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Identification
NameAlogliptin
Accession NumberDB06203
TypeSmall Molecule
GroupsApproved
DescriptionAlogliptin is a selective, orally-bioavailable inhibitor of enzymatic activity of dipeptidyl peptidase-4 (DPP-4). Chemically, alogliptin is prepared as a benzoate salt and exists predominantly as the R-enantiomer (>99%). It undergoes little or no chiral conversion in vivo to the (S)-enantiomer. FDA approved January 25, 2013.
Structure
Thumb
Synonyms
Alogliptina
Alogliptine
Alogliptinum
SYR-322
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AlogliptinTablet, film coated12.5 mg/1OralPerrigo New York Inc2016-04-08Not applicableUs
AlogliptinTablet, film coated25 mg/1OralPerrigo New York Inc2016-04-08Not applicableUs
AlogliptinTablet, film coated6.25 mg/1OralPerrigo New York Inc2016-04-08Not applicableUs
NesinaTablet6.25 mgOralTakeda Canada Inc2014-04-30Not applicableCanada
NesinaTablet, film coated25 mg/1OralTakeda Pharmaceuticals America, Inc.2013-01-25Not applicableUs
NesinaTablet12.5 mgOralTakeda Canada Inc2014-04-30Not applicableCanada
NesinaTablet, film coated6.25 mg/1OralTakeda Pharmaceuticals America, Inc.2013-01-25Not applicableUs
NesinaTablet25 mgOralTakeda Canada Inc2014-05-13Not applicableCanada
NesinaTablet, film coated12.5 mg/1OralTakeda Pharmaceuticals America, Inc.2013-01-25Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
Alogliptin and Metformin HydrochloridePerrigo New York Inc
Alogliptin and PioglitazonePerrigo New York Inc
IncresyncTakeda Pharma A/S
KazanoTakeda Canada Inc
OseniTakeda Canada Inc
Salts
Name/CASStructureProperties
Alogliptin Benzoate
Thumb
  • InChI Key: KEJICOXJTRHYAK-XFULWGLBSA-N
  • Monoisotopic Mass: 461.206304377
  • Average Mass: 461.513
DBSALT000007
Categories
UNIIJHC049LO86
CAS number850649-61-5
WeightAverage: 339.3916
Monoisotopic: 339.169524941
Chemical FormulaC18H21N5O2
InChI KeyZSBOMTDTBDDKMP-OAHLLOKOSA-N
InChI
InChI=1S/C18H21N5O2/c1-21-17(24)9-16(22-8-4-7-15(20)12-22)23(18(21)25)11-14-6-3-2-5-13(14)10-19/h2-3,5-6,9,15H,4,7-8,11-12,20H2,1H3/t15-/m1/s1
IUPAC Name
2-({6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl}methyl)benzonitrile
SMILES
CN1C(=O)C=C(N2CCC[C@@H](N)C2)N(CC2=C(C=CC=C2)C#N)C1=O
Pharmacology
IndicationIndicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Structured Indications
PharmacodynamicsPeak inhibition of DPP-4 occurs within 2-3 hours after a single-dose administration to healthy subjects. The peak inhibition of DPP-4 exceeded 93% across doses of 12.5 mg to 800 mg. Inhibition of DPP-4 remained above 80% at 24 hours for doses greater than or equal to 25 mg. Alogliptin also demonstrated decreases in postprandial glucagon while increasing postprandial active GLP-1 levels compared to placebo over an 8-hour period following a standardized meal. Alogliptin does not affect the QTc interval.
Mechanism of actionAlogliptin inhibits dipeptidyl peptidase 4 (DPP-4), which normally degrades the incretins glucose-dependent insulinotropic polypeptide (GIP) and glucagon like peptide 1 ( GLP-1). The inhibition of DPP-4 increases the amount of active plasma incretins which helps with glycemic control. GIP and GLP-1 stimulate glucose dependent secretion of insulin in pancreatic beta cells. GLP-1 has the additional effects of suppressing glucose dependent glucagon secretion, inducing satiety, reducing food intake, and reducing gastric emptying.
TargetKindPharmacological actionActionsOrganismUniProt ID
Dipeptidyl peptidase 4Proteinyes
inhibitor
HumanP27487 details
Related Articles
AbsorptionThe pharmacokinetics of NESINA was also shown to be similar in healthy subjects and in patients with type 2 diabetes. When single, oral doses up to 800 mg in healthy subjects and type 2 diabetes patients are given, the peak plasma alogliptin concentration (median Tmax) occurred 1 to 2 hours after dosing. Accumulation of aloglipin is minimal. The absolute bioavailability of NESINA is approximately 100%. Food does not affect the absorption of alogliptin.
Volume of distribution

Following a single, 12.5 mg intravenous infusion of alogliptin to healthy subjects, the volume of distribution during the terminal phase was 417 L, indicating that the drug is well distributed into tissues.

