Glanatec (ripasudil) / Kowa - LARVOL DELTA

Study to Assess Safety and Tolerability of Multiple Doses of EO2002 (clinicaltrials.gov) - P1 | N=12 | Recruiting | Sponsor: Asociación para Evitar la Ceguera en México | Trial primary completion date: Jul 2025 ➔ Dec 2025

Trial primary completion date • Ophthalmology

A human-specific RPGR isoform and a clinically approved Rho/ROCK inhibitor ameliorate defects associated with RPGR dysfunction. (PubMed, Mol Ther Nucleic Acids) - "Conversely, treatment with ripasudil-a clinically approved Rho/ROCK inhibitor-rescued both ciliary and actin-related defects in RPGR_KO lines without observable cellular side effects. In summary, our findings highlight the therapeutic relevance of the human-specific isoform RPGR s14/15 and identify ripasudil as a promising candidate for treating RPGR-associated retinal degeneration."

Journal • Genetic Disorders • Inherited Retinal Dystrophy • Ocular Inflammation • Ophthalmology • Retinal Disorders • Retinitis Pigmentosa • TERT

Isoform-specific regulation of PKM by acetylation. (PubMed, Proc Natl Acad Sci U S A) - "We also show that, in contrast to K115 acetylation, previously reported acetylation of K305 inhibits PKM2 but has no effect on the activity and oligomerization of PKM1. These findings propose the existence of both uniform and isoform-specific regulatory mechanisms of PKM, mediated by acetylation."

Journal • PKM

A Study to Investigate the Safety and Efficacy of K-321 Eye Drops After Simultaneous Cataract Surgery and Descemetorhexis in Participants With Fuchs Endothelial Corneal Dystrophy (FECD) (clinicaltrials.gov) - P3 | N=110 | Completed | Sponsor: Kowa Research Institute, Inc. | Active, not recruiting ➔ Completed

Trial completion • Cataract • Ophthalmology • Transplantation

SENP3 mediated DeSUMOylation of macrophage derived CCL17 accelerates atherosclerosis via regulation of Treg. (PubMed, Cell Biol Toxicol) - "This study showed that SENP3 mediated deSUMOylation of CCL17, increase CCL17 expression in macrophage. CCL17 secreted by macrophage regulating Treg recruitment through the competitive interaction between CCL17 and CCL22 and thus aggravated AS. Our findings provide a new regulatory mechanism and potential target for AS treatment."

Journal • Atherosclerosis • Cardiovascular • Dyslipidemia • Inflammation • APOE • CCL2 • CCL22 • SENP3

Ripasudil as a treatment for corneal bullae: a potential role in enhancing corneal endothelial function. (PubMed, Eye (Lond)) - No abstract available

Journal

Design, development, and in vivo characterization of ocular pH-based in situ thixotropic gelling system for the therapy of Glaucoma. (PubMed, Int J Biol Macromol) - "The objective of this work was to formulate a preservative-free single-dose topical thixotropic in situ gel loaded with Ripasudil hydrochloride hydrate, a Rho kinase (ROCK) inhibitor that enhances conventional aqueous outflow via the trabecular meshwork and Schlemm's canal...A significant reduction in the intraocular pressure was observed in diseased BALB/c mice. The findings confirmed the safe and stable nature of the developed formulation; however, it warrants further investigation via pharmacokinetics studies and clinical trials."

Journal • Preclinical • Glaucoma • Ophthalmology

Identification of Amino acid substitutions in the Hepatitis C virus core region associated with the development of hepatocellular carcinoma in treatment-naive patients in Cameroon - a 10-year retrospective cross-sectional study. (PubMed, Virus Res) - "The analysis revealed mutations significantly related to sex and year, such as (K115R, N106S, T48A) with p-values of (0.0023; 0.0006), (0.0012; 0.0004) and (0.0045; 0.0058) respectively. This study provides the first comprehensive mapping of HCV core mutations in Cameroon, identifying variants potentially linked to HCC. Although limited by the lack of clinical follow-up, it underscores the urgency of monitoring these mutations in national HCV elimination programs, in line with the WHO's goals for 2030."

