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Identification
NameAstemizole
Accession NumberDB00637  (APRD00585)
TypeSmall Molecule
GroupsApproved, Withdrawn
DescriptionAstemizole is a long-acting, non-sedating second generation antihistamine used in the treatment of allergy symptoms. It was withdrawn from market by the manufacturer in 1999 due to the potential to cause arrhythmias at high doses, especially when when taken with CYP inhibitors or grapefruit juice.
Structure
Thumb
Synonyms
1-(P-Fluorobenzyl)-2-((1-(2-(P-methoxyphenyl)ethyl)piperid-4-yl)amino)benzimidazole
1-(P-Fluorobenzyl)-2-((1-(P-methoxyphenethyl)-4-piperidyl)amino)benzimidazole
Astemison
Astemizol
Astemizol
Astémizole
Astemizolum
External Identifiers
  • BRN 4830190
  • R43512
  • UNII-7HU6337315
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Hismanal - Tab 10mgtablet10 mgoralJohnson & Johnson Merck Consumer Pharmaceuticals Of Canada1997-01-211999-03-04Canada
Hismanal Suspension 2mg/mlsuspension2 mgoralJanssen Pharmaceutica, Division Of Janssen Ortho Inc.1984-12-311997-08-12Canada
Hismanal Tab 10mgtablet10 mgoralJanssen Pharmaceutica, Division Of Janssen Ortho Inc.1984-12-311997-08-12Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AcemizLupin
AlerkinIncobra
AstesenSenosiain
HismanalJanssen
HistalongBiofarma
LergibrumizolBruluart
StemizCadila HC
Brand mixturesNot Available
SaltsNot Available
Categories
UNII7HU6337315
CAS number68844-77-9
WeightAverage: 458.5703
Monoisotopic: 458.248189839
Chemical FormulaC28H31FN4O
InChI KeyInChIKey=GXDALQBWZGODGZ-UHFFFAOYSA-N
InChI
InChI=1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31)
IUPAC Name
1-[(4-fluorophenyl)methyl]-N-{1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl}-1H-1,3-benzodiazol-2-amine
SMILES
COC1=CC=C(CCN2CCC(CC2)NC2=NC3=CC=CC=C3N2CC2=CC=C(F)C=C2)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzimidazoles. These are organic compounds containing a benzene ring fused to an imidazole ring (five member ring containing a nitrogen atom, 4 carbon atoms, and two double bonds).
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzimidazoles
Sub ClassNot Available
Direct ParentBenzimidazoles
Alternative Parents
Substituents
  • Phenethylamine
  • Benzimidazole
  • Methoxybenzene
  • Phenylmethylamine
  • Phenol ether
  • Anisole
  • Aralkylamine
  • Secondary aliphatic/aromatic amine
  • Halobenzene
  • Fluorobenzene
  • 4-aminopiperidine
  • Alkyl aryl ether
  • Benzenoid
  • Piperidine
  • N-substituted imidazole
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Aminoimidazole
  • Heteroaromatic compound
  • Imidazole
  • Azole
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Secondary amine
  • Ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationAstemizole was indicated for use in the relieving allergy symptoms, particularly rhinitis and conjunctivitis. It has been withdrawn from the market however due to concerns of arrhythmias.
PharmacodynamicsAstemizole is a second generation H1-receptor antagonist. It does not significantly cross the blood brain barrier and therefore does not cause drowsiness or CNS depression at normal doses.
Mechanism of actionAstemizole competes with histamine for binding at H1-receptor sites in the GI tract, uterus, large blood vessels, and bronchial muscle. This reversible binding of astemizole to H1-receptors suppresses the formation of edema, flare, and pruritus resulting from histaminic activity. As the drug does not readily cross the blood-brain barrier and preferentially binds at H1 receptors in the peripehery rather than within the brain, CNS depression is minimal. Astemizole may also act on H3-receptors, producing adverse effects.
Related Articles
AbsorptionRapidly absorbed from the gastrointestinal tract.
