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Identification
NameNelfinavir
Accession NumberDB00220  (APRD00003)
TypeSmall Molecule
GroupsApproved
Description

A potent HIV-1 protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children. [PubChem]

Structure
Thumb
Synonyms
Viracept
External Identifiers
  • AG1343
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Viracepttablet, film coated625 mg/1oralREMEDYREPACK INC.2013-03-272016-03-11Us
Viracepttablet, film coated625 mg/1oralAGOURON2003-04-30Not applicableUs
Viraceptpowder50 mg/goralAGOURON1997-03-142016-02-26Us
Viracepttablet, film coated250 mg/1oralAGOURON1997-03-14Not applicableUs
Viracepttablet, film coated250 mg/1oralPd Rx Pharmaceuticals, Inc.1997-03-14Not applicableUs
Viracepttablet, film coated625 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Viracepttablet625 mgoralPfizer Canada Inc2004-08-11Not applicableCanada
Viracepttablet, film coated250 mg/1oralH.J. Harkins Company, Inc.1997-03-14Not applicableUs
Viracept -250mgtablet250 mgoralPfizer Canada Inc1998-09-21Not applicableCanada
Viracept -50mgpowder50 mgoralPfizer Canada Inc1998-09-21Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Nelfinavir mesylate
ThumbNot applicableDBSALT000885
Categories
UNIIHO3OGH5D7I
CAS number159989-64-7
WeightAverage: 567.782
Monoisotopic: 567.313077633
Chemical FormulaC32H45N3O4S
InChI KeyInChIKey=QAGYKUNXZHXKMR-HKWSIXNMSA-N
InChI
InChI=1S/C32H45N3O4S/c1-21-25(15-10-16-28(21)36)30(38)33-26(20-40-24-13-6-5-7-14-24)29(37)19-35-18-23-12-9-8-11-22(23)17-27(35)31(39)34-32(2,3)4/h5-7,10,13-16,22-23,26-27,29,36-37H,8-9,11-12,17-20H2,1-4H3,(H,33,38)(H,34,39)/t22-,23+,26-,27-,29+/m0/s1
IUPAC Name
(3S,4aS,8aS)-N-tert-butyl-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylphenyl)formamido]-4-(phenylsulfanyl)butyl]-decahydroisoquinoline-3-carboxamide
SMILES
[H][C@@]12CCCC[C@]1([H])CN(C[C@@H](O)[[email protected]](CSC1=CC=CC=C1)NC(=O)C1=C(C)C(O)=CC=C1)[C@@H](C2)C(=O)NC(C)(C)C
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as alpha amino acid amides. These are amide derivatives of alpha amino acids.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassAmino acids, peptides, and analogues
Direct ParentAlpha amino acid amides
Alternative Parents
Substituents
  • Alpha-amino acid amide
  • Piperidinecarboxylic acid
  • Piperidinecarboxamide
  • 2-piperidinecarboxamide
  • Benzoic acid or derivatives
  • Benzamide
  • Thiophenol ether
  • O-cresol
  • Benzoyl
  • Alkylarylthioether
  • Toluene
  • Phenol
  • Benzenoid
  • Piperidine
  • Monocyclic benzene moiety
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Secondary alcohol
  • Carboxamide group
  • 1,2-aminoalcohol
  • Azacycle
  • Organoheterocyclic compound
  • Sulfenyl compound
  • Thioether
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationUsed in combination with other antiviral drugs in the treatment of HIV in both adults and children.
PharmacodynamicsNelfinavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Nelfinavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs.
Mechanism of actionNelfinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.
Related Articles
AbsorptionWell absorbed following oral administration.
Volume of distribution
  • 2 to 7 L/kg
Protein binding>98%
Metabolism

Primarily hepatic via cytochrome P450 (CYP450) enzymes. CYP3A and CYP2C19 appear to be the predominant enzymes that metabolize nelfinavir in humans. One major and several minor metabolites are found in plasma; the major oxidative metabolite has in vitro antiviral activity comparable to that of the parent drug.

Route of eliminationThe terminal half-life in plasma was typically 3.5 to 5 hours. The majority (87%) of an oral 750 mg dose containing 14C-nelfinavir was recovered in the feces; fecal radioactivity consisted of numerous oxidative metabolites (78%) and unchanged nelfinavir (22%). Only 1–2% of the dose was recovered in urine, of which unchanged nelfinavir was the major component.
Half life3.5 - 5 hours
ClearanceNot Available
ToxicityOral LD50 is over 5g/kg in rats. Side effects include thirst and hunger, unexplained weight loss, increased urination, fatigue, and dry, itchy skin.
