FASUDIL

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C14H17N3O2S
Molecular Weight	291.369
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O=S(=O)(N1CCCNCC1)C2=C3C=CN=CC3=CC=C2

InChI

InChIKey=NGOGFTYYXHNFQH-UHFFFAOYSA-N

InChI=1S/C14H17N3O2S/c18-20(19,17-9-2-6-15-8-10-17)14-4-1-3-12-11-16-7-5-13(12)14/h1,3-5,7,11,15H,2,6,8-10H2

HIDE SMILES / InChI

Molecular Formula	C14H17N3O2S
Molecular Weight	291.369
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: http://library.corporate-ir.net/library/17/177/177285/items/203435/FasudilfactsheetJune262006.pdf

Fasudil is a potent Rho kinase inhibitor, which was developed by Asahi Kasei. The drug is used in Asia for the prevention of cerebral vasospasm in patients with subarachnoid hemorrhage.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Rho-associated protein kinase 7 Target ID: CHEMBL2111459 Sources: http://library.corporate-ir.net/library/17/177/177285/items/203435/FasudilfactsheetJune262006.pdf	Inhibitor 8504		0.4 µM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Cerebral vasospasm 9 Sources: http://www.pharm.or.jp/eng/126th/data/AL07.pdf	Preventing		Approved 8583	ERIL Approved Use Improvement of cerebral vasospasm and cerebral ischemic symptoms associated with cerebral vasospasm after subarachnoid hemorrhage.

C_max

Value	Dose	Analyte	Population
100.4 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=21 \| https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=23	0.2 mg/kg bw single, intravenous dose: 0.2 mg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	FASUDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
215.7 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=21	0.4 mg/kg bw single, intravenous dose: 0.4 mg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	FASUDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
71.7 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=22	0.2 mg/kg bw 2 times / day multiple, intravenous dose: 0.2 mg/kg bw route of administration: Intravenous experiment type: MULTIPLE co-administered:	FASUDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
74.8 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=22	0.2 mg/kg bw 2 times / day multiple, intravenous dose: 0.2 mg/kg bw route of administration: Intravenous experiment type: MULTIPLE co-administered:	FASUDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
125 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=22	30 mg 3 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	FASUDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
166.9 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=22	30 mg 3 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	FASUDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
126.9 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=22	30 mg 3 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	FASUDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
46.1 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=21 \| https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=23	0.2 mg/kg bw single, intravenous dose: 0.2 mg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	FASUDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
94.8 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=21	0.4 mg/kg bw single, intravenous dose: 0.4 mg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	FASUDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
27.2 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=22	0.2 mg/kg bw 2 times / day multiple, intravenous dose: 0.2 mg/kg bw route of administration: Intravenous experiment type: MULTIPLE co-administered:	FASUDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
31.4 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=22	0.2 mg/kg bw 2 times / day multiple, intravenous dose: 0.2 mg/kg bw route of administration: Intravenous experiment type: MULTIPLE co-administered:	FASUDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
86.9 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=22	30 mg 3 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	FASUDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
120 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=22	30 mg 3 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	FASUDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
89 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=22	30 mg 3 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	FASUDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
14.2 min OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=21 \| https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=23	0.2 mg/kg bw single, intravenous dose: 0.2 mg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	FASUDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
15.6 min OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=21	0.4 mg/kg bw single, intravenous dose: 0.4 mg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	FASUDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
10.3 min OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=22	0.2 mg/kg bw 2 times / day multiple, intravenous dose: 0.2 mg/kg bw route of administration: Intravenous experiment type: MULTIPLE co-administered:	FASUDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
10.6 min OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=22	0.2 mg/kg bw 2 times / day multiple, intravenous dose: 0.2 mg/kg bw route of administration: Intravenous experiment type: MULTIPLE co-administered:	FASUDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
24.4 min OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=22	30 mg 3 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	FASUDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
21.6 min OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=22	30 mg 3 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	FASUDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
28.6 min OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=22	30 mg 3 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	FASUDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
63.8% OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=21 \| https://www.info.pmda.go.jp/go/interview/1/100898_2190414A1033_1_1F.pdf#page=23	0.2 mg/kg bw single, intravenous dose: 0.2 mg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:		FASUDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
30 mg 3 times / day multiple, intravenous Studied dose Dose: 30 mg, 3 times / day Route: intravenous Route: multiple Dose: 30 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/22027241/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/22027241/	Other AEs: AST increased, ALT increased... Other AEs: AST increased (2%) ALT increased (4%) ALP increased (2%) Gamma-glutamyltransferase increased (2%) Sources: https://pubmed.ncbi.nlm.nih.gov/22027241/
40 mg 3 times / day multiple, intravenous Studied dose Dose: 40 mg, 3 times / day Route: intravenous Route: multiple Dose: 40 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/12409984/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/12409984/	Sources: https://pubmed.ncbi.nlm.nih.gov/12409984/
60 mg 1 times / day multiple, intravenous Studied dose Dose: 60 mg, 1 times / day Route: intravenous Route: multiple Dose: 60 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/31166081/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/31166081/	Sources: https://pubmed.ncbi.nlm.nih.gov/31166081/

