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Details

Stereochemistry RACEMIC
Molecular Formula C20H17F3N2O4
Molecular Weight 406.3552
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of FLOCTAFENINE

SMILES

OCC(O)COC(=O)C1=C(NC2=C3C=CC=C(C3=NC=C2)C(F)(F)F)C=CC=C1

InChI

InChIKey=APQPGQGAWABJLN-UHFFFAOYSA-N
InChI=1S/C20H17F3N2O4/c21-20(22,23)15-6-3-5-13-17(8-9-24-18(13)15)25-16-7-2-1-4-14(16)19(28)29-11-12(27)10-26/h1-9,12,26-27H,10-11H2,(H,24,25)

HIDE SMILES / InChI

Molecular Formula C20H17F3N2O4
Molecular Weight 406.3552
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description

Floctafenine is an analgesic agent used for the treatment of pain. The drug exerts its anti-inflammatory action by inhibiting COX-1 and COX-2, with a slight preference towards COX-1. Floctafenine is marketed in Canada under the name Floctafenine and it is withdrawn in Europe (Idarac Brand name).

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
2.33 mM [IC50]
3.47 mM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
FLOCTAFENINE

Cmax

ValueDoseCo-administeredAnalytePopulation
1.57 μg/mL
400 mg single, oral
FLOCTAFENIC ACID blood
Homo sapiens

Doses

AEs

PubMed

Sample Use Guides

In Vivo Use Guide
The usual adult dose of floctafenine is 200 to 400 mg every 6 to 8 hours as required. The maximum recommended daily dose is 1200 mg.
Route of Administration: Oral
In Vitro Use Guide
The effects of floctafenine and its active metabolite on platelet COX-1, monocyte and 5-LO activities of whole blood in vitro were assessed by incubating increasing concentrations of floctafenine or floctafenic acid (0.001-100 mM) with peripheral whole blood samples drawn from healthy volunteers.
Substance Class Chemical
Record UNII
O04HVX6A9Q
Record Status Validated (UNII)
Record Version