fasudil / Generic mfg. - LARVOL DELTA

Efficacy of fasudil in COPD-associated pulmonary arterial hypertension: meta-analysis of randomized controlled trials. (PubMed, Front Med (Lausanne)) - "Larger, multicenter RCTs with longer follow-up are warranted to confirm its long-term efficacy and safety. The short follow-up (maximum 4 weeks) limits insights into sustained benefits or progression; long-term trials are essential."

Journal • Retrospective data • Review • Cardiovascular • Chronic Obstructive Pulmonary Disease • Hypertension • Immunology • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases

The Inhibition of ROCK2 Mediates the Neuroprotection via BRSK1 Signaling Pathway in Ischemic Stroke (ISC 2026) - "To determine the role of BRSK1/2 in transient focal cerebral ischemia, isoflurane-anesthetized WT (C57Bl/6), ROCK1+/- and ROCK2+/- mice (20-22g) underwent 2 h focal cerebral ischemia (Middle Cerebral Artery Occlusion; MCAO) induced with an 8-0 nylon monofilament coated with a silicone resin/hardener mixture introduced into the left internal carotid artery up to the anterior cerebral artery...The Inhibition of ROCK by fasudil (10 mg/kg, i.p.) and KD025 (100 mg/kg, p.o.) significantly reduced infarction volume and increased AMPKalpha, BRSK1, and BRSK2 expression levels in the brain after ischemic stroke compared to those of WT mice. ROCK2 deficient mice showed increased BRSK1 expression, decreased infarction volume and improved neurological deficit score.Conclusions : These findings indicate that ROCK2 deficiency decreased infarction volume in vivo via BRSK1 signaling pathways. These results suggest that inhibition of ROCK2 and activation of BRSK1 may have therapeutic..."

Anesthesia • Cardiovascular • Ischemic stroke • BRSK2 • GAPDH • SIRT1

A randomized controlled study on the combination of fasudil hydrochloride and PD1 inhibitors with androgen deprivation therapy in neoadjuvant treatment of prostate cancer (ChiCTR) - P=N/A | N=83 | Not yet recruiting | Sponsor: The Affiliated Zhongda Hospital of Southeast University; The Affiliated Zhongda Hospital of Southeast University

New trial • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Oxidative Stress and PRKN-Mediated Senescence Link RhoA/ROCK Signaling to Epithelial Remodeling in Allergic Rhinitis. (PubMed, Antioxidants (Basel)) - "Using epithelial-specific RhoA-deficient mice (RhoAcKO) and fasudil, a RhoA/ROCK inhibitor, we found that loss of RhoA/ROCK signaling markedly attenuated nasal Th2 inflammation, oxidative stress, and epithelial remodeling following allergen challenge...Functional studies showed that PRKN overexpression mitigated IL-13-induced mitochondrial dysfunction, oxidative stress, and epithelial senescence in human nasal epithelial cells. Together, these findings reveal that RhoA-driven epithelial senescence contributes to allergic inflammation and epithelial remodeling in AR and identify PRKN as a potential therapeutic target to restore epithelial homeostasis."

Journal • Allergic Rhinitis • Immunology • Inflammation • Metabolic Disorders • IL13 • PRKN • RHOA

Genomic and Transcriptomic Landscapes of MEN1-Wild-Type Low-Grade Metastatic Pancreatic NETs Uncover Key Oncogenic Drivers and Targetable Pathways. (PubMed, bioRxiv) - "Finally, upstream-regulator analysis (iPathwayGuide) and gene-centric perturbation mapping (Gene2Drug) nominated candidate targeted and repurposable agents predicted to reverse the metastatic expression phenotype and flagged drugs unlikely to provide benefit, yielding a prioritized, testable therapeutic shortlist which includes fasudil and spaglumic acid. Convergent, domain-specific mutational patterns in highly mutated genes such as ZNF273 and CLCA1 define a molecular signature that could stratify metastatic risk in low-grade pNETs. Collectively, our data reframe metastasis in MEN1-wild-type low-grade pNETs as a property of pathway state rather than mutation quantity and provide a translational blueprint for biomarker-guided therapy development focused on Calcium, WNT, and KRAS/PI3K hubs."