Protein bindingAlogliptin is 20% bound to plasma proteins.
Metabolism

Alogliptin does not undergo extensive metabolism. Two minor metabolites that were detected are N-demethylated alogliptin (<1% of parent compound) and N-acetylated alogliptin (<6% of parent compound). The N-demethylated metabolite is active and an inhibitor of DPP-4. The N-acetylated metabolite is inactive. Cytochrome enzymes that are involved with the metabolism of alogliptin are CYP2D6 and CYP3A4 but the extent to which this occurs is minimal. Approximately 10-20% of the dose is hepatically metabolized by cytochrome enzymes.

Route of eliminationRenal excretion (76%) and feces (13%). 60% to 71% of the dose is excreted as unchanged drug in the urine.
Half lifeTerminal half-life = 21 hours
Clearance

Renal clearance = 9.6 L/h (this value indicates some active renal tubular secretion);
Systemic clearance = 14.0 L/h.

ToxicityCommon adverse reactions (reported in ≥4% of patients treated with alogliptin 25 mg and more frequently than in patients who received placebo) are: nasopharyngitis, headache, and upper respiratory tract infection.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypoglycemic activities of Alogliptin.Experimental
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Alogliptin.Approved, Investigational
AbirateroneThe serum concentration of Alogliptin can be increased when it is combined with Abiraterone.Approved
AcetohexamideAlogliptin may increase the hypoglycemic activities of Acetohexamide.Withdrawn
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Alogliptin.Approved, Vet Approved
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Alogliptin.Approved, Investigational
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Alogliptin.Approved, Illicit, Investigational
Ambroxol acefyllinateThe serum concentration of Ambroxol acefyllinate can be decreased when it is combined with Alogliptin.Experimental
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Alogliptin.Illicit, Withdrawn
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Alogliptin.Approved
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Alogliptin.Approved
AmiodaroneThe metabolism of Alogliptin can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Alogliptin.Approved
AprepitantThe serum concentration of Alogliptin can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Aripiprazole.Approved, Investigational
Arsenic trioxideThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Arsenic trioxide.Approved, Investigational
ArtemetherThe metabolism of Alogliptin can be decreased when combined with Artemether.Approved
ArticaineThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Articaine.Approved
AsenapineThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Asenapine.Approved
AtazanavirThe metabolism of Alogliptin can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Alogliptin can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Alogliptin.Approved
BalsalazideBalsalazide may increase the hypoglycemic activities of Alogliptin.Approved, Investigational
BenazeprilThe risk or severity of adverse effects can be increased when Alogliptin is combined with Benazepril.Approved, Investigational
BendroflumethiazideThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Bendroflumethiazide.Approved
BenmoxinBenmoxin may increase the hypoglycemic activities of Alogliptin.Withdrawn
BetamethasoneThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Betamethasone.Approved, Vet Approved
BetaxololThe metabolism of Alogliptin can be decreased when combined with Betaxolol.Approved
BexaroteneThe serum concentration of Alogliptin can be decreased when it is combined with Bexarotene.Approved, Investigational
BoceprevirThe serum concentration of Alogliptin can be decreased when it is combined with Boceprevir.Approved
BortezomibThe metabolism of Alogliptin can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Alogliptin can be decreased when it is combined with Bosentan.Approved, Investigational
BrexpiprazoleThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Brexpiprazole.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Alogliptin.Approved, Investigational
BumetanideThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Bumetanide.Approved
BupropionThe metabolism of Alogliptin can be decreased when combined with Bupropion.Approved
BuserelinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Buserelin.Approved
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Alogliptin.Approved
CandoxatrilThe risk or severity of adverse effects can be increased when Alogliptin is combined with Candoxatril.Experimental
CaptoprilThe risk or severity of adverse effects can be increased when Alogliptin is combined with Captopril.Approved
CarbamazepineThe metabolism of Alogliptin can be increased when combined with Carbamazepine.Approved, Investigational
CaroxazoneCaroxazone may increase the hypoglycemic activities of Alogliptin.Withdrawn
CelecoxibThe metabolism of Alogliptin can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Alogliptin can be increased when it is combined with Ceritinib.Approved
ChloroquineThe metabolism of Alogliptin can be decreased when combined with Chloroquine.Approved, Vet Approved
ChlorothiazideThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Chlorothiazide.Approved, Vet Approved
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Alogliptin.Withdrawn
ChlorpromazineThe metabolism of Alogliptin can be decreased when combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideAlogliptin may increase the hypoglycemic activities of Chlorpropamide.Approved
ChlorthalidoneThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Chlorthalidone.Approved
CholecalciferolThe metabolism of Alogliptin can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CilazaprilThe risk or severity of adverse effects can be increased when Alogliptin is combined with Cilazapril.Approved