Affected organisms
  • Human Immunodeficiency Virus
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.7472
Blood Brain Barrier-0.9659
Caco-2 permeable-0.7148
P-glycoprotein substrateSubstrate0.9332
P-glycoprotein inhibitor IInhibitor0.8121
P-glycoprotein inhibitor IIInhibitor0.7572
Renal organic cation transporterNon-inhibitor0.8178
CYP450 2C9 substrateNon-substrate0.7482
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.7408
CYP450 1A2 substrateNon-inhibitor0.9085
CYP450 2C9 inhibitorNon-inhibitor0.7994
CYP450 2D6 inhibitorNon-inhibitor0.8071
CYP450 2C19 inhibitorNon-inhibitor0.6335
CYP450 3A4 inhibitorInhibitor0.5465
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8977
Ames testNon AMES toxic0.8008
CarcinogenicityNon-carcinogens0.8547
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.4704 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9786
hERG inhibition (predictor II)Inhibitor0.785
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Agouron pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
Powderoral50 mg/g
Tabletoral625 mg
Tablet, film coatedoral250 mg/1
Tablet, film coatedoral625 mg/1
Tabletoral250 mg
Powderoral50 mg
Prices
Unit descriptionCostUnit
Viracept 625 mg tablet11.24USD tablet
Viracept 250 mg tablet3.46USD tablet
Viracept 50 mg/gm Powder0.54USD gm
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2173328 No1999-08-312014-10-07Canada
US5484926 No1994-04-072014-04-07Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point349.84 °CNot Available
water solubilitySlightly solubleNot Available
logP6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00191 mg/mLALOGPS
logP4.61ALOGPS
logP4.72ChemAxon
logS-5.5ALOGPS
pKa (Strongest Acidic)9.32ChemAxon
pKa (Strongest Basic)8.18ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area101.9 Å2ChemAxon
Rotatable Bond Count10ChemAxon
Refractivity162.67 m3·mol-1ChemAxon
Polarizability63.8 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

DrugSyn.org

US5461154
General References
  1. Kaldor SW, Kalish VJ, Davies JF 2nd, Shetty BV, Fritz JE, Appelt K, Burgess JA, Campanale KM, Chirgadze NY, Clawson DK, Dressman BA, Hatch SD, Khalil DA, Kosa MB, Lubbehusen PP, Muesing MA, Patick AK, Reich SH, Su KS, Tatlock JH: Viracept (nelfinavir mesylate, AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease. J Med Chem. 1997 Nov 21;40(24):3979-85. [PubMed:9397180 ]
External Links
ATC CodesJ05AE04
AHFS Codes
  • 08:18.08.08
PDB Entries
FDA labelDownload (294 KB)
MSDSDownload (56.6 KB)
Interactions
Drug Interactions
Drug
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Nelfinavir.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Nelfinavir.
Ado-trastuzumab emtansineThe serum concentration of the active metabolites of ado-trastuzumab emtansine can be increased when ado-trastuzumab emtansine is used in combination with Nelfinavir.
AlfentanilThe metabolism of Alfentanil can be decreased when combined with Nelfinavir.
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Nelfinavir.
AlitretinoinThe metabolism of Alitretinoin can be decreased when combined with Nelfinavir.
AlmotriptanThe serum concentration of Almotriptan can be increased when it is combined with Nelfinavir.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Nelfinavir.
AlosetronThe serum concentration of Alosetron can be increased when it is combined with Nelfinavir.
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Nelfinavir.
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Nelfinavir.
AmiodaroneThe serum concentration of Amiodarone can be increased when it is combined with Nelfinavir.
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Nelfinavir.
AmlodipineThe metabolism of Amlodipine can be decreased when combined with Nelfinavir.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Nelfinavir.
AprepitantThe metabolism of Aprepitant can be decreased when combined with Nelfinavir.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Nelfinavir.
ArmodafinilThe metabolism of Armodafinil can be decreased when combined with Nelfinavir.
ArtemetherThe serum concentration of Artemether can be increased when it is combined with Nelfinavir.
AstemizoleThe serum concentration of Astemizole can be increased when it is combined with Nelfinavir.
AtazanavirThe metabolism of Atazanavir can be decreased when combined with Nelfinavir.
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Nelfinavir.
AvanafilThe serum concentration of Avanafil can be increased when it is combined with Nelfinavir.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Nelfinavir.
AzelastineThe serum concentration of Azelastine can be increased when it is combined with Nelfinavir.
AzithromycinThe serum concentration of Azithromycin can be increased when it is combined with Nelfinavir.
BarnidipineThe serum concentration of Barnidipine can be increased when it is combined with Nelfinavir.
BatimastatThe serum concentration of Nelfinavir can be increased when it is combined with Batimastat.
