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Identification
NameTroleandomycin
Accession NumberDB01361
TypeSmall Molecule
GroupsApproved
DescriptionA macrolide antibiotic that is similar to erythromycin.
Structure
Thumb
Synonyms
TAO
Triacetyloleandomycin
Troleandomycin
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
TaoNot Available
TriocetinNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIC4DZ64560D
CAS number2751-09-9
WeightAverage: 813.9684
Monoisotopic: 813.451070479
Chemical FormulaC41H67NO15
InChI KeyLQCLVBQBTUVCEQ-QTFUVMRISA-N
InChI
InChI=1S/C41H67NO15/c1-19-17-41(18-49-41)38(46)23(5)34(53-27(9)43)21(3)25(7)52-39(47)24(6)35(56-32-16-31(48-14)36(26(8)51-32)54-28(10)44)22(4)33(19)57-40-37(55-29(11)45)30(42(12)13)15-20(2)50-40/h19-26,30-37,40H,15-18H2,1-14H3/t19-,20+,21-,22+,23+,24+,25+,26-,30-,31-,32-,33-,34-,35-,36-,37+,40-,41+/m0/s1
IUPAC Name
(3R,5R,6S,7S,8R,11R,12S,13R,14S,15S)-14-{[(2S,3R,4S,6R)-3-(acetyloxy)-4-(dimethylamino)-6-methyloxan-2-yl]oxy}-12-{[(2R,4S,5S,6S)-5-(acetyloxy)-4-methoxy-6-methyloxan-2-yl]oxy}-5,7,8,11,13,15-hexamethyl-4,10-dioxo-1,9-dioxaspiro[2.13]hexadecan-6-yl acetate
SMILES
CO[[email protected]]1C[[email protected]](O[[email protected]]2[[email protected]](C)[C@@H](O[C@@H]3O[[email protected]](C)C[C@@H]([[email protected]]3OC(C)=O)N(C)C)[C@@H](C)C[C@@]3(CO3)C(=O)[[email protected]](C)[C@@H](OC(C)=O)[C@@H](C)[C@@H](C)OC(=O)[C@@H]2C)O[C@@H](C)[C@@H]1OC(C)=O
Pharmacology
IndicationFor the treatment of Pneumococcal pneumonia due to susceptible strains and group A beta-hemolytic streptococcal infections of the upper respiratory tract.
Structured Indications Not Available
PharmacodynamicsTroleandomycin is a macrolide antibiotic that is similar to erythromycin. It is active in vitro against the following gram-positive organisms: Streptococcus pyogenes and Diplococcus pneumoniae.
Mechanism of actionTroleandomycin acts by penetrating the bacterial cell membrane and reversibly binding to the 50 S subunit of bacterial ribosomes or near the "P" or donor site so that binding of tRNA (transfer RNA) to the donor site is blocked. Translocation of peptides from the "A" or acceptor site to the "P" or donor site is prevented, and subsequent protein synthesis is inhibited.
TargetKindPharmacological actionActionsOrganismUniProt ID
50S ribosomal protein L32Proteinyes
inhibitor
Deinococcus radiodurans (strain ATCC 13939 / DSM 20539 / JCM 16871 / LMG 4051 / NBRC 15346 / NCIMB 9279 / R1 / VKM B-1422)P49228 details
50S ribosomal protein L4Proteinyes
inhibitor
Escherichia coli (strain K12)P60723 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicitySymptoms of overdose include diarrhea, nausea, stomach cramps, and vomiting.