CimetidineThe metabolism of Alogliptin can be decreased when combined with Cimetidine.Approved
CinacalcetThe metabolism of Alogliptin can be decreased when combined with Cinacalcet.Approved
CinoxacinCinoxacin may increase the hypoglycemic activities of Alogliptin.Approved, Withdrawn
CiprofloxacinCiprofloxacin may increase the hypoglycemic activities of Alogliptin.Approved, Investigational
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Alogliptin.Approved, Investigational, Withdrawn
CitalopramThe metabolism of Alogliptin can be decreased when combined with Citalopram.Approved
ClarithromycinThe therapeutic efficacy of Clarithromycin can be decreased when used in combination with Alogliptin.Approved
ClemastineThe metabolism of Alogliptin can be decreased when combined with Clemastine.Approved
ClobazamThe metabolism of Alogliptin can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Alogliptin.Approved, Vet Approved
ClotrimazoleThe metabolism of Alogliptin can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Alogliptin can be decreased when combined with Clozapine.Approved
CobicistatThe serum concentration of Alogliptin can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Alogliptin can be decreased when combined with Cocaine.Approved, Illicit
ConivaptanThe serum concentration of Alogliptin can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be decreased when it is combined with Alogliptin.Approved
CorticotropinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Corticotropin.Approved, Vet Approved
Cortisone acetateThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Cortisone acetate.Approved
CrizotinibThe metabolism of Alogliptin can be decreased when combined with Crizotinib.Approved
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Alogliptin.Approved
CyclophosphamideThe risk or severity of adverse effects can be increased when Alogliptin is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Alogliptin.Approved, Investigational, Vet Approved
CyclosporineThe metabolism of Alogliptin can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Alogliptin can be decreased when it is combined with Dabrafenib.Approved
DanazolThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Danazol.Approved
DapoxetineDapoxetine may increase the hypoglycemic activities of Alogliptin.Investigational
DarifenacinThe metabolism of Alogliptin can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Alogliptin can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Alogliptin can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Alogliptin can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Alogliptin.Approved
dersalazinedersalazine may increase the hypoglycemic activities of Alogliptin.Investigational
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Alogliptin.Approved
DesogestrelThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Desogestrel.Approved
DesvenlafaxineDesvenlafaxine may increase the hypoglycemic activities of Alogliptin.Approved
DexamethasoneThe serum concentration of Alogliptin can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DiazoxideThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Diazoxide.Approved
DienestrolThe serum concentration of Dienestrol can be decreased when it is combined with Alogliptin.Approved
DienogestThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Dienogest.Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Alogliptin.Approved
DiflunisalDiflunisal may increase the hypoglycemic activities of Alogliptin.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Alogliptin.Approved
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Alogliptin.Approved
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Alogliptin.Illicit
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Alogliptin.Approved
DiphenhydramineThe metabolism of Alogliptin can be decreased when combined with Diphenhydramine.Approved
DisopyramideAlogliptin may increase the hypoglycemic activities of Disopyramide.Approved
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Alogliptin.Approved
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Alogliptin.Approved
DoxycyclineThe metabolism of Alogliptin can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Alogliptin can be decreased when combined with Dronedarone.Approved
DrospirenoneThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Drospirenone.Approved
DuloxetineThe metabolism of Alogliptin can be decreased when combined with Duloxetine.Approved
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Alogliptin.Approved
EfavirenzThe serum concentration of Alogliptin can be decreased when it is combined with Efavirenz.Approved, Investigational
EliglustatThe metabolism of Alogliptin can be decreased when combined with Eliglustat.Approved
EnalaprilThe risk or severity of adverse effects can be increased when Alogliptin is combined with Enalapril.Approved, Vet Approved
EnalaprilatThe risk or severity of adverse effects can be increased when Alogliptin is combined with Enalaprilat.Approved
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Alogliptin.Approved, Investigational
EnoxacinEnoxacin may increase the hypoglycemic activities of Alogliptin.Approved
EnzalutamideThe serum concentration of Alogliptin can be decreased when it is combined with Enzalutamide.Approved
EpinephrineThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Epinephrine.Approved, Vet Approved
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Alogliptin.Approved
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Alogliptin.Approved
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Alogliptin.Approved
ErythromycinThe metabolism of Alogliptin can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramEscitalopram may increase the hypoglycemic activities of Alogliptin.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Alogliptin can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Alogliptin.Investigational