BedaquilineThe serum concentration of Bedaquiline can be increased when it is combined with Nelfinavir.
BenzphetamineThe metabolism of Benzphetamine can be decreased when combined with Nelfinavir.
BepridilThe metabolism of Bepridil can be decreased when combined with Nelfinavir.
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Nelfinavir.
BexaroteneThe serum concentration of Nelfinavir can be decreased when it is combined with Bexarotene.
BisoprololThe metabolism of Bisoprolol can be decreased when combined with Nelfinavir.
BoceprevirThe serum concentration of Nelfinavir can be decreased when it is combined with Boceprevir.
BortezomibThe serum concentration of Bortezomib can be increased when it is combined with Nelfinavir.
BosentanThe serum concentration of Bosentan can be increased when it is combined with Nelfinavir.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Nelfinavir.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Nelfinavir.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Nelfinavir.
BrinzolamideThe serum concentration of Brinzolamide can be increased when it is combined with Nelfinavir.
BromocriptineThe metabolism of Bromocriptine can be decreased when combined with Nelfinavir.
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Nelfinavir.
BuprenorphineThe metabolism of Buprenorphine can be decreased when combined with Nelfinavir.
BuspironeThe metabolism of Buspirone can be decreased when combined with Nelfinavir.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Nelfinavir.
CabozantinibThe serum concentration of Cabozantinib can be increased when it is combined with Nelfinavir.
CalcitriolThe metabolism of Calcitriol can be decreased when combined with Nelfinavir.
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Nelfinavir.
CarbamazepineThe metabolism of Nelfinavir can be increased when combined with Carbamazepine.
CeritinibThe serum concentration of Ceritinib can be increased when it is combined with Nelfinavir.
ChlordiazepoxideThe metabolism of Chlordiazepoxide can be decreased when combined with Nelfinavir.
ChloroquineThe metabolism of Chloroquine can be decreased when combined with Nelfinavir.
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Nelfinavir.
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Nelfinavir.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Nelfinavir.
CimetidineThe serum concentration of Nelfinavir can be decreased when it is combined with Cimetidine.
CinacalcetThe metabolism of Cinacalcet can be decreased when combined with Nelfinavir.
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Nelfinavir.
CitalopramThe metabolism of Citalopram can be decreased when combined with Nelfinavir.
ClarithromycinThe therapeutic efficacy of Clarithromycin can be decreased when used in combination with Nelfinavir.
ClidiniumThe metabolism of Clidinium can be decreased when combined with Nelfinavir.
ClonazepamThe metabolism of Clonazepam can be decreased when combined with Nelfinavir.
ClorazepateThe metabolism of Clorazepate can be decreased when combined with Nelfinavir.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Nelfinavir.
CocaineThe metabolism of Cocaine can be decreased when combined with Nelfinavir.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Nelfinavir.
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Nelfinavir.
CorticotropinThe serum concentration of Corticotropin can be increased when it is combined with Nelfinavir.
Cortisone acetateThe serum concentration of Cortisone acetate can be increased when it is combined with Nelfinavir.
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Nelfinavir.
CyclophosphamideThe risk or severity of adverse effects can be increased when Nelfinavir is combined with Cyclophosphamide.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Nelfinavir.
Cyproterone acetateThe metabolism of Cyproterone acetate can be decreased when combined with Nelfinavir.
DabrafenibThe serum concentration of Nelfinavir can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Daclatasvir can be increased when it is combined with Nelfinavir.
DantroleneThe metabolism of Dantrolene can be decreased when combined with Nelfinavir.
DapoxetineThe serum concentration of Dapoxetine can be increased when it is combined with Nelfinavir.
DapsoneThe metabolism of Dapsone can be decreased when combined with Nelfinavir.
DarifenacinThe metabolism of Darifenacin can be decreased when combined with Nelfinavir.
DarunavirThe metabolism of Darunavir can be decreased when combined with Nelfinavir.
DasatinibThe serum concentration of Dasatinib can be increased when it is combined with Nelfinavir.
DeferasiroxThe serum concentration of Nelfinavir can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Nelfinavir.
DexamethasoneThe metabolism of Dexamethasone can be decreased when combined with Nelfinavir.
DiazepamThe metabolism of Diazepam can be decreased when combined with Nelfinavir.
DienogestThe serum concentration of Dienogest can be increased when it is combined with Nelfinavir.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Nelfinavir.
DihydroergotamineThe metabolism of Dihydroergotamine can be decreased when combined with Nelfinavir.
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Nelfinavir.
DisopyramideThe metabolism of Disopyramide can be decreased when combined with Nelfinavir.
DocetaxelThe metabolism of Docetaxel can be decreased when combined with Nelfinavir.
