You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameIdelalisib
Accession NumberDB09054
TypeSmall Molecule
GroupsApproved
Description

Idelalisib is a phosphoinositide 3-kinase inhibitor indicated in the treatment of chronic lymphocytic leukemia (CLL), relapsed follicular B-cell non-Hodgkin lymphoma (FL), and relapsed small lymphocytic lymphoma (SLL). For the treatment of relapsed CLL, it is currently indicated as a second-line agent in combination with rituximab in patients for whom rituximab alone would be considered appropriate therapy due to other co-morbidities, while in the treatment of FL and SLL it is intended to be used in patients who have received at least two prior systemic therapies. More specifically, idelalisib targets P110δ, the delta isoform of the enzyme phosphatidylinositol-4,5-bisphosphate 3-kinase, also known as PI-3K. The PI-3Ks are a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. In contrast to the other class IA PI3Ks p110α and p110β, p110δ is principally expressed in leukocytes (white blood cells) and is important for the function of T cells, B cell, mast cells and neutrophils. By inhibiting this enzyme, idelalisib induces apoptosis of malignant cells and inhibits several cell signaling pathways, including B-cell receptor (BCR) signaling and C-X-C chemokine receptors type 5 and type 4 signalling, which are involved in trafficking and homing of B-cells to the lymph nodes and bone marrow. Treatment of lymphoma cells with idelalisib has been shown to result in inhibition of chemotaxis and adhesion, and reduced cell viability.

Structure
Thumb
Synonyms
5-Fluoro-3-phenyl-2-((S)-1-(9H-purin-6-ylamino)-propyl)-3H-quinazolin-4-one
5-fluoro-3-phenyl-2-[(1S)-1-(3H-purin-6-ylamino)propyl]quinazolin-4(3H)-one
External Identifiers
  • CAL 101
  • CAL-101
  • CAL101
  • GS 1101
  • GS-1101
  • GS1101
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Zydeligtablet, film coated100 mg/1oralGilead Sciences, Inc.2014-07-23Not applicableUs
Zydeligtablet150 mgoralGilead Sciences Canada Inc2015-04-21Not applicableCanada
Zydeligtablet100 mgoralGilead Sciences Canada Inc2015-04-21Not applicableCanada
Zydeligtablet, film coated150 mg/1oralGilead Sciences, Inc.2014-07-23Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIYG57I8T5M0
CAS number870281-82-6
WeightAverage: 415.432
Monoisotopic: 415.155686391
Chemical FormulaC22H18FN7O
InChI KeyIFSDAJWBUCMOAH-HNNXBMFYSA-N
InChI
InChI=1S/C22H18FN7O/c1-2-15(28-20-18-19(25-11-24-18)26-12-27-20)21-29-16-10-6-9-14(23)17(16)22(31)30(21)13-7-4-3-5-8-13/h3-12,15H,2H2,1H3,(H2,24,25,26,27,28)/t15-/m0/s1
IUPAC Name
5-fluoro-3-phenyl-2-[(1S)-1-[(9H-purin-6-yl)amino]propyl]-3,4-dihydroquinazolin-4-one
SMILES
[H][C@@](CC)(NC1=NC=NC2=C1N=CN2)C1=NC2=CC=CC(F)=C2C(=O)N1C1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as 6-alkylaminopurines. These are compounds that contain an alkylamine group attached at the 6-position of a purine. Purine is a bicyclic aromatic compound made up of a pyrimidine ring fused to an imidazole ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassImidazopyrimidines
Sub ClassPurines and purine derivatives
Direct Parent6-alkylaminopurines
Alternative Parents
Substituents
  • 6-alkylaminopurine
  • Quinazoline
  • Pyrimidone
  • Secondary aliphatic/aromatic amine
  • Aryl fluoride
  • Aryl halide
  • Monocyclic benzene moiety
  • Pyrimidine
  • Benzenoid
  • Imidolactam
  • Imidazole
  • Heteroaromatic compound
  • Azole
  • Vinylogous halide
  • Lactam
  • Secondary amine
  • Azacycle
  • Hydrocarbon derivative
  • Organic oxide
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationIdelalisib is indicated in the treatment of chronic lymphocytic leukemia (CLL), relapsed follicular B-cell non-Hodgkin lymphoma (FL), and relapsed small lymphocytic lymphoma (SLL). For the treatment of relapsed CLL, it is currently indicated as a second-line agent in combination with rituximab in patients for whom rituximab alone would be considered appropriate therapy due to other co-morbidities, while in the treatment of FL and SLL it is intended to be used in patients who have received at least two prior systemic therapies.
PharmacodynamicsNot Available
Mechanism of actionIdelalisib specifically inhibits P110δ, the delta isoform of the enzyme phosphatidylinositol-4,5-bisphosphate 3-kinase, also known as PI-3K. The PI-3Ks are a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. In contrast to the other class IA PI3Ks p110α and p110β, p110δ is principally expressed in leukocytes (white blood cells) and is important for the function of T cells, B cell, mast cells and neutrophils. By inhibiting this enzyme, idelalisib induces apoptosis of malignant cells and inhibits several cell signaling pathways, including B-cell receptor (BCR) signaling and C-X-C chemokine receptors type 5 and type 4 signalling, which are involved in trafficking and homing of B-cells to the lymph nodes and bone marrow. Treatment of lymphoma cells with idelalisib has been shown to result in inhibition of chemotaxis and adhesion, and reduced cell viability.
Related Articles
AbsorptionFollowing oral administration, the median Tmax was observed at 1.5 hours.
Volume of distribution