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Alogliptin.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Estramustine can be decreased when it is combined with Alogliptin.Approved
Estrogens, esterifiedThe serum concentration of Estrogens, esterified can be decreased when it is combined with Alogliptin.Approved
Estrone sulfateThe serum concentration of Estrone sulfate can be decreased when it is combined with Alogliptin.Approved
Etacrynic acidThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Etacrynic acid.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Alogliptin.Approved
Ethynodiol diacetateThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Ethynodiol diacetate.Approved
EtonogestrelThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Etonogestrel.Approved, Investigational
EtoperidoneEtoperidone may increase the hypoglycemic activities of Alogliptin.Approved
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Alogliptin.Approved
EverolimusThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Everolimus.Approved
FleroxacinFleroxacin may increase the hypoglycemic activities of Alogliptin.Approved
FluconazoleThe metabolism of Alogliptin can be decreased when combined with Fluconazole.Approved
FludrocortisoneThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Fludrocortisone.Approved
FlumequineFlumequine may increase the hypoglycemic activities of Alogliptin.Withdrawn
FluoxetineThe metabolism of Alogliptin can be decreased when combined with Fluoxetine.Approved, Vet Approved
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Alogliptin.Approved, Illicit
FluvoxamineThe metabolism of Alogliptin can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Alogliptin can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Alogliptin can be increased when it is combined with Fosaprepitant.Approved
FosinoprilThe risk or severity of adverse effects can be increased when Alogliptin is combined with Fosinopril.Approved
FosphenytoinThe metabolism of Alogliptin can be increased when combined with Fosphenytoin.Approved
FurazolidoneFurazolidone may increase the hypoglycemic activities of Alogliptin.Approved, Vet Approved
FurosemideThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Furosemide.Approved, Vet Approved
Fusidic AcidThe serum concentration of Alogliptin can be increased when it is combined with Fusidic Acid.Approved
GarenoxacinGarenoxacin may increase the hypoglycemic activities of Alogliptin.Investigational
GarlicThe serum concentration of Alogliptin can be decreased when it is combined with Garlic.Approved
GatifloxacinGatifloxacin may increase the hypoglycemic activities of Alogliptin.Approved, Investigational
GemifloxacinGemifloxacin may increase the hypoglycemic activities of Alogliptin.Approved, Investigational
GlibornurideAlogliptin may increase the hypoglycemic activities of Glibornuride.Withdrawn
GliclazideAlogliptin may increase the hypoglycemic activities of Gliclazide.Approved
GlimepirideAlogliptin may increase the hypoglycemic activities of Glimepiride.Approved
GlipizideAlogliptin may increase the hypoglycemic activities of Glipizide.Approved
GliquidoneAlogliptin may increase the hypoglycemic activities of Gliquidone.Approved
GlisoxepideAlogliptin may increase the hypoglycemic activities of Glisoxepide.Approved
GlyburideAlogliptin may increase the hypoglycemic activities of Glyburide.Approved
GoserelinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Goserelin.Approved
GrepafloxacinGrepafloxacin may increase the hypoglycemic activities of Alogliptin.Withdrawn
HaloperidolThe metabolism of Alogliptin can be decreased when combined with Haloperidol.Approved
HexestrolThe serum concentration of Hexestrol can be decreased when it is combined with Alogliptin.Withdrawn
HistrelinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Histrelin.Approved
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Alogliptin.Approved
HydrochlorothiazideThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Hydrochlorothiazide.Approved, Vet Approved
HydrocortisoneThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Hydroflumethiazide.Approved
Hydroxyprogesterone caproateThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
IdelalisibThe serum concentration of Alogliptin can be increased when it is combined with Idelalisib.Approved
IloperidoneThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Iloperidone.Approved
ImatinibThe metabolism of Alogliptin can be decreased when combined with Imatinib.Approved
ImidaprilThe risk or severity of adverse effects can be increased when Alogliptin is combined with Imidapril.Investigational
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Alogliptin.Approved
IndalpineIndalpine may increase the hypoglycemic activities of Alogliptin.Investigational, Withdrawn
IndapamideThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Indapamide.Approved
IndinavirThe metabolism of Alogliptin can be decreased when combined with Indinavir.Approved
Insulin AspartAlogliptin may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirAlogliptin may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineAlogliptin may increase the hypoglycemic activities of Insulin Glargine.Approved
Insulin GlulisineAlogliptin may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanAlogliptin may increase the hypoglycemic activities of Insulin Human.Approved, Investigational
Insulin LisproAlogliptin may increase the hypoglycemic activities of Insulin Lispro.Approved
Insulin PorkAlogliptin may increase the hypoglycemic activities of Insulin Pork.Approved
IproclozideIproclozide may increase the hypoglycemic activities of Alogliptin.Withdrawn
IproniazidIproniazid may increase the hypoglycemic activities of Alogliptin.Withdrawn