Volume of distributionNot Available
Protein binding96.7%
Metabolism

Almost completely metabolized in the liver and primarily excreted in the feces.

SubstrateEnzymesProduct
Astemizole
desmethylastemizoleDetails
Route of eliminationNot Available
Half life1 day
ClearanceNot Available
ToxicityLD50=2052mg/kg in mice
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.765
Caco-2 permeable+0.5217
P-glycoprotein substrateSubstrate0.8162
P-glycoprotein inhibitor IInhibitor0.8563
P-glycoprotein inhibitor IIInhibitor0.8995
Renal organic cation transporterInhibitor0.7708
CYP450 2C9 substrateNon-substrate0.8732
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.6777
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorInhibitor0.8994
CYP450 3A4 inhibitorNon-inhibitor0.5127
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9096
Ames testNon AMES toxic0.6444
CarcinogenicityNon-carcinogens0.9553
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.2847 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.9267
hERG inhibition (predictor II)Inhibitor0.8575
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tabletoral10 mg
Suspensionoral2 mg
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point149.1 °CPhysProp
water solubility432 mg/LNot Available
logP5.8Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0012 mg/mLALOGPS
logP5.92ALOGPS
logP5.39ChemAxon
logS-5.6ALOGPS
pKa (Strongest Basic)8.75ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area42.32 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity135.64 m3·mol-1ChemAxon
Polarizability52.08 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis Reference

Godelieve Irma Christine Maria Heylen, Cornelus Gerardus Maria Janssen, Jurzak Mirek, Henricus Petrus Martinus Maria Van Assouw, “Radiolabeled astemizole and method of making.” U.S. Patent US07541476, issued June 02, 2009.

US07541476
General References
  1. Wang X, Hockerman GH, Green HW 3rd, Babbs CF, Mohammad SI, Gerrard D, Latour MA, London B, Hannon KM, Pond AL: Merg1a K+ channel induces skeletal muscle atrophy by activating the ubiquitin proteasome pathway. FASEB J. 2006 Jul;20(9):1531-3. Epub 2006 May 24. [PubMed:16723379 ]
  2. Chong CR, Chen X, Shi L, Liu JO, Sullivan DJ Jr: A clinical drug library screen identifies astemizole as an antimalarial agent. Nat Chem Biol. 2006 Aug;2(8):415-6. Epub 2006 Jul 2. [PubMed:16816845 ]
External Links
ATC CodesR06AX11
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (57.2 KB)
Interactions
Drug Interactions
Drug
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may decrease the sedative activities of Astemizole.
3,4-Methylenedioxymethamphetamine3,4-Methylenedioxymethamphetamine may decrease the sedative activities of Astemizole.
AbirateroneThe metabolism of Astemizole can be decreased when combined with Abiraterone.
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Astemizole.
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Astemizole.
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Astemizole.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Astemizole.
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Astemizole.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Astemizole.
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Astemizole.
AmiodaroneThe serum concentration of Astemizole can be increased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Astemizole.
AmphetamineAmphetamine may decrease the sedative activities of Astemizole.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Astemizole.
AprepitantThe serum concentration of Astemizole can be increased when it is combined with Aprepitant.
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Astemizole.
ArtemetherThe metabolism of Astemizole can be decreased when combined with Artemether.
AtazanavirThe serum concentration of Astemizole can be increased when it is combined with Atazanavir.
AtenololThe serum concentration of Atenolol can be increased when it is combined with Astemizole.
AtomoxetineThe metabolism of Astemizole can be decreased when combined with Atomoxetine.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Astemizole.
BenzphetamineBenzphetamine may decrease the sedative activities of Astemizole.
Benzylpenicilloyl PolylysineAstemizole may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Astemizole.
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Astemizole.
BetaxololThe metabolism of Astemizole can be decreased when combined with Betaxolol.
BexaroteneThe serum concentration of Astemizole can be decreased when it is combined with Bexarotene.
BicalutamideThe serum concentration of Astemizole can be increased when it is combined with Bicalutamide.
BoceprevirThe serum concentration of Astemizole can be increased when it is combined with Boceprevir.