AEs

AE	Significance	Dose	Population
ALP increased	2%	30 mg 3 times / day multiple, intravenous Studied dose Dose: 30 mg, 3 times / day Route: intravenous Route: multiple Dose: 30 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/22027241/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/22027241/
AST increased	2%	30 mg 3 times / day multiple, intravenous Studied dose Dose: 30 mg, 3 times / day Route: intravenous Route: multiple Dose: 30 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/22027241/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/22027241/
Gamma-glutamyltransferase increased	2%	30 mg 3 times / day multiple, intravenous Studied dose Dose: 30 mg, 3 times / day Route: intravenous Route: multiple Dose: 30 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/22027241/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/22027241/
ALT increased	4%	30 mg 3 times / day multiple, intravenous Studied dose Dose: 30 mg, 3 times / day Route: intravenous Route: multiple Dose: 30 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/22027241/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/22027241/

PubMed

Title	Date	PubMed
Statins decrease Toll-like receptor 4 expression and downstream signaling in human CD14+ monocytes.	2005-07	15860745
Fasudil prevents KATP channel-induced improvement in postischemic functional recovery.	2005-06	15695558
Activation of Rho-associated kinase during augmented contraction of the basilar artery to serotonin after subarachnoid hemorrhage.	2005-06	15665056
Fasudil, a Rho-kinase inhibitor, attenuates angiotensin II-induced abdominal aortic aneurysm in apolipoprotein E-deficient mice by inhibiting apoptosis and proteolysis.	2005-05-03	15851596
Negative regulation of RhoA/Rho kinase by angiotensin II type 2 receptor in vascular smooth muscle cells: role in angiotensin II-induced vasodilation in stroke-prone spontaneously hypertensive rats.	2005-05	15834290
Long term Rho-kinase inhibition ameliorates endothelial dysfunction in LDL-Receptor deficient mice.	2005-04-11	15840411
Inhibition of Rho-kinase by fasudil attenuated angiotensin II-induced cardiac hypertrophy in apolipoprotein E deficient mice.	2005-04-11	15840407
Role of Rho-kinase and p27 in angiotensin II-induced vascular injury.	2005-04	15699465
Inhaled Rho kinase inhibitors are potent and selective vasodilators in rat pulmonary hypertension.	2005-03-01	15563635
High-throughput screening for kinase inhibitors.	2005-03	15742384
Small guanine nucleotide-binding protein Rho and myocardial function.	2005-03	15715922
Acute vasodilator effects of a Rho-kinase inhibitor, fasudil, in patients with severe pulmonary hypertension.	2005-03	15710736
Rho-kinase and myosin II activities are required for cell type and environment specific migration.	2005-02	15676022
Prostacyclin does not inhibit rho-kinase: an implication for the treatment of pulmonary hypertension.	2005-02	15654260
[Role of calcium desensitization in vascular hyporeactivity in hemorrhagic shock].	2005-01	15636706
Therapeutic potential of rho-kinase inhibitors in cardiovascular diseases.	2005	15631536
Inhibition of protein kinase C-mediated contraction by Rho kinase inhibitor fasudil in rabbit aorta.	2004-11	15459803
Rho-kinase, a potential therapeutic target for the treatment of hypertension.	2004-10	15605112
[Inhibition of Rho-kinase by fasudil preventing anginal attacks associated with spastic angina: a case report].	2004-10	15532247
Expression of Rho-kinase (ROCK-1 and ROCK-2) and its substantial role in the contractile activity of the sheep ureter.	2004-10	15351780
Inhibition of Rho-kinase leads to rapid activation of phosphatidylinositol 3-kinase/protein kinase Akt and cardiovascular protection.	2004-10	15319269
Mechanisms underlying postjunctional synergism between responses of the vas deferens to noradrenaline and ATP.	2004-09-13	15364001
Usefulness of fasudil, a Rho-kinase inhibitor, to treat intractable severe coronary spasm after coronary artery bypass surgery.	2004-09	15475822
Fasudil, a Rho-kinase inhibitor, attenuates glomerulosclerosis in Dahl salt-sensitive rats.	2004-09	15311108
Involvement of RhoA and possible neuroprotective effect of fasudil, a Rho kinase inhibitor, in NMDA-induced neurotoxicity in the rat retina.	2004-08-20	15262212
Involvement of Rho-kinase in cold ischemia-reperfusion injury after liver transplantation in rats.	2004-08-15	15316365
[Development of drug delivery system for intrathecal administration and its therapeutic effect on cerebral vasospasm and ischemia].	2004-08	15297723
Rho kinase mediates cold-induced constriction of cutaneous arteries: role of alpha2C-adrenoceptor translocation.	2004-05-28	15087420
Stent implantation activates RhoA in human arteries: inhibitory effect of rapamycin.	2004-05-19	15627783
Long-term inhibition of Rho-kinase suppresses left ventricular remodeling after myocardial infarction in mice.	2004-05-11	15096457
Regulation of osteoblast differentiation by Pasteurella multocida toxin (PMT): a role for Rho GTPase in bone formation.	2004-04	15005854
The Rho-ROCK system as a new therapeutic target for preventing interstitial fibrosis.	2004-03-03	14993932
[Involvement of small GTPase Rho and Rho-kinase in the pathogenesis of hypertension and hypertensive target organ damage].	2004-03	15171369
Involvement of RhoA and Rho kinase in neutrophil-stimulated endothelial hyperpermeability.	2004-03	14630629
Rho kinase inhibition initiates apoptosis in human airway epithelial cells.	2004-03	12933355
Long-term treatment with a Rho-kinase inhibitor improves monocrotaline-induced fatal pulmonary hypertension in rats.	2004-02-20	14670839
Rho-kinase expression and its contribution to the control of perfusion pressure in the isolated rat mesenteric vascular bed.	2004-02-06	14757149
[Rho-kinase inhibitor].	2004-02	15035192
Long-term treatment with a specific Rho-kinase inhibitor suppresses cardiac allograft vasculopathy in mice.	2004-01-09	14615290
Differential effects of Rho-kinase inhibition on artery wall mass and remodeling.	2004-01	14718843
Long-term inhibition of Rho-kinase suppresses neointimal formation after stent implantation in porcine coronary arteries: involvement of multiple mechanisms.	2004-01	14592842
Effects of HA-1077 and Y-27632, two rho-kinase inhibitors, in the human umbilical artery.	2004	15509884
Role of the Rhoa/Rho kinase system in flow-related remodeling of rat mesenteric small arteries in vivo.	2003-12-09	15192268
Protein kinase A in complex with Rho-kinase inhibitors Y-27632, Fasudil, and H-1152P: structural basis of selectivity.	2003-12	14656443
Effect of fasudil on Rho-kinase and nephropathy in subtotally nephrectomized spontaneously hypertensive rats.	2003-12	14633123
Rho kinase inhibitors block activation of pancreatic stellate cells.	2003-12	14581180
Long-term inhibition of Rho-kinase suppresses angiotensin II-induced cardiovascular hypertrophy in rats in vivo: effect on endothelial NAD(P)H oxidase system.	2003-10-17	14500337
Expression of Rho-kinase and its functional role in the contractile activity of the mouse vas deferens.	2003-10	14504141
Synthesis and pharmacological study of Rho-kinase inhibitors: pharmacomodulations on the lead compound Fasudil.	2003-04	12943196
Hypoxia and Rho/Rho-kinase signaling. Lung development versus hypoxic pulmonary hypertension.	2003	14713118

