Identification

Name
Talniflumate
Accession Number
DB09295
Type
Small Molecule
Groups
Approved
Description

Talniflumate, is an anti-inflammatory molecule studied and used as a mucin regulator in the treatment of cystic fibrosis, chronic obstructive pulmonary disease (COPD) and asthma [5]. In addition, it is used in inflammatory conditions such as rheumatoid arthritis. Phase I trials with talniflumate for the treatment of cystic fibrosis and COPD were completed in August 2001, and phase II trials were performed in Ireland for the treatment of cystic fibrosis but this research has now been discontinued [7, 10]. Talniflumate has been approved for approximately 20 years in Argentina other countries (excluding the United States, Europe, and Japan) [10].

Structure
Thumb
Synonyms
Not Available
International/Other Brands
Huluma (Myungmoon) / Somalgen / Stofen (Shin poong) / Talmain (Korea United Pharm) / Talmen (Daewoo) / Talniflumate Hanall (Hanall Biopharma) / Talumat (Taiguk) / Tariful (KWANG DONG)
Categories
UNII
JFK78S0U9S
CAS number
66898-62-2
Weight
Average: 414.34
Monoisotopic: 414.082741396
Chemical Formula
C21H13F3N2O4
InChI Key
ANMLJLFWUCQGKZ-UHFFFAOYSA-N
InChI
InChI=1S/C21H13F3N2O4/c22-21(23,24)12-5-3-6-13(11-12)26-17-16(9-4-10-25-17)19(28)30-20-15-8-2-1-7-14(15)18(27)29-20/h1-11,20H,(H,25,26)
IUPAC Name
3-oxo-1,3-dihydro-2-benzofuran-1-yl 2-{[3-(trifluoromethyl)phenyl]amino}pyridine-3-carboxylate
SMILES
FC(F)(F)C1=CC(NC2=C(C=CC=N2)C(=O)OC2OC(=O)C3=CC=CC=C23)=CC=C1

Pharmacology

Indication

Talnifumate is a phthalidyl ester of nifumic acid, which has potent analgesic and anti-inflammatory effects and is widely used to treat inflammatory disorders, such as rheumatoid arthritis and osteoarthritis [13], and has also been studied for the management of cystic fibrosis [8].

Pharmacodynamics

Talniflumate is metabolized to its prodrug, niflumic acid, which has several pharmacodynamic effects. Firstly, it blocks synthesis of mucin. Secondly, talniflumate blocks prostaglandin synthesis by cyclooxygenases, which aids in pain and inflammation management.

Mechanism of action

Talniflumate is a strong and selective inhibitor of core mucin-synthesizing enzyme GCNT3 (core 2 b-1,6 N-acetylglucosaminyltransferase). Talniflumate decreases gene expression of GCNT3 and production of mucins in vivo and in vitro. Talniflumate improves response of pancreatic tumors to gefitinib (chemotherapy drug). Talniflumate is a strong calcium-activated chloride channel (CaCC) blocker.

TargetActionsOrganism
UProstaglandin G/H synthase 1
antagonist
Human
UProstaglandin G/H synthase 2
antagonist
Human
UChloride channel protein ClC-Ka
antagonist
Human
Absorption
Not Available
Volume of distribution

In 12 subjects after a single oral administration, total plasma clearance of the main metabolite, niflumic acid, averaged 45 ml/min giving a distribution volume of 0.12 l/kg on average [3].

Protein binding

Niflumic acid, the active form of Talniflumate, is weak acid that is strongly bound to plasma proteins. Bioavailability was 100% in a study of 12 volunteers. It is a weak acid, strongly bound to plasma proteins [3].

Metabolism

Extensive liver metabolism.

Route of elimination
Not Available
Half life

Approximately 2h in 12 subjects [3]

Clearance

This drug undergoes extensive first pass effect.

Toxicity

LD50 orally in rats: 12000 mg/kg [14]