IsavuconazoniumThe metabolism of Alogliptin can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Alogliptin.Approved
IsoniazidThe metabolism of Alogliptin can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Alogliptin can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Alogliptin can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Alogliptin can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Alogliptin can be decreased when combined with Ketoconazole.Approved, Investigational
LanreotideThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Lanreotide.Approved
LeuprolideThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Leuprolide.Approved, Investigational
LevofloxacinLevofloxacin may increase the hypoglycemic activities of Alogliptin.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Alogliptin.Approved
LevonorgestrelThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Levonorgestrel.Approved, Investigational
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Alogliptin.Approved, Nutraceutical
LisinoprilThe risk or severity of adverse effects can be increased when Alogliptin is combined with Lisinopril.Approved, Investigational
LomefloxacinLomefloxacin may increase the hypoglycemic activities of Alogliptin.Approved
LopinavirThe metabolism of Alogliptin can be decreased when combined with Lopinavir.Approved
LorcaserinThe metabolism of Alogliptin can be decreased when combined with Lorcaserin.Approved
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Alogliptin.Approved, Investigational
LuliconazoleThe serum concentration of Alogliptin can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Alogliptin can be increased when combined with Lumacaftor.Approved
LumefantrineThe metabolism of Alogliptin can be decreased when combined with Lumefantrine.Approved
LurasidoneThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Lurasidone.Approved
MebanazineMebanazine may increase the hypoglycemic activities of Alogliptin.Withdrawn
MecaserminAlogliptin may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
Medroxyprogesterone acetateThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Medroxyprogesterone acetate.Approved, Investigational
Megestrol acetateThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Megestrol acetate.Approved, Vet Approved
MesalazineMesalazine may increase the hypoglycemic activities of Alogliptin.Approved
MestranolThe serum concentration of Mestranol can be decreased when it is combined with Alogliptin.Approved
MethadoneThe metabolism of Alogliptin can be decreased when combined with Methadone.Approved
MethallenestrilThe serum concentration of Methallenestril can be decreased when it is combined with Alogliptin.Experimental
MethotrimeprazineThe metabolism of Alogliptin can be decreased when combined with Methotrimeprazine.Approved
MethyclothiazideThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Methyclothiazide.Approved
Methylene blueMethylene blue may increase the hypoglycemic activities of Alogliptin.Investigational
MethylprednisoloneThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Methylprednisolone.Approved, Vet Approved
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Alogliptin.Approved
MetolazoneThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Metolazone.Approved
MetoprololThe metabolism of Alogliptin can be decreased when combined with Metoprolol.Approved, Investigational
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Alogliptin.Approved, Illicit
MifepristoneThe serum concentration of Alogliptin can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranMilnacipran may increase the hypoglycemic activities of Alogliptin.Approved
MinaprineMinaprine may increase the hypoglycemic activities of Alogliptin.Approved
MirabegronThe metabolism of Alogliptin can be decreased when combined with Mirabegron.Approved
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Alogliptin.Approved
MitotaneThe serum concentration of Alogliptin can be decreased when it is combined with Mitotane.Approved
MoclobemideMoclobemide may increase the hypoglycemic activities of Alogliptin.Approved
ModafinilThe serum concentration of Alogliptin can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilThe risk or severity of adverse effects can be increased when Alogliptin is combined with Moexipril.Approved
MoxifloxacinMoxifloxacin may increase the hypoglycemic activities of Alogliptin.Approved, Investigational
NafcillinThe serum concentration of Alogliptin can be decreased when it is combined with Nafcillin.Approved
Nalidixic AcidNalidixic Acid may increase the hypoglycemic activities of Alogliptin.Approved
NateglinideAlogliptin may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
NCX 4016NCX 4016 may increase the hypoglycemic activities of Alogliptin.Investigational
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Alogliptin.Approved, Withdrawn
NelfinavirThe metabolism of Alogliptin can be decreased when combined with Nelfinavir.Approved
NemonoxacinNemonoxacin may increase the hypoglycemic activities of Alogliptin.Investigational
NetupitantThe serum concentration of Alogliptin can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Alogliptin can be increased when combined with Nevirapine.Approved
NiacinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Niacin.Approved, Investigational, Nutraceutical
NialamideNialamide may increase the hypoglycemic activities of Alogliptin.Withdrawn
NicardipineThe metabolism of Alogliptin can be decreased when combined with Nicardipine.Approved
NilotinibThe metabolism of Alogliptin can be decreased when combined with Nilotinib.Approved, Investigational
NitroaspirinNitroaspirin may increase the hypoglycemic activities of Alogliptin.Investigational
NorethisteroneThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Norethisterone.Approved
NorfloxacinNorfloxacin may increase the hypoglycemic activities of Alogliptin.Approved
NorgestimateThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Norgestimate.Approved
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Alogliptin.Approved
OctamoxinOctamoxin may increase the hypoglycemic activities of Alogliptin.Withdrawn
OctreotideThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Octreotide.Approved, Investigational
OfloxacinOfloxacin may increase the hypoglycemic activities of Alogliptin.Approved
OlanzapineThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Olanzapine.Approved, Investigational
OlaparibThe metabolism of Alogliptin can be decreased when combined with Olaparib.Approved
OlsalazineOlsalazine may increase the hypoglycemic activities of Alogliptin.Approved
OmapatrilatThe risk or severity of adverse effects can be increased when Alogliptin is combined with Omapatrilat.Investigational
OpipramolThe serum concentration of Opipramol can be increased when it is combined with Alogliptin.Investigational
OsimertinibThe serum concentration of Alogliptin can be increased when it is combined with Osimertinib.Approved
OxandroloneOxandrolone may increase the hypoglycemic activities of Alogliptin.Approved, Investigational
OxymetholoneOxymetholone may increase the hypoglycemic activities of Alogliptin.Approved, Illicit
PalbociclibThe serum concentration of Alogliptin can be increased when it is combined with Palbociclib.Approved
PaliperidoneThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Paliperidone.Approved
PanobinostatThe serum concentration of Alogliptin can be increased when it is combined with Panobinostat.Approved, Investigational
PargylinePargyline may increase the hypoglycemic activities of Alogliptin.Approved
ParoxetineThe metabolism of Alogliptin can be decreased when combined with Paroxetine.Approved, Investigational
PasireotideThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Pasireotide.Approved
PazufloxacinPazufloxacin may increase the hypoglycemic activities of Alogliptin.Investigational
PefloxacinPefloxacin may increase the hypoglycemic activities of Alogliptin.Approved
Peginterferon alfa-2bThe serum concentration of Alogliptin can be decreased when it is combined with Peginterferon alfa-2b.Approved
PegvisomantPegvisomant may increase the hypoglycemic activities of Alogliptin.Approved
PentamidineThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Pentamidine.Approved
PentobarbitalThe metabolism of Alogliptin can be increased when combined with Pentobarbital.Approved, Vet Approved
PerindoprilThe risk or severity of adverse effects can be increased when Alogliptin is combined with Perindopril.Approved
PethidineThe risk or severity of adverse effects can be increased when Alogliptin is combined with Pethidine.Approved
PhenelzinePhenelzine may increase the hypoglycemic activities of Alogliptin.Approved
PheniprazinePheniprazine may increase the hypoglycemic activities of Alogliptin.Withdrawn
PhenobarbitalThe metabolism of Alogliptin can be increased when combined with Phenobarbital.Approved
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Alogliptin.Withdrawn
PhenytoinThe metabolism of Alogliptin can be increased when combined with Phenytoin.Approved, Vet Approved
PimozideThe serum concentration of Pimozide can be increased when it is combined with Alogliptin.Approved
PiperazineThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Piperazine.Approved, Vet Approved
PipotiazineThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Pipotiazine.Approved
PirlindolePirlindole may increase the hypoglycemic activities of Alogliptin.Approved
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Alogliptin.Withdrawn
PolythiazideThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Polythiazide.Approved
PosaconazoleThe metabolism of Alogliptin can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrednisoloneThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Prednisolone.Approved, Vet Approved
PrednisoneThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Prednisone.Approved, Vet Approved
PrimidoneThe metabolism of Alogliptin can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Progesterone.Approved, Vet Approved
PromazineThe metabolism of Alogliptin can be decreased when combined with Promazine.Approved, Vet Approved
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Alogliptin.Approved
PrulifloxacinPrulifloxacin may increase the hypoglycemic activities of Alogliptin.Investigational
QuetiapineThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Quetiapine.Approved
QuinaprilThe risk or severity of adverse effects can be increased when Alogliptin is combined with Quinapril.Approved, Investigational
QuinethazoneThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Quinethazone.Approved
QuinidineThe metabolism of Alogliptin can be decreased when combined with Quinidine.Approved
QuinineThe metabolism of Alogliptin can be decreased when combined with Quinine.Approved
RamiprilThe risk or severity of adverse effects can be increased when Alogliptin is combined with Ramipril.Approved
RanolazineThe metabolism of Alogliptin can be decreased when combined with Ranolazine.Approved, Investigational
RasagilineRasagiline may increase the hypoglycemic activities of Alogliptin.Approved
RepaglinideAlogliptin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
RescinnamineThe risk or severity of adverse effects can be increased when Alogliptin is combined with Rescinnamine.Approved
RifabutinThe metabolism of Alogliptin can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Alogliptin can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Alogliptin can be increased when combined with Rifapentine.Approved
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Alogliptin.Approved
RisperidoneThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Risperidone.Approved, Investigational
RitonavirThe metabolism of Alogliptin can be decreased when combined with Ritonavir.Approved, Investigational