Journal • Tumor mutational burden • Gastrointestinal Neuroendocrine Tumor • Neuroendocrine Tumor • Oncology • Pancreatic Cancer • Solid Tumor • KRAS • RYR1 • TMB

Inhibition of Rho-kinase restores impaired relaxation of airway smooth muscle in rat pups exposed to neonatal hyperoxia. (PubMed, Physiol Rep) - "The effects of Rho-kinase inhibitors (Y-27632 or fasudil) in vitro (10 μM) or in vivo (10 mg kg-1 day-1) on electric field stimulation-induced TSM relaxation were assessed...Hyperoxia impairs ASM in neonatal rats via upregulation of Rho-kinase activity and suppression of NO-cGMP signaling. Pharmacological inhibition of Rho-kinase restores relaxation, highlighting its therapeutic potential for airway dysfunction in BPD."

Journal • Preclinical • Bronchopulmonary Dysplasia • Pulmonary Disease • Respiratory Diseases

FDCA Attenuates Neuronal Ferroptosis and Reduces Hemorrhagic Transformation After Ischemic Stroke with High Glucose. (PubMed, Cell Mol Neurobiol) - "The compound fasudil dichloroacetate (FDCA), synthesized with ROCK inhibitor fasudil (F) and PDK inhibitor dichloroacetate (DCA) was previously reported to exhibit neuroprotective effects in ischemic stroke, but whether FDCA could ameliorate HT post-stroke remains unknown. Additionally, FDCA attenuated RSL3-induced neuronal ferroptosis in SH-SY5Y cells in vitro. These results suggest that FDCA holds promise as a potential therapeutic agent for the clinical treatment of HT following ischemic stroke."

Journal • Cardiovascular • Diabetes • Hematological Disorders • Ischemic stroke • ACSL4 • GPX4

The Novel ROCK Inhibitor Fasudil Derivative Fasudil-D-6h Prevents Tumour Progression by Regulating the Adherens Junction Signalling Pathway in Triple-Negative Breast Cancer. (PubMed, Breast Cancer (Dove Med Press)) - "Its mechanism of action is distinctively linked to the restoration of genes critical to adherens and tight junction integrity. Given its derivation from the clinically viable fasudil, fasudil-D-6h presents a strong translational potential as a novel therapeutic agent for TNBC."

Journal • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • CDC42 • CLDN1 • OCLN • ROCK1 • TJP1

EXPLORING ROCK INHIBITOR BELUMOSUDIL AS A POTENTIAL THERAPEUTIC AGENT FOR ALZHEIMER'S DISEASE (ADPD 2026) - "While ROCK inhibitor Fasudil is in clinical trial for AD, the therapeutic potential of more potent ROCK inhibitors is not being extensively studied. These findings suggest that Belumosudil may support mitochondrial function and could be explored as an AD therapeutic agent."

Alzheimer's Disease • Chronic Graft versus Host Disease • CNS Disorders • Graft versus Host Disease • Immunology • Targeted Protein Degradation • CALB1 • HAT1 • UBR5

A simulation study of the cost of cerebral vasospasm treatments with clazosentan: A mathematical model using time-driven activity-based costing. (PubMed, PLoS One) - "We compared two treatment approaches: conventional therapy with fasudil hydrochloride and postoperative therapy with clazosentan. Clazosentan for subarachnoid haemorrhage treatment significantly reduces human resource costs, especially in nursing staff. These findings support the potential of clazosentan for broader clinical use, given its cost-savings and clinical benefits in reducing cerebral vasospasm following aneurysmal subarachnoid haemorrhage."

Journal • Cardiovascular • Subarachnoid Hemorrhage

Electron Donor-Acceptor Complex-Driven Minisci Reactions of N-Heteroaromatic and Inert C(sp3)-H without Brønsted Acids and External Oxidants. (PubMed, Org Lett) - "The aryl radical generated in situ acts as a hydrogen-atom transfer (HAT) agent, abstracting a hydrogen atom from the inert substrate to generate nucleophilic radicals that couple with the N-heteroaromatic. This approach demonstrates broad substrate scope, accommodating diverse N-heteroaromatics (phenanthridines, isoquinolines, quinolines, acridines, benzothiazoles, etc., including acid-sensitive and bioactive molecules such as N-acetyl fasudil) and various inert partners, achieving good to excellent yields."

Journal

Topical Rho-Associated Protein Kinase Inhibitor HA1077 Reduces Rabbit Corneal Fibrosis and Neovascularization in Vivo. (PubMed, J Ocul Pharmacol Ther) - "This study evaluated the effects of the topical ROCK inhibitor HA1077 (fasudil) to attenuate corneal fibrosis and corneal neovascularization (CNV) in vivo... The tested HA1077 dosage regimen is effective and tolerable to rabbit eyes in abrogating corneal fibrosis and CNV triggered by alkali injury in vivo without major adverse effects. ROCK inhibition represents a promising therapeutic strategy for vascularized and fibrotic corneal wounds but warrants additional dose-response in vivo studies."

