Fasudil

Fasudil
Clinical data
AHFS/Drugs.com	International Drug Names
ATC code	C04AX32 (WHO) ;
Pharmacokinetic data
Metabolites	Hydroxyfasudil
Elimination half-life	0.76 hours. Active metabolite (hydroxyfasudil) 4.66 hours.
Identifiers
	IUPAC name 5-(1,4-Diazepane-1-sulfonyl)isoquinoline;
CAS Number	103745-39-7 ;
PubChem CID	3547;
IUPHAR/BPS	5181;
DrugBank	DB08162 ;
ChemSpider	3426 ;
UNII	Q0CH43PGXS;
KEGG	D07941 ;
ChEBI	CHEBI:43871;
ChEMBL	ChEMBL38380 ;
PDB ligand	M77 (PDBe, RCSB PDB);
CompTox Dashboard (EPA)	DTXSID4048569 ;
ECHA InfoCard	100.250.347
Chemical and physical data
Formula	C14H17N3O2S
Molar mass	291.37 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3;
	InChI 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 ; Key:NGOGFTYYXHNFQH-UHFFFAOYSA-N ;
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Fasudil (INN) is a potent Rho-kinase inhibitor and vasodilator.^[1] Since it was discovered, it has been used for the treatment of cerebral vasospasm, which is often due to subarachnoid hemorrhage,^[2] as well as to improve the cognitive decline seen in stroke patients. It has been found to be effective for the treatment of pulmonary hypertension.^[3] It has been demonstrated that fasudil could improve memory in normal mice, identifying the drug as a possible treatment for age-related or neurodegenerative memory loss.^[4]^[5]^[6]

It has been approved for use in Japan and China since 1995,^[7] but has not been approved by the United States Food and Drug Administration or by the European Medicines Agency. Woolsey Pharmaceuticals is developing BRAVYL (oral fasudil) for various neurodegenerative diseases.^[8]

^ "Drug Found That Could Reduce Risk Of Alzheimer's". Science Daily.
^ Shibuya M, Suzuki Y (Sep 1993). "[Treatment of cerebral vasospasm by a protein kinase inhibitor AT 877]". Nō to Shinkei - Brain and Nerve (in Japanese). 45 (9): 819–24. PMID 8217408.
^ Doggrell SA (Sep 2005). "Rho-kinase inhibitors show promise in pulmonary hypertension". Expert Opinion on Investigational Drugs. 14 (9): 1157–9. doi:10.1517/13543784.14.9.1157. PMID 16144499. S2CID 35237787.
^ Huentelman MJ, Stephan DA, Talboom J, Corneveaux JJ, Reiman DM, Gerber JD, Barnes CA, Alexander GE, Reiman EM, Bimonte-Nelson HA (Feb 2009). "Peripheral delivery of a ROCK inhibitor improves learning and working memory". Behavioral Neuroscience. 123 (1): 218–23. doi:10.1037/a0014260. PMC 2701389. PMID 19170447.
^ Kumar M, Bansal N (October 2018). "Fasudil hydrochloride ameliorates memory deficits in rat model of streptozotocin-induced Alzheimer's disease: Involvement of PI3-kinase, eNOS and NFκB". Behavioural Brain Research. 351: 4–16. doi:10.1016/j.bbr.2018.05.024. PMID 29807069. S2CID 44121036.
^ Song X, He R, Han W, Li T, Xie L, Cheng L, et al. (April 2019). "Protective effects of the ROCK inhibitor fasudil against cognitive dysfunction following status epilepticus in male rats". Journal of Neuroscience Research. 97 (4): 506–519. doi:10.1002/jnr.24355. PMID 30421453. S2CID 53289377.
^ Zhao J, Zhou D, Guo J, Ren Z, Zhou L, Wang S, et al. (September 2006). "Effect of fasudil hydrochloride, a protein kinase inhibitor, on cerebral vasospasm and delayed cerebral ischemic symptoms after aneurysmal subarachnoid hemorrhage". Neurologia Medico-Chirurgica. 46 (9): 421–8. doi:10.2176/nmc.46.421. PMID 16998274.
^ Jacobson S (February 18, 2021). "Woolsey Pharmaceuticals Emerges from Stealth Mode to Announce Patients Enrolled in Two New CNS Studies". Businesswire.

[1] "Drug Found That Could Reduce Risk Of Alzheimer's". Science Daily.

[pmid8217408-2] Shibuya M, Suzuki Y (Sep 1993). "[Treatment of cerebral vasospasm by a protein kinase inhibitor AT 877]". Nō to Shinkei - Brain and Nerve (in Japanese). 45 (9): 819–24. PMID 8217408.

[Doggrell2005-3] Doggrell SA (Sep 2005). "Rho-kinase inhibitors show promise in pulmonary hypertension". Expert Opinion on Investigational Drugs. 14 (9): 1157–9. doi:10.1517/13543784.14.9.1157. PMID 16144499. S2CID 35237787.

[Huentelman2009-4] Huentelman MJ, Stephan DA, Talboom J, Corneveaux JJ, Reiman DM, Gerber JD, Barnes CA, Alexander GE, Reiman EM, Bimonte-Nelson HA (Feb 2009). "Peripheral delivery of a ROCK inhibitor improves learning and working memory". Behavioral Neuroscience. 123 (1): 218–23. doi:10.1037/a0014260. PMC 2701389. PMID 19170447.

[5] Kumar M, Bansal N (October 2018). "Fasudil hydrochloride ameliorates memory deficits in rat model of streptozotocin-induced Alzheimer's disease: Involvement of PI3-kinase, eNOS and NFκB". Behavioural Brain Research. 351: 4–16. doi:10.1016/j.bbr.2018.05.024. PMID 29807069. S2CID 44121036.

[6] Song X, He R, Han W, Li T, Xie L, Cheng L, et al. (April 2019). "Protective effects of the ROCK inhibitor fasudil against cognitive dysfunction following status epilepticus in male rats". Journal of Neuroscience Research. 97 (4): 506–519. doi:10.1002/jnr.24355. PMID 30421453. S2CID 53289377.

[7] Zhao J, Zhou D, Guo J, Ren Z, Zhou L, Wang S, et al. (September 2006). "Effect of fasudil hydrochloride, a protein kinase inhibitor, on cerebral vasospasm and delayed cerebral ischemic symptoms after aneurysmal subarachnoid hemorrhage". Neurologia Medico-Chirurgica. 46 (9): 421–8. doi:10.2176/nmc.46.421. PMID 16998274.

[jacobson-8] Jacobson S (February 18, 2021). "Woolsey Pharmaceuticals Emerges from Stealth Mode to Announce Patients Enrolled in Two New CNS Studies". Businesswire.

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