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
(4R)-limoneneThe risk or severity of adverse effects can be increased when Talniflumate is combined with (4R)-limonene.Investigational
16-BromoepiandrosteroneThe risk or severity of adverse effects can be increased when 16-Bromoepiandrosterone is combined with Talniflumate.Investigational
19-norandrostenedioneThe risk or severity of adverse effects can be increased when 19-norandrostenedione is combined with Talniflumate.Experimental, Illicit
5-androstenedioneThe risk or severity of adverse effects can be increased when 5-androstenedione is combined with Talniflumate.Experimental, Illicit
AceclofenacThe risk or severity of adverse effects can be increased when Talniflumate is combined with Aceclofenac.Approved, Investigational
AcemetacinThe risk or severity of adverse effects can be increased when Talniflumate is combined with Acemetacin.Approved, Experimental, Investigational
AcenocoumarolTalniflumate may increase the anticoagulant activities of Acenocoumarol.Approved, Investigational
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Talniflumate.Approved, Vet Approved
AdapaleneThe risk or severity of adverse effects can be increased when Talniflumate is combined with Adapalene.Approved
AlaproclateAlaproclate may increase the antiplatelet activities of Talniflumate.Experimental
AlclofenacThe risk or severity of adverse effects can be increased when Talniflumate is combined with Alclofenac.Approved, Withdrawn
AlclometasoneThe risk or severity of adverse effects can be increased when Alclometasone is combined with Talniflumate.Approved
AldosteroneThe risk or severity of adverse effects can be increased when Aldosterone is combined with Talniflumate.Experimental, Investigational
AlminoprofenThe risk or severity of adverse effects can be increased when Talniflumate is combined with Alminoprofen.Experimental
AmcinonideThe risk or severity of adverse effects can be increased when Amcinonide is combined with Talniflumate.Approved
AmikacinThe risk or severity of nephrotoxicity can be increased when Talniflumate is combined with Amikacin.Approved, Investigational, Vet Approved
AmlodipineThe therapeutic efficacy of Amlodipine can be decreased when used in combination with Talniflumate.Approved
AndrographolideThe risk or severity of adverse effects can be increased when Talniflumate is combined with Andrographolide.Investigational
AndrostenedioneThe risk or severity of adverse effects can be increased when Androstenedione is combined with Talniflumate.Experimental, Illicit
AnecortaveThe risk or severity of adverse effects can be increased when Anecortave is combined with Talniflumate.Investigational
anecortave acetateThe risk or severity of adverse effects can be increased when anecortave acetate is combined with Talniflumate.Investigational
AnisodamineThe risk or severity of adverse effects can be increased when Talniflumate is combined with Anisodamine.Investigational
AntipyrineThe risk or severity of adverse effects can be increased when Talniflumate is combined with Antipyrine.Approved, Investigational
ApocyninThe risk or severity of adverse effects can be increased when Talniflumate is combined with Apocynin.Investigational
ApremilastThe risk or severity of adverse effects can be increased when Talniflumate is combined with Apremilast.Approved, Investigational
AtamestaneThe risk or severity of adverse effects can be increased when Atamestane is combined with Talniflumate.Investigational
AzapropazoneThe risk or severity of adverse effects can be increased when Talniflumate is combined with Azapropazone.Withdrawn
AzelastineThe risk or severity of adverse effects can be increased when Talniflumate is combined with Azelastine.Approved
BacitracinThe risk or severity of nephrotoxicity can be increased when Talniflumate is combined with Bacitracin.Approved, Vet Approved
BalsalazideThe risk or severity of adverse effects can be increased when Talniflumate is combined with Balsalazide.Approved, Investigational
BazedoxifeneTalniflumate may increase the thrombogenic activities of Bazedoxifene.Approved, Investigational
Beclomethasone dipropionateThe risk or severity of gastrointestinal irritation can be increased when Beclomethasone dipropionate is combined with Talniflumate.Approved, Investigational
BendazacThe risk or severity of adverse effects can be increased when Talniflumate is combined with Bendazac.Experimental
BenorilateThe risk or severity of adverse effects can be increased when Talniflumate is combined with Benorilate.Experimental
BenoxaprofenThe risk or severity of adverse effects can be increased when Talniflumate is combined with Benoxaprofen.Withdrawn
BenzydamineThe risk or severity of adverse effects can be increased when Talniflumate is combined with Benzydamine.Approved
BepridilThe therapeutic efficacy of Bepridil can be decreased when used in combination with Talniflumate.Approved, Withdrawn
BetamethasoneThe risk or severity of adverse effects can be increased when Betamethasone is combined with Talniflumate.Approved, Vet Approved
BevoniumThe risk or severity of adverse effects can be increased when Talniflumate is combined with Bevonium.Experimental
BromfenacThe risk or severity of adverse effects can be increased when Talniflumate is combined with Bromfenac.Approved
BucillamineThe risk or severity of adverse effects can be increased when Talniflumate is combined with Bucillamine.Investigational
BudesonideThe risk or severity of gastrointestinal irritation can be increased when Budesonide is combined with Talniflumate.Approved
BufexamacThe risk or severity of adverse effects can be increased when Talniflumate is combined with Bufexamac.Approved, Experimental
BumadizoneThe risk or severity of adverse effects can be increased when Talniflumate is combined with Bumadizone.Experimental
Carbaspirin calciumThe risk or severity of adverse effects can be increased when Talniflumate is combined with Carbaspirin calcium.Experimental, Investigational
CarprofenThe risk or severity of adverse effects can be increased when Talniflumate is combined with Carprofen.Approved, Vet Approved, Withdrawn
CarvedilolTalniflumate may decrease the antihypertensive activities of Carvedilol.Approved, Investigational
CastanospermineThe risk or severity of adverse effects can be increased when Talniflumate is combined with Castanospermine.Experimental
CelecoxibThe risk or severity of adverse effects can be increased when Talniflumate is combined with Celecoxib.Approved, Investigational
ChloroquineThe risk or severity of adverse effects can be increased when Talniflumate is combined with Chloroquine.Approved, Investigational, Vet Approved
ChlorotrianiseneTalniflumate may increase the thrombogenic activities of Chlorotrianisene.Investigational, Withdrawn
