Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C15H18FN3O2S.ClH |
| Molecular Weight | 359.847 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.C[C@H]1CNCCCN1S(=O)(=O)C2=CC=CC3=C2C(F)=CN=C3
InChI
InChIKey=COBSKSLDBJBGEK-MERQFXBCSA-N
InChI=1S/C15H18FN3O2S.ClH/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/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 | C15H18FN3O2S |
| Molecular Weight | 323.386 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionCurator'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
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.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3231 |
51.0 nM [IC50] | ||
Target ID: CHEMBL2973 |
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 Penetration and Pharmacokinetics of Ripasudil Following Topical Administration to Rabbits. | 2016 Sep |
|
| Ocular hypotensive effects of a Rho-associated protein kinase inhibitor in rabbits. | 2017 |
|
| Efficacy of the Additional Use of Ripasudil, a Rho-Kinase Inhibitor, in Patients With Glaucoma Inadequately Controlled Under Maximum Medical Therapy. | 2017 Feb |
|
| 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
| Substance Class |
Chemical
Created
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| Related Record | Type | Details | ||
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SOLVATE->ANHYDROUS |
| Related Record | Type | Details | ||
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ACTIVE MOIETY |