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Nelfinavir.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Nelfinavir.
DoxazosinThe metabolism of Doxazosin can be decreased when combined with Nelfinavir.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Nelfinavir.
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Nelfinavir.
DronedaroneThe serum concentration of Dronedarone can be increased when it is combined with Nelfinavir.
DrospirenoneThe serum concentration of Drospirenone can be increased when it is combined with Nelfinavir.
DutasterideThe serum concentration of Dutasteride can be increased when it is combined with Nelfinavir.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Nelfinavir.
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Nelfinavir.
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Nelfinavir.
EnzalutamideThe serum concentration of Enzalutamide can be increased when it is combined with Nelfinavir.
EplerenoneThe serum concentration of Eplerenone can be increased when it is combined with Nelfinavir.
Ergoloid mesylateThe metabolism of Ergoloid mesylate can be decreased when combined with Nelfinavir.
ErgonovineThe metabolism of Ergonovine can be decreased when combined with Nelfinavir.
ErgotamineThe metabolism of Ergotamine can be decreased when combined with Nelfinavir.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Nelfinavir.
ErythromycinThe metabolism of Erythromycin can be decreased when combined with Nelfinavir.
EscitalopramThe metabolism of Escitalopram can be decreased when combined with Nelfinavir.
EsomeprazoleThe serum concentration of the active metabolites of Nelfinavir can be reduced when Nelfinavir is used in combination with Esomeprazole resulting in a loss in efficacy.
EstazolamThe serum concentration of Estazolam can be increased when it is combined with Nelfinavir.
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Nelfinavir.
EszopicloneThe metabolism of Eszopiclone can be decreased when combined with Nelfinavir.
EthosuximideThe metabolism of Ethosuximide can be decreased when combined with Nelfinavir.
EtizolamThe serum concentration of Etizolam can be increased when it is combined with Nelfinavir.
EtonogestrelThe serum concentration of Etonogestrel can be decreased when it is combined with Nelfinavir.
EtoposideThe metabolism of Etoposide can be decreased when combined with Nelfinavir.
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Nelfinavir.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Nelfinavir.
FamotidineThe serum concentration of Nelfinavir can be decreased when it is combined with Famotidine.
FelbamateThe metabolism of Felbamate can be decreased when combined with Nelfinavir.
FelodipineThe metabolism of Felodipine can be decreased when combined with Nelfinavir.
FentanylThe serum concentration of Fentanyl can be increased when it is combined with Nelfinavir.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Nelfinavir.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Nelfinavir.
FludrocortisoneThe serum concentration of Fludrocortisone can be increased when it is combined with Nelfinavir.
FlunisolideThe serum concentration of Flunisolide can be increased when it is combined with Nelfinavir.
FlurazepamThe metabolism of Flurazepam can be decreased when combined with Nelfinavir.
FlutamideThe metabolism of Flutamide can be decreased when combined with Nelfinavir.
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Nelfinavir.
Fluticasone PropionateThe serum concentration of Fluticasone Propionate can be increased when it is combined with Nelfinavir.
FosaprepitantThe metabolism of Fosaprepitant can be decreased when combined with Nelfinavir.
FosphenytoinThe serum concentration of Nelfinavir can be decreased when it is combined with Fosphenytoin.
GarlicThe serum concentration of Nelfinavir can be decreased when it is combined with Garlic.
GefitinibThe metabolism of Gefitinib can be decreased when combined with Nelfinavir.
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Nelfinavir.
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Nelfinavir.
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Nelfinavir.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Nelfinavir.
GoserelinNelfinavir may increase the QTc-prolonging activities of Goserelin.
GuanfacineThe serum concentration of Guanfacine can be increased when it is combined with Nelfinavir.
HalofantrineThe serum concentration of Halofantrine can be increased when it is combined with Nelfinavir.
HaloperidolThe metabolism of Haloperidol can be decreased when combined with Nelfinavir.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Nelfinavir.
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Nelfinavir.
Hydroxyprogesterone caproateThe metabolism of Hydroxyprogesterone caproate can be decreased when combined with Nelfinavir.
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Nelfinavir.
IdelalisibThe serum concentration of Idelalisib can be increased when it is combined with Nelfinavir.
IfosfamideThe serum concentration of the active metabolites of Ifosfamide can be reduced when Ifosfamide is used in combination with Nelfinavir resulting in a loss in efficacy.
IloperidoneThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Nelfinavir.
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Nelfinavir.
ImidafenacinThe serum concentration of Imidafenacin can be increased when it is combined with Nelfinavir.
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Nelfinavir.
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Nelfinavir.
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Nelfinavir.
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Nelfinavir.