Choline magnesium trisalicylateThe risk or severity of adverse effects can be increased when Talniflumate is combined with Choline magnesium trisalicylate.Approved
CiclesonideThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Talniflumate.Approved, Investigational
CiprofloxacinTalniflumate may increase the neuroexcitatory activities of Ciprofloxacin.Approved, Investigational
CitalopramCitalopram may increase the antiplatelet activities of Talniflumate.Approved
ClobetasolThe risk or severity of adverse effects can be increased when Clobetasol is combined with Talniflumate.Approved, Investigational
Clobetasol propionateThe risk or severity of adverse effects can be increased when Clobetasol propionate is combined with Talniflumate.Approved
ClobetasoneThe risk or severity of adverse effects can be increased when Clobetasone is combined with Talniflumate.Approved
ClocortoloneThe risk or severity of adverse effects can be increased when Clocortolone is combined with Talniflumate.Approved
ClonixinThe risk or severity of adverse effects can be increased when Talniflumate is combined with Clonixin.Approved
ClorindioneTalniflumate may increase the anticoagulant activities of Clorindione.Experimental
Conjugated estrogensTalniflumate may increase the thrombogenic activities of Conjugated estrogens.Approved
Cortexolone 17α-propionateThe risk or severity of adverse effects can be increased when Cortexolone 17α-propionate is combined with Talniflumate.Investigational
CorticosteroneThe risk or severity of adverse effects can be increased when Corticosterone is combined with Talniflumate.Experimental
Cortisone acetateThe risk or severity of adverse effects can be increased when Cortisone acetate is combined with Talniflumate.Approved, Investigational
CurcuminThe risk or severity of adverse effects can be increased when Talniflumate is combined with Curcumin.Approved, Investigational
CyclosporineThe risk or severity of renal failure and hypertension can be increased when Talniflumate is combined with Cyclosporine.Approved, Investigational, Vet Approved
DaidzeinTalniflumate may increase the thrombogenic activities of Daidzein.Experimental
DapoxetineDapoxetine may increase the antiplatelet activities of Talniflumate.Investigational
DeflazacortThe risk or severity of adverse effects can be increased when Deflazacort is combined with Talniflumate.Approved, Investigational
DesonideThe risk or severity of adverse effects can be increased when Desonide is combined with Talniflumate.Approved, Investigational
DesoximetasoneThe risk or severity of adverse effects can be increased when Desoximetasone is combined with Talniflumate.Approved
Desoxycorticosterone acetateThe risk or severity of adverse effects can be increased when Desoxycorticosterone acetate is combined with Talniflumate.Approved
Desoxycorticosterone PivalateThe risk or severity of adverse effects can be increased when Desoxycorticosterone Pivalate is combined with Talniflumate.Experimental, Vet Approved
DesvenlafaxineThe risk or severity of gastrointestinal bleeding and gastrointestinal ulceration can be increased when Desvenlafaxine is combined with Talniflumate.Approved, Investigational
DexamethasoneThe risk or severity of gastrointestinal irritation can be increased when Dexamethasone is combined with Talniflumate.Approved, Investigational, Vet Approved
Dexamethasone isonicotinateThe risk or severity of adverse effects can be increased when Dexamethasone isonicotinate is combined with Talniflumate.Vet Approved
DexniguldipineThe therapeutic efficacy of Dexniguldipine can be decreased when used in combination with Talniflumate.Experimental
DiclofenacThe risk or severity of adverse effects can be increased when Diclofenac is combined with Talniflumate.Approved, Vet Approved
DicoumarolTalniflumate may increase the anticoagulant activities of Dicoumarol.Approved
DienestrolTalniflumate may increase the thrombogenic activities of Dienestrol.Approved, Investigational
DiethylstilbestrolTalniflumate may increase the thrombogenic activities of Diethylstilbestrol.Approved, Investigational
DifenpiramideThe risk or severity of adverse effects can be increased when Talniflumate is combined with Difenpiramide.Experimental
DiflorasoneThe risk or severity of adverse effects can be increased when Diflorasone is combined with Talniflumate.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Talniflumate is combined with Diflunisal.Approved, Investigational
DifluocortoloneThe risk or severity of adverse effects can be increased when Difluocortolone is combined with Talniflumate.Approved, Investigational, Withdrawn
DifluprednateThe risk or severity of adverse effects can be increased when Difluprednate is combined with Talniflumate.Approved
DiltiazemThe therapeutic efficacy of Diltiazem can be decreased when used in combination with Talniflumate.Approved, Investigational
DiphenadioneTalniflumate may increase the anticoagulant activities of Diphenadione.Experimental
DoxazosinThe therapeutic efficacy of Doxazosin can be decreased when used in combination with Talniflumate.Approved
DroxicamThe risk or severity of adverse effects can be increased when Talniflumate is combined with Droxicam.Withdrawn
DuloxetineDuloxetine may increase the antiplatelet activities of Talniflumate.Approved
DuvelisibThe risk or severity of adverse effects can be increased when Talniflumate is combined with Duvelisib.Investigational
E-6201The risk or severity of adverse effects can be increased when Talniflumate is combined with E-6201.Investigational
EfonidipineThe therapeutic efficacy of Efonidipine can be decreased when used in combination with Talniflumate.Approved, Investigational
EpimestrolTalniflumate may increase the thrombogenic activities of Epimestrol.Experimental
EpirizoleThe risk or severity of adverse effects can be increased when Talniflumate is combined with Epirizole.Approved
EquileninThe risk or severity of adverse effects can be increased when Equilenin is combined with Talniflumate.Experimental
EquilinThe risk or severity of adverse effects can be increased when Equilin is combined with Talniflumate.Approved
EquolTalniflumate may increase the thrombogenic activities of Equol.Investigational
EscitalopramEscitalopram may increase the antiplatelet activities of Talniflumate.Approved, Investigational
EstradiolTalniflumate may increase the thrombogenic activities of Estradiol.Approved, Investigational, Vet Approved
Estradiol acetateTalniflumate may increase the thrombogenic activities of Estradiol acetate.Approved, Investigational, Vet Approved
Estradiol cypionateTalniflumate may increase the thrombogenic activities of Estradiol cypionate.Approved, Investigational, Vet Approved
Estradiol valerateTalniflumate may increase the thrombogenic activities of Estradiol valerate.Approved, Investigational, Vet Approved
EstriolTalniflumate may increase the thrombogenic activities of Estriol.Approved, Investigational, Vet Approved
