DRUGphase2small molecule
fasudil
Brand names: HA-1077, Eril
Mechanism
ROCK1/2 inhibitor. Improves NMJ morphology and survival in SMNΔ7 mice (Bowerman 2012). Approved for cerebral vasospasm in Japan. Our Track 1 lead — baseline 100 ns apo-ROCK2 MD published 2026-04-12.
Approved indications
cerebral-vasospasm-japan
Related claims (50)
| Type | Predicate | Conf | Source |
|---|---|---|---|
| gene expression | fasudil (30 μM) specifically increased glial cell line-derived neurotrophic factor (GDNF) among the secreted proteins at the transcription and secretion levels (in vitro). | 69% | 25185536 |
| drug efficacy | The dual ROCK1/2 inhibitor, fasudil (10 mg/kg), reduced infarct size (mouse model). | 69% | 41704339 |
| motor function | Fasudil (ROCK inhibitor) improves the hindlimb locomotor function in ASCI rats (rat model). | 65% | 30094982 |
| drug efficacy | ROCK inhibitors such as fasudil can be novel, and efficacious treatment for inflammatory neurodegenerative diseases. | 65% | 30552558 |
| motor function | SOD1(G93A) mice benefited from oral treatment with Fasudil showing improved motor function (observed in mouse model). | 65% | 24311453 |
| drug efficacy | The pan-ROCK inhibitor Fasudil has been clinically approved to treat hypertension, heart failure, glaucoma, spinal cord injury, and stroke (clinical). | 65% | 31302146 |
| drug efficacy | Inhibition of ROCK with Y-27632 and Fasudil reduces the engulfment of neuronal debris (in vitro). | 65% | 27178562 |
| motor function | Fasudil treatment improved motor and cognitive functions in α-Syn(A53T) mice as determined by Catwalk(TM) gait analysis and novel object recognition (NOR), without apparent side effects (mouse model). | 65% | 27101974 |
| gene expression | Environmental enrichment combined with fasudil downregulated ROCK, p-LIM domain kinase (LIMK)1, and p-cofilin expression (mouse model). | 65% | 33907042 |
| neuroprotection | ROCK inhibitors such as fasudil protected against dopaminergic degeneration and other neurodegenerative processes in several experimental models through inhibition of neuroinflammation and activation of survival signaling pathways. | 65% | 39915220 |
| drug efficacy | Inhibition of ROCK by Fasudil may represent a useful therapeutic perspective by inhibiting microglial inflammatory responses in the CNS. | 65% | 20882700 |
| drug efficacy | The ET-1-induced actin polymerization response was blunted by the ROCK inhibitor fasudil (rat model). | 65% | 29373038 |
| drug efficacy | Fasudil treatment significantly reduced α-Syn aggregation in vitro in a H4 cell culture model as well as in a cell-free assay. | 65% | 27101974 |
| neuroprotection | In mice, the neuroprotective effect of Fasudil depends on the expression of PPARα induced by ROCK-PPARα-NOX axis-mediated reduction in ROS and associated oxidative damage (in vivo). | 65% | 38055403 |
| drug efficacy | The combination therapy of fasudil (3 mg/kg i.p.) and ozagrel (10 mg/kg i.p.), which are noneffective doses, resulted in reduction of cerebral infarction (mouse model). | 65% | 21493751 |
| drug efficacy | Inhibition of ROCK with Fasudil reduces the engulfment of neuronal debris (in vitro). | 65% | 27178562 |
| drug efficacy | Treatment with Fasudil (5 mg/kg rat weight/day) for 8 weeks significantly improved the motor deficits in the Cylinder and Rotarod tests (rat model). | 65% | 32568105 |