Journal • Observational data • Retrospective data • Hepatitis C • Hepatocellular Cancer • Infectious Disease • Liver Cirrhosis • Oncology • Solid Tumor

Efficacy and safety of descemet stripping only combined with ripasudil for treating fuchs dystrophy at a leading center in Spain (EVER 2025) - No abstract available

Clinical • Ophthalmology

Unveiling New Process Impurities in Ripasudil Hydrochloride Dihydrate: Identification, Synthesis, and Characterization. (PubMed, Curr Org Synth) - "The two new process impurities have been prepared and used as impurities for the method development and quality evaluation of the Ripasudil drug substance. Given the regulatory significance of Ripasudil hydrochloride, our successful synthesis and characterization efforts have proven to be valuable. This research offers valuable insights into the generic pharmaceutical industry."

Journal • Cardiovascular • Glaucoma • Ophthalmology

Co-Delivery of Ripasudil and Dexamethasone in Trabecular Meshwork Cells for Potential Prevention of GC-Induced Ocular Hypertension. (PubMed, Exp Cell Res) - "Additionally, Rip upregulated ITGA11, a gene that promotes actin cytoskeleton reorganization and TM cell relaxation by inhibiting the Rho-ROCK pathway. Overall, co-delivery or sequential delivery of Rip can reverse or prevent Dex-induced ocular hypertension and glaucoma formation by modulating the expression of glaucoma-related genes at the transcriptional level."

Journal • Cardiovascular • Glaucoma • Ophthalmology • ACTA2 • COL11A1 • COL1A1 • ECM2 • ITGA1

RhoKinase (ROCK) Inhibition as a Therapeutic Strategy for Pseudophakic Bullous Keratopathy: A Comprehensive Review. (PubMed, J Clin Med) - "ROCK inhibitors represent a novel pharmacological strategy for PBK prevention and management, potentially reducing dependency on donor grafts. Further research is needed to determine long-term safety, optimal dosing, and efficacy."

Journal • Review • Cataract • Ophthalmology • Pain • Transplant Rejection • Transplantation

Invigorating effect on corneal endothelium observed with ripasudil. (PubMed, Eye (Lond)) - No abstract available

Journal

Management of corneal oedema in Fuchs' endothelial dystrophy using ripasudil. (PubMed, BMJ Case Rep) - No abstract available

Journal • Ophthalmology

LncRNA BASP1-AS1 Drives PCBP2 K115 Lactylation to Suppress Ferroptosis and Confer Oxaliplatin Resistance in Gastric Cancer. (PubMed, Free Radic Biol Med) - "Concurrently, BASP1-AS1-mediated histone H3K14 lactylation transcriptionally upregulates both LDHA and PCBP2, generating a self-amplifying metabolic-epigenetic circuit. This axis critically suppresses ferroptosis and maintains chemoresistance, providing actionable targets for overcoming oxaliplatin resistance in GC."

Journal • Gastric Cancer • Oncology • Solid Tumor • Targeted Protein Degradation • BASP1 • LDHA

A Comprehensive Review of the Role of Rho-Kinase Inhibitors in Corneal Diseases. (PubMed, Life (Basel)) - "ROCKI, such as ripasudil and netarsudil, enhances endothelial cell migration, and promotes repair in conditions characterized by endothelial dysfunction. This narrative review provides a comprehensive evaluation of ROCKI's mechanism of action, pharmacological properties, safety profile, applications in corneal disease management, emerging clinical trials, and novel approaches. We emphasize both preclinical and clinical findings, highlight existing evidence gaps, and outline future research priorities."

Journal • Review • Cataract • Inflammation • Ophthalmology • Transplantation

Clinical Evaluation of Ripasudil for Corneal Edema: A Large-Scale Retrospective Cohort Study. (PubMed, J Clin Med) - " No adverse events or progression of edema were recorded during the follow-up period. These findings support the role of Ripasudil as a non-invasive pharmacological approach to managing corneal edema and delaying or possibly avoiding surgical interventions, such as corneal transplantation, in selected cases."

Journal • Retrospective data • Cataract • Ophthalmology • Transplantation

Therapeutic Potential of Rho Kinase Inhibitors in Corneal Disease: A Systematic Review of Preclinical and Clinical Studies. (PubMed, Biomedicines) - "Preclinical models (rabbit, porcine, human explants) uniformly showed ROCKis (Y-27632, Ripasudil, Netarsudil, H-1152) accelerate corneal endothelial cell proliferation, migration, and restoration of a hexagonal monolayer with improved barrier and pump function over days to weeks. ROCKis demonstrate consistent pro-regenerative effects on corneal endothelium in multiple models and show promising clinical efficacy in Fuchs endothelial dystrophy and pseudophakic endothelial failure. Future work should explore novel delivery systems and larger controlled trials to optimize dosing, safety, and long-term outcomes."