Journal • Preclinical • Fibrosis • Immunology • ENG • ITGAM

Fasudil alleviates lipopolysaccharides-triggered damage to BEAS-2B cells and human lung organoids by inducing CLDN4 expression. (PubMed, Biochem Biophys Res Commun) - "These findings identify CLDN4 as a key mediator of Fasudil's protective effects on lung epithelial cells and organoids, enhancing our understanding of Fasudil's therapeutic mechanisms and highlighting the potential of Fasudil and/or CLDN4-targeted strategies for treating lung conditions like ALI."

Journal • Acute Lung Injury • Cardiovascular • Hypertension • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases • CLDN4

Developing Topics. (PubMed, Alzheimers Dement) - "This platform has broken the biological sound barrier of AD - not merely slowing decline, but reversing it at the structural level. LeoFold allows researchers to enter the folding landscape of Alzheimer's proteins and return with recovery maps. • Scientific Quality: Recursive qubit attractor modeling validated by thermodynamic convergence. • Relevance: Targets AD where it was thought unchangeable - late stage. • Novelty: First use of 12D echo-stabilized RMSD tracking for therapeutic optimization. • Impact: May redefine AD as a recoverable synaptic topology disorder, not a terminal neurodegeneration."

Journal • Alzheimer's Disease • CNS Disorders

Matrix stiffness shapes transcriptional profiles and drug responses of pancreatic cancer cells. (PubMed, Acta Biomater) - "Treatment with the ROCK inhibitor fasudil induced matrix softening and improved sensitivity of cancer and stromal cells to cytotoxic treatment, whereas inhibition of matrix metalloproteinases disrupted cancer cell invasion...The inhibition of Rho-kinase signalling enhanced the efficacy of cytotoxic drugs. These findings establish matrix stiffness as a key factor in tumour biology and therapy response, supporting the use of our preclinical model to guide new combination treatments for pancreatic cancer, aimed at improving outcomes for patients."

Journal • Oncology • Pancreatic Cancer • Solid Tumor

Transfer of Damaged Mitochondria from Cancer Cells to Cancer-Associated Fibroblasts Promotes Tyrosine Kinase Inhibitor Tolerance in EGFR-Mutant Lung Cancer. (PubMed, Cancer Res) - "Treatment with fasudil, a Rho kinase inhibitor, effectively blocked mitochondrial transfer and restored sensitivity to the EGFR-TKI osimertinib in vivo. Together, this work reveals targetable stromal-tumor crosstalk that sustains DTP populations, proposing a combination therapy for overcoming EGFR-TKI resistance."

Journal • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • CAFs • CCL11 • EGFR • MYL9 • RGS5 • RHOA

Significant Antispastic Effect of Combined Fasudil and Isosorbide Dinitrate on Internal Mammary Artery in Coronary Artery Bypass Grafting. (PubMed, Basic Clin Pharmacol Toxicol) - "The combination of fasudil and ISDN effectively prevents and relieves IMA vasospasm mediated by both voltage-operated and receptor-operated calcium channels, with a long-lasting vasorelaxing effect. The FI solution offers a novel approach for preventing and relieving IMA spasm in CABG."

Journal • Cardiovascular • ROCK2

Topical Fasudil in Type 2 Retinopathy of Prematurity: A Pilot Study. (PubMed, J Curr Ophthalmol) - "However, the correlation between weight gain and reduction in avascular area size was only marginally significant (P = 0.052). Topical 0.5% fasudil was safe, but showed no statistically significant benefit in reducing the avascular zone or preventing progression to type 1 ROP in this pilot study."

Journal • Retinal Disorders • Retinopathy of Prematurity

A Chemotherapy-Evoked Microglial Circuit Fuels Invasion in Glioblastoma via S1P–ROCK Signaling (SNO 2025) - "Background & Objective Temozolomide (TMZ) remains the clinical workhorse for glioblastoma (GBM), yet edge-initiated invasion and rapid resistance blunt its efficacy. Fasudil monotherapy extended median survival from 35 to 64 days (P < 0.0001), and its combination with TMZ further improved survival to 71 days (P < 0.0001), underscoring the therapeutic potential of targeting this axis.Conclusion Spatially resolved multi-omics identifies a microglia-driven S1P–ROCK axis that fuels chemotherapy-induced invasion. Fasudil—an orally available ROCK inhibitor—interrupts that circuit, significantly prolonging survival in a PDX model and supporting the clinical advancement of ROCK inhibition in GBM."