| drug efficacy | Immunohistochemical analysis revealed a significant reduction of α-Syn pathology in the midbrain of α-Syn(A53T) mice after Fasudil treatment (mouse model). | 65% | 27101974 |
| drug efficacy | Chronic treatment with Fasudil induces anxiety-like behaviors that are likely the consequence of ROCK1 and/or ROCK2 inhibition (mouse model). | 65% | 31302146 |
| drug efficacy | Src inhibitor (PP2) or ROCK inhibitors (fasudil and H1152) alone could not reduce the occurrence Ator-induced ICH (zebrafish model). | 65% | 29730311 |
| drug efficacy | Deficiency of Rock1 or treatment with ROCK inhibitor Fasudil protected mice against IgE-mediated challenge in passive cutaneous anaphylaxis model (mouse model). | 65% | 26943578 |
| gene expression | In vitro, LIMK1, collagen I, collagen III, p-MLC, α-SMA, and p-Cofilin expression was significantly attenuated in both the fasudil-treated and untreated LIMK1 KD groups (P < 0.05). | 64% | 30861189 |
| drug efficacy | In vitro, apoptosis was enhanced in the LIMK1 KD group treated with fasudil (P < 0.05). | 64% | 30861189 |
| gene expression | The expression of p110-PI3K, p-Akt, WNT1, Fzd1 and β-catenin were increased after fasudil administration (P<0.05) in MPTP-based mice model (mouse model). | 64% | 26045742 |
| drug efficacy | In vitro, cell migration was attenuated in the LIMK1 KD group treated with fasudil (P < 0.05). | 64% | 30861189 |
| drug efficacy | Environmental enrichment combined with fasudil treatment (mouse model) can ameliorate memory dysfunction through inhibition of the hippocampal ROCK/cofilin pathway, alteration of the dynamic distribution of F-actin, and inhibition of neuron... | 60% | 33433459 |
| drug efficacy | Fasudil treatment ameliorated memory deficits in APP/PS1 Tg mice, accompanied by the reduction of Aβ deposition and Tau protein phosphorylation, the decrease of BACE and the increase of PSD-95, as well as inhibition of TLRs-NF-κB-MyD88 infl... | 60% | 27401064 |
| neuroprotection | The combination treatment of fasudil and ozagrel exhibits additive effects for neuroprotection after MCAO (mouse model). | 59% | 21493751 |
| drug efficacy | Fasudil significantly reduced the number of newly affected muscles compared to placebo in a dose dependent manner over different thresholds at day 90 (clinical trial result). | 59% | 40950480 |
| survival | SOD1(G93A) mice benefited from oral treatment with Fasudil showing prolonged survival (observed in mouse model). | 59% | 24311453 |
| drug efficacy | Inhibition of ROCK with Fasudil attenuates the production of the inflammatory mediator nitric oxide during stimulation with lipopolysaccharide (in vitro). | 59% | 27178562 |
| drug efficacy | Fasudil exhibited multitarget therapeutic effect in APP/PS1 Tg mice (mouse model). | 59% | 27401064 |
| drug efficacy | The ROCK inhibitor, fasudil, prevented Aβo-induced actin stabilization, synaptic impairment, and synaptic loss by blocking cofilin phosphorylation (in vitro). | 59% | 30341179 |
| neuroprotection | Fasudil has neuroprotective effects against ischemic spinal cord injury in rabbits. | 59% | 20141964 |
| drug efficacy | Small molecule ROCK inhibitors, including belumosudil and fasudil, ameliorate the characteristic mitochondrial defects in cultured FA iPSCs, neurons, cardiomyocytes, and FA patient primary fibroblasts (in vitro). | 59% | 40404357 |
| drug target | Fasudil hydrochloride is a potent, broadly selective Rho-associated coiled-coil-containing protein kinase (ROCK) inhibitor (in vitro). | 59% | 40253509 |
