting in inflammation cascades and renal fibrosis associated with HBV-GN."

Journal • Fibrosis • Glomerulonephritis • Hepatitis B • Immunology • Infectious Disease • Inflammation • Lupus Nephritis • Nephrology • Renal Disease • CD68 • ICAM1 • NLRP3

A pathway to next-generation mast cell stabilizers identified through the novel Phytomedical Analytics for Research Optimization at Scale data platform. (PubMed, bioRxiv) - "Despite their potential, current MCS (e.g., cromolyn sodium, Tranilast, nedocromil) in clinical use are hindered by poor bioavailability, frequent dosing, long lags to onset of relief, and enigmatic mechanisms of action...The current study validates a subset of candidate phytomedical ngMCS using in silico workflow and in vitro pharmacology, and develops a new harmonic mean-based 'MCS score' for further streamlining of the candidate prioritization process. This proof-of-concept study may have particular relevance for complex presentations such as Mast Cell Activation Syndrome (MCAS) where ngMCS may outperform current management approaches."

Journal • Allergy • Immunology • Inflammation

TRPV2 Inhibition Prevents Right Ventricular Remodeling and Arrhythmia in Experimental Pulmonary Hypertension. (PubMed, FASEB J) - "This study aimed to explore whether TRPV2 contributes to SU5416/hypoxia (SuHx)-induced ventricular remodeling and arrhythmias, and its possible mechanisms...In the SuHx-induced PH rat model, TRPV2 inhibitor tranilast significantly reduced mean pulmonary artery pressure (mPAP) and pulmonary vascular remodeling; relieved ventricular remodeling, myocardial fibrosis, and hypertrophy; shortened the prolongation of QT, QTc, Tpeak-Tend interval, effective refractory period (ERP) and action potential duration (APD); reduced susceptibility to ventricular fibrillation (VF)...TRPV2 inhibition suppressed the IGF1-mediated Wnt/β-catenin signaling pathway. Our data support TRPV2 inhibition prevents PH-induced right ventricular remodeling and VF susceptibility; TRPV2 can serve as a therapeutic target for PH-induced VF."

Journal • Cardiovascular • Congestive Heart Failure • Fibrosis • Heart Failure • Hypertension • Immunology • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases • IGF1 • TRPV2

Ulcerative Sarcoidosis With Cutaneous Sarcoid Granulomatous Vasculitis Successfully Treated by Combination Therapy of Tranilast and Roxithromycin. (PubMed, J Dermatol) - No abstract available

Journal • Immunology • Sarcoidosis • Vasculitis

Montelukast vs Tranilast Administration in the Prevention of Capsular Contracture in Alloplastic Breast Surgeries: An Experimental Mice Model. (PubMed, Aesthet Surg J) - "Prophylactic tranilast administration significantly attenuates capsular contracture by reducing inflammation, macrophage infiltration, and collagen deposition, surpassing both postoperative tranilast and montelukast. These findings support prioritizing preoperative tranilast in clinical trials to improve breast implant outcomes."

Journal • Preclinical • Inflammation

TGF-β1-mediated downregulation of L1CAM in pancreatic ductal adenocarcinoma drives upregulation of collagen 17A1 and MMP2, facilitating tumor invasiveness and metastasis. (PubMed, Cell Death Dis) - "In vivo studies demonstrate that L1low cells correlate with increased collagen deposition, reduced sensitivity to gemcitabine, and heightened liver metastasis. By modulating collagen dynamics and enhancing drug delivery, Tranilast may improve treatment outcomes for patients with low L1CAM-expressing tumors. Understanding the mechanisms by which L1low cells contribute to collagen secretion and tumor aggressiveness is essential for developing effective interventions in pancreatic cancer."

Journal • Fibrosis • Oncology • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • Solid Tumor • COL17A1 • L1CAM • MMP2 • TGFB1

Therapeutic Effect of Tranilast on Lung Tumors Suspected of Being Staple Line Granulomas: Report of Two Cases. (PubMed, Surg Case Rep) - "Administration of tranilast can be a safe and effective diagnostic treatment for SG, when the treatment is performed with strict imaging follow-up and histologic biopsy in mind."