BortezomibThe metabolism of Astemizole can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Astemizole can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Astemizole.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Astemizole.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Astemizole.
BupropionThe metabolism of Astemizole can be decreased when combined with Bupropion.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Astemizole.
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Astemizole.
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Astemizole.
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Astemizole.
CarbamazepineThe metabolism of Astemizole can be increased when combined with Carbamazepine.
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Astemizole.
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Astemizole.
CelecoxibThe metabolism of Astemizole can be decreased when combined with Celecoxib.
CeritinibThe serum concentration of Astemizole can be increased when it is combined with Ceritinib.
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Astemizole.
ChloroquineThe metabolism of Astemizole can be decreased when combined with Chloroquine.
ChlorphentermineChlorphentermine may decrease the sedative activities of Astemizole.
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Astemizole.
ChlorpromazineThe metabolism of Astemizole can be decreased when combined with Chlorpromazine.
CholecalciferolThe metabolism of Astemizole can be decreased when combined with Cholecalciferol.
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Astemizole.
CimetidineThe metabolism of Astemizole can be decreased when combined with Cimetidine.
CinacalcetThe metabolism of Astemizole can be decreased when combined with Cinacalcet.
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Astemizole.
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Astemizole.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Astemizole.
CitalopramThe metabolism of Astemizole can be decreased when combined with Citalopram.
ClarithromycinThe serum concentration of Astemizole can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Astemizole can be decreased when combined with Clemastine.
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Astemizole.
ClobazamThe metabolism of Astemizole can be decreased when combined with Clobazam.
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Astemizole.
ClomipramineThe metabolism of Astemizole can be decreased when combined with Clomipramine.
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Astemizole.
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Astemizole.
ClotrimazoleThe metabolism of Astemizole can be decreased when combined with Clotrimazole.
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Astemizole.
ClozapineThe metabolism of Astemizole can be decreased when combined with Clozapine.
CobicistatThe serum concentration of Astemizole can be increased when it is combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Astemizole.
CocaineThe metabolism of Astemizole can be decreased when combined with Cocaine.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Astemizole.
ConivaptanThe serum concentration of Astemizole can be increased when it is combined with Conivaptan.
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Astemizole.
CrizotinibThe metabolism of Astemizole can be decreased when combined with Crizotinib.
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Astemizole.
CyclosporineThe metabolism of Astemizole can be decreased when combined with Cyclosporine.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Astemizole.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be increased when it is combined with Astemizole.
DabrafenibThe serum concentration of Astemizole can be decreased when it is combined with Dabrafenib.
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Astemizole.
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Astemizole.
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Astemizole.
DarifenacinThe metabolism of Astemizole can be decreased when combined with Darifenacin.
DarunavirThe serum concentration of Astemizole can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Astemizole can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Astemizole.
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Astemizole.
DeferasiroxThe serum concentration of Astemizole can be decreased when it is combined with Deferasirox.
DelavirdineDelavirdine may increase the arrhythmogenic activities of Astemizole.
DesipramineThe metabolism of Astemizole can be decreased when combined with Desipramine.
DexamethasoneThe serum concentration of Astemizole can be decreased when it is combined with Dexamethasone.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Astemizole.
DextroamphetamineDextroamphetamine may decrease the sedative activities of Astemizole.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Astemizole.
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Astemizole.
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Astemizole.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Astemizole.
DihydroergotamineThe metabolism of Astemizole can be decreased when combined with Dihydroergotamine.
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Astemizole.
DiltiazemThe metabolism of Astemizole can be decreased when combined with Diltiazem.
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Astemizole.
DiphenhydramineThe metabolism of Astemizole can be decreased when combined with Diphenhydramine.
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Astemizole.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Astemizole.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Astemizole.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Astemizole.
DoxycyclineThe metabolism of Astemizole can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Astemizole can be decreased when combined with Dronedarone.
DuloxetineThe metabolism of Astemizole can be decreased when combined with Duloxetine.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Astemizole.