Affected organisms
  • Enteric bacteria and other eubacteria
Pathways
PathwayCategorySMPDB ID
Troleandomycin Action PathwayDrug actionSMP00730
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Troleandomycin.Approved
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Troleandomycin.Approved
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Troleandomycin.Approved
AcetyldigitoxinThe serum concentration of Acetyldigitoxin can be increased when it is combined with Troleandomycin.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Troleandomycin.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Troleandomycin.Approved
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Troleandomycin.Experimental
AlfentanilThe serum concentration of Alfentanil can be increased when it is combined with Troleandomycin.Approved, Illicit
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Troleandomycin.Approved, Investigational
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Troleandomycin.Approved, Illicit, Investigational
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Troleandomycin.Approved, Investigational
Ambroxol acefyllinateThe metabolism of Ambroxol acefyllinate can be decreased when combined with Troleandomycin.Experimental
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Troleandomycin.Approved
AmiodaroneThe metabolism of Troleandomycin can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Troleandomycin.Approved
AmlodipineThe metabolism of Amlodipine can be decreased when combined with Troleandomycin.Approved
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Troleandomycin.Approved
AmrinoneThe metabolism of Amrinone can be decreased when combined with Troleandomycin.Approved
AnvirzelThe serum concentration of Anvirzel can be increased when it is combined with Troleandomycin.Investigational
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Troleandomycin.Approved
AprepitantThe serum concentration of Troleandomycin can be increased when it is combined with Aprepitant.Approved, Investigational
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Troleandomycin.Approved, Investigational
ArtesunateThe serum concentration of the active metabolites of Artesunate can be reduced when Artesunate is used in combination with Troleandomycin resulting in a loss in efficacy.Approved
AtazanavirThe metabolism of Troleandomycin can be decreased when combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Atenolol can be increased when it is combined with Troleandomycin.Approved
AtomoxetineThe metabolism of Troleandomycin can be decreased when combined with Atomoxetine.Approved
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Troleandomycin.Approved, Investigational
AzelnidipineThe metabolism of Azelnidipine can be decreased when combined with Troleandomycin.Approved
AzimilideThe metabolism of Azimilide can be decreased when combined with Troleandomycin.Investigational
BarnidipineThe metabolism of Barnidipine can be decreased when combined with Troleandomycin.Approved
BcgThe therapeutic efficacy of Bcg can be decreased when used in combination with Troleandomycin.Investigational
BenidipineThe metabolism of Benidipine can be decreased when combined with Troleandomycin.Approved
BepridilThe metabolism of Bepridil can be decreased when combined with Troleandomycin.Approved, Withdrawn
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Troleandomycin.Approved, Vet Approved
BexaroteneThe serum concentration of Troleandomycin can be decreased when it is combined with Bexarotene.Approved, Investigational
BoceprevirThe metabolism of Troleandomycin can be decreased when combined with Boceprevir.Approved
BortezomibThe metabolism of Troleandomycin can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Troleandomycin can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Troleandomycin.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Troleandomycin.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Troleandomycin.Approved, Investigational
BuspironeThe metabolism of Buspirone can be decreased when combined with Troleandomycin.Approved, Investigational
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Troleandomycin.Approved
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Troleandomycin.Approved
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Troleandomycin.Approved
CaiThe metabolism of Cai can be decreased when combined with Troleandomycin.Investigational
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Troleandomycin.Experimental
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Troleandomycin.Approved
CarbamazepineThe metabolism of Carbamazepine can be decreased when combined with Troleandomycin.Approved, Investigational
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Troleandomycin.Approved
CeritinibThe serum concentration of Troleandomycin can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Troleandomycin.Withdrawn
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Troleandomycin.Approved, Vet Approved
CilnidipineThe metabolism of Cilnidipine can be decreased when combined with Troleandomycin.Approved
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Troleandomycin.Approved
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Troleandomycin.Approved
CinnarizineThe metabolism of Cinnarizine can be decreased when combined with Troleandomycin.Approved
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Troleandomycin.Approved, Investigational
CisaprideThe metabolism of Cisapride can be decreased when combined with Troleandomycin.Approved, Investigational, Withdrawn
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Troleandomycin.Approved
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Troleandomycin.Approved
ClarithromycinThe metabolism of Troleandomycin can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Troleandomycin can be decreased when combined with Clemastine.Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Troleandomycin.Approved, Illicit
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Troleandomycin.Approved, Investigational