23 L

Protein bindingIdelalisib is greater than 84% bound to human plasma proteins with no concentration dependence.
Metabolism

Idelalisib is metabolized by aldehyde oxidase and CYP3A to its major metabolite GS-563117, which is inactive against P110δ. Idelalisib is also metabolized to a minor extent by UGT1A4.

SubstrateEnzymesProduct
Idelalisib
GS-563117Details
Route of eliminationFollowing a single dose of 150 mg of [14C] idelalisib, 78% and 14% of the radioactivity was excreted in feces and urine, respectively. GS-563117, idelalisib's major metabolite, accounted for 49% of the radioactivity in the urine and 44% in the feces.
Half lifeThe terminal elimination half-life is 8.2 hours.
Clearance

14.9 L/hr

ToxicityNot Available
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 AbsorptionNot AvailableNot Available
Blood Brain BarrierNot AvailableNot Available
Caco-2 permeableNot AvailableNot Available
P-glycoprotein substrateNot AvailableNot Available
P-glycoprotein inhibitor INot AvailableNot Available
P-glycoprotein inhibitor IINot AvailableNot Available
Renal organic cation transporterNot AvailableNot Available
CYP450 2C9 substrateNot AvailableNot Available
CYP450 2D6 substrateNot AvailableNot Available
CYP450 3A4 substrateNot AvailableNot Available
CYP450 1A2 substrateNot AvailableNot Available
CYP450 2C9 inhibitorNot AvailableNot Available
CYP450 2D6 inhibitorNot AvailableNot Available
CYP450 2C19 inhibitorNot AvailableNot Available
CYP450 3A4 inhibitorNot AvailableNot Available
CYP450 inhibitory promiscuityNot AvailableNot Available
Ames testNot AvailableNot Available
CarcinogenicityNot AvailableNot Available
BiodegradationNot AvailableNot Available
Rat acute toxicityNot AvailableNot applicable
hERG inhibition (predictor I)Not AvailableNot Available
hERG inhibition (predictor II)Not AvailableNot Available
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tabletoral100 mg
Tabletoral150 mg
Tablet, film coatedoral100 mg/1
Tablet, film coatedoral150 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6800620 No2001-04-242021-04-24Us
US6949535 No2001-04-242021-04-24Us
US8138195 No2001-04-242021-04-24Us
US8492389 No2001-04-242021-04-24Us
US8637533 No2001-04-242021-04-24Us
US8865730 No2013-03-052033-03-05Us
US8980901 No2005-05-122025-05-12Us
US9149477 No2005-05-122025-05-12Us
USRE44599 No2005-07-212025-07-21Us
USRE44638 No2005-08-052025-08-05Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.0255 mg/mLALOGPS
logP3.03ALOGPS
logP3.36ChemAxon
logS-4.2ALOGPS
pKa (Strongest Acidic)9.86ChemAxon
pKa (Strongest Basic)4.27ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area99.16 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity116.83 m3·mol-1ChemAxon
Polarizability41.41 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General References
  1. Jin F, Robeson M, Zhou H, Moyer C, Wilbert S, Murray B, Ramanathan S: Clinical drug interaction profile of idelalisib in healthy subjects. J Clin Pharmacol. 2015 Aug;55(8):909-19. doi: 10.1002/jcph.495. Epub 2015 May 6. [PubMed:25760671 ]
  2. Fiorcari S, Brown WS, McIntyre BW, Estrov Z, Maffei R, O'Brien S, Sivina M, Hoellenriegel J, Wierda WG, Keating MJ, Ding W, Kay NE, Lannutti BJ, Marasca R, Burger JA: The PI3-kinase delta inhibitor idelalisib (GS-1101) targets integrin-mediated adhesion of chronic lymphocytic leukemia (CLL) cell to endothelial and marrow stromal cells. PLoS One. 2013 Dec 23;8(12):e83830. doi: 10.1371/journal.pone.0083830. eCollection 2013. [PubMed:24376763 ]
  3. Flinn IW, Kahl BS, Leonard JP, Furman RR, Brown JR, Byrd JC, Wagner-Johnston ND, Coutre SE, Benson DM, Peterman S, Cho Y, Webb HK, Johnson DM, Yu AS, Ulrich RG, Godfrey WR, Miller LL, Spurgeon SE: Idelalisib, a selective inhibitor of phosphatidylinositol 3-kinase-delta, as therapy for previously treated indolent non-Hodgkin lymphoma. Blood. 2014 May 29;123(22):3406-13. doi: 10.1182/blood-2013-11-538546. Epub 2014 Mar 10. [PubMed:24615776 ]
  4. Brown JR, Byrd JC, Coutre SE, Benson DM, Flinn IW, Wagner-Johnston ND, Spurgeon SE, Kahl BS, Bello C, Webb HK, Johnson DM, Peterman S, Li D, Jahn TM, Lannutti BJ, Ulrich RG, Yu AS, Miller LL, Furman RR: Idelalisib, an inhibitor of phosphatidylinositol 3-kinase p110delta, for relapsed/refractory chronic lymphocytic leukemia. Blood. 2014 May 29;123(22):3390-7. doi: 10.1182/blood-2013-11-535047. Epub 2014 Mar 10. [PubMed:24615777 ]
External Links
ATC CodesL01XX47
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (496 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AlfentanilThe serum concentration of Alfentanil can be increased when it is combined with Idelalisib.
