fasudil / Generic mfg. - LARVOL DELTA

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

Rho-ROCK signaling and α-Catenin mediate β-Catenin-driven hyperplasia in the adrenal via adherens junctions. (PubMed, bioRxiv) - "This study demonstrates that β-Catenin-driven hyperplasia in the adrenal cortex, a key feature of primary aldosteronism, is mediated through Rho-ROCK signaling and α-Catenin-dependent stabilization of adherens junctions, with significant implications for patients with primary aldosteronism. Rho-ROCK signaling drives AJ enrichment in the adrenalROCK inhibition via fasudil blunts aldosterone productionβCat drives adrenal hyperplasia via enhanced AJ enrichmentROCK inhibition or ɑCat deletion block zG hyperplasia."

Journal • Cardiovascular • Endocrine Disorders • CTNNB1

Phillyrin improves pulmonary epithelial barrier dysfunction in LPS-induced acute lung injury through the RhoA/ROCK signaling pathway. (PubMed, J Pharm Pharmacol) - "Phillyrin inhibits pulmonary edema, suppresses inflammation and oxidative stress in ALI rats, and improves LPS-induced alveolar epithelial barrier dysfunction by inhibiting RhoA/ROCK pathways."

Journal • Acute Lung Injury • Infectious Disease • Inflammation • Respiratory Diseases • MPO • MYLK • RHOA

Potential for multidrug combination therapy in patients with World Federation of Neurological Surgeons grade V subarachnoid hemorrhage. (PubMed, Neurosurg Rev) - "This study aimed to investigate whether any of the drugs currently used in Japan, where nimodipine is not approved, are effective for WFNS grade V SAH patients...Multivariate analyses revealed that pre-onset mRS 1-2, admission modified Fisher grade 4, ruptured middle cerebral artery aneurysm, acute hydrocephalus, and older age were independently associated with poor outcomes, while combination drug therapy with fasudil hydrochloride (Rho-kinase inhibitor) + cilostazol (phosphodiesterase type III inhibitor) + eicosapentaenoic acid (omega-3 polyunsaturated fatty acid) or clazosentan (endothelin receptor subtype A antagonist) + cilostazol was the only independent determinant of good outcomes. The combination drug therapies were also independent inhibitors of delayed cerebral infarction (non-iatrogenic cerebral infarction on computed tomography after SAH), but not of cerebral vasospasm (≥ 50% angiographic vasospasm of a major cerebral artery) and rescue therapy (endovascular..."

Journal • Retrospective data • Cardiovascular • CNS Disorders • Hematological Disorders • Subarachnoid Hemorrhage • Ventriculomegaly

Fasudil Alleviates Lipopolysaccharide-Mediated Injury in Rat Cardiomyocyte H9c2 Cells by Inducing Autophagy. (PubMed, Ann Clin Lab Sci) - "Fasudil induces autophagy in H9c2 cells. Treatment with LPS promotes autophagic flux and inhibits apoptosis, thereby exerting protective effects on the cells."

IO biomarker • Journal • Preclinical • Cardiomyopathy • Cardiovascular • Inflammation • BAX • BCL2 • CASP3

A Chemotherapy-Evoked Microglial Circuit Fuels Invasion in Glioblastoma via S1P–ROCK Signaling (WFNOS 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 • Oncology • Solid Tumor • RAC1

A Chemotherapy-Evoked Microglial Circuit Fuels Invasion in Glioblastoma via S1P–ROCK Signaling (WFNOS 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 • Oncology • Solid Tumor • RAC1

Clinical Study of Fasudil Hydrochloride and PD1 Inhibitor Combined With Androgen Deprivation in Neoadjuvant Therapy of Prostate Cancer (clinicaltrials.gov) - P2/3 | N=83 | Recruiting | Sponsor: baotai Liang | Not yet recruiting ➔ Recruiting

Enrollment open • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Effects of fasudil against photothrombotic stroke in genetically modified obese (ob/ob) mice. (PubMed, Metab Brain Dis) - "Collectively, these findings suggest that Fasudil confers neuroprotective effects following stroke in genetically modified obese (ob/ob) mouse model, independent of glycemic modulation. This study highlights the potential of Fasudil as a therapeutic target for acute ischemic stroke in the context of obesity and metabolic dysfunction, warranting further investigation in preclinical and clinical settings, particularly in patients with obesity and diabetes."