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Troleandomycin.Approved
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Troleandomycin.Approved, Nutraceutical
ClotrimazoleThe metabolism of Troleandomycin can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Troleandomycin.Approved
CobicistatThe metabolism of Troleandomycin can be decreased when combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Troleandomycin.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Troleandomycin.Approved
ConivaptanThe serum concentration of Troleandomycin can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Troleandomycin.Approved
CrizotinibThe metabolism of Troleandomycin can be decreased when combined with Crizotinib.Approved
CyclosporineThe metabolism of Cyclosporine can be decreased when combined with Troleandomycin.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Troleandomycin.Approved
DabrafenibThe serum concentration of Troleandomycin can be decreased when it is combined with Dabrafenib.Approved
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Troleandomycin.Approved
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Troleandomycin.Approved
DarodipineThe metabolism of Darodipine can be decreased when combined with Troleandomycin.Experimental
DarunavirThe metabolism of Troleandomycin can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Troleandomycin can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Troleandomycin.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Troleandomycin.Approved
DeferasiroxThe serum concentration of Troleandomycin can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Troleandomycin can be decreased when combined with Delavirdine.Approved
DeslanosideThe serum concentration of Deslanoside can be increased when it is combined with Troleandomycin.Approved
DexamethasoneThe serum concentration of Troleandomycin can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Troleandomycin.Approved, Illicit, Vet Approved
DicoumarolThe serum concentration of Dicoumarol can be increased when it is combined with Troleandomycin.Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Troleandomycin.Approved
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Troleandomycin.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Troleandomycin.Approved
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Troleandomycin.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Troleandomycin.Illicit
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Troleandomycin.Approved
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Troleandomycin.Approved
DisopyramideTroleandomycin may increase the QTc-prolonging activities of Disopyramide.Approved
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Troleandomycin.Approved, Investigational
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Troleandomycin.Approved, Investigational, Vet Approved
DotarizineThe metabolism of Dotarizine can be decreased when combined with Troleandomycin.Investigational
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Troleandomycin.Approved, Investigational
DoxycyclineThe metabolism of Troleandomycin can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Troleandomycin can be decreased when combined with Dronedarone.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Troleandomycin.Approved
EfavirenzThe serum concentration of Troleandomycin can be decreased when it is combined with Efavirenz.Approved, Investigational
EfonidipineThe metabolism of Efonidipine can be decreased when combined with Troleandomycin.Approved
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Troleandomycin.Approved, Investigational
EnzalutamideThe serum concentration of Troleandomycin can be decreased when it is combined with Enzalutamide.Approved
EperisoneThe metabolism of Eperisone can be decreased when combined with Troleandomycin.Approved, Investigational
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Troleandomycin.Approved, Investigational
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Troleandomycin.Approved
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Troleandomycin.Approved
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Troleandomycin.Approved
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Troleandomycin.Approved, Investigational
ErythromycinThe metabolism of Troleandomycin can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Troleandomycin can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstazolamThe serum concentration of Estazolam can be increased when it is combined with Troleandomycin.Approved, Illicit
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Troleandomycin.Approved, Investigational, Vet Approved
EstriolThe serum concentration of Estriol can be increased when it is combined with Troleandomycin.Approved, Vet Approved
EstroneThe serum concentration of Estrone can be increased when it is combined with Troleandomycin.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Troleandomycin.Approved
Ethyl biscoumacetateThe serum concentration of Ethyl biscoumacetate can be increased when it is combined with Troleandomycin.Withdrawn
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Troleandomycin.Approved
EtravirineThe serum concentration of Troleandomycin can be decreased when it is combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Troleandomycin.Approved
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Troleandomycin.Approved
FelodipineThe metabolism of Felodipine can be decreased when combined with Troleandomycin.Approved, Investigational
FendilineThe metabolism of Fendiline can be decreased when combined with Troleandomycin.Withdrawn
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Troleandomycin.Approved
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Troleandomycin.Approved
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Troleandomycin.Approved
FluconazoleThe metabolism of Troleandomycin can be decreased when combined with Fluconazole.Approved
FluindioneThe serum concentration of Fluindione can be increased when it is combined with Troleandomycin.Investigational