RolapitantThe metabolism of Alogliptin can be decreased when combined with Rolapitant.Approved
RopiniroleThe metabolism of Alogliptin can be decreased when combined with Ropinirole.Approved, Investigational
RosoxacinRosoxacin may increase the hypoglycemic activities of Alogliptin.Approved
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Alogliptin.Approved
SafrazineSafrazine may increase the hypoglycemic activities of Alogliptin.Withdrawn
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Alogliptin.Approved, Vet Approved
SaquinavirThe metabolism of Alogliptin can be decreased when combined with Saquinavir.Approved, Investigational
SelegilineSelegiline may increase the hypoglycemic activities of Alogliptin.Approved, Investigational, Vet Approved
SertralineThe metabolism of Alogliptin can be decreased when combined with Sertraline.Approved
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Alogliptin.Approved, Investigational
SiltuximabThe serum concentration of Alogliptin can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Alogliptin.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Alogliptin.Approved
SirolimusThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Sirolimus.Approved, Investigational
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Alogliptin.Approved
SpiraprilThe risk or severity of adverse effects can be increased when Alogliptin is combined with Spirapril.Approved
St. John's WortThe metabolism of Alogliptin can be increased when combined with St. John&#39;s Wort.Nutraceutical
StanozololStanozolol may increase the hypoglycemic activities of Alogliptin.Approved, Vet Approved
StiripentolThe serum concentration of Alogliptin can be increased when it is combined with Stiripentol.Approved
SulfadiazineAlogliptin may increase the hypoglycemic activities of Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleAlogliptin may increase the hypoglycemic activities of Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Alogliptin can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SunitinibAlogliptin may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
Synthetic Conjugated Estrogens, AThe serum concentration of Synthetic Conjugated Estrogens, A can be decreased when it is combined with Alogliptin.Approved
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Alogliptin.Approved, Investigational
TacrolimusThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Tacrolimus.Approved, Investigational
TelaprevirThe metabolism of Alogliptin can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Alogliptin can be decreased when combined with Telithromycin.Approved
TemafloxacinTemafloxacin may increase the hypoglycemic activities of Alogliptin.Withdrawn
TemocaprilThe risk or severity of adverse effects can be increased when Alogliptin is combined with Temocapril.Experimental, Investigational
TemsirolimusThe risk or severity of adverse effects can be increased when Alogliptin is combined with Temsirolimus.Approved
TerbinafineThe metabolism of Alogliptin can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TestosteroneTestosterone may increase the hypoglycemic activities of Alogliptin.Approved, Investigational
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Alogliptin.Approved
ThioridazineThe metabolism of Alogliptin can be decreased when combined with Thioridazine.Approved
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Alogliptin.Approved
TiclopidineThe metabolism of Alogliptin can be decreased when combined with Ticlopidine.Approved
TipranavirThe serum concentration of Alogliptin can be decreased when it is combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Alogliptin can be decreased when it is combined with Tocilizumab.Approved
TolazamideAlogliptin may increase the hypoglycemic activities of Tolazamide.Approved
TolbutamideAlogliptin may increase the hypoglycemic activities of Tolbutamide.Approved
ToloxatoneToloxatone may increase the hypoglycemic activities of Alogliptin.Approved
TorasemideThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Torasemide.Approved
TrandolaprilThe risk or severity of adverse effects can be increased when Alogliptin is combined with Trandolapril.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Alogliptin.Experimental
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Alogliptin.Approved
TriamcinoloneThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Triamcinolone.Approved, Vet Approved
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Alogliptin.Approved
TrichlormethiazideThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Trichlormethiazide.Approved, Vet Approved
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Alogliptin.Approved
TriptorelinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Triptorelin.Approved, Vet Approved
TrovafloxacinTrovafloxacin may increase the hypoglycemic activities of Alogliptin.Approved, Withdrawn
Valproic AcidThe serum concentration of Valproic Acid can be decreased when it is combined with Alogliptin.Approved, Investigational
VenlafaxineThe metabolism of Alogliptin can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Verapamil can be decreased when combined with Alogliptin.Approved
VoriconazoleThe metabolism of Alogliptin can be decreased when combined with Voriconazole.Approved, Investigational
VorinostatThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Vorinostat.Approved, Investigational
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Alogliptin.Approved
ZimelidineZimelidine may increase the hypoglycemic activities of Alogliptin.Withdrawn
ZiprasidoneThe metabolism of Alogliptin can be decreased when combined with Ziprasidone.Approved
Food InteractionsNot Available
References
Synthesis Reference

Kenji Nakamura, Kenichiro Kiyoshima, Junya Nomura, “SOLID PREPARATION COMPRISING ALOGLIPTIN AND PIOGLITAZONE.” U.S. Patent US20100092551, issued April 15, 2010.

