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

Stem definitionDrug idCAS RN
prostaglandins 4229 209860-87-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tafluprost
  • tafluprost ophthalmic solution
  • zioptan
  • taflotan
  • tapros
a prostaglandin analog is a selective FP prostanoid receptor agonist which is believed to reduce intraocular pressure by increasing uveoscleral outflow
  • Molecular weight: 452.54
  • Formula: C25H34F2O5
  • CLOGP: 4.26
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 75.99
  • ALOGS: -4.93
  • ROTB: 13

  • 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 ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK7,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CG,PRKDC,TEK,TGFBR1 22
kinase-selectivity-class AXL,GRK2 2
pfas-class PFAS structural alert (1 = True, 0 = False) 1

Approvals:

DateAgencyCompanyOrphan
Feb. 10, 2012 FDA OAK PHARMS 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
Ocular hyperaemia 219.94 32.78 57 1167 33741 90593482
Eye irritation 158.02 32.78 44 1180 33934 90593289
Eye pain 150.96 32.78 45 1179 44123 90583100
Eye pruritus 114.12 32.78 33 1191 28994 90598229
Intraocular pressure increased 66.09 32.78 16 1208 7077 90620146
Eye swelling 58.95 32.78 20 1204 29366 90597857
Vision blurred 44.41 32.78 24 1200 110269 90516954

FDA Adverse Event Reporting System (Male)

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
Ocular hyperaemia 81.32 48.61 21 422 15942 42604950
Eye irritation 63.01 48.61 16 427 11302 42609590

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
Ocular hyperaemia 145.32 30.55 42 1362 39244 110548651
Eye pain 94.37 30.55 32 1372 50067 110537828
Eye irritation 77.52 30.55 25 1379 33427 110554468
Eye pruritus 61.92 30.55 21 1383 32754 110555141
Intraocular pressure increased 55.54 30.55 15 1389 10861 110577034
Atrioventricular block second degree 40.44 30.55 11 1393 8170 110579725
Vision blurred 36.93 30.55 22 1382 129000 110458895
Pemphigoid 34.75 30.55 12 1392 19695 110568200
Cardiovascular insufficiency 34.11 30.55 8 1396 3280 110584615

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC S01EE05 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Prostaglandin analogues
FDA CS M0017805 Prostaglandins
FDA MoA N0000000106 Prostaglandin Receptor Agonists
FDA PE N0000009526 Increased Prostaglandin Activity
FDA EPC N0000175454 Prostaglandin Analog
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:39456 antiglaucoma drug
CHEBI has role CHEBI:66900 prostaglandin receptor agonist

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
0.0015% ZIOPTAN THEA PHARMA N202514 Feb. 10, 2012 RX SOLUTION/DROPS OPHTHALMIC 10864159 May 28, 2029 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE 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 CHEMBL CHEMBL

External reference:

IDSource
4031331 VUID
N0000184322 NUI
D06274 KEGG_DRUG
4031331 VANDF
C1451502 UMLSCUI
CHEBI:66899 CHEBI
CHEMBL1963683 ChEMBL_ID
DB08819 DRUGBANK_ID
C485333 MESH_SUPPLEMENTAL_RECORD_UI
7451 IUPHAR_LIGAND_ID
8374 INN_ID
1O6WQ6T7G3 UNII
9868491 PUBCHEM_CID
1244607 RXNORM
187543 MMSL
26696 MMSL
013244 NDDF
699181001 SNOMEDCT_US
704470009 SNOMEDCT_US
1O6WQ6T7G3 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Tafluprost HUMAN PRESCRIPTION DRUG LABEL 1 0781-6184 SOLUTION/ DROPS 0.00 mg OPHTHALMIC ANDA 24 sections
ZIOPTAN HUMAN PRESCRIPTION DRUG LABEL 1 17478-609 SOLUTION/ DROPS 0.00 mg OPHTHALMIC NDA 25 sections
tafluprost HUMAN PRESCRIPTION DRUG LABEL 1 42571-264 SOLUTION/ DROPS 0.00 mg OPHTHALMIC ANDA 23 sections
Tafluprost HUMAN PRESCRIPTION DRUG LABEL 1 50742-339 SOLUTION/ DROPS 0.02 mg OPHTHALMIC ANDA 23 sections
Tafluprost Ophthalmic HUMAN PRESCRIPTION DRUG LABEL 1 66993-429 SOLUTION/ DROPS 0.00 mg OPHTHALMIC NDA authorized generic 25 sections
ZIOPTAN HUMAN PRESCRIPTION DRUG LABEL 1 82584-609 SOLUTION/ DROPS 0.02 mg OPHTHALMIC NDA 26 sections