FlunarizineThe metabolism of Flunarizine can be decreased when combined with Troleandomycin.Approved
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Troleandomycin.Approved
FluvoxamineThe metabolism of Troleandomycin can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Troleandomycin can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Troleandomycin can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Troleandomycin can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Troleandomycin can be increased when it is combined with Fusidic Acid.Approved
GabapentinThe metabolism of Gabapentin can be decreased when combined with Troleandomycin.Approved, Investigational
GallopamilThe metabolism of Gallopamil can be decreased when combined with Troleandomycin.Investigational
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Troleandomycin.Approved, Investigational
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Troleandomycin.Approved
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Troleandomycin.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Troleandomycin.Withdrawn
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Troleandomycin.Approved
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Troleandomycin.Approved, Vet Approved
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Troleandomycin.Approved
IdelalisibThe serum concentration of Troleandomycin can be increased when it is combined with Idelalisib.Approved
ImatinibThe metabolism of Troleandomycin can be decreased when combined with Imatinib.Approved
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Troleandomycin.Approved
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Troleandomycin.Approved
IndinavirThe metabolism of Troleandomycin can be decreased when combined with Indinavir.Approved
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Troleandomycin.Approved, Investigational
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Troleandomycin.Approved, Investigational
IsavuconazoniumThe metabolism of Troleandomycin can be decreased when combined with Isavuconazonium.Approved, Investigational
IsradipineThe metabolism of Isradipine can be decreased when combined with Troleandomycin.Approved
ItraconazoleThe metabolism of Troleandomycin can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Troleandomycin can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Troleandomycin.Approved, Vet Approved
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Troleandomycin.Approved
KetoconazoleThe metabolism of Troleandomycin can be decreased when combined with Ketoconazole.Approved, Investigational
LacidipineThe metabolism of Lacidipine can be decreased when combined with Troleandomycin.Approved
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Troleandomycin.Approved, Investigational
LamotrigineThe metabolism of Lamotrigine can be decreased when combined with Troleandomycin.Approved, Investigational
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Troleandomycin.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Troleandomycin.Approved
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Troleandomycin.Approved
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Troleandomycin.Approved
LercanidipineThe metabolism of Lercanidipine can be decreased when combined with Troleandomycin.Approved, Investigational
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Troleandomycin.Approved, Investigational
LevofloxacinThe serum concentration of Levofloxacin can be increased when it is combined with Troleandomycin.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Troleandomycin.Approved
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Troleandomycin.Approved
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Troleandomycin.Approved
LopinavirThe metabolism of Troleandomycin can be decreased when combined with Lopinavir.Approved
LosartanThe serum concentration of Losartan can be increased when it is combined with Troleandomycin.Approved
LovastatinThe metabolism of Troleandomycin can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Troleandomycin can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Troleandomycin can be increased when combined with Lumacaftor.Approved
Magnesium SulfateThe metabolism of Magnesium Sulfate can be decreased when combined with Troleandomycin.Approved, Vet Approved
ManidipineThe metabolism of Manidipine can be decreased when combined with Troleandomycin.Approved
MannitolThe serum concentration of Mannitol can be increased when it is combined with Troleandomycin.Approved, Investigational
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Troleandomycin.Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Troleandomycin.Approved, Vet Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Troleandomycin.Approved, Investigational
MibefradilThe metabolism of Mibefradil can be decreased when combined with Troleandomycin.Withdrawn
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Troleandomycin.Approved, Illicit
MifepristoneThe serum concentration of Troleandomycin can be increased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Troleandomycin.Approved
MitotaneThe serum concentration of Troleandomycin can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Troleandomycin.Approved, Investigational
ModafinilThe serum concentration of Troleandomycin can be decreased when it is combined with Modafinil.Approved, Investigational
MorphineThe serum concentration of Morphine can be increased when it is combined with Troleandomycin.Approved, Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Troleandomycin.Approved, Investigational
NadololThe serum concentration of Nadolol can be increased when it is combined with Troleandomycin.Approved
NafcillinThe serum concentration of Troleandomycin can be decreased when it is combined with Nafcillin.Approved
NaftopidilThe metabolism of Naftopidil can be decreased when combined with Troleandomycin.Investigational
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Troleandomycin.Approved
