Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C15H18FN3O2S.ClH.2H2O |
Molecular Weight | 395.877 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O.O.Cl.C[C@H]1CNCCCN1S(=O)(=O)C2=CC=CC3=C2C(F)=CN=C3
InChI
InChIKey=CMDJNMACGABCKQ-XVSRHIFFSA-N
InChI=1S/C15H18FN3O2S.ClH.2H2O/c1-11-8-17-6-3-7-19(11)22(20,21)14-5-2-4-12-9-18-10-13(16)15(12)14;;;/h2,4-5,9-11,17H,3,6-8H2,1H3;1H;2*1H2/t11-;;;/m0.../s1
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | H2O |
Molecular Weight | 18.0153 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C15H18FN3O2S |
Molecular Weight | 323.386 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/24502505Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/25414122 | http://dwti.co.jp/english/business-outline/product-pipeline/glanatec
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24502505
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/25414122 | http://dwti.co.jp/english/business-outline/product-pipeline/glanatec
Ripasudil (K-115) is a selective Rho-associated coiled coil-containing protein kinase (ROCK) inhibitor. This compound, which was originally discovered by D. Western Therapeutics Institute, Inc., reduces intraocular pressure (IOP) by directly acting on the trabecular meshwork, thereby increasing conventional outflow through the Schlemm's canal. As a result of this mechanism of action, ripasudil may offer additive effects in the treatment of glaucoma and ocular hypertension when used in combination with agents such as prostaglandin analogues (which increase uveoscleral outflow) and β blockers (which reduce aqueous production). GLANATEC® (Ripasudil hydrochloride hydrate) ophthalmic solution 0.4% is launched in Japan for the treatment of glaucoma and ocular hypertension.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3231 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24502505 |
51.0 nM [IC50] | ||
Target ID: CHEMBL2973 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24502505 |
19.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | GLANATEC Approved UseGLANATEC® (Ripasudil hydrochloride hydrate) ophthalmic solution 0.4% inhibits Rho kinase and promotes drainage of aqueous humor from main outflow. It consequently
decreases intraocular pressure. It is usually used to treat glaucoma and ocular hypertension when other medicines for glaucoma have insufficient effect or can not be used. Launch Date2014 |
|||
Primary | GLANATEC Approved UseGLANATEC® (Ripasudil hydrochloride hydrate) ophthalmic solution 0.4% inhibits Rho kinase and promotes drainage of aqueous humor from main outflow. It consequently
decreases intraocular pressure. It is usually used to treat glaucoma and ocular hypertension when other medicines for glaucoma have insufficient effect or can not be used. Launch Date2014 |
PubMed
Title | Date | PubMed |
---|---|---|
Effects of K-115, a rho-kinase inhibitor, on aqueous humor dynamics in rabbits. | 2014 Aug |
|
Ripasudil: first global approval. | 2014 Dec |
|
Vascular Normalization by ROCK Inhibitor: Therapeutic Potential of Ripasudil (K-115) Eye Drop in Retinal Angiogenesis and Hypoxia. | 2016 Apr 1 |
|
Ocular hypotensive effects of a Rho-associated protein kinase inhibitor in rabbits. | 2017 |
|
Efficacy of Ripasudil as a Second-line Medication in Addition to a Prostaglandin Analog in Patients with Exfoliation Glaucoma: A Pilot Study. | 2017 Jun |
|
Time Course of Conjunctival Hyperemia Induced by a Rho-kinase Inhibitor Anti-glaucoma Eye Drop: Ripasudil 0.4. | 2017 May |
|
Efficacy and safety of adding ripasudil to existing treatment regimens for reducing intraocular pressure. | 2018 Feb |
Patents
Sample Use Guides
GLANATEC® (Ripasudil hydrochloride hydrate) ophthalmic solution 0.4% one drop twice daily
Route of Administration:
Topical
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27124322
Ripasudil but not fasudil significantly reduced VEGF-induced MYPT-1 phosphorylation in human retinal microvascular endothelial cells (HRMECs) at 30 μmol/L. Ripasudil significantly inhibited VEGF-induced HRMECs migration and proliferation.
Substance Class |
Chemical
Created
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admin
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Edited
Sat Dec 16 11:00:12 GMT 2023
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Record UNII |
016TTR32QF
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Record Status |
Validated (UNII)
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Record Version |
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Related Record | Type | Details | ||
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ANHYDROUS->SOLVATE | |||
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PARENT -> SALT/SOLVATE |
Related Record | Type | Details | ||
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ACTIVE MOIETY |