Glanatec (ripasudil) / Kowa - LARVOL DELTA

Efficacy, effectiveness, and safety of rho-kinase inhibitors in uveitic glaucoma and ocular hypertension secondary to uveitis: a systematic review and meta-analysis. (PubMed, Graefes Arch Clin Exp Ophthalmol) - "ROCK inhibitors demonstrate significant and sustained IOP-lowering effects in UG and OHT-SU with a favorable safety profile. Their additive effect with conventional treatments and potential benefits in surgical outcomes highlight their role as promising therapeutic agents. Further clinical trials are needed to compare different ROCK inhibitors and assess their long-term safety and effectiveness in different populations."

Journal • Retrospective data • Review • Cardiovascular • Glaucoma • Ocular Inflammation • Ophthalmology • Pain • Uveitis

Rapid Isolation and Characterization of High-Affinity Single-Domain Antibodies for Broad-Spectrum Detection of SARS-CoV-2 Variants. (PubMed, Protein Eng Des Sel) - "Moreover, it enabled sensitive detection in western blotting and flow cytometry, highlighting its applicability across diverse diagnostic applications. Collectively, these findings identify K115.2-Fc as a promising candidate with potential for SARS-CoV-2 diagnostic utility."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

UBE2O-mediated monoubiquitination licenses NLRP6 inflammasome activation in the intestine. (PubMed, Cell Host Microbe) - "We demonstrate that the E3 ligase UBE2O catalyzes dual-site monoubiquitination of NLRP6: at K680-687 to drive oligomerization via a conformational change, and at K115/130 within the nuclear localization signal to enforce cytoplasmic sequestration through steric hindrance. Furthermore, the UBE2O inhibitor arsenic trioxide suppresses NLRP6-dependent interleukin (IL)-18 secretion in acute promyelocytic leukemia (APL) patients. Thus, UBE2O-mediated dual-site monoubiquitination emerges as a central mechanism licensing NLRP6 inflammasome activation, revealing a new target for modulating intestinal immunity."

Journal • Acute Promyelocytic Leukemia • Hematological Malignancies • Infectious Disease • Inflammation • Leukemia • Oncology • Rotavirus Infections • Targeted Protein Degradation • NLRP6

DETECT II: Descemet Endothelial Thickness Comparison Trial II (clinicaltrials.gov) - P3 | N=60 | Recruiting | Sponsor: Stanford University | Trial completion date: Aug 2028 ➔ Nov 2028 | Trial primary completion date: Aug 2027 ➔ Nov 2027

Trial completion date • Trial primary completion date • Ophthalmology

DETECT I: Descemet Endothelial Thickness Comparison Trial I (clinicaltrials.gov) - P3 | N=160 | Active, not recruiting | Sponsor: Stanford University | Recruiting ➔ Active, not recruiting

Enrollment closed

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