Brain Cancer • Glioblastoma • Solid Tumor • RAC1

A Chemotherapy-Evoked Microglial Circuit Fuels Invasion in Glioblastoma via S1P–ROCK Signaling (SNO 2025) - "Background & Objective Temozolomide (TMZ) remains the clinical workhorse for glioblastoma (GBM), yet edge-initiated invasion and rapid resistance blunt its efficacy. Fasudil monotherapy extended median survival from 35 to 64 days (P < 0.0001), and its combination with TMZ further improved survival to 71 days (P < 0.0001), underscoring the therapeutic potential of targeting this axis.Conclusion Spatially resolved multi-omics identifies a microglia-driven S1P–ROCK axis that fuels chemotherapy-induced invasion. Fasudil—an orally available ROCK inhibitor—interrupts that circuit, significantly prolonging survival in a PDX model and supporting the clinical advancement of ROCK inhibition in GBM."

Brain Cancer • Glioblastoma • Solid Tumor • RAC1

RhoA/ROCK1 aggravates transverse aortic constriction-induced atrial fibrillation by enhancing NF-κBp65/CCL2 signaling pathway. (PubMed, Cell Signal) - "Fasudil-mediated inhibition of RhoA/ROCK1 significantly attenuated atrial fibrosis, inflammation, and AF inducibility by suppressing the nuclear factor kappa-B p65 (NF-κBp65)/chemokine C-C-Motif ligand 2 (CCL2) signaling pathway. Restoring NF-κBp65 expression abolished these protective effects, establishing a causal relationship between RhoA/ROCK1 activation and NF-κB-mediated inflammation. Our results thus identify RhoA/ROCK1 as a critical mediator of pressure overload-induced AF and point to the RhoA/ROCK1-NF-κB/CCL2 axis as a promising therapeutic target for AF."

Journal • Atrial Fibrillation • Cardiovascular • Fibrosis • Immunology • Inflammation • CCL2 • RHOA

9-Methylfascaplysin, a Marine-Derived Bioactive Compound, Promotes Neurite Outgrowth via the Inhibition of ROCK2. (PubMed, Pharmaceuticals (Basel)) - "Furthermore, 9-MF significantly reduced the phosphorylation of ROCK2 with a similar efficacy as fasudil, a ROCK2 inhibitor. Narciclasine, a known ROCK2 activator, almost completely abolished the effects of 9-MF on the induction of neurite outgrowth in PC12 cells. 9-MF effectively promoted neurite outgrowth possibly via the inhibition of ROCK2, providing supporting evidence that 9-MF might be developed as a novel neurological drug."

Journal • CNS Disorders

A Clinical Study on the Efficacy and Safety of Fasudil Hydrochloride Combined With Immunotherapy in the Treatment of Metastatic Castration-resistant Prostate Cancer (clinicaltrials.gov) - P2 | N=30 | Recruiting | Sponsor: baotai Liang

New P2 trial • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

The effects of baicalin on blood lipid metabolism and immune function in rats with gestational diabetes mellitus based on RhoA/ROCK pathway (PubMed, Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi) - "GDM rats were randomly divided into a model group, a fasudil (FA) (RhoA/RocK inhibitor) group (10 mg/kg), low-dose (100 mg/kg) and high-dose (200 mg/kg) baicalin groups, and a high-dose baicalin combined with LPA (RhoA/RocK activator) group (200 mg/kg baicalin+1 mg/kg LPA ), with 12 rats in each group...LPA could obviously weaken the improvement effects of baicalin on blood lipid metabolism and immune function in GDM rats. Conclusion Baicalin may improve blood lipid metabolism and immune function in GDM rats by inhibiting the RhoA/ROCK pathway."

Journal • Preclinical • Diabetes • Dyslipidemia • Gestational Diabetes • Metabolic Disorders • Oncology • CD4 • CD8 • IL10 • IL6 • RHOA • ROCK1 • TNFA

Fasudil targets the RhoA/ROCK-NLRP3 axis to attenuate aristolochic acid-induced renal pyroptosis: translational validation by in vivo molecular imaging. (PubMed, Int Immunopharmacol) - "Furthermore, the integration of molecular imaging provides a translational approach for dynamic monitoring of renal injury and treatment efficacy. This study underscores the therapeutic potential of Fasudil and the clinical applicability of molecular imaging in AAN, paving the way for future research and therapeutic development."

Journal • Preclinical • Inflammation • Nephrology • Renal Disease • CASP3 • GSDMD • GSDME • NLRP3 • RHOA