Insulin HumanThe therapeutic efficacy of Insulin Regular can be decreased when used in combination with Nelfinavir.
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Nelfinavir.
IrinotecanThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Nelfinavir.
IsavuconazoniumThe serum concentration of the active metabolites of Isavuconazonium can be increased when Isavuconazonium is used in combination with Nelfinavir.
IsoflurophateThe serum concentration of Nelfinavir can be increased when it is combined with Isoflurophate.
IsosorbideThe metabolism of Isosorbide can be decreased when combined with Nelfinavir.
Isosorbide DinitrateThe metabolism of Isosorbide Dinitrate can be decreased when combined with Nelfinavir.
Isosorbide MononitrateThe metabolism of Isosorbide Mononitrate can be decreased when combined with Nelfinavir.
IsradipineThe metabolism of Isradipine can be decreased when combined with Nelfinavir.
ItraconazoleThe metabolism of Itraconazole can be decreased when combined with Nelfinavir.
IvabradineThe serum concentration of Ivabradine can be increased when it is combined with Nelfinavir.
IvacaftorThe serum concentration of Ivacaftor can be increased when it is combined with Nelfinavir.
IxabepiloneThe serum concentration of Ixabepilone can be increased when it is combined with Nelfinavir.
KetamineThe metabolism of Ketamine can be decreased when combined with Nelfinavir.
LacosamideThe serum concentration of Lacosamide can be increased when it is combined with Nelfinavir.
LansoprazoleThe serum concentration of the active metabolites of Nelfinavir can be reduced when Nelfinavir is used in combination with Lansoprazole resulting in a loss in efficacy.
LapatinibThe serum concentration of Lapatinib can be increased when it is combined with Nelfinavir.
LercanidipineThe serum concentration of Lercanidipine can be increased when it is combined with Nelfinavir.
LeuprolideNelfinavir may increase the QTc-prolonging activities of Leuprolide.
LevobupivacaineThe serum concentration of Levobupivacaine can be increased when it is combined with Nelfinavir.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Nelfinavir.
LevonorgestrelThe serum concentration of Levonorgestrel can be decreased when it is combined with Nelfinavir.
LidocaineThe metabolism of Lidocaine can be decreased when combined with Nelfinavir.
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Nelfinavir.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Nelfinavir.
LopinavirThe serum concentration of Lopinavir can be decreased when it is combined with Nelfinavir.
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Nelfinavir.
LumefantrineThe serum concentration of Lumefantrine can be increased when it is combined with Nelfinavir.
LurasidoneThe serum concentration of Lurasidone can be increased when it is combined with Nelfinavir.
MacitentanThe serum concentration of MACITENTAN can be increased when it is combined with Nelfinavir.
MaravirocThe serum concentration of Maraviroc can be increased when it is combined with Nelfinavir.
Medroxyprogesterone AcetateThe serum concentration of Medroxyprogesterone Acetate can be decreased when it is combined with Nelfinavir.
MefloquineThe metabolism of Mefloquine can be decreased when combined with Nelfinavir.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Nelfinavir.
MethadoneThe serum concentration of Methadone can be decreased when it is combined with Nelfinavir.
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Nelfinavir.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Nelfinavir.
MifepristoneThe serum concentration of Mifepristone can be increased when it is combined with Nelfinavir.
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Nelfinavir.
MitotaneThe serum concentration of Nelfinavir can be decreased when it is combined with Mitotane.
ModafinilThe metabolism of Modafinil can be decreased when combined with Nelfinavir.
MometasoneThe serum concentration of Mometasone can be increased when it is combined with Nelfinavir.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Nelfinavir.
NateglinideThe metabolism of Nateglinide can be decreased when combined with Nelfinavir.
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Nelfinavir.
NevirapineThe serum concentration of the active metabolites of Nelfinavir can be reduced when Nelfinavir is used in combination with Nevirapine resulting in a loss in efficacy.
NicardipineThe metabolism of Nicardipine can be decreased when combined with Nelfinavir.
NifedipineThe metabolism of Nifedipine can be decreased when combined with Nelfinavir.
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Nelfinavir.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Nelfinavir.
NisoldipineThe serum concentration of Nisoldipine can be increased when it is combined with Nelfinavir.
NizatidineThe serum concentration of Nelfinavir can be decreased when it is combined with Nizatidine.
NorethisteroneThe serum concentration of Norethindrone can be decreased when it is combined with Nelfinavir.
OlaparibThe serum concentration of Olaparib can be increased when it is combined with Nelfinavir.
OmeprazoleThe serum concentration of the active metabolites of Nelfinavir can be reduced when Nelfinavir is used in combination with Omeprazole resulting in a loss in efficacy.
OsimertinibThe serum concentration of Osimertinib can be increased when it is combined with Nelfinavir.