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Troleandomycin.Approved, Vet Approved
NefazodoneThe metabolism of Troleandomycin can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Troleandomycin can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Troleandomycin can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Troleandomycin can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Nicardipine can be decreased when combined with Troleandomycin.Approved
NifedipineThe metabolism of Nifedipine can be decreased when combined with Troleandomycin.Approved
NiguldipineThe metabolism of Niguldipine can be decreased when combined with Troleandomycin.Experimental
NilotinibThe metabolism of Troleandomycin can be decreased when combined with Nilotinib.Approved, Investigational
NiludipineThe metabolism of Niludipine can be decreased when combined with Troleandomycin.Experimental
NilvadipineThe metabolism of Nilvadipine can be decreased when combined with Troleandomycin.Approved
NimesulideThe metabolism of Nimesulide can be decreased when combined with Troleandomycin.Approved, Withdrawn
NimodipineThe metabolism of Nimodipine can be decreased when combined with Troleandomycin.Approved
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Troleandomycin.Approved
NisoldipineThe metabolism of Nisoldipine can be decreased when combined with Troleandomycin.Approved
NitrendipineThe metabolism of Nitrendipine can be decreased when combined with Troleandomycin.Approved
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Troleandomycin.Approved
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Troleandomycin.Approved, Investigational
OlaparibThe metabolism of Troleandomycin can be decreased when combined with Olaparib.Approved
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Troleandomycin.Approved
OsimertinibThe serum concentration of Troleandomycin can be increased when it is combined with Osimertinib.Approved
OuabainThe serum concentration of Ouabain can be increased when it is combined with Troleandomycin.Approved
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Troleandomycin.Approved, Vet Approved
PalbociclibThe serum concentration of Troleandomycin can be increased when it is combined with Palbociclib.Approved
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Troleandomycin.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Troleandomycin.Approved
PentobarbitalThe metabolism of Troleandomycin can be increased when combined with Pentobarbital.Approved, Vet Approved
PerhexilineThe metabolism of Perhexiline can be decreased when combined with Troleandomycin.Approved
PhenindioneThe serum concentration of Phenindione can be increased when it is combined with Troleandomycin.Approved
PhenobarbitalThe metabolism of Troleandomycin can be increased when combined with Phenobarbital.Approved
PhenprocoumonThe serum concentration of Phenprocoumon can be increased when it is combined with Troleandomycin.Approved
PhenytoinThe metabolism of Troleandomycin can be increased when combined with Phenytoin.Approved, Vet Approved
Picosulfuric acidThe therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Troleandomycin.Approved
PimozideTroleandomycin may increase the QTc-prolonging activities of Pimozide.Approved
PinaveriumThe metabolism of Pinaverium can be decreased when combined with Troleandomycin.Approved
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Troleandomycin.Approved
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Troleandomycin.Approved
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Troleandomycin.Approved
PosaconazoleThe metabolism of Troleandomycin can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Troleandomycin.Approved
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Troleandomycin.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Troleandomycin.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Troleandomycin.Approved, Vet Approved
PregabalinThe metabolism of Pregabalin can be decreased when combined with Troleandomycin.Approved, Illicit, Investigational
PrenylamineThe metabolism of Prenylamine can be decreased when combined with Troleandomycin.Withdrawn
PrimidoneThe metabolism of Troleandomycin can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Troleandomycin.Approved, Vet Approved
PropranololThe serum concentration of Propranolol can be increased when it is combined with Troleandomycin.Approved, Investigational
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Troleandomycin.Approved
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Troleandomycin.Approved
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Troleandomycin.Approved
QuinineThe serum concentration of Quinine can be increased when it is combined with Troleandomycin.Approved
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Troleandomycin.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Troleandomycin.Approved, Investigational
RepaglinideThe serum concentration of Repaglinide can be increased when it is combined with Troleandomycin.Approved, Investigational
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Troleandomycin.Approved
RifabutinThe metabolism of Troleandomycin can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Troleandomycin can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Troleandomycin can be increased when combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Troleandomycin.Approved, Investigational
RilpivirineThe serum concentration of Rilpivirine can be increased when it is combined with Troleandomycin.Approved
RisedronateThe metabolism of Risedronate can be decreased when combined with Troleandomycin.Approved, Investigational
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Troleandomycin.Approved, Investigational
RitonavirThe metabolism of Troleandomycin can be decreased when combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Troleandomycin.Approved
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Troleandomycin.Approved, Investigational
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Troleandomycin.Approved, Vet Approved