Estrogens, esterifiedTalniflumate may increase the thrombogenic activities of Estrogens, esterified.Approved
EstroneTalniflumate may increase the thrombogenic activities of Estrone.Approved
Estrone sulfateThe risk or severity of adverse effects can be increased when Estrone sulfate is combined with Talniflumate.Approved
EtanerceptThe risk or severity of adverse effects can be increased when Talniflumate is combined with Etanercept.Approved, Investigational
EthenzamideThe risk or severity of adverse effects can be increased when Talniflumate is combined with Ethenzamide.Experimental
Ethinyl EstradiolTalniflumate may increase the thrombogenic activities of Ethinyl Estradiol.Approved
Ethyl biscoumacetateTalniflumate may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EtodolacThe risk or severity of adverse effects can be increased when Talniflumate is combined with Etodolac.Approved, Investigational, Vet Approved
EtofenamateThe risk or severity of adverse effects can be increased when Talniflumate is combined with Etofenamate.Approved, Investigational
EtoperidoneEtoperidone may increase the antiplatelet activities of Talniflumate.Withdrawn
EtoricoxibThe risk or severity of adverse effects can be increased when Talniflumate is combined with Etoricoxib.Approved, Investigational
Evening primrose oilThe risk or severity of adverse effects can be increased when Talniflumate is combined with Evening primrose oil.Investigational, Nutraceutical
ExisulindThe risk or severity of adverse effects can be increased when Talniflumate is combined with Exisulind.Investigational
FelbinacThe risk or severity of adverse effects can be increased when Talniflumate is combined with Felbinac.Experimental
FelodipineThe therapeutic efficacy of Felodipine can be decreased when used in combination with Talniflumate.Approved, Investigational
FenbufenThe risk or severity of adverse effects can be increased when Talniflumate is combined with Fenbufen.Approved
FenoprofenThe risk or severity of adverse effects can be increased when Talniflumate is combined with Fenoprofen.Approved
FentiazacThe risk or severity of adverse effects can be increased when Talniflumate is combined with Fentiazac.Experimental
FeprazoneThe risk or severity of adverse effects can be increased when Talniflumate is combined with Feprazone.Experimental
Ferulic acidThe risk or severity of adverse effects can be increased when Talniflumate is combined with Ferulic acid.Experimental
FloctafenineThe risk or severity of adverse effects can be increased when Talniflumate is combined with Floctafenine.Approved, Withdrawn
FluasteroneThe risk or severity of adverse effects can be increased when Fluasterone is combined with Talniflumate.Investigational
FludrocortisoneThe risk or severity of adverse effects can be increased when Fludrocortisone is combined with Talniflumate.Approved, Investigational
FluindioneTalniflumate may increase the anticoagulant activities of Fluindione.Approved, Investigational
FlumethasoneThe risk or severity of adverse effects can be increased when Flumethasone is combined with Talniflumate.Approved, Vet Approved
FlunisolideThe risk or severity of adverse effects can be increased when Flunisolide is combined with Talniflumate.Approved, Investigational
FlunixinThe risk or severity of adverse effects can be increased when Talniflumate is combined with Flunixin.Vet Approved
FlunoxaprofenThe risk or severity of adverse effects can be increased when Talniflumate is combined with Flunoxaprofen.Experimental
Fluocinolone AcetonideThe risk or severity of adverse effects can be increased when Fluocinolone Acetonide is combined with Talniflumate.Approved, Investigational, Vet Approved
FluocinonideThe risk or severity of adverse effects can be increased when Fluocinonide is combined with Talniflumate.Approved, Investigational
FluocortoloneThe risk or severity of adverse effects can be increased when Fluocortolone is combined with Talniflumate.Approved, Withdrawn
FluorometholoneThe risk or severity of adverse effects can be increased when Fluorometholone is combined with Talniflumate.Approved, Investigational
FluoxetineThe risk or severity of gastrointestinal bleeding and gastrointestinal ulceration can be increased when Fluoxetine is combined with Talniflumate.Approved, Vet Approved
FluprednideneThe risk or severity of adverse effects can be increased when Fluprednidene is combined with Talniflumate.Approved, Withdrawn
FluprednisoloneThe risk or severity of adverse effects can be increased when Fluprednisolone is combined with Talniflumate.Approved
FlurandrenolideThe risk or severity of adverse effects can be increased when Flurandrenolide is combined with Talniflumate.Approved
FlurbiprofenThe risk or severity of adverse effects can be increased when Talniflumate is combined with Flurbiprofen.Approved, Investigational
FluticasoneThe risk or severity of adverse effects can be increased when Fluticasone is combined with Talniflumate.Approved, Experimental, Investigational
Fluticasone furoateThe risk or severity of adverse effects can be increased when Fluticasone furoate is combined with Talniflumate.Approved
Fluticasone propionateThe risk or severity of gastrointestinal irritation can be increased when Fluticasone propionate is combined with Talniflumate.Approved
FluvoxamineThe risk or severity of gastrointestinal bleeding and gastrointestinal ulceration can be increased when Fluvoxamine is combined with Talniflumate.Approved, Investigational
FormestaneThe risk or severity of adverse effects can be increased when Formestane is combined with Talniflumate.Approved, Investigational, Withdrawn
FosinoprilThe risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Talniflumate is combined with Fosinopril.Approved
FurosemideThe therapeutic efficacy of Furosemide can be decreased when used in combination with Talniflumate.Approved, Vet Approved
GenisteinTalniflumate may increase the thrombogenic activities of Genistein.Investigational
GlipizideThe protein binding of Glipizide can be decreased when combined with Talniflumate.Approved, Investigational
GlyburideThe protein binding of Glyburide can be decreased when combined with Talniflumate.Approved
GuacetisalThe risk or severity of adverse effects can be increased when Talniflumate is combined with Guacetisal.Experimental
GuanfacineThe therapeutic efficacy of Guanfacine can be decreased when used in combination with Talniflumate.Approved, Investigational
HalcinonideThe risk or severity of adverse effects can be increased when Halcinonide is combined with Talniflumate.Approved, Investigational, Withdrawn
HE3286The risk or severity of adverse effects can be increased when HE3286 is combined with Talniflumate.Investigational
HexestrolTalniflumate may increase the thrombogenic activities of Hexestrol.Withdrawn