| drug efficacy | The ROCK inhibitor Fasudil has shown symptomatic and disease-modifying effects in Parkinson's disease (PD) models (in vitro) and (in vivo). | 59% | 38419648 |
| drug target | Fasudil, next to its effects mediated by ROCK-inhibition, directly interacts with α-Syn and attenuates α-Syn pathology. | 59% | 27101974 |
| neuroprotection | ROCK inhibition by Fasudil, protecting neurons and mobilizating neural stem cells, might represent a useful therapeutic perspective for various neurological disorders characterized by neuron death. | 59% | 19447168 |
| drug efficacy | Fasudil treatment was accompanied by reduced Aβ deposition, Tau protein phosphorylation, and BACE expression, as well as increased PSD-95 expression in hippocampus (mouse model). | 59% | 27401064 |
| neuroprotection | Fasudil, a Rho kinase inhibitor, has neuroprotection in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-based Parkinson's disease (PD) (mouse model). | 59% | 26045742 |
| drug target | Fasudil is a small molecule inhibitor of Rho-associated kinase (ROCK). | 59% | 39424560 |
| pathway membership | The present study highlights a significant role of ROCK/p-Akt/eNOS pathway in the protective effects of fasudil and simvastatin on neurotoxicity and mitochondrial dysfunction induced by 3-NP (in rat model). | 59% | 26169112 |
| drug efficacy | Fasudil, a clinically approved ROCK inhibitor, suppressed rough eye phenotype and mitigated pathogenic tau levels by inducing autophagic pathways in a Drosophila model of tauopathy (mouse model). | 59% | 26818518 |
| drug efficacy | Hydroxyfasudil (HF) inhibited infiltration of CD4<sup>+</sup> T cells and CD68<sup>+</sup> macrophages in the brain in the cuprizone (CPZ) mouse model. | 59% | 30660624 |
| drug efficacy | Inhibition of ROCK with Y-27632 and Fasudil attenuates the production of the inflammatory mediator nitric oxide during stimulation with lipopolysaccharide (in vitro). | 59% | 27178562 |
| neuroprotection | Fasudil-induced neuroprotection and/or neurogenesis are mediated partially through astrocyte-derived G-CSF (in vitro). | 59% | 19447168 |
| motor function | In the MPTP-mouse model of PD, the administration of Fasudil improved the motor function recovery. | 59% | 25908255 |
| gene expression | Combined intervention of MSCs and Fasudil further increased the expression of BDNF and GDNF compared with the delivery of MSCs alone (mouse model). | 59% | 27573128 |
| drug efficacy | Fasudil inhibits gene expression profiles of motor and autophagic cellular cascades and inflammatory/angiogenic responses (in vitro). | 59% | 25750613 |
Off-Target Findings (238)
T1: 6T3: 200T4: 11untiered: 21
| Target | Role | Tier | Boltz-2 iPTM | Chai-1 iPTM | Verdict |
|---|---|---|---|---|---|
| GAP43 | SMA | T1 | 0.880 | — | Primary SMA hit |
| NCALD | SMA | T1 | 0.820 | — | Primary SMA hit |
| PFN2 | SMA | T1 | 0.677 | — | Primary SMA hit |
| STMN1 | SMA | T1 | 0.676 | — | Primary SMA hit |
| CHRNGion_channel | SMA | T1 | 0.554 | — | Primary SMA hit |
| CFL1 | SMA | T1 | 0.501 | — | Primary SMA hit |
| CHEK1kinase | OFF-TARGET | T3 | 0.979 | — | Selectivity flag (off-target substrate) |
| GRK4kinase | OFF-TARGET | T3 | 0.978 | — | Selectivity flag (off-target substrate) |
| DRD4gpcr | OFF-TARGET | T3 | 0.978 | — | Selectivity flag (off-target substrate) |
| PRKG1kinase | OFF-TARGET | T3 | 0.977 | — | Selectivity flag (off-target substrate) |
| PRKCAkinase | OFF-TARGET | T3 | 0.976 | — | Selectivity flag (off-target substrate) |
