fasudil / Generic mfg. - LARVOL DELTA

Comparing Gas and Inhaled Pharmacologic Interventions During Ex Vivo Lung Perfusion: A Systematic Review. (PubMed, Transplant Direct) - "Among the interventions examined, 10% carbon dioxide, carbon monoxide (CO), 40% oxygen (O2), hydrogen, 40 ppm nitric oxide (NO) with 60% O2, 2% sevoflurane with 40%-50% O2, 2-S-amino-6-boronohexanoic acid, fasudil, and β2-adrenoreceptor agonists most effectively improved lung function...In contrast, argon, xenon, N-acetylcysteine, sevoflurane or NO with 6% O2, and liquid ventilation demonstrated minimal benefit. Inhaled interventions can attenuate both mechanical damage and inflammatory pathways, particularly when used in tailored combinations with 40%-60% O2. Future research should prioritize standardizing protocols, optimizing gas composition and timing, and assessing long-term posttransplant outcomes to translate these findings into clinical practice."

Journal • Preclinical • Cardiovascular • Reperfusion Injury • Respiratory Diseases • Transplantation

Neuroprotective effects of ROCK inhibition on hippocampal energy metabolism in a rat model of metabolic syndrome. (PubMed, Iran J Basic Med Sci) - "Phosphatidylinositol 3-kinase/Protein kinase B/Mechanistic target of rapamycin (PI3K/AKT/mTOR) pathway components, including phosphorylated PI3K, AKT, mTOR, Phosphatase and tensin homolog (PTEN), and Ras homolog enriched in brain (Rheb), were analyzed by Western blotting. These findings demonstrate that ROCK overactivation contributes to central insulin resistance and hippocampal energy dysfunction in MS. ROCK inhibition with fasudil effectively reverses these alterations, highlighting ROCK as a potential therapeutic target for preserving hippocampal metabolic function in MS."

Journal • Preclinical • Diabetes • Dyslipidemia • Metabolic Disorders • PTEN • RHEB

Clazosentan Administration Was Not Associated with Intracranial Pressure Elevation in Aneurysmal Subarachnoid Hemorrhage: A Retrospective Study with Direct ICP Monitoring. (PubMed, J Clin Med) - " This single-center retrospective study included 59 patients with aSAH who underwent continuous direct ICP monitoring, of whom 23 received clazosentan and 24 received fasudil. In this retrospective single-center cohort, no statistically significant ICP elevation was observed during clazosentan administration under standard neurosurgical management. Although the small sample size limits statistical power and a false-negative result cannot be excluded, these findings may help inform clinical decision-making regarding clazosentan use in patients with poor-grade aSAH."

Journal • Retrospective data • Cardiovascular • Cerebral Hemorrhage • Hematological Disorders • Subarachnoid Hemorrhage

The Clinical Factors Associated with Clazosentan Discontinuation and Exploratory Associations with Discharge and Six-Month Outcomes in Aneurysmal Subarachnoid Hemorrhage: A Multicenter DCI Japan Registry Study. (PubMed, J Clin Med) - "Clazosentan discontinuation was associated with age ≥ 76 years (OR for discontinuation: 2.33, 95% CI 1.03-5.28), World Federation of Neurosurgical Societies Grade V (OR 6.52 [2.70-15.78]), larger aneurysm size (OR 1.15 [1.03-1.29]), Fisher computed tomography group 4 (OR 2.61 [1.08-6.30]), and Fasudil hydrochloride hydrate use (OR 3.96 [1.77-8.87]). Clazosentan discontinuation was associated with poor outcome at discharge and at 6 months, although the latter was attenuated in sensitivity analysis. Some factors were associated with clazosentan discontinuation, highlighting the clinical relevance of careful systemic monitoring during clazosentan therapy, particularly in patient populations underrepresented in prior trials."

Journal • Cardiovascular • Hematological Disorders • Subarachnoid Hemorrhage

Safety, Tolerability and Symptomatic Efficacy of the ROCK-Inhibitor Fasudil in Patients With Parkinson's Disease (clinicaltrials.gov) - P2 | N=81 | Completed | Sponsor: Technical University of Munich | Active, not recruiting ➔ Completed

Trial completion • CNS Disorders • Movement Disorders • Parkinson's Disease

Ginsenoside Rb1 ameliorates endothelial dysfunction in sepsis: Targeting the RhoA/ROCK pathway to modulate mitochondrial homeostasis and inflammation. (PubMed, J Ginseng Res) - "RhoA/ROCK inhibitor (Fasudil) and Drp1 inhibitor (Mdivi-1) served as mechanistic controls...G-Rb1 alleviates sepsis-induced endothelial dysfunction by suppressing the RhoA/ROCK/Drp1 axis, thereby restoring mitochondrial homeostasis and barrier integrity. These findings highlight G-Rb1 as a promising therapeutic candidate for sepsis management via dual modulation of cytoskeletal dynamics and mitochondrial quality control."