OspemifeneThe serum concentration of Ospemifene can be increased when it is combined with Nelfinavir.
OxybutyninThe serum concentration of Oxybutynin can be increased when it is combined with Nelfinavir.
OxycodoneThe risk or severity of adverse effects can be increased when Nelfinavir is combined with Oxycodone.
PaclitaxelThe metabolism of Paclitaxel can be decreased when combined with Nelfinavir.
PalbociclibThe serum concentration of Palbociclib can be increased when it is combined with Nelfinavir.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Nelfinavir.
PantoprazoleThe serum concentration of the active metabolites of Nelfinavir can be reduced when Nelfinavir is used in combination with Pantoprazole resulting in a loss in efficacy.
ParecoxibThe serum concentration of Parecoxib can be increased when it is combined with Nelfinavir.
ParicalcitolThe serum concentration of Paricalcitol can be increased when it is combined with Nelfinavir.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Nelfinavir.
PethidineThe risk or severity of adverse effects can be increased when Nelfinavir is combined with Pethidine.
PhenytoinThe serum concentration of Phenytoin can be decreased when it is combined with Nelfinavir.
PimecrolimusThe metabolism of Pimecrolimus can be decreased when combined with Nelfinavir.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Nelfinavir.
PipotiazineThe metabolism of Pipotiazine can be decreased when combined with Nelfinavir.
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Nelfinavir.
PranlukastThe serum concentration of Pranlukast can be increased when it is combined with Nelfinavir.
PrasugrelThe serum concentration of the active metabolites of Prasugrel can be reduced when Prasugrel is used in combination with Nelfinavir resulting in a loss in efficacy.
PravastatinThe serum concentration of Pravastatin can be decreased when it is combined with Nelfinavir.
PraziquantelThe metabolism of Praziquantel can be decreased when combined with Nelfinavir.
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Nelfinavir.
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Nelfinavir.
PropafenoneThe serum concentration of Propafenone can be increased when it is combined with Nelfinavir.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Nelfinavir.
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Nelfinavir.
QuinineThe metabolism of Quinine can be decreased when combined with Nelfinavir.
RabeprazoleThe serum concentration of the active metabolites of Nelfinavir can be reduced when Nelfinavir is used in combination with Rabeprazole resulting in a loss in efficacy.
RamelteonThe serum concentration of Ramelteon can be increased when it is combined with Nelfinavir.
RanitidineThe serum concentration of Nelfinavir can be decreased when it is combined with Ranitidine.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Nelfinavir.
RegorafenibThe serum concentration of Regorafenib can be increased when it is combined with Nelfinavir.
RepaglinideThe serum concentration of Repaglinide can be increased when it is combined with Nelfinavir.
Repository corticotropinThe serum concentration of Repository corticotropin can be increased when it is combined with Nelfinavir.
RetapamulinThe serum concentration of Retapamulin can be increased when it is combined with Nelfinavir.
RifabutinThe serum concentration of the active metabolites of Rifabutin can be increased when Rifabutin is used in combination with Nelfinavir.
RifampicinThe serum concentration of Nelfinavir can be decreased when it is combined with Rifampicin.
RilpivirineThe serum concentration of Rilpivirine can be increased when it is combined with Nelfinavir.
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Nelfinavir.
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Nelfinavir.
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Nelfinavir.
RuxolitinibThe serum concentration of Ruxolitinib can be increased when it is combined with Nelfinavir.
SalmeterolThe serum concentration of Salmeterol can be increased when it is combined with Nelfinavir.
SaquinavirThe serum concentration of Nelfinavir can be increased when it is combined with Saquinavir.
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Nelfinavir.
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Nelfinavir.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Nelfinavir.
SiltuximabThe serum concentration of Nelfinavir can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Nelfinavir.
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Nelfinavir.
SirolimusThe serum concentration of Sirolimus can be increased when it is combined with Nelfinavir.
SolifenacinThe metabolism of Solifenacin can be decreased when combined with Nelfinavir.
SonidegibThe serum concentration of Sonidegib can be increased when it is combined with Nelfinavir.
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Nelfinavir.
SpiramycinThe metabolism of Spiramycin can be decreased when combined with Nelfinavir.
St. John's WortThe metabolism of Nelfinavir can be increased when combined with St. John's Wort.
StiripentolThe metabolism of Stiripentol can be decreased when combined with Nelfinavir.
SufentanilThe metabolism of Sufentanil can be decreased when combined with Nelfinavir.
SulfisoxazoleThe metabolism of Sulfisoxazole can be decreased when combined with Nelfinavir.
SunitinibThe metabolism of Sunitinib can be decreased when combined with Nelfinavir.