EfavirenzThe serum concentration of Astemizole can be decreased when it is combined with Efavirenz.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Astemizole.
EliglustatThe metabolism of Astemizole can be decreased when combined with Eliglustat.
EnzalutamideThe serum concentration of Astemizole can be decreased when it is combined with Enzalutamide.
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Astemizole.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Astemizole.
ErythromycinThe metabolism of Astemizole can be decreased when combined with Erythromycin.
ErythromycinThe serum concentration of Erythromycin can be increased when it is combined with Astemizole.
Eslicarbazepine acetateThe serum concentration of Astemizole can be decreased when it is combined with Eslicarbazepine acetate.
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Astemizole.
EstriolThe serum concentration of Estriol can be increased when it is combined with Astemizole.
EstroneThe serum concentration of Estrone can be increased when it is combined with Astemizole.
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Astemizole.
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Astemizole.
EtravirineThe serum concentration of Astemizole can be decreased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Astemizole.
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Astemizole.
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Astemizole.
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Astemizole.
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Astemizole.
FluconazoleThe metabolism of Astemizole can be decreased when combined with Fluconazole.
FluoxetineThe metabolism of Astemizole can be decreased when combined with Fluoxetine.
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Astemizole.
FluvoxamineThe metabolism of Astemizole can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Astemizole can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Astemizole can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Astemizole can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Astemizole can be increased when it is combined with Fusidic Acid.
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Astemizole.
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Astemizole.
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Astemizole.
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Astemizole.
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Astemizole.
HaloperidolThe metabolism of Astemizole can be decreased when combined with Haloperidol.
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Astemizole.
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Astemizole.
Hydroxyamphetamine hydrobromideHydroxyamphetamine hydrobromide may decrease the sedative activities of Astemizole.
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Astemizole.
IdelalisibThe serum concentration of Astemizole can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Astemizole can be decreased when combined with Imatinib.
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Astemizole.
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Astemizole.
ImipramineThe metabolism of Astemizole can be decreased when combined with Imipramine.
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Astemizole.
IndinavirThe serum concentration of Astemizole can be increased when it is combined with Indinavir.
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Astemizole.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Astemizole.
IsavuconazoniumThe metabolism of Astemizole can be decreased when combined with Isavuconazonium.
IsoniazidThe metabolism of Astemizole can be decreased when combined with Isoniazid.
IsradipineThe metabolism of Astemizole can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Astemizole can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Astemizole can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Astemizole.
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Astemizole.
KetoconazoleKetoconazole may increase the QTc-prolonging activities of Astemizole.
KetoconazoleThe serum concentration of Ketoconazole can be increased when it is combined with Astemizole.
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Astemizole.
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Astemizole.
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Astemizole.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Astemizole.
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Astemizole.
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Astemizole.
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Astemizole.
LevofloxacinThe serum concentration of Levofloxacin can be increased when it is combined with Astemizole.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Astemizole.
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Astemizole.
LisdexamfetamineLisdexamfetamine may decrease the sedative activities of Astemizole.
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Astemizole.
LopinavirThe serum concentration of Astemizole can be increased when it is combined with Lopinavir.
LorcaserinThe metabolism of Astemizole can be decreased when combined with Lorcaserin.
LosartanThe serum concentration of Losartan can be increased when it is combined with Astemizole.
LovastatinThe metabolism of Astemizole can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Astemizole can be increased when it is combined with Luliconazole.
LumefantrineThe metabolism of Astemizole can be decreased when combined with Lumefantrine.
MannitolThe serum concentration of Mannitol can be increased when it is combined with Astemizole.
MephentermineMephentermine may decrease the sedative activities of Astemizole.
MethadoneThe metabolism of Astemizole can be decreased when combined with Methadone.
MethamphetamineMethamphetamine may decrease the sedative activities of Astemizole.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Astemizole.
MethotrimeprazineThe metabolism of Astemizole can be decreased when combined with Methotrimeprazine.
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Astemizole.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Astemizole.
MetoprololThe metabolism of Astemizole can be decreased when combined with Metoprolol.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Astemizole.