Journal • Infectious Disease • Inflammation • Respiratory Diseases • Septic Shock • CDH5 • CLDN5 • IL1B • IL6 • RHOA • TJP1 • TNFA

Clazosentan, Endothelin-A Receptor Antagonist, Suppresses Interleukin-6 Expression in Cerebrospinal Fluid after Subarachnoid Hemorrhage. (PubMed, Neurol Med Chir (Tokyo)) - "Ten patients received fasudil hydrochloride (FH), a Rho kinase inhibitor, and 12 received CLA. CLA suppressed IL-6 expression during the acute phase, which may contribute to delayed upregulation of IP-10 and MIG. Suppression of IL-6 may represent a key mechanism underlying the anti-inflammatory effects of CLA following SAH."

Journal • Hematological Disorders • Subarachnoid Hemorrhage • CCL2 • IFNG • IL6

Addition of Clazosentan to Fasudil Is Associated with Increased Cerebral Blood Volume without Changes in Cerebral Blood Flow after Aneurysmal Subarachnoid Hemorrhage: A CT Perfusion Study. (PubMed, World Neurosurg) - "The addition of clazosentan to fasudil was associated with increased cerebral blood volume, without significant changes in cerebral blood flow or mean transit time. These findings may be consistent with altered microvascular capacitance but should not be interpreted as evidence of improved tissue perfusion or clinical outcomes."

Journal • Cardiovascular • Cerebral Hemorrhage • Hematological Disorders • Subarachnoid Hemorrhage

Phenotypic shift of astrocytes from A1 to A2 induced by fasudil improves demyelination recovery in cuprizone-treated mice. (PubMed, Metab Brain Dis) - "The study further revealed that these phenotypic transformation was mediated through the inhibition of NF-κB and LCN2 signaling pathways. This work identifies FSD as a promising therapeutic candidate for inhibiting demyelination through the regulation of AST polarization via specific signaling mechanism."

Journal • Preclinical • CNS Disorders • Immunology • Inflammation • Multiple Sclerosis • Solid Tumor • CXCL1 • CXCL10 • FGF2

Clinical outcomes before and after the introduction of clazosentan in aneurysmal subarachnoid hemorrhage: a multicenter retrospective study of clipping and endovascular treatment. (PubMed, Neurosurg Rev) - "Functional outcomes appeared more favorable in both the clipping and EVT groups during the clazosentan era. Across all study periods, the observed proportion of patients with favorable functional outcomes was higher in the EVT group than in the clipping group. However, because formal interaction testing did not identify statistically significant effect modification, the apparent reduction in between-group differences observed in the clazosentan era should be interpreted with caution and considered hypothesis-generating. Further prospective studies are needed to clarify the clinical relevance of these era-based observations."

Clinical data • Journal • Retrospective data • Cardiovascular • Cerebral Hemorrhage • CNS Disorders • Hematological Disorders • Hypotension • Subarachnoid Hemorrhage • Vascular Neurology

Targeting Novel Pathways in Pulmonary Arterial Hypertension: A Systematic Review and Meta-Analysis of New Therapeutic Agents. (PubMed, Niger Med J) - "Udenafil and fasudil showed modest benefits, while anastrozole had mixed results with possible sex-specific effects. At the individual trial level, sotatercept (0.7 mg/kg), riociguat (2.5 mg), and metformin (500 mg with bosentan) showed the most favourable benefit profiles. Standardised trial designs and consistent outcome reporting are needed to confirm these potential disease-modifying effects."

Journal • Retrospective data • Cardiovascular • Heart Failure • Hypertension • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases

Fasudil Attenuates Concanavalin A-Induced Autoimmune Hepatitis and Is Associated with Suppression of RhoA/ROCK and TLR4/NF-κB Signaling and Modulation of Immune Responses. (PubMed, Pharmaceuticals (Basel)) - "Our results demonstrate that fasudil has potent immunomodulatory, anti-inflammatory, antioxidant, and anti-apoptotic effects in AIH. Its protective effects are associated with the suppression of RhoA/ROCK and TLR4/NF-κB signaling, supporting further investigation into the contribution of these pathways to the therapeutic actions of fasudil in AIH."