Journal • Preclinical • Cardiovascular • CNS Disorders • Diabetes • Genetic Disorders • Hematological Disorders • Ischemic stroke • Metabolic Disorders • Obesity • Thrombosis • NGFR • TXNIP

Oral treatment with Fasudil diminishes the capacity of ALS patient-derived exosomes to induce TDP-43 neuropathology in vitro (Neuroscience 2025) - "Our findings suggests that NDEs from ALS patients harbor pathogenic cargo capable of inducing TDP-43 redistribution and aggregation in motor neuron-like cells in vitro, and that this activity is attenuated following oral ROCK inhibition with Fasudil. Ongoing work will investigate changes in exosome proteomic signatures and alterations in TDP-43 structure or post-translational modifications that may contribute to the pathogenic potential of ALS patient-derived NDEs."

Preclinical • Amyotrophic Lateral Sclerosis • CNS Disorders • TARDBP

Non-monotonic pharmacodynamic effects of an oral Rho kinase inhibitor, fasudil, on neurofilament light chain and CNS target engagement: an open-label phase 2a study to assess safety and biomarker changes in patients with amyotrophic lateral sclerosis (Neuroscience 2025) - "These data indicate that oral fasudil is safe and well-tolerated among patients with ALS. The statistically significant reduction in NfL, which was negatively correlated with ALSFRS-R, and demonstration of CNS target engagement in the 180 mg group warrants advancing oral fasudil in a larger double-bind placebo-controlled study. The lack of dose response between the 180 mg group and the 300 mg group is consistent with animal models and indicates that the appropriate dose for further study is 180 mg per day."

Biomarker • Clinical • Late-breaking abstract • P2a data • PK/PD data • Amyotrophic Lateral Sclerosis • CNS Disorders • NEFL

Involvement of Neuroinflammation and Oxidative Stress in L-DOPA-Induced Dyskinesia in Parkinson's Disease: Role of Renin-Angiotensin System and ROCK Pathway. (PubMed, Antioxidants (Basel)) - "Additionally, the use of ROCK inhibitors, such as fasudil, and RAS blockers has shown potent anti-dyskinetic effects. Therefore, compounds acting on the RAS and ROCK pathways could have a dual role, slowing down the degeneration of dopaminergic neurons and reducing the development of LID."

Journal • Review • CNS Disorders • Inflammation • Movement Disorders • Parkinson's Disease

Decoding ROCK1 Inhibition: A Comprehensive Computational Analysis of Key Binding Determinants for Rational Design of Novel Neurotherapeutics. (PubMed, Arch Biochem Biophys) - "Molecular docking studies followed by detailed interaction analysis were conducted on previously reported ROCK1 inhibitors, including standard approved ROCK1 drugs, Netrasudil and Fasudil...These amino acids significantly influenced the ROCK1-inhibitor complexes' overall binding free energy, indicating their importance in optimal inhibitor binding. The present work makes use of classical molecular mechanics-based and steered molecular dynamics simulations to provide a thorough understanding of the mechanisms underlying ROCK1 inhibition, which can be of significance in the discovery and design of potential drugs."

Journal • CNS Disorders

Modeling Ischemia-Reperfusion Injury in Stroke Using the BBB Chip. (PubMed, ACS Omega) - "Drug screening experiments revealed that acetazolamide (AZA), edaravone (EDA), and fasudil (FAS) could significantly reduce the damage in an ischemic stroke model. Overall, the ischemic stroke model recapitulated the physiological and pathological responses of ischemic stroke, and it was innovative that our model focused on reperfusion injury using microfluidic organ-on-a-chip technology. This ischemic stroke brain model holds promise for advancing the development and testing of therapeutic drugs for ischemic stroke, thus contributing to the evolution of treatment strategies."

Journal • Cardiovascular • Ischemic stroke • Metabolic Disorders • Reperfusion Injury

Prognostic factors in aneurysmal subarachnoid hemorrhage during the clazosentan era: a multicenter study using multivariate analyses and machine learning model. (PubMed, Neurosurg Rev) - "Clinical status at aSAH onset and age are uncontrollable factors; therefore, improving prognosis requires targeted prevention of DCI and effective management of brain edema. The administration of therapies such as clazosentan, cilostazol, and statins may contribute to favorable outcomes."

Biomarker • Clinical • Journal • Observational data • Retrospective data • Cardiovascular • CNS Disorders • Hematological Disorders • Subarachnoid Hemorrhage