MifepristoneThe metabolism of Astemizole can be decreased when combined with Mifepristone.
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Astemizole.
MirabegronThe metabolism of Astemizole can be decreased when combined with Mirabegron.
MitotaneThe serum concentration of Astemizole can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Astemizole.
ModafinilThe serum concentration of Astemizole can be decreased when it is combined with Modafinil.
MorphineThe serum concentration of Morphine can be increased when it is combined with Astemizole.
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Astemizole.
NadololThe serum concentration of Nadolol can be increased when it is combined with Astemizole.
NafcillinThe serum concentration of Astemizole can be decreased when it is combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Astemizole.
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Astemizole.
NefazodoneThe serum concentration of Astemizole can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Astemizole can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Astemizole can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Astemizole can be decreased when combined with Nevirapine.
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Astemizole.
NicardipineThe metabolism of Astemizole can be decreased when combined with Nicardipine.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Astemizole.
NilotinibThe metabolism of Astemizole can be decreased when combined with Nilotinib.
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Astemizole.
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Astemizole.
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Astemizole.
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Astemizole.
OlaparibThe metabolism of Astemizole can be decreased when combined with Olaparib.
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Astemizole.
OsimertinibThe serum concentration of Astemizole can be increased when it is combined with Osimertinib.
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Astemizole.
PalbociclibThe serum concentration of Astemizole can be increased when it is combined with Palbociclib.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Astemizole.
PanobinostatThe metabolism of Astemizole can be decreased when combined with Panobinostat.
ParoxetineThe metabolism of Astemizole can be decreased when combined with Paroxetine.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Astemizole.
Peginterferon alfa-2bThe serum concentration of Astemizole can be decreased when it is combined with Peginterferon alfa-2b.
PentobarbitalThe metabolism of Astemizole can be increased when combined with Pentobarbital.
PhenobarbitalThe metabolism of Astemizole can be increased when combined with Phenobarbital.
PhenobarbitalThe serum concentration of Phenobarbital can be increased when it is combined with Astemizole.
PhenterminePhentermine may decrease the sedative activities of Astemizole.
PhenytoinThe metabolism of Astemizole can be increased when combined with Phenytoin.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Astemizole.
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Astemizole.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Astemizole.
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Astemizole.
PosaconazoleThe serum concentration of Astemizole can be increased when it is combined with Posaconazole.
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Astemizole.
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Astemizole.
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Astemizole.
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Astemizole.
PrimidoneThe metabolism of Astemizole can be increased when combined with Primidone.
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Astemizole.
PromazineThe metabolism of Astemizole can be decreased when combined with Promazine.
PropranololThe serum concentration of Propranolol can be increased when it is combined with Astemizole.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Astemizole.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Astemizole.
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Astemizole.
QuinidineThe metabolism of Astemizole can be decreased when combined with Quinidine.
QuinineThe serum concentration of Quinine can be increased when it is combined with Astemizole.
QuinineThe metabolism of Astemizole can be decreased when combined with Quinine.
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Astemizole.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Astemizole.
RanolazineThe metabolism of Astemizole can be decreased when combined with Ranolazine.
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Astemizole.
RifabutinThe metabolism of Astemizole can be increased when combined with Rifabutin.
RifampicinThe metabolism of Astemizole can be increased when combined with Rifampicin.
RifampicinThe serum concentration of Rifampicin can be increased when it is combined with Astemizole.
RifapentineThe metabolism of Astemizole can be increased when combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Astemizole.
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Astemizole.
RitonavirThe serum concentration of Astemizole can be increased when it is combined with Ritonavir.
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Astemizole.
RolapitantThe metabolism of Astemizole can be decreased when combined with Rolapitant.
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Astemizole.
RopiniroleThe metabolism of Astemizole can be decreased when combined with Ropinirole.
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Astemizole.
SaquinavirThe serum concentration of Astemizole can be increased when it is combined with Saquinavir.
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Astemizole.
SertralineThe metabolism of Astemizole can be decreased when combined with Sertraline.