SuvorexantThe serum concentration of Suvorexant can be increased when it is combined with Nelfinavir.
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Nelfinavir.
TadalafilThe serum concentration of Tadalafil can be increased when it is combined with Nelfinavir.
TamoxifenThe metabolism of Tamoxifen can be decreased when combined with Nelfinavir.
TamsulosinThe serum concentration of Tamsulosin can be increased when it is combined with Nelfinavir.
TasimelteonThe serum concentration of Tasimelteon can be increased when it is combined with Nelfinavir.
TelaprevirThe metabolism of Telaprevir can be decreased when combined with Nelfinavir.
TelithromycinThe metabolism of Telithromycin can be decreased when combined with Nelfinavir.
TemsirolimusThe risk or severity of adverse effects can be increased when Nelfinavir is combined with Temsirolimus.
TeniposideThe metabolism of Teniposide can be decreased when combined with Nelfinavir.
TerfenadineThe serum concentration of Terfenadine can be increased when it is combined with Nelfinavir.
TheophyllineThe metabolism of Theophylline can be decreased when combined with Nelfinavir.
TiagabineThe metabolism of Tiagabine can be decreased when combined with Nelfinavir.
TicagrelorThe serum concentration of the active metabolites of Ticagrelor can be reduced when Ticagrelor is used in combination with Nelfinavir resulting in a loss in efficacy.
TipranavirThe serum concentration of Nelfinavir can be decreased when it is combined with Tipranavir.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Nelfinavir.
TocilizumabThe serum concentration of Nelfinavir can be decreased when it is combined with Tocilizumab.
TofacitinibThe serum concentration of Tofacitinib can be increased when it is combined with Nelfinavir.
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Nelfinavir.
TolterodineThe serum concentration of Tolterodine can be increased when it is combined with Nelfinavir.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Nelfinavir.
ToremifeneThe risk or severity of adverse effects can be increased when Nelfinavir is combined with Toremifene.
TrabectedinThe serum concentration of Trabectedin can be increased when it is combined with Nelfinavir.
TramadolThe serum concentration of Tramadol can be increased when it is combined with Nelfinavir.
TrazodoneThe serum concentration of Trazodone can be increased when it is combined with Nelfinavir.
TriamcinoloneThe serum concentration of Triamcinolone can be increased when it is combined with Nelfinavir.
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Nelfinavir.
TrimipramineThe metabolism of Trimipramine can be decreased when combined with Nelfinavir.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Nelfinavir.
Valproic AcidThe serum concentration of Valproic Acid can be decreased when it is combined with Nelfinavir.
VardenafilThe serum concentration of Vardenafil can be increased when it is combined with Nelfinavir.
VemurafenibThe serum concentration of Vemurafenib can be increased when it is combined with Nelfinavir.
VenlafaxineThe metabolism of Venlafaxine can be decreased when combined with Nelfinavir.
VerapamilThe serum concentration of Nelfinavir can be increased when it is combined with Verapamil.
VilanterolThe serum concentration of Vilanterol can be increased when it is combined with Nelfinavir.
VilazodoneThe serum concentration of Vilazodone can be increased when it is combined with Nelfinavir.
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Nelfinavir.
VinblastineThe metabolism of Vinblastine can be decreased when combined with Nelfinavir.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Nelfinavir.
VindesineThe serum concentration of Vindesine can be increased when it is combined with Nelfinavir.
VinorelbineThe metabolism of Vinorelbine can be decreased when combined with Nelfinavir.
VorapaxarThe serum concentration of Vorapaxar can be increased when it is combined with Nelfinavir.
VoriconazoleThe serum concentration of Nelfinavir can be increased when it is combined with Voriconazole.
WarfarinThe serum concentration of Warfarin can be decreased when it is combined with Nelfinavir.
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Nelfinavir.
ZolpidemThe metabolism of Zolpidem can be decreased when combined with Nelfinavir.
ZonisamideThe metabolism of Zonisamide can be decreased when combined with Nelfinavir.
ZopicloneThe serum concentration of Zopiclone can be increased when it is combined with Nelfinavir.
ZuclopenthixolThe serum concentration of Zuclopenthixol can be increased when it is combined with Nelfinavir.
Food Interactions
  • Food significantly increases absorption (2 to 3 times).
  • Take with food.

Targets

Kind
Protein
Organism
Human immunodeficiency virus
Pharmacological action
yes
Actions
inhibitor
General Function:
Aspartic-type endopeptidase activity
Specific Function:
Not Available
Gene Name:
HIV-1 protease
Uniprot ID:
O90777
Molecular Weight:
10724.61 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Garriga C, Perez-Elias MJ, Delgado R, Ruiz L, Najera R, Pumarola T, Alonso-Socas Mdel M, Garcia-Bujalance S, Menendez-Arias L: Mutational patterns and correlated amino acid substitutions in the HIV-1 protease after virological failure to nelfinavir- and lopinavir/ritonavir-based treatments. J Med Virol. 2007 Nov;79(11):1617-28. [PubMed:17854027 ]
  4. Wittayanarakul K, Hannongbua S, Feig M: Accurate prediction of protonation state as a prerequisite for reliable MM-PB(GB)SA binding free energy calculations of HIV-1 protease inhibitors. J Comput Chem. 2008 Apr 15;29(5):673-85. [PubMed:17849388 ]
  5. Dandache S, Sevigny G, Yelle J, Stranix BR, Parkin N, Schapiro JM, Wainberg MA, Wu JJ: In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. Antimicrob Agents Chemother. 2007 Nov;51(11):4036-43. Epub 2007 Jul 16. [PubMed:17638694 ]
  6. Perez MA, Fernandes PA, Ramos MJ: Drug design: new inhibitors for HIV-1 protease based on Nelfinavir as lead. J Mol Graph Model. 2007 Oct;26(3):634-42. Epub 2007 Mar 24. [PubMed:17459746 ]
  7. Velazquez-Campoy A, Kiso Y, Freire E: The binding energetics of first- and second-generation HIV-1 protease inhibitors: implications for drug design. Arch Biochem Biophys. 2001 Jun 15;390(2):169-75. [PubMed:11396919 ]
  8. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Hesse LM, von Moltke LL, Shader RI, Greenblatt DJ: Ritonavir, efavirenz, and nelfinavir inhibit CYP2B6 activity in vitro: potential drug interactions with bupropion. Drug Metab Dispos. 2001 Feb;29(2):100-2. [PubMed:11159797 ]
  2. Tanabe M, Hashimoto M, Ono H: Imidazoline I(1) receptor-mediated reduction of muscle rigidity in the reserpine-treated murine model of Parkinson's disease. Eur J Pharmacol. 2008 Jul 28;589(1-3):102-5. doi: 10.1016/j.ejphar.2008.06.013. Epub 2008 Jun 7. [PubMed:18602099 ]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Oxygen binding
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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Oxygen binding
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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitorinducer
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Perloff MD, von Moltke LL, Fahey JM, Daily JP, Greenblatt DJ: Induction of P-glycoprotein expression by HIV protease inhibitors in cell culture. AIDS. 2000 Jun 16;14(9):1287-9. [PubMed:10894301 ]
  2. Choo EF, Leake B, Wandel C, Imamura H, Wood AJ, Wilkinson GR, Kim RB: Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes. Drug Metab Dispos. 2000 Jun;28(6):655-60. [PubMed:10820137 ]
  3. Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. [PubMed:12699389 ]
  4. Kim RB, Fromm MF, Wandel C, Leake B, Wood AJ, Roden DM, Wilkinson GR: The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors. J Clin Invest. 1998 Jan 15;101(2):289-94. [PubMed:9435299 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Secondary active organic cation transmembrane transporter activity
Specific Function:
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine...
Gene Name:
SLC22A1
Uniprot ID:
O15245
Molecular Weight:
61153.345 Da
References
  1. Zhang L, Gorset W, Washington CB, Blaschke TF, Kroetz DL, Giacomini KM: Interactions of HIV protease inhibitors with a human organic cation transporter in a mammalian expression system. Drug Metab Dispos. 2000 Mar;28(3):329-34. [PubMed:10681378 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibited by the grapefruit juice component naringin.
Gene Name:
SLCO1A2
Uniprot ID:
P46721
Molecular Weight:
74144.105 Da
References
  1. Cvetkovic M, Leake B, Fromm MF, Wilkinson GR, Kim RB: OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine. Drug Metab Dispos. 1999 Aug;27(8):866-71. [PubMed:10421612 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
References
  1. Gupta A, Zhang Y, Unadkat JD, Mao Q: HIV protease inhibitors are inhibitors but not substrates of the human breast cancer resistance protein (BCRP/ABCG2). J Pharmacol Exp Ther. 2004 Jul;310(1):334-41. Epub 2004 Mar 8. [PubMed:15007102 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Molecular Weight:
76447.99 Da
References
  1. Tirona RG, Leake BF, Wolkoff AW, Kim RB: Human organic anion transporting polypeptide-C (SLC21A6) is a major determinant of rifampin-mediated pregnane X receptor activation. J Pharmacol Exp Ther. 2003 Jan;304(1):223-8. [PubMed:12490595 ]
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Drug created on June 13, 2005 07:24 / Updated on October 08, 2013 14:24