SaquinavirThe metabolism of Troleandomycin can be decreased when combined with Saquinavir.Approved, Investigational
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Troleandomycin.Approved
SildenafilThe metabolism of Troleandomycin can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Troleandomycin.Approved
SiltuximabThe serum concentration of Troleandomycin can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Troleandomycin can be increased when it is combined with Simeprevir.Approved
SirolimusThe metabolism of Sirolimus can be decreased when combined with Troleandomycin.Approved, Investigational
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Troleandomycin.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Troleandomycin.Approved
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Troleandomycin.Approved, Investigational
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Troleandomycin.Approved
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Troleandomycin.Experimental
St. John's WortThe serum concentration of Troleandomycin can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Troleandomycin can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Troleandomycin can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Troleandomycin.Approved, Investigational
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Troleandomycin.Approved
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Troleandomycin.Experimental
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Troleandomycin.Approved
TelaprevirThe metabolism of Troleandomycin can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Troleandomycin can be decreased when combined with Telithromycin.Approved
TemsirolimusThe risk or severity of adverse effects can be increased when Troleandomycin is combined with Temsirolimus.Approved
TerfenadineTroleandomycin may increase the QTc-prolonging activities of Terfenadine.Withdrawn
TheophyllineThe metabolism of Theophylline can be decreased when combined with Troleandomycin.Approved
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Troleandomycin.Approved
TiclopidineThe metabolism of Troleandomycin can be decreased when combined with Ticlopidine.Approved
TimololThe serum concentration of Timolol can be increased when it is combined with Troleandomycin.Approved
TocilizumabThe serum concentration of Troleandomycin can be decreased when it is combined with Tocilizumab.Approved
Tolfenamic AcidThe metabolism of Tolfenamic Acid can be decreased when combined with Troleandomycin.Approved
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Troleandomycin.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Troleandomycin.Approved, Investigational
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Troleandomycin.Approved, Investigational
TranilastThe metabolism of Tranilast can be decreased when combined with Troleandomycin.Approved, Investigational
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Troleandomycin.Approved
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Troleandomycin.Approved
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Troleandomycin.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Troleandomycin.Approved
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Troleandomycin.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Troleandomycin.Approved
VenlafaxineThe metabolism of Troleandomycin can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Verapamil can be decreased when combined with Troleandomycin.Approved
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Troleandomycin.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Troleandomycin.Approved, Investigational
VindesineThe serum concentration of Vindesine can be increased when it is combined with Troleandomycin.Approved
VinorelbineThe serum concentration of Vinorelbine can be increased when it is combined with Troleandomycin.Approved, Investigational
VinpocetineThe metabolism of Vinpocetine can be decreased when combined with Troleandomycin.Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Troleandomycin.Approved
VoriconazoleThe metabolism of Troleandomycin can be decreased when combined with Voriconazole.Approved, Investigational
WarfarinThe serum concentration of Warfarin can be increased when it is combined with Troleandomycin.Approved
XylometazolineThe metabolism of Xylometazoline can be decreased when combined with Troleandomycin.Approved
ZiconotideThe metabolism of Ziconotide can be decreased when combined with Troleandomycin.Approved
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Troleandomycin.Approved
ZiprasidoneThe metabolism of Troleandomycin can be decreased when combined with Ziprasidone.Approved
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesJ01FA08
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9048
Blood Brain Barrier-0.945
Caco-2 permeable-0.522
P-glycoprotein substrateSubstrate0.662
P-glycoprotein inhibitor IInhibitor0.9188
P-glycoprotein inhibitor IINon-inhibitor0.631
Renal organic cation transporterNon-inhibitor0.8177
CYP450 2C9 substrateNon-substrate0.7897
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7407
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9075
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorInhibitor0.7959
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9223
Ames testAMES toxic0.5213
CarcinogenicityNon-carcinogens0.8564
BiodegradationNot ready biodegradable0.9949
Rat acute toxicity2.2177 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9881
hERG inhibition (predictor II)Non-inhibitor0.9163
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.0192 mg/mLALOGPS
logP3.76ALOGPS
logP4.3ChemAxon
logS-4.6ALOGPS
pKa (Strongest Acidic)16.75ChemAxon
pKa (Strongest Basic)7.87ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count12ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area184.19 Å2ChemAxon
Rotatable Bond Count12ChemAxon
Refractivity201.15 m3·mol-1ChemAxon
Polarizability86.08 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as macrolides and analogues. These are organic compounds containing a lactone ring of at least twelve members.