Journal • Preclinical • Review • Ophthalmology

Human endogenous retrovirus-K envelope protein is aberrantly expressed in serous ovarian cancer and promotes chemosensitivity via NF-κB/P-glycoprotein pathway inhibition. (PubMed, J Ovarian Res) - "HERV-K env was expressed in serous ovarian carcinoma and significantly associated with chemosensitivity. HERV-K env attenuated NF-κB/P-glycoprotein, a mechanism of chemoresistance. Hence, it could have therapeutic potential in chemoresistant ovarian cancers."

Journal • Oncology • Ovarian Cancer • Ovarian Serous Adenocarcinoma • Solid Tumor

DETECT I: Descemet Endothelial Thickness Comparison Trial I (clinicaltrials.gov) - P3 | N=160 | Recruiting | Sponsor: Stanford University | Trial completion date: Aug 2027 ➔ Nov 2027 | Trial primary completion date: Jul 2026 ➔ Oct 2026

Trial completion date • Trial primary completion date

Neuroprotective effect of ripasudil on retinal ganglion cells via an antioxidative mechanism. (PubMed, Jpn J Ophthalmol) - "Ripasudil may have neuroprotective effects via an antioxidative mechanism, which could be useful as an intraocular pressure-independent additive."

Journal • Glaucoma • Ophthalmology

A Case of Corneal Endothelial Cell Loss After PreserFlo MicroShunt Implantation Requiring Device Removal and Ahmed Glaucoma Valve Implantation With Tube Insertion Into the Vitreous Cavity. (PubMed, Cureus) - "After the second surgery, IOP stabilized between 10 and 14 mmHg with topical treatment, including ripasudil, and ECD remained stable at approximately 1,200 cells/mm². This case demonstrates the potential for significant and progressive ECL following PMS implantation and highlights that timely intervention with PMS removal and AGV implantation with tube insertion into the vitreous cavity can effectively stabilize ECD and achieve adequate IOP control, emphasizing the importance of close postoperative monitoring and the prompt management of complications."

Journal • Cataract • Glaucoma • Ophthalmology

Rho kinase inhibitors: a patent review (2017 - 2023). (PubMed, Expert Opin Ther Pat) - "Fasudil, ripasudil, netarsudil, and belumosudil are the primary ROCK inhibitors approved for human use. Despite some pharmacokinetic challenges, research in this field continues to advance, with significant potential for further clinical development."

Journal • Review

LINC00525 drives aggressive phenotypes in bladder cancer via YAP stabilization-mediated transcriptional activation. (PubMed, Cancer Cell Int) - "Additionally, LINC00525 inhibited YAP ubiquitination by acting on YAP lysine 321 (K321), thereby increasing its stability to prevent degradation. Through in vivo and in vitro experiments, we demonstrated the YAP-mediated promoting effect of LINC00525 on bladder cancer cells and tumor growth. Our study reveals the involvement of the LINC00525/YAP axis in regulating bladder cancer development, suggesting a potential therapeutic strategy for malignant tumors characterized by high levels of LINC00525 expression."

Journal • Bladder Cancer • Genito-urinary Cancer • Oncology • Solid Tumor • Targeted Protein Degradation

Liposome Encapsulation Enhances Ripasudil Therapeutic Efficacy Against Proliferative Vitreoretinal Diseases: Implications in Advanced Ocular Treatment. (PubMed, Invest Ophthalmol Vis Sci) - "These characteristics resulted in a sustained elevation of drug concentration within the ocular tissues over time. Our findings suggest that liposomal encapsulation of ripasudil supports enhanced bioavailability and effectiveness of the drug, presenting a promising innovative therapeutic approach for the treatment of proliferative vitreoretinopathy."

Journal • Age-related Macular Degeneration • Fibrosis • Immunology • Macular Degeneration • Ophthalmology • Retinal Disorders • Wet Age-related Macular Degeneration