fasudil / Generic mfg. - LARVOL DELTA

Anti-inflammatory and pro-proliferative effects of fasudil in human trisomy 21 neural progenitor cells. (PubMed, bioRxiv) - "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

Molecular Interplay of Small Molecules and Calcium Ions with α-Synuclein Revealed by NMR and Molecular Dynamics Simulations. (PubMed, ACS Chem Neurosci) - "Despite this, fasudil retains dynamic, reversible contacts with key tyrosine residues. Overall, exposed α-synuclein conformations allow simultaneous, ligand-specific interactions, highlighting side-chain hotspots governing binding in Ca2+-rich conditions."

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

EFFICACY AND SAFETY OF INTRAOPERATIVE FASUDIL HYDROCHLORIDE ADMINISTRATION ON EARLY ARTERIOVENOUS FISTULA CREATION: A PROPENSITY SCORE-MATCHED PILOT STUDY (ISN-WCN 2026) - "While traditional agents like heparin or papaverine are sometimes administered, clear evidence supporting their practice is lacking. The significantly improved postoperative Q preliminarily suggests efficacy in preventing intraoperative vasospasm during AVF creation. These findings strongly support proceeding to a large-scale Randomized Controlled Trial to verify the definitive efficacy and long-term outcomes of the use of fasudil hydrochloride."

Clinical • Cardiovascular • Hematological Disorders • Hypotension • Thrombosis

DISTINCT TRANSCRIPTOMIC RESPONSES REVEAL A REGULATORY ROLE OF PIEZO1 IN PODOCYTE ADAPTATION TO MECHANICAL STRESS (ISN-WCN 2026) - "Podocyte injury in AII/HS-treated pPiezo1 KO mice was prevented by losartan and hydralazine, and partially ameliorated by the Rho kinase inhibitor fasudil.Conclusion Piezo1 is dispensable for podocyte maintenance under basal conditions but is essential for adaptation to mechanical stress. Its absence leads to severe podocyte injury, albuminuria, and glomerulosclerosis under both short- and long-term hypertensive stress. These findings highlight Piezo1 as a key mechanosensor in podocytes, with both insufficient and excessive activity potentially driving injury through distinct signaling pathways."

Cardiovascular • Chronic Kidney Disease • Glomerulonephritis • Hypertension

The beneficial effects of clazosentan on the perioperative management of patients with subarachnoid hemorrhage. (PubMed, Neurosurg Rev) - "Furthermore, the length of hospital stay was significantly shorter in the clazosentan group than in the fasudil group (22.3 days vs. 29.6 days, p < 0.01). Conclusion clazosentan-based management was associated with reduced angiographic vasospasm, earlier rehabilitation, and shorter hospitalization compared with fasudil-based management."

Journal • Cardiovascular • Hematological Disorders • Subarachnoid Hemorrhage

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

Safety, Tolerability and Symptomatic Efficacy of the ROCK-Inhibitor Fasudil in Patients With Parkinson's Disease (clinicaltrials.gov) - P2 | N=75 | Recruiting | Sponsor: Technical University of Munich | Trial completion date: Sep 2024 ➔ Sep 2026 | Trial primary completion date: Sep 2024 ➔ Sep 2026

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

Mechanism of Shenmai Injection in inducing immediate hypersensitivity by activating RhoA/ROCK signaling pathway (PubMed, Zhongguo Zhong Yao Za Zhi) - "Additionally, the ROCK inhibitor fasudil could significantly reduce the SMI-induced vascular hyperpermeability, indicating the key role of the RhoA/ROCK signaling pathway in SMI-induced hypersensitivity reactions. The results suggest that the risk of SMl-induced immediate hypersensitivity reactions may be associated with excessively high doses or rapid administration, and that the RhoA/ROCK signaling pathway plays an important role in this response."

Journal • Immunology • RHOA

Endovascular treatment for symptomatic vasospasm following traumatic brain injury: illustrative case. (PubMed, J Neurosurg Case Lessons) - "Fluctuations in consciousness or neuropsychological symptoms after TBI should prompt evaluation for CV using perfusion imaging, even in the absence of focal neurological deficits. When a high risk of severe vasospasm accompanied by perfusion reduction is identified, prompt, stepwise therapeutic intervention should be implemented, beginning with the least invasive treatment option to optimize clinical outcomes. https://thejns.org/doi/abs/10.3171/CASE25943."

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

Selective ROCK2 inhibition reduces microvascular obstruction but does not reduce myocardial infarction after ischaemia and reperfusion. (PubMed, J Mol Cell Cardiol Plus) - "The non-selective ROCK inhibitor fasudil, used for cerebral vasospasm, limits infarct size after myocardial I/R, but the roles of individual ROCK isoforms in limiting infarction and MVO remain unclear...Dual ROCK1/2 inhibition protects myocardium from I/R injury, whereas selective ROCK2 inhibition or deficiency does not, implicating ROCK1 in infarct limitation. In contrast, ROCK2 inhibition reduced MVO, identifying ROCK2 as a potential microvascular target."

Journal • Cardiovascular • Myocardial Infarction • Reperfusion Injury • ROCK1

Chronic fasudil treatment induces benzodiazepine-like tolerance via modulation of GABA-A receptor γ2 subunit expression and impairs contextual fear memory in mice. (PubMed, Pharmacol Rep) - No abstract available

Journal • Preclinical

Fasudil improves neutrophilic asthma by influencing M1 macrophage polarization and the expression of the NF-κB/TLR-2/RPS3 pathway. (PubMed, Am J Transl Res) - "BALB/C mice were randomized into an NA group, a dexamethasone intervention group (DI, 1 mg/kg), and a Fasudil intervention group (FI, 40 mg/kg). Fasudil ameliorates NA via regulating M1 macrophage polarization, inhibiting the NF-κB/TLR-2/RPS3 pathway, and reducing pro-inflammatory cytokines, with S100A8/A9 and CXCL2 as potential biomarkers. These findings support Fasudil as a promising NA therapy, warranting further clinical translational research."

IO biomarker • Journal • Asthma • Immunology • Oncology • Pulmonary Disease • Respiratory Diseases • IL12A • IL1B • IL6 • MMP9 • RPS3 • S100A8 • S100A9 • TLR2 • TNFA

Research progress on regulatory mechanisms of mucosal barriers and their applications in allergic diseases. (PubMed, Front Immunol) - "In allergic diseases, this network exhibits organ-specific imbalances: respiratory barrier damage is primarily characterized by RhoA/ROCK-mediated abnormal mucus secretion (asthma) and JAK-STAT-driven Th2 inflammation (rhinitis), whereas the intestinal barrier relies more on the epithelial regenerative capacity of the Wnt pathway.We innovatively propose a "phased-organ-targeting strategy": during the acute inflammatory phase (0-72 hours), JAK inhibitors (such as CYT387 nasal spray) are utilized to block STAT6 phosphorylation and control the immune storm; in the repair phase (72 hours to 2 weeks), Wnt agonists (WNT2b-pH microspheres) are employed to promote epithelial regeneration, or RhoA regulators (fasudil inhalation) are used to reconstruct the mucus layer; in the chronic remodeling phase, a temporally regulated dual-pathway therapy (such as JAK-STAT inhibition combined with Wnt activation hydrogels) is applied. The current challenges lie in overcoming..."

Journal • Review • Allergy • Asthma • Immunology • Inflammation • Pulmonary Disease • Respiratory Diseases • CTNNB1 • ITK • MUC2 • MUC5AC • OCLN • RHOA • SMAD4 • SMAD7 • STAT6 • TGFB1 • TJP1

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

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