US20100092551
General References
  1. Christopher R, Covington P, Davenport M, Fleck P, Mekki QA, Wann ER, Karim A: Pharmacokinetics, pharmacodynamics, and tolerability of single increasing doses of the dipeptidyl peptidase-4 inhibitor alogliptin in healthy male subjects. Clin Ther. 2008 Mar;30(3):513-27. doi: 10.1016/j.clinthera.2008.03.005. [PubMed:18405789 ]
  2. Covington P, Christopher R, Davenport M, Fleck P, Mekki QA, Wann ER, Karim A: Pharmacokinetic, pharmacodynamic, and tolerability profiles of the dipeptidyl peptidase-4 inhibitor alogliptin: a randomized, double-blind, placebo-controlled, multiple-dose study in adult patients with type 2 diabetes. Clin Ther. 2008 Mar;30(3):499-512. doi: 10.1016/j.clinthera.2008.03.004. [PubMed:18405788 ]
  3. Golightly LK, Drayna CC, McDermott MT: Comparative clinical pharmacokinetics of dipeptidyl peptidase-4 inhibitors. Clin Pharmacokinet. 2012 Aug 1;51(8):501-14. doi: 10.2165/11632930-000000000-00000. [PubMed:22686547 ]
External Links
ATC CodesA10BD13A10BD09A10BH04
AHFS Codes
  • 68:20.05
PDB EntriesNot Available
FDA labelDownload (648 KB)
MSDSDownload (479 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9942
Blood Brain Barrier+0.9738
Caco-2 permeable-0.5492
P-glycoprotein substrateSubstrate0.6453
P-glycoprotein inhibitor INon-inhibitor0.6811
P-glycoprotein inhibitor IINon-inhibitor0.9238
Renal organic cation transporterNon-inhibitor0.591
CYP450 2C9 substrateNon-substrate0.8003
CYP450 2D6 substrateNon-substrate0.7259
CYP450 3A4 substrateSubstrate0.5528
CYP450 1A2 substrateNon-inhibitor0.9169
CYP450 2C9 inhibitorNon-inhibitor0.8475
CYP450 2D6 inhibitorNon-inhibitor0.9038
CYP450 2C19 inhibitorNon-inhibitor0.8527
CYP450 3A4 inhibitorNon-inhibitor0.7608
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9363
Ames testNon AMES toxic0.5595
CarcinogenicityNon-carcinogens0.8887
BiodegradationNot ready biodegradable0.9931
Rat acute toxicity2.5603 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.5507
hERG inhibition (predictor II)Inhibitor0.8389
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
TabletOral12.5 mg
TabletOral25 mg
TabletOral6.25 mg
Tablet, film coatedOral12.5 mg/1
Tablet, film coatedOral25 mg/1
Tablet, film coatedOral6.25 mg/1
TabletOral
Tablet, film coatedOral
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5965584 No1996-06-192016-06-19Us
US6150383 No1996-06-192016-06-19Us
US6150384 No1996-06-192016-06-19Us
US6166042 No1996-06-192016-06-19Us
US6166043 No1996-06-192016-06-19Us
US6172090 No1996-06-192016-06-19Us
US6211205 No1996-06-192016-06-19Us
US6271243 No1996-06-192016-06-19Us
US6303640 No1996-08-092016-08-09Us
US6303661 No1997-04-242017-04-24Us
US6329404 No1996-06-192016-06-19Us
US6890898 No1999-02-022019-02-02Us
US7078381 No1999-02-022019-02-02Us
US7459428 No1999-02-022019-02-02Us
US7807689 No2008-06-272028-06-27Us
US8173663 No2005-03-152025-03-15Us
US8288539 No2005-03-152025-03-15Us
US8637079 No2009-06-042029-06-04Us
US8697125 No2009-01-222029-01-22Us
US8900638 No2009-05-242029-05-24Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilitySparingly soluble FDA label
Predicted Properties
PropertyValueSource
Water Solubility0.58 mg/mLALOGPS
logP0.66ALOGPS
logP1.16ChemAxon
logS-2.8ALOGPS
pKa (Strongest Basic)9.47ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area93.67 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity104.26 m3·mol-1ChemAxon
Polarizability35.44 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylmethylamines. These are compounds containing a phenylmethtylamine moiety, which consists of a phenyl group substituted by an methanamine.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenylmethylamines
Direct ParentPhenylmethylamines
Alternative Parents
Substituents
  • Dialkylarylamine
  • Phenylmethylamine
  • Benzonitrile
  • Pyrimidone
  • Aminopyrimidine
  • 3-aminopiperidine
  • Pyrimidine
  • Piperidine
  • Hydropyrimidine
  • Heteroaromatic compound
  • Vinylogous amide
  • Urea
  • Tertiary amine
  • Lactam
  • Azacycle
  • Organoheterocyclic compound
  • Nitrile
  • Carbonitrile
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Primary aliphatic amine
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Virus receptor activity
Specific Function:
Cell surface glycoprotein receptor involved in the costimulatory signal essential for T-cell receptor (TCR)-mediated T-cell activation. Acts as a positive regulator of T-cell coactivation, by binding at least ADA, CAV1, IGF2R, and PTPRC. Its binding to CAV1 and CARD11 induces T-cell proliferation and NF-kappa-B activation in a T-cell receptor/CD3-dependent manner. Its interaction with ADA also ...
Gene Name:
DPP4
Uniprot ID:
P27487
Molecular Weight:
88277.935 Da

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
Comments
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Drug created on March 19, 2008 10:17 / Updated on December 06, 2016 02:42