SildenafilThe metabolism of Astemizole can be decreased when combined with Sildenafil.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Astemizole.
SiltuximabThe serum concentration of Astemizole can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Astemizole can be increased when it is combined with Simeprevir.
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Astemizole.
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Astemizole.
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Astemizole.
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Astemizole.
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Astemizole.
St. John's WortThe serum concentration of Astemizole can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Astemizole can be increased when it is combined with Stiripentol.
SulfisoxazoleThe metabolism of Astemizole can be decreased when combined with Sulfisoxazole.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Astemizole.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Astemizole.
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Astemizole.
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Astemizole.
TelaprevirThe serum concentration of Astemizole can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Astemizole can be increased when it is combined with Telithromycin.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Astemizole.
TerbinafineThe metabolism of Astemizole can be decreased when combined with Terbinafine.
ThioridazineThe metabolism of Astemizole can be decreased when combined with Thioridazine.
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Astemizole.
TiclopidineThe metabolism of Astemizole can be decreased when combined with Ticlopidine.
TimololThe serum concentration of Timolol can be increased when it is combined with Astemizole.
TipranavirThe metabolism of Astemizole can be decreased when combined with Tipranavir.
TocilizumabThe serum concentration of Astemizole can be decreased when it is combined with Tocilizumab.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Astemizole.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Astemizole.
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Astemizole.
TranylcypromineThe metabolism of Astemizole can be decreased when combined with Tranylcypromine.
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Astemizole.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Astemizole.
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Astemizole.
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Astemizole.
VenlafaxineThe metabolism of Astemizole can be decreased when combined with Venlafaxine.
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Astemizole.
VerapamilThe metabolism of Astemizole can be decreased when combined with Verapamil.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Astemizole.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Astemizole.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Astemizole.
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Astemizole.
VoriconazoleThe serum concentration of Astemizole can be increased when it is combined with Voriconazole.
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Astemizole.
ZiprasidoneThe metabolism of Astemizole can be decreased when combined with Ziprasidone.
Food Interactions
  • Take on an empty stomach, food decreases absorption by 60%.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Histamine receptor activity
Specific Function:
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
Molecular Weight:
55783.61 Da
References
  1. Salata JJ, Jurkiewicz NK, Wallace AA, Stupienski RF 3rd, Guinosso PJ Jr, Lynch JJ Jr: Cardiac electrophysiological actions of the histamine H1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine. Circ Res. 1995 Jan;76(1):110-9. [PubMed:8001268 ]
  2. Howarth PH, Emanuel MB, Holgate ST: Astemizole, a potent histamine H1-receptor antagonist: effect in allergic rhinoconjunctivitis, on antigen and histamine induced skin weal responses and relationship to serum levels. Br J Clin Pharmacol. 1984 Jul;18(1):1-8. [PubMed:6146346 ]
  3. Kaliner MA, Check WA: Non-sedating antihistamines. Allergy Proc. 1988 Nov-Dec;9(6):649-63. [PubMed:3147222 ]
  4. Cavero I, Mestre M, Guillon JM, Heuillet E, Roach AG: Preclinical in vitro cardiac electrophysiology: a method of predicting arrhythmogenic potential of antihistamines in humans? Drug Saf. 1999;21 Suppl 1:19-31; discussion 81-7. [PubMed:10597865 ]
  5. Llenas J, Cardelus I, Heredia A, de Mora F, Gristwood RW: Cardiotoxicity of histamine and the possible role of histamine in the arrhythmogenesis produced by certain antihistamines. Drug Saf. 1999;21 Suppl 1:33-8; discussion 81-7. [PubMed:10597866 ]
  6. Richards DM, Brogden RN, Heel RC, Speight TM, Avery GS: Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1984 Jul;28(1):38-61. [PubMed:6204835 ]
  7. Krstenansky PM, Cluxton RJ Jr: Astemizole: a long-acting, nonsedating antihistamine. Drug Intell Clin Pharm. 1987 Dec;21(12):947-53. [PubMed:2892659 ]
  8. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization
Specific Function:
Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the delayed rectifying potassium current in heart (IKr). Isoforms USO have no channel activity by themself, but modulates channel characteristics by forming heterotetramers with other isoforms which are r...