Journal • Kidney Cancer • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor

Design of Tranilast-Loaded Cation-Type Contact Lens for Sustainable Ocular Drug Delivery. (PubMed, Pharmaceutics) - "Furthermore, the TRA-loaded CL sustainably released TRA into the lacrimal fluid in the rabbit. The TRA-loaded CL prepared using the AC-method overcame the limitations normally associated with the stir-method, such as the high burst release and low drug uptake."

Journal

Noninvasive PET Imaging of Tumor Fibrosis and Immune Activation in Mechano-Immunotherapy (SNMMI 2025) - "We successfully developed a biomimetic antifibrotic nanoplatform, CPZT, which leverages the antifibrotic properties of tranilast to remodel the TME, enhance drug delivery, and facilitate immune cell infiltration. By utilizing [68Ga]Ga-FAPI PET to noninvasively visualize tumor fibrosis and [68Ga]Ga-GZP PET to assess CTL effector activity, we demonstrated the potential of CPZT for TME remodeling and immunotherapy enhancement. CPZT administration significantly improved the efficacy of immune checkpoint inhibitors, emphasizing the critical role of stromal modulation in overcoming therapeutic resistance."

Non-invasive • Breast Cancer • Fibrosis • Immunology • Oncology • Solid Tumor • CAFs

Lupus miliaris disseminatus faciei: A rare facial granulomatous disorder (CDA 2025) - "Variable improvement has been reported with systemic steroids, isotretinoin, dapsone, tetracycline or nitroimidazole-based antibiotics, antimalarials, antituberculosis therapy, tranilast, apremilast, tacrolimus, cyclosporine, and JAK inhibitors...Although doxycycline treatment failed, the patient improved with a tapering prednisone course and isotretinoin 60 mg daily...While it often resolves spontaneously, early intervention is crucial to minimize cosmetic and psychological impacts. The variable efficacy of treatments highlights the need for tailored therapeutic approaches."

Aesthetic Medicine • Dermatitis • Dermatology • Immunology • Infectious Disease • Inflammation • Inflammatory Arthritis • Lupus • Respiratory Diseases • Rosacea • Sarcoidosis • Tuberculosis

TRPV2 channels facilitate pulmonary endothelial barrier recovery after ROS-induced permeability. (PubMed, Redox Biol) - "The inhibition of either TRPV2 with tranilast or a disintegrin and metalloprotease domain-containing protein 10 (ADAM10) with GI254023X significantly reduced H2O2-induced VE-cadherin cleavage, while TRPM2 inhibition by econazole significantly increased H2O2-driven VE-cadherin cleavage and blockage of TRPV4 showed no effect...This process of cadherin-switching did not occur upon inhibition of TRPV2 or ADAM10. Our results highlight a novel role for TRPV2 as a redox sensitive ion channels in the microvascular endothelium and provide insight into the mechanisms underlying pulmonary microvascular endothelial barrier recovery."

Journal • ADAM10 • CDH2 • CDH5 • TRPV2

Successful Treatment of Both Cutaneous and Extracutaneous Lesions in Systemic Sarcoidosis With Tranilast. (PubMed, J Dermatol) - No abstract available

Journal • Immunology • Sarcoidosis

Combating Breast Cancer-associated Metastasis using Paclitaxel and Tranilast-loaded Human Serum Albumin Nanoparticles. (PubMed, Drug Dev Ind Pharm) - "HSA nanoparticles enhance the delivery and accumulation of hydrophobic drugs (PTX and TRA) in breast cancer cells, offering improved therapeutic outcomes. This combinatorial strategy permits further preclinical investigation for synergistic breast cancer management."

Journal • Breast Cancer • Oncology • Solid Tumor • TGFB1

Tranilast Reduces Intestinal Ischemia Reperfusion Injury in Rats Through the Upregulation of Heme-Oxygenase (HO)-1. (PubMed, J Clin Med) - "Administration of Tranilast led to a marked reduction in mortality, inflammation and intestinal permeability and damage. The study proved that Tranilast functions through upregulation of heme oxygenase-1."

Journal • Preclinical • Cardiovascular • Infectious Disease • Inflammation • Reperfusion Injury • Septic Shock • Transplantation • HMOX1