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Idelalisib.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Idelalisib.
AlmotriptanThe serum concentration of Almotriptan can be increased when it is combined with Idelalisib.
AlosetronThe serum concentration of Alosetron can be increased when it is combined with Idelalisib.
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Idelalisib.
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Idelalisib.
AmiodaroneThe serum concentration of Amiodarone can be increased when it is combined with Idelalisib.
AmlodipineThe serum concentration of Amlodipine can be increased when it is combined with Idelalisib.
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Idelalisib.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Idelalisib.
AprepitantThe serum concentration of Aprepitant can be increased when it is combined with Idelalisib.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Idelalisib.
ArmodafinilThe serum concentration of Armodafinil can be increased when it is combined with Idelalisib.
AstemizoleThe serum concentration of Astemizole can be increased when it is combined with Idelalisib.
AtazanavirThe serum concentration of Atazanavir can be increased when it is combined with Idelalisib.
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Idelalisib.
AvanafilThe serum concentration of Avanafil can be increased when it is combined with Idelalisib.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Idelalisib.
BarnidipineThe serum concentration of Barnidipine can be increased when it is combined with Idelalisib.
BedaquilineThe serum concentration of Bedaquiline can be increased when it is combined with Idelalisib.
BenzphetamineThe serum concentration of Benzphetamine can be increased when it is combined with Idelalisib.
BexaroteneThe serum concentration of Idelalisib can be decreased when it is combined with Bexarotene.
BisoprololThe serum concentration of Bisoprolol can be increased when it is combined with Idelalisib.
BoceprevirThe serum concentration of Idelalisib can be increased when it is combined with Boceprevir.
BortezomibThe serum concentration of Bortezomib can be increased when it is combined with Idelalisib.
BosentanThe serum concentration of Idelalisib can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Idelalisib.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Idelalisib.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Idelalisib.
BrinzolamideThe serum concentration of Brinzolamide can be increased when it is combined with Idelalisib.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Idelalisib.
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Idelalisib.
BuprenorphineThe serum concentration of Buprenorphine can be increased when it is combined with Idelalisib.
BuspironeThe serum concentration of Buspirone can be increased when it is combined with Idelalisib.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Idelalisib.
CabozantinibThe serum concentration of Cabozantinib can be increased when it is combined with Idelalisib.
CalcitriolThe serum concentration of Calcitriol can be increased when it is combined with Idelalisib.
CarbamazepineThe serum concentration of Idelalisib can be decreased when it is combined with Carbamazepine.
CeritinibThe serum concentration of Ceritinib can be increased when it is combined with Idelalisib.
ChlordiazepoxideThe serum concentration of Chlordiazepoxide can be increased when it is combined with Idelalisib.
ChloroquineThe serum concentration of Chloroquine can be increased when it is combined with Idelalisib.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Idelalisib.
CinacalcetThe serum concentration of Cinacalcet can be increased when it is combined with Idelalisib.
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Idelalisib.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Idelalisib.
ClarithromycinThe serum concentration of Clarithromycin can be increased when it is combined with Idelalisib.
ClonazepamThe serum concentration of Clonazepam can be increased when it is combined with Idelalisib.
ClorazepateThe serum concentration of Clorazepate can be increased when it is combined with Idelalisib.
CobicistatThe serum concentration of Idelalisib can be increased when it is combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Idelalisib.
CocaineThe serum concentration of Cocaine can be increased when it is combined with Idelalisib.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Idelalisib.
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Idelalisib.
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Idelalisib.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