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dosage is 30 mg fasudil hydrochloride should be diluted in 50-100 mL solution and administered by intravenous infusion over 30 minutes 2-3 times daily.

Route of Administration: Intravenous

In Vitro Use Guide

The rat aortic rings were contracted by KCl; when the contraction reached a plateau, fasudil was added at concentrations from 10(-9) to 10(-5) M. The relaxation IC50 was 0.74 uM. When rabbit aortic rings were used, IC50 values were 37,15 uM and 27,54 uM for KCl and Methoxamine-induced contraction, respectively.

Substance Class	Chemical Created by `admin` on `Wed Apr 02 08:32:01 GMT 2025` Edited by `admin` on `Wed Apr 02 08:32:01 GMT 2025`
Record UNII	Q0CH43PGXS
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

AT 877

Preferred Name

English

FASUDIL

Official Name

English

AT-877

Code

English

HA 1077

Code

English

1-(5-ISOQUINOLINESULFONYL)HOMOPIPERAZINE

Systematic Name

English

HA-1077

Code

English

HEXAHYDRO-1-(5-ISOQUINOLYLSULFONYL)-1H-1,4-DIAZEPINE

Systematic Name

English

ZK-258594

Code

English

N-(5-ISOQUINOLINESULFONYL)-1,4-PERHYDRODIAZEPINE

Common Name

English

fasudil [INN]

Common Name

English

ISOQUINOLINE, 5-((HEXAHYDRO-1H-1,4-DIAZEPIN-1-YL)SULFONYL)-

Systematic Name

English

FASUDIL [MI]

Common Name

English

NSC-759827

Code

English

5-((HEXAHYDRO-1H-1,4-DIAZEPIN-1-YL)SULFONYL)ISOQUINOLINE

Systematic Name

English

Fasudil [WHO-DD]

Common Name

English

Classification Tree Code System Code

WHO-ATC

C04AX32