HigenamineThe risk or severity of adverse effects can be increased when Talniflumate is combined with Higenamine.Investigational
HydrochlorothiazideThe therapeutic efficacy of Hydrochlorothiazide can be decreased when used in combination with Talniflumate.Approved, Vet Approved
HydrocortisoneThe risk or severity of gastrointestinal irritation can be increased when Hydrocortisone is combined with Talniflumate.Approved, Vet Approved
Hydrocortisone acetateThe risk or severity of gastrointestinal irritation can be increased when Hydrocortisone acetate is combined with Talniflumate.Approved, Vet Approved
Hydrocortisone butyrateThe risk or severity of gastrointestinal irritation can be increased when Hydrocortisone butyrate is combined with Talniflumate.Approved, Vet Approved
IbandronateThe risk or severity of gastrointestinal bleeding can be increased when Talniflumate is combined with Ibandronate.Approved, Investigational
IbuprofenThe risk or severity of adverse effects can be increased when Ibuprofen is combined with Talniflumate.Approved
IbuproxamThe risk or severity of adverse effects can be increased when Talniflumate is combined with Ibuproxam.Withdrawn
IcatibantThe risk or severity of adverse effects can be increased when Talniflumate is combined with Icatibant.Approved, Investigational
Imidazole salicylateThe risk or severity of adverse effects can be increased when Talniflumate is combined with Imidazole salicylate.Experimental
IndalpineIndalpine may increase the antiplatelet activities of Talniflumate.Investigational, Withdrawn
IndobufenThe risk or severity of adverse effects can be increased when Talniflumate is combined with Indobufen.Investigational
IndomethacinThe risk or severity of adverse effects can be increased when Talniflumate is combined with Indomethacin.Approved, Investigational
IndoprofenThe risk or severity of adverse effects can be increased when Talniflumate is combined with Indoprofen.Withdrawn
IsoxicamThe risk or severity of adverse effects can be increased when Talniflumate is combined with Isoxicam.Withdrawn
IsradipineThe therapeutic efficacy of Isradipine can be decreased when used in combination with Talniflumate.Approved, Investigational
IstaroximeThe risk or severity of adverse effects can be increased when Istaroxime is combined with Talniflumate.Investigational
KebuzoneThe risk or severity of adverse effects can be increased when Talniflumate is combined with Kebuzone.Experimental
KetoprofenThe risk or severity of adverse effects can be increased when Talniflumate is combined with Ketoprofen.Approved, Vet Approved
KetorolacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Talniflumate.Approved
LabetalolTalniflumate may decrease the antihypertensive activities of Labetalol.Approved
LacidipineThe therapeutic efficacy of Lacidipine can be decreased when used in combination with Talniflumate.Approved, Investigational
LatanoprostThe therapeutic efficacy of Latanoprost can be decreased when used in combination with Talniflumate.Approved, Investigational
LeflunomideThe risk or severity of adverse effects can be increased when Talniflumate is combined with Leflunomide.Approved, Investigational
LercanidipineThe therapeutic efficacy of Lercanidipine can be decreased when used in combination with Talniflumate.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the antiplatelet activities of Talniflumate.Approved, Investigational
LisofyllineThe risk or severity of adverse effects can be increased when Talniflumate is combined with Lisofylline.Investigational
LonazolacThe risk or severity of adverse effects can be increased when Talniflumate is combined with Lonazolac.Experimental
LornoxicamThe risk or severity of adverse effects can be increased when Talniflumate is combined with Lornoxicam.Approved, Investigational
LosartanThe risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Losartan is combined with Talniflumate.Approved
LoteprednolThe risk or severity of adverse effects can be increased when Loteprednol is combined with Talniflumate.Approved
LoxoprofenThe risk or severity of adverse effects can be increased when Talniflumate is combined with Loxoprofen.Approved, Investigational
LumiracoxibThe risk or severity of adverse effects can be increased when Talniflumate is combined with Lumiracoxib.Approved, Investigational
Magnesium salicylateThe risk or severity of adverse effects can be increased when Talniflumate is combined with Magnesium salicylate.Approved
ManidipineThe therapeutic efficacy of Manidipine can be decreased when used in combination with Talniflumate.Approved, Investigational
MasoprocolThe risk or severity of adverse effects can be increased when Talniflumate is combined with Masoprocol.Approved, Investigational
ME-609The risk or severity of adverse effects can be increased when ME-609 is combined with Talniflumate.Investigational
Meclofenamic acidThe risk or severity of adverse effects can be increased when Talniflumate is combined with Meclofenamic acid.Approved, Vet Approved
MedrysoneThe risk or severity of adverse effects can be increased when Medrysone is combined with Talniflumate.Approved
Mefenamic acidThe risk or severity of adverse effects can be increased when Talniflumate is combined with Mefenamic acid.Approved
MelengestrolThe risk or severity of adverse effects can be increased when Melengestrol is combined with Talniflumate.Vet Approved
MeloxicamThe risk or severity of adverse effects can be increased when Talniflumate is combined with Meloxicam.Approved, Vet Approved
MesalazineThe risk or severity of adverse effects can be increased when Talniflumate is combined with Mesalazine.Approved
MestranolTalniflumate may increase the thrombogenic activities of Mestranol.Approved
MetamizoleThe risk or severity of adverse effects can be increased when Talniflumate is combined with Metamizole.Approved, Investigational, Withdrawn
MethallenestrilTalniflumate may increase the thrombogenic activities of Methallenestril.Experimental
MethylprednisoloneThe risk or severity of gastrointestinal irritation can be increased when Methylprednisolone is combined with Talniflumate.Approved, Vet Approved
MetoprololTalniflumate may decrease the antihypertensive activities of Metoprolol.Approved, Investigational
MibefradilThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Talniflumate.Investigational, Withdrawn
MilnacipranMilnacipran may increase the antiplatelet activities of Talniflumate.Approved, Investigational
MinoxidilThe therapeutic efficacy of Minoxidil can be decreased when used in combination with Talniflumate.Approved, Investigational
MizoribineThe risk or severity of adverse effects can be increased when Talniflumate is combined with Mizoribine.Investigational
MofebutazoneThe risk or severity of adverse effects can be increased when Talniflumate is combined with Mofebutazone.Experimental
MometasoneThe risk or severity of adverse effects can be increased when Mometasone is combined with Talniflumate.Approved, Vet Approved