| MAPK7kinase | OFF-TARGET | T3 | 0.975 | — | Selectivity flag (off-target substrate) |
| AURKCkinase | OFF-TARGET | T3 | 0.975 | — | Selectivity flag (off-target substrate) |
| GRK1kinase | OFF-TARGET | T3 | 0.975 | — | Selectivity flag (off-target substrate) |
| CAMK2Gkinase | OFF-TARGET | T3 | 0.971 | — | Selectivity flag (off-target substrate) |
| AMHR2kinase | OFF-TARGET | T3 | 0.970 | — | Selectivity flag (off-target substrate) |
| AURKBkinase | OFF-TARGET | T3 | 0.968 | — | Selectivity flag (off-target substrate) |
| GPR42gpcr | OFF-TARGET | T3 | 0.966 | — | Selectivity flag (off-target substrate) |
| MAPK10kinase | OFF-TARGET | T3 | 0.964 | — | Selectivity flag (off-target substrate) |
| NTRK1kinase | OFF-TARGET | T3 | 0.964 | — | Selectivity flag (off-target substrate) |
| HRH2gpcr | OFF-TARGET | T3 | 0.963 | — | Selectivity flag (off-target substrate) |
| PAK2kinase | OFF-TARGET | T3 | 0.958 | — | Selectivity flag (off-target substrate) |
| AAK1kinase | OFF-TARGET | T3 | 0.957 | — | Selectivity flag (off-target substrate) |
| GPR65gpcr | OFF-TARGET | T3 | 0.951 | — | Selectivity flag (off-target substrate) |
| PRKD3kinase | OFF-TARGET | T3 | 0.948 | — | Selectivity flag (off-target substrate) |
| DRD1gpcr | OFF-TARGET | T3 | 0.947 | — | Selectivity flag (off-target substrate) |
| ITKkinase | OFF-TARGET | T3 | 0.946 | — | Selectivity flag (off-target substrate) |
| KITkinase | OFF-TARGET | T3 | 0.944 | — | Selectivity flag (off-target substrate) |
| FGFR1kinase | OFF-TARGET | T3 | 0.942 | — | Selectivity flag (off-target substrate) |
| ADORA2Bgpcr | OFF-TARGET | T3 | 0.942 | — | Selectivity flag (off-target substrate) |
| ULK3kinase | OFF-TARGET | T3 | 0.941 | — | Selectivity flag (off-target substrate) |
| PDGFRAkinase | OFF-TARGET | T3 | 0.940 | — | Selectivity flag (off-target substrate) |
| TGFBR1kinase | SMA | T3 | 0.939 | — | Selectivity flag (off-target substrate) |
| MAP3K3kinase | OFF-TARGET | T3 | 0.937 | — | Selectivity flag (off-target substrate) |
| MAST4kinase | OFF-TARGET | T3 | 0.937 | — | Selectivity flag (off-target substrate) |
| RHOgpcr | OFF-TARGET | T3 | 0.934 | — | Selectivity flag (off-target substrate) |
| STK17Akinase | OFF-TARGET | T3 | 0.934 | — | Selectivity flag (off-target substrate) |
| PDPK1kinase | OFF-TARGET | T3 | 0.934 | — | Selectivity flag (off-target substrate) |
| CDC42BPAkinase | OFF-TARGET | T3 | 0.933 | — | Selectivity flag (off-target substrate) |
| ACVR2Akinase | OFF-TARGET | T3 | 0.932 | — | Selectivity flag (off-target substrate) |
| ADORA3gpcr | OFF-TARGET | T3 | 0.931 | — | Selectivity flag (off-target substrate) |
| FFAR4gpcr | OFF-TARGET | T3 | 0.926 | — | Selectivity flag (off-target substrate) |
| HCRTR2gpcr | OFF-TARGET | T3 | 0.925 | — | Selectivity flag (off-target substrate) |
| RIPK2kinase | OFF-TARGET | T3 | 0.923 | — | Selectivity flag (off-target substrate) |
| QRFPRgpcr | OFF-TARGET | T3 | 0.923 | — | Selectivity flag (off-target substrate) |
| CCR3gpcr | OFF-TARGET | T3 | 0.923 | — | Selectivity flag (off-target substrate) |
| SYKkinase | OFF-TARGET | T3 | 0.922 | — | Selectivity flag (off-target substrate) |
| GALR2gpcr | OFF-TARGET | T3 | 0.919 | — | Selectivity flag (off-target substrate) |
| ADRB3gpcr | OFF-TARGET | T3 | 0.919 | — | Selectivity flag (off-target substrate) |
| HTR5Agpcr | OFF-TARGET | T3 | 0.918 | — | Selectivity flag (off-target substrate) |
Showing top 50 of 238 targets.