KingdomOrganic compounds
Super ClassPhenylpropanoids and polyketides
ClassMacrolides and analogues
Sub ClassNot Available
Direct ParentMacrolides and analogues
Alternative Parents
Substituents
  • Macrolide
  • Amino sugar
  • Desosamine
  • Amino saccharide
  • Oxane
  • Monosaccharide
  • Acetate salt
  • Tertiary aliphatic amine
  • Tertiary amine
  • Lactone
  • Ketone
  • Carboxylic acid ester
  • Oxacycle
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Ether
  • Oxirane
  • Dialkyl ether
  • Carboxylic acid derivative
  • Acetal
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aliphatic heteropolycyclic compound
Molecular FrameworkAliphatic heteropolycyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Deinococcus radiodurans (strain ATCC 13939 / DSM 20539 / JCM 16871 / LMG 4051 / NBRC 15346 / NCIMB 9279 / R1 / VKM B-1422)
Pharmacological action
yes
Actions
inhibitor
General Function:
Structural constituent of ribosome
Specific Function:
Forms a cluster with L17 and L22, and with L22, a pair of "tweezers" that hold together all the domains of the 23S rRNA. Interacts with the antibiotic troleandomycin which blocks the peptide exit tunnel.
Gene Name:
rpmF
Uniprot ID:
P49228
Molecular Weight:
6791.905 Da
References
  1. Scharre KA, Eckels DD, Gershwin ME: Depression of colony formation by human thymus-derived lymphocytes with rifampin and other antimicrobial agents. J Infect Dis. 1981 Jun;143(6):832-5. [PubMed:6972981 ]
Kind
Protein
Organism
Escherichia coli (strain K12)
Pharmacological action
yes
Actions
inhibitor
General Function:
Translation repressor activity
Specific Function:
One of the primary rRNA binding proteins, this protein initially binds near the 5'-end of the 23S rRNA. It is important during the early stages of 50S assembly. It makes multiple contacts with different domains of the 23S rRNA in the assembled 50S subunit and ribosome.Protein L4 is a both a transcriptional repressor and a translational repressor protein; these two functions are independent of e...
Gene Name:
rplD
Uniprot ID:
P60723
Molecular Weight:
22086.36 Da
References
  1. Scharre KA, Eckels DD, Gershwin ME: Depression of colony formation by human thymus-derived lymphocytes with rifampin and other antimicrobial agents. J Infect Dis. 1981 Jun;143(6):832-5. [PubMed:6972981 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
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. Ono S, Hatanaka T, Hotta H, Satoh T, Gonzalez FJ, Tsutsui M: Specificity of substrate and inhibitor probes for cytochrome P450s: evaluation of in vitro metabolism using cDNA-expressed human P450s and human liver microsomes. Xenobiotica. 1996 Jul;26(7):681-93. [PubMed:8819299 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. 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
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. Klees TM, Sheffels P, Dale O, Kharasch ED: Metabolism of alfentanil by cytochrome p4503a (cyp3a) enzymes. Drug Metab Dispos. 2005 Mar;33(3):303-11. Epub 2004 Nov 22. [PubMed:15557344 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Monooxygenase activity
Specific Function:
Exhibits low testosterone 6-beta-hydroxylase activity.
Gene Name:
CYP3A43
Uniprot ID:
Q9HB55
Molecular Weight:
57669.21 Da
References
  1. Ledirac N, de Sousa G, Fontaine F, Agouridas C, Gugenheim J, Lorenzon G, Rahmani R: Effects of macrolide antibiotics on CYP3A expression in human and rat hepatocytes: interspecies differences in response to troleandomycin. Drug Metab Dispos. 2000 Dec;28(12):1391-3. [PubMed:11095572 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Molecular Weight:
56501.005 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.
Gene Name:
CYP2C18
Uniprot ID:
P33260
Molecular Weight:
55710.075 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. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 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
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. 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. Wang EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. [PubMed:11716514 ]
  2. Ekins S, Kim RB, Leake BF, Dantzig AH, Schuetz EG, Lan LB, Yasuda K, Shepard RL, Winter MA, Schuetz JD, Wikel JH, Wrighton SA: Three-dimensional quantitative structure-activity relationships of inhibitors of P-glycoprotein. Mol Pharmacol. 2002 May;61(5):964-73. [PubMed:11961113 ]
  3. Yasuda K, Lan LB, Sanglard D, Furuya K, Schuetz JD, Schuetz EG: Interaction of cytochrome P450 3A inhibitors with P-glycoprotein. J Pharmacol Exp Ther. 2002 Oct;303(1):323-32. [PubMed:12235267 ]
Comments
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Drug created on July 06, 2007 13:54 / Updated on August 17, 2016 12:23