MoxestrolTalniflumate may increase the thrombogenic activities of Moxestrol.Experimental
MoxifloxacinTalniflumate may increase the neuroexcitatory activities of Moxifloxacin.Approved, Investigational
Mycophenolate mofetilThe risk or severity of adverse effects can be increased when Talniflumate is combined with Mycophenolate mofetil.Approved, Investigational
Mycophenolic acidThe risk or severity of adverse effects can be increased when Talniflumate is combined with Mycophenolic acid.Approved
NabumetoneThe risk or severity of adverse effects can be increased when Talniflumate is combined with Nabumetone.Approved
NafamostatThe risk or severity of adverse effects can be increased when Talniflumate is combined with Nafamostat.Approved, Investigational
NaftifineThe risk or severity of adverse effects can be increased when Talniflumate is combined with Naftifine.Approved
NaftopidilThe therapeutic efficacy of Naftopidil can be decreased when used in combination with Talniflumate.Investigational
NaproxenThe risk or severity of adverse effects can be increased when Naproxen is combined with Talniflumate.Approved, Vet Approved
NCX 1022The risk or severity of adverse effects can be increased when NCX 1022 is combined with Talniflumate.Investigational
NefazodoneNefazodone may increase the antiplatelet activities of Talniflumate.Approved, Withdrawn
NeomycinThe risk or severity of nephrotoxicity can be increased when Talniflumate is combined with Neomycin.Approved, Vet Approved
NepafenacThe risk or severity of adverse effects can be increased when Talniflumate is combined with Nepafenac.Approved, Investigational
NicardipineThe therapeutic efficacy of Nicardipine can be decreased when used in combination with Talniflumate.Approved, Investigational
NifenazoneThe risk or severity of adverse effects can be increased when Talniflumate is combined with Nifenazone.Experimental
Niflumic AcidThe risk or severity of adverse effects can be increased when Talniflumate is combined with Niflumic Acid.Approved
NiguldipineThe therapeutic efficacy of Niguldipine can be decreased when used in combination with Talniflumate.Experimental
NilvadipineThe therapeutic efficacy of Nilvadipine can be decreased when used in combination with Talniflumate.Approved, Investigational
NimesulideThe risk or severity of adverse effects can be increased when Nimesulide is combined with Talniflumate.Approved, Investigational, Withdrawn
NimodipineThe therapeutic efficacy of Nimodipine can be decreased when used in combination with Talniflumate.Approved, Investigational
NisoldipineThe therapeutic efficacy of Nisoldipine can be decreased when used in combination with Talniflumate.Approved
NitrendipineThe therapeutic efficacy of Nitrendipine can be decreased when used in combination with Talniflumate.Approved, Investigational
NitroaspirinThe risk or severity of adverse effects can be increased when Talniflumate is combined with Nitroaspirin.Investigational
Oleoyl-estroneThe risk or severity of adverse effects can be increased when Oleoyl-estrone is combined with Talniflumate.Investigational
OlopatadineThe risk or severity of adverse effects can be increased when Talniflumate is combined with Olopatadine.Approved
OlsalazineThe risk or severity of adverse effects can be increased when Talniflumate is combined with Olsalazine.Approved
OrgoteinThe risk or severity of adverse effects can be increased when Talniflumate is combined with Orgotein.Vet Approved
OxaprozinThe risk or severity of adverse effects can be increased when Talniflumate is combined with Oxaprozin.Approved
OxyphenbutazoneThe risk or severity of adverse effects can be increased when Talniflumate is combined with Oxyphenbutazone.Approved, Withdrawn
ParamethasoneThe risk or severity of adverse effects can be increased when Paramethasone is combined with Talniflumate.Approved
ParecoxibThe risk or severity of adverse effects can be increased when Talniflumate is combined with Parecoxib.Approved
ParomomycinThe risk or severity of nephrotoxicity can be increased when Talniflumate is combined with Paromomycin.Approved, Investigational
ParoxetineThe risk or severity of gastrointestinal bleeding and gastrointestinal ulceration can be increased when Paroxetine is combined with Talniflumate.Approved, Investigational
ParthenolideThe risk or severity of adverse effects can be increased when Talniflumate is combined with Parthenolide.Approved, Investigational
PhenindioneTalniflumate may increase the anticoagulant activities of Phenindione.Approved, Investigational
PhenprocoumonTalniflumate may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
PhenylbutazoneThe risk or severity of adverse effects can be increased when Talniflumate is combined with Phenylbutazone.Approved, Vet Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Talniflumate is combined with Pimecrolimus.Approved, Investigational
PirfenidoneThe risk or severity of adverse effects can be increased when Talniflumate is combined with Pirfenidone.Approved, Investigational
PiroxicamThe risk or severity of adverse effects can be increased when Talniflumate is combined with Piroxicam.Approved, Investigational
PirprofenThe risk or severity of adverse effects can be increased when Talniflumate is combined with Pirprofen.Experimental
Polyestradiol phosphateTalniflumate may increase the thrombogenic activities of Polyestradiol phosphate.Approved
PranoprofenThe risk or severity of adverse effects can be increased when Talniflumate is combined with Pranoprofen.Experimental, Investigational
PrasteroneThe risk or severity of adverse effects can be increased when Prasterone is combined with Talniflumate.Approved, Investigational, Nutraceutical
Prasterone sulfateThe risk or severity of adverse effects can be increased when Prasterone sulfate is combined with Talniflumate.Investigational
PrednicarbateThe risk or severity of adverse effects can be increased when Prednicarbate is combined with Talniflumate.Approved, Investigational
PrednisoloneThe risk or severity of gastrointestinal irritation can be increased when Prednisolone is combined with Talniflumate.Approved, Vet Approved
PrednisoneThe risk or severity of adverse effects can be increased when Prednisone is combined with Talniflumate.Approved, Vet Approved
PregnenoloneThe risk or severity of adverse effects can be increased when Pregnenolone is combined with Talniflumate.Approved, Experimental, Investigational
ProglumetacinThe risk or severity of adverse effects can be increased when Talniflumate is combined with Proglumetacin.Experimental
PromestrieneTalniflumate may increase the thrombogenic activities of Promestriene.Investigational
PropacetamolThe risk or severity of adverse effects can be increased when Talniflumate is combined with Propacetamol.Approved, Investigational