IO biomarker • Journal • Autoimmune Hepatitis • B Cell Lymphoma • Hepatology • Immunology • Inflammation • Liver Failure • Lymphoma • Oncology • BAX • CASP3 • CD8 • IFNG • IL17A • IL6 • RHOA • TLR4 • TNFA

Adjunctive Fasudil Use and Outcomes After Clazosentan Treatment for Aneurysmal Subarachnoid Hemorrhage: A Multicenter DCI Japan Registry Study. (PubMed, J Clin Med) - "Adjunctive Fasudil was independently associated with higher odds of AVS (adjusted odds ratio [aOR] 2.41, 95% confidence interval [CI] 1.21-4.81), cerebral infarction (aOR 2.10, 95% CI 1.08-4.09), and poor 6-month outcome (aOR 2.88, 95% CI 1.08-7.71), but not with poor functional outcome at discharge (aOR 1.37, 95% CI 0.62-3.03). In clazosentan-treated aneurysmal SAH, adjunctive Fasudil use was not associated with additional benefit and was associated with higher odds of AVS, cerebral infarction, and poor functional outcome at 6 months."

Journal • Cardiovascular • CNS Disorders • Hematological Disorders • Subarachnoid Hemorrhage

Fasudil Protects Against Diclofenac-Induced Hepatorenal and Gastric Injury via Modulation of ROCK/TLR4/SIRT1 Signaling and Preservation of Tight Junctions. (PubMed, J Xenobiot) - "Fasudil dose-dependently ameliorates diclofenac-induced hepatic, renal, and gastric injury by silencing the ROCK2/TLR4 inflammatory axis, restoring SIRT1 survival networks, and protecting epithelial tight junctions."

Journal • Acute Kidney Injury • Inflammation • Nephrology • Peptic Ulcer • Renal Disease • CASP3 • RHOA • TLR4 • TNFA

Fasudil induces anti-inflammatory transcriptomic changes and increased proliferation in human trisomy 21 neural progenitor cells. (PubMed, Biol Open) - "The Rho-associated coiled-coil kinase (ROCK) inhibitor fasudil increased proliferation of T21 NPCs, reduced expression of inflammatory pathway genes in T21 NPCs, and reduced markers of inflammation in LPS-stimulated microglia model systems. These results demonstrate that fasudil can alter multiple T21-associated abnormalities in a beneficial manner, suggesting that fasudil warrants further study as a candidate prenatal pharmacotherapy for DS."

Journal • Developmental Disorders • Genetic Disorders • Inflammation • Mental Retardation

Therapeutic targeting of ROCK reverses EMT in lung cancer cells by impeding TAZ in Hippo signalling pathway. (PubMed, Mol Cell Biochem) - "At a lower IC50 than the controlled drug Fasudil, Lomitapide also induced increase in cellular ROS, mitochondrial membrane depolarization, G1/S phase cell cycle arrest with increase in apoptotic cell population. Reduction in migration, invasion, colony and sphere forming abilities also supported the annihilation of cancer progression. Overall, the therapeutic potency of Lomitapide was established to target Hippo pathway through disrupting ROCK activity in EMT dynamics."

Journal • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • CCND1 • MYC • TAFAZZIN

Mapping the immune-genetic architecture of Epstein-Barr virus-related phenotypes and multiple sclerosis through a single-cell genetic framework for target prioritization and pharmacologic hypothesis generation. (PubMed, Mult Scler Relat Disord) - "This study provides a single-cell genetic framework for prioritizing immune-cell-specific candidate targets for EBV-related phenotypes and MS, and nominates genetically supported targets and pharmacologic hypotheses for experimental investigation."

Journal • CNS Disorders • Epstein-Barr Virus Infections • Infectious Disease • Inflammation • Multiple Sclerosis

Fasudil Attenuates Fluoride-induced Neuronal Synaptic Damage by Inhibiting Microglial Inflammation. (PubMed, Environ Toxicol Pharmacol) - "Conversely, fasudil attenuated these effects by downregulating Iba1, TNF-α, and ROCK2 expression. Taken together, these findings establish that RhoA/ROCK signaling critically mediates fluoride-induced neuroinflammation and synaptic damage, thereby offering a mechanistic basis for assessing the neurotoxic risk of environmental fluoride exposure."

