ripasudil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
Rho protein kinase inhibitors	4938	223645-67-8

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ripasudil
ripasudil hydrochloride hydrate
ripasudil hydrochloride
glanatec
glanatec ophthalmic solution
ripasudil HCl

Rho-associated kinase inhibitor for the treatment of glaucoma and ocular hypertension

Molecular weight: 323.39
Formula: C15H18FN3O2S
CLOGP: 1.73
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 62.30
ALOGS: -3.03
ROTB: 1

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Sept. 26, 2014	PMDA	Kowa Company, Ltd

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	S01EX07	SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Other antiglaucoma preparations

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Ocular hypertension	indication	4210003	DOID:9282
Glaucoma	indication	23986001	DOID:1686

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.12	Basic
pKa2	4.91	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Rho-associated protein kinase 1	Kinase	Q13464	ROCK1_HUMAN	INHIBITOR	IC50	7.29		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Rho-associated protein kinase 2	Kinase	O75116	ROCK2_HUMAN	INHIBITOR	IC50	7.72		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Serine/threonine-protein kinase MARK2	Kinase	Q7KZI7	MARK2_HUMAN		Kd	5.22		CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-1	Kinase	Q13131	AAPK1_HUMAN		Kd	5.49		CHEMBL
Serine/threonine-protein kinase PLK4	Kinase	O00444	PLK4_HUMAN		Kd	5.09		CHEMBL
Serine/threonine-protein kinase N1	Kinase	Q16512	PKN1_HUMAN		Kd	6.38		CHEMBL
MAP/microtubule affinity-regulating kinase 3	Kinase	P27448	MARK3_HUMAN		Kd	4.24		CHEMBL
Cyclin-dependent kinase 9	Kinase	P50750	CDK9_HUMAN		Kd	4.88		CHEMBL
Serine/threonine-protein kinase N2	Kinase	Q16513	PKN2_HUMAN		Kd	6.54		CHEMBL
Ribosyldihydronicotinamide dehydrogenase [quinone]	Enzyme	P16083	NQO2_HUMAN		Kd	5.43		CHEMBL
cAMP-dependent protein kinase catalytic subunit alpha	Kinase	P17612	KAPCA_HUMAN	INHIBITOR	IC50	5.68		IUPHAR
Mitogen-activated protein kinase kinase kinase kinase 3	Kinase	Q8IVH8	M4K3_HUMAN		Kd	5.49		CHEMBL
Aurora kinase B	Kinase	Q96GD4	AURKB_HUMAN		Kd	5.94		CHEMBL
Serine/threonine-protein kinase D2	Kinase	Q9BZL6	KPCD2_HUMAN		Kd	5.43		CHEMBL
Serine/threonine-protein kinase TAO3	Kinase	Q9H2K8	TAOK3_HUMAN		Kd	4.93		CHEMBL
5'-AMP-activated protein kinase subunit gamma-1	Kinase	P54619	AAKG1_HUMAN		Kd	5.74		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 3	Kinase	P46734	MP2K3_HUMAN		Kd	5.51		CHEMBL
Protein kinase C delta type	Kinase	Q05655	KPCD_HUMAN		Kd	5.61		CHEMBL

External reference:

ID	Source
D10463	KEGG_DRUG
CHEBI:136046	CHEBI
CHEMBL3426621	ChEMBL_ID
C584679	MESH_SUPPLEMENTAL_RECORD_UI
10423	IUPHAR_LIGAND_ID
DB13165	DRUGBANK_ID
018524	NDDF
018525	NDDF
C4045501	UMLSCUI
CHEMBL4594454	ChEMBL_ID
9691	INN_ID
9863672	PUBCHEM_CID
11978226XX	UNII

Pharmaceutical products:

None