PropafenoneTalniflumate may decrease the antihypertensive activities of Propafenone.Approved
PropranololTalniflumate may decrease the antihypertensive activities of Propranolol.Approved, Investigational
PropyphenazoneThe risk or severity of adverse effects can be increased when Talniflumate is combined with Propyphenazone.Experimental
ProquazoneThe risk or severity of adverse effects can be increased when Talniflumate is combined with Proquazone.Experimental
PTC299The risk or severity of adverse effects can be increased when Talniflumate is combined with PTC299.Investigational
QuinestrolTalniflumate may increase the thrombogenic activities of Quinestrol.Approved
ResveratrolThe risk or severity of adverse effects can be increased when Talniflumate is combined with Resveratrol.Approved, Experimental, Investigational
RimexoloneThe risk or severity of adverse effects can be increased when Rimexolone is combined with Talniflumate.Approved
RofecoxibThe risk or severity of adverse effects can be increased when Talniflumate is combined with Rofecoxib.Approved, Investigational, Withdrawn
SalicylamideThe risk or severity of adverse effects can be increased when Talniflumate is combined with Salicylamide.Approved
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Talniflumate.Approved, Investigational, Vet Approved
SalsalateThe risk or severity of adverse effects can be increased when Talniflumate is combined with Salsalate.Approved
SecoisolariciresinolTalniflumate may increase the thrombogenic activities of Secoisolariciresinol.Investigational
SemapimodThe risk or severity of adverse effects can be increased when Talniflumate is combined with Semapimod.Investigational
SeratrodastThe risk or severity of adverse effects can be increased when Talniflumate is combined with Seratrodast.Approved
SerrapeptaseThe risk or severity of adverse effects can be increased when Talniflumate is combined with Serrapeptase.Investigational
SertralineSertraline may increase the antiplatelet activities of Talniflumate.Approved
Sodium CitrateThe risk or severity of bleeding and hemorrhage can be increased when Talniflumate is combined with Sodium Citrate.Approved, Investigational
Sodium phosphate, monobasicThe risk or severity of renal failure can be increased when Sodium phosphate, monobasic is combined with Talniflumate.Approved
SpironolactoneThe risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Talniflumate is combined with Spironolactone.Approved
SRT501The risk or severity of adverse effects can be increased when Talniflumate is combined with SRT501.Investigational
SulfasalazineThe risk or severity of adverse effects can be increased when Sulfasalazine is combined with Talniflumate.Approved
SulindacThe risk or severity of adverse effects can be increased when Sulindac is combined with Talniflumate.Approved, Investigational
SuprofenThe risk or severity of adverse effects can be increased when Talniflumate is combined with Suprofen.Approved, Withdrawn
SuxibuzoneThe risk or severity of adverse effects can be increased when Talniflumate is combined with Suxibuzone.Experimental
Synthetic Conjugated Estrogens, ATalniflumate may increase the thrombogenic activities of Synthetic Conjugated Estrogens, A.Approved
Synthetic Conjugated Estrogens, BTalniflumate may increase the thrombogenic activities of Synthetic Conjugated Estrogens, B.Approved
TarenflurbilThe risk or severity of adverse effects can be increased when Talniflumate is combined with Tarenflurbil.Investigational
TenidapThe risk or severity of adverse effects can be increased when Talniflumate is combined with Tenidap.Experimental
TenoxicamThe risk or severity of adverse effects can be increased when Talniflumate is combined with Tenoxicam.Approved
TepoxalinThe risk or severity of adverse effects can be increased when Talniflumate is combined with Tepoxalin.Vet Approved
TeriflunomideThe risk or severity of adverse effects can be increased when Talniflumate is combined with Teriflunomide.Approved
TetrahydropalmatineThe therapeutic efficacy of Tetrahydropalmatine can be decreased when used in combination with Talniflumate.Investigational
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Talniflumate is combined with Tiaprofenic acid.Approved
TiboloneTalniflumate may increase the thrombogenic activities of Tibolone.Approved, Investigational
TinoridineThe risk or severity of adverse effects can be increased when Talniflumate is combined with Tinoridine.Investigational
TioclomarolTalniflumate may increase the anticoagulant activities of Tioclomarol.Experimental
TixocortolThe risk or severity of adverse effects can be increased when Tixocortol is combined with Talniflumate.Approved, Withdrawn
Tolfenamic AcidThe risk or severity of adverse effects can be increased when Tolfenamic Acid is combined with Talniflumate.Approved, Investigational
TolmetinThe risk or severity of adverse effects can be increased when Talniflumate is combined with Tolmetin.Approved
TriamcinoloneThe risk or severity of adverse effects can be increased when Triamcinolone is combined with Talniflumate.Approved, Vet Approved
TribenosideThe risk or severity of adverse effects can be increased when Talniflumate is combined with Tribenoside.Experimental
TriptolideThe risk or severity of adverse effects can be increased when Talniflumate is combined with Triptolide.Investigational
Trolamine salicylateThe risk or severity of adverse effects can be increased when Trolamine salicylate is combined with Talniflumate.Approved
UlobetasolThe risk or severity of adverse effects can be increased when Ulobetasol is combined with Talniflumate.Approved
ValdecoxibThe risk or severity of adverse effects can be increased when Talniflumate is combined with Valdecoxib.Approved, Investigational, Withdrawn
VancomycinTalniflumate may decrease the excretion rate of Vancomycin which could result in a higher serum level.Approved
VenlafaxineThe risk or severity of gastrointestinal bleeding and gastrointestinal ulceration can be increased when Venlafaxine is combined with Talniflumate.Approved
WarfarinTalniflumate may increase the anticoagulant activities of Warfarin.Approved
ZaltoprofenThe risk or severity of adverse effects can be increased when Talniflumate is combined with Zaltoprofen.Approved, Investigational
ZeranolTalniflumate may increase the thrombogenic activities of Zeranol.Vet Approved
ZileutonThe risk or severity of adverse effects can be increased when Talniflumate is combined with Zileuton.Approved, Investigational, Withdrawn
ZimelidineZimelidine may increase the antiplatelet activities of Talniflumate.Withdrawn
Zoledronic acidThe risk or severity of gastrointestinal bleeding can be increased when Talniflumate is combined with Zoledronic acid.Approved
ZomepiracThe risk or severity of adverse effects can be increased when Talniflumate is combined with Zomepirac.Withdrawn
Food Interactions
Not Available