Journal • Alzheimer's Disease • Cognitive Disorders • Inflammation • RHOA • ROCK2 • TNFA

Hyperuricaemia induced-hypertension in rats by regulating the RhoA/ ROCK pathway. (PubMed, Kidney Blood Press Res) - "HUA promotes hypertension by activating the RhoA/ROCK pathway, leading to vascular remodeling and dysfunction. Inhibition of this pathway attenuates HUA-induced hypertension, highlighting the mechanistic relevance of the RhoA/ROCK pathway."

Journal • Preclinical • Cardiovascular • Hypertension • RHOA • ROCK1 • ROCK2

Rescue clazosentan for symptomatic cerebral vasospasm following subarachnoid hemorrhage due to anterior cranial fossa dural arteriovenous fistula: A case report with serial angiographic evaluation. (PubMed, Surg Neurol Int) - "Following surgical occlusion, intravenous fasudil hydrochloride was administered for vasospasm prophylaxis. This case suggests that rescue administration of clazosentan may have contributed to improvement as part of multimodal vasospasm management following dAVF-related SAH, with vasodilatory effects comparable to those observed in aneurysmal SAH cases. Furthermore, short-term rescue administration of clazosentan may be tolerable in patients at high risk of fluid retention-related complications when careful fluid management and appropriate diuretic use are implemented."

Journal • Cardiovascular • CNS Disorders • Hematological Disorders • Subarachnoid Hemorrhage • Vascular Neurology

Safety, Tolerability and Symptomatic Efficacy of the ROCK-Inhibitor Fasudil in Patients With Parkinson's Disease (clinicaltrials.gov) - P2 | N=75 | Active, not recruiting | Sponsor: Technical University of Munich | Recruiting ➔ Active, not recruiting

Enrollment closed • CNS Disorders • Movement Disorders • Parkinson's Disease

An open-label Phase 2a study of fasudil in amyotrophic lateral sclerosis: safety and exploratory endpoints. (PubMed, Amyotroph Lateral Scler Frontotemporal Degener) - "Oral fasudil is safe and well-tolerated in ALS patients. The reduction in NfL and demonstration of CNS target engagement, supports studying the 180 mg dose in a double-blind placebo-controlled study."

Journal • P2a data • Amyotrophic Lateral Sclerosis • CNS Disorders

Exploratory Endpoints From An Open-Label Phase 2a Study Of Fasudil In Amyotrophic Lateral Sclerosis (ENCALS 2026) - "The statistically significant reduction in NfL from baseline in the 180 mg cohort, which was inversely correlated with ALSFRS-R, is consistent with a therapeutic effect. Finally, CNS and neuronal target engagement confirms fasudil's pharmacodynamic activity in the CNS."

Clinical • P2a data • Amyotrophic Lateral Sclerosis • CNS Disorders • NEFL

Oral Treatment With Fasudil Diminishes The Capacity Of ALS Patient-Derived Exosomes To Induce TDP-43 Neuropathology And ALS-Relevant Proteomics Changes In Vitro (ENCALS 2026) - "We cannot rule out that the altered cargo is TDP-43 or a fragment of TDP-43, but the inability to titrate based on TDP-43 content suggests it may not be. Proteomic analyses show fasudil treatment affects multiple TDP-43-relevant pathways and so it is possible that the altered cargo is an unidentified stressor that can induce TDP-43 pathology."

Preclinical • Alzheimer's Disease • Amyotrophic Lateral Sclerosis • CNS Disorders • Movement Disorders • Parkinson's Disease • TARDBP

Phosphoproteomics identifies Rho-Kinase-associated phospho-signaling in the medial prefrontal cortex of a schizophrenia-related mouse model and discloses autophagy dysfunction (CINP 2026) - "These mice exhibited activated Rho-kinase (ROCK) signaling cascade, schizophrenia-related behavioral and neurobiological phenotypes that were ameliorated by the ROCK inhibitor fasudil... This study provides the first phosphoproteomic network map of the mPFC in the Arhgap10 mouse model of schizophrenia, demonstrating increased ROCK-dependent phosphoproteins and autophagy dysfunction."

Preclinical • CNS Disorders • Mental Retardation • Psychiatry • Schizophrenia • ARHGAP10 • MAPT