latanoprostene bunod 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
nitrogen monoxide (nitric oxide, NO) donors 5261 860005-21-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • latanoprostene bunod
  • NCX 116
  • BOL-303259-X
  • PF-3187207
  • vyzulta
Latanoprostene bunod is thought to lower intraocular pressure by increasing outflow of aqueous humor through both the trabecular meshwork and uveoscleral routes. Intraocular pressure is a major modifiable risk factor for glaucoma progression. Reduction of intraocular pressure reduces risk of glaucomatous visual field loss.
  • Molecular weight: 507.62
  • Formula: C27H41NO8
  • CLOGP: 3.70
  • LIPINSKI: 1
  • HAC: 9
  • HDO: 3
  • TPSA: 139.36
  • ALOGS: -5.20
  • ROTB: 19

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AKT2,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CG,PIM2,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 45
kinase-selectivity-class AXL,GRK2,MAP2K6,STK33,TEK 5
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Nov. 2, 2017 FDA BAUSCH AND LOMB INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hypoglycaemia 50.23 39.68 16 328 69832 90558271
Eye pain 43.97 39.68 13 331 44155 90583948

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hypoglycaemia 46.24 40.53 16 310 116088 110472885

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC S01EE06 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Prostaglandin analogues
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:39456 antiglaucoma drug

Related Drugs by ATC class:

S01EE Prostaglandin analogues 6 drugs

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

DiseaseRelationSNOMED_IDDOID
Ocular hypertension indication 4210003 DOID:9282
Open-angle glaucoma indication 84494001 DOID:1067




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.024% VYZULTA BAUSCH AND LOMB N207795 Nov. 2, 2017 RX SOLUTION/DROPS OPHTHALMIC 8058467 Feb. 21, 2029 REDUCTION OF INTRAOCULAR PRESSURE (IOP) IN PATIENTS WITH OPEN-ANGLE GLAUCOMA OR OCULAR HYPERTENSION

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Prostaglandin F2-alpha receptor GPCR AGONIST Ki 8.60 IUPHAR SCIENTIFIC LITERATURE
Prostaglandin F2-alpha receptor GPCR Ki 7.01 CHEMBL

External reference:

IDSource
I6393O0922 UNII
4037152 VANDF
C4279599 UMLSCUI
CHEBI:177703 CHEBI
CHEMBL2364612 ChEMBL_ID
11156438 PUBCHEM_CID
DB11660 DRUGBANK_ID
D10441 KEGG_DRUG
9629 INN_ID
C568859 MESH_SUPPLEMENTAL_RECORD_UI
9635 IUPHAR_LIGAND_ID
763040006 SNOMEDCT_US
763567008 SNOMEDCT_US
C5888541 UMLSCUI
CHEMBL1050 ChEMBL_ID
41639-83-2 SECONDARY_CAS_RN
267110 MMSL
33340 MMSL
6441636 PUBCHEM_CID
017395 NDDF
1988390 RXNORM
EJ85341990 UNII
CHEBI:63925 CHEBI
EJ85341990 INXIGHT DRUGS
I6393O0922 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Vyzulta HUMAN PRESCRIPTION DRUG LABEL 1 24208-504 SOLUTION/ DROPS 0.24 mg OPHTHALMIC NDA 24 sections
Latanoprostene Bunod Ophthalmic Solution, 0.024% Human Prescription Drug Label 1 68083-563 SOLUTION/ DROPS 0.24 mg OPHTHALMIC ANDA 23 sections
Latanoprostene Bunod Ophthalmic Solution, 0.024% Human Prescription Drug Label 1 68083-564 SOLUTION/ DROPS 0.24 mg OPHTHALMIC ANDA 23 sections