References

General References
  1. Knight D: Talniflumate (Genaera). Curr Opin Investig Drugs. 2004 May;5(5):557-62. [PubMed:15202731]
  2. Rao CV, Janakiram NB, Madka V, Kumar G, Scott EJ, Pathuri G, Bryant T, Kutche H, Zhang Y, Biddick L, Gali H, Zhao YD, Lightfoot S, Mohammed A: Small-Molecule Inhibition of GCNT3 Disrupts Mucin Biosynthesis and Malignant Cellular Behaviors in Pancreatic Cancer. Cancer Res. 2016 Apr 1;76(7):1965-74. doi: 10.1158/0008-5472.CAN-15-2820. Epub 2016 Feb 15. [PubMed:26880801]
  3. Houin G, Tremblay D, Bree F, Dufour A, Ledudal P, Tillement JP: The pharmacokinetics and availability of niflumic acid in humans. Int J Clin Pharmacol Ther Toxicol. 1983 Mar;21(3):130-4. [PubMed:6852999]
  4. Talniflumate [Link]
  5. Screening study for genetic polymorphisms af­fecting pharmacokinetics of talnifumate [Link]
  6. Pharmacokinetics of talniflumate, a prodrug of niflumic acid, following oral administration to man [Link]
  7. Talniflumate (Genaera) [Link]
  8. Talniflunate [Link]
  9. Chemistry Dashboard: Talniflumate [Link]
  10. TALNIFLUMATE [Link]
  11. Talniflumate Increases Survival in a Cystic Fibrosis Mouse Model of Distal Intestinal Obstructive Syndrome [Link]
  12. TALNIFLUMATE [Link]
  13. KWANG DONG TARIFUL TAB [Link]
  14. Talniflumate [Link]
External Links
KEGG Drug
D02701
PubChem Compound
48229
PubChem Substance
310265187
ChemSpider
43868
ChEBI
91991
ChEMBL
CHEMBL1081506
Drugs.com
Drugs.com Drug Page

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)177[L1404]
boiling point (°C)454[L1404]
water solubility5 mg/mL clear[L1399]
logP4.47[L1404]
Predicted Properties
PropertyValueSource
Water Solubility0.00417 mg/mLALOGPS
logP4ALOGPS
logP6.65ChemAxon
logS-5ALOGPS
pKa (Strongest Acidic)13.33ChemAxon
pKa (Strongest Basic)3.5ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area77.52 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity100.11 m3·mol-1ChemAxon
Polarizability37.83 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as benzofuranones. These are organic compounds containing a benzene ring fused to a furanone.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzofurans
Sub Class
Benzofuranones
Direct Parent
Benzofuranones
Alternative Parents
Trifluoromethylbenzenes / Phthalides / Pyridinecarboxylic acids / Aniline and substituted anilines / Aminopyridines and derivatives / Dicarboxylic acids and derivatives / Imidolactams / Vinylogous amides / Heteroaromatic compounds / Amino acids and derivatives
show 11 more
Substituents
Trifluoromethylbenzene / Benzofuranone / Isobenzofuranone / Phthalide / Pyridine carboxylic acid / Pyridine carboxylic acid or derivatives / Isocoumaran / Aniline or substituted anilines / Aminopyridine / Monocyclic benzene moiety
show 27 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Prostaglandin-endoperoxide synthase activity
Specific Function
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gas...
Gene Name
PTGS1
Uniprot ID
P23219
Uniprot Name
Prostaglandin G/H synthase 1
Molecular Weight
68685.82 Da
References
  1. TALNIFLUMATE [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Prostaglandin-endoperoxide synthase activity
Specific Function
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and...
Gene Name
PTGS2
Uniprot ID
P35354
Uniprot Name
Prostaglandin G/H synthase 2
Molecular Weight
68995.625 Da
References
  1. TALNIFLUMATE [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Voltage-gated chloride channel activity
Specific Function
Voltage-gated chloride channel. Chloride channels have several functions including the regulation of cell volume; membrane potential stabilization, signal transduction and transepithelial transport...
Gene Name
CLCNKA
Uniprot ID
P51800
Uniprot Name
Chloride channel protein ClC-Ka
Molecular Weight
75284.08 Da
References
  1. TALNIFLUMATE [Link]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Prostaglandin-endoperoxide synthase activity
Specific Function
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gas...
Gene Name
PTGS1
Uniprot ID
P23219
Uniprot Name
Prostaglandin G/H synthase 1
Molecular Weight
68685.82 Da
References
  1. TALNIFLUMATE [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Prostaglandin-endoperoxide synthase activity
Specific Function
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and...
Gene Name
PTGS2
Uniprot ID
P35354
Uniprot Name
Prostaglandin G/H synthase 2
Molecular Weight
68995.625 Da
References
  1. TALNIFLUMATE [Link]

Drug created on October 30, 2015 09:27 / Updated on August 02, 2018 06:16