Gene Name:
KCNH2
Uniprot ID:
Q12809
Molecular Weight:
126653.52 Da
References
  1. Zhou Z, Vorperian VR, Gong Q, Zhang S, January CT: Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole. J Cardiovasc Electrophysiol. 1999 Jun;10(6):836-43. [PubMed:10376921 ]
  2. Chachin M, Katayama Y, Yamada M, Horio Y, Ohmura T, Kitagawa H, Uchida S, Kurachi Y: Epinastine, a nonsedating histamine H1 receptor antagonist, has a negligible effect on HERG channel. Eur J Pharmacol. 1999 Jun 25;374(3):457-60. [PubMed:10422790 ]
  3. Taglialatela M, Castaldo P, Pannaccione A, Giorgio G, Genovese A, Marone G, Annunziato L: Cardiac ion channels and antihistamines: possible mechanisms of cardiotoxicity. Clin Exp Allergy. 1999 Jul;29 Suppl 3:182-9. [PubMed:10444235 ]
  4. Grzelewska-Rzymowska I, Pietrzkowicz M, Gorska M: [The effect of second generation histamine antagonists on the heart]. Pneumonol Alergol Pol. 2001;69(3-4):217-26. [PubMed:11575008 ]
  5. Chiu PJ, Marcoe KF, Bounds SE, Lin CH, Feng JJ, Lin A, Cheng FC, Crumb WJ, Mitchell R: Validation of a [3H]astemizole binding assay in HEK293 cells expressing HERG K+ channels. J Pharmacol Sci. 2004 Jul;95(3):311-9. [PubMed:15272206 ]

Enzymes

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. Nicolas JM, Whomsley R, Collart P, Roba J: In vitro inhibition of human liver drug metabolizing enzymes by second generation antihistamines. Chem Biol Interact. 1999 Nov 15;123(1):63-79. [PubMed:10597902 ]
  2. Matsumoto S, Yamazoe Y: Involvement of multiple human cytochromes P450 in the liver microsomal metabolism of astemizole and a comparison with terfenadine. Br J Clin Pharmacol. 2001 Feb;51(2):133-42. [PubMed:11259984 ]
  3. Cvetkovic RS, Goa KL: Lopinavir/ritonavir: a review of its use in the management of HIV infection. Drugs. 2003;63(8):769-802. [PubMed:12662125 ]
  4. Goto A, Adachi Y, Inaba A, Nakajima H, Kobayashi H, Sakai K: Identification of human p450 isoforms involved in the metabolism of the antiallergic drug, oxatomide, and its inhibitory effect on enzyme activity. Biol Pharm Bull. 2004 May;27(5):684-90. [PubMed:15133245 ]
  5. Goto A, Ueda K, Inaba A, Nakajima H, Kobayashi H, Sakai K: Identification of human P450 isoforms involved in the metabolism of the antiallergic drug, oxatomide, and its kinetic parameters and inhibition constants. Biol Pharm Bull. 2005 Feb;28(2):328-34. [PubMed:15684493 ]
  6. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
  7. 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 ]
  8. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
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
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
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
This enzyme metabolizes arachidonic acid predominantly via a NADPH-dependent olefin epoxidation to all four regioisomeric cis-epoxyeicosatrienoic acids. One of the predominant enzymes responsible for the epoxidation of endogenous cardiac arachidonic acid pools.
Gene Name:
CYP2J2
Uniprot ID:
P51589
Molecular Weight:
57610.165 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
inhibitor
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. 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 ]
  2. Ishikawa M, Fujita R, Takayanagi M, Takayanagi Y, Sasaki K: Reversal of acquired resistance to doxorubicin in K562 human leukemia cells by astemizole. Biol Pharm Bull. 2000 Jan;23(1):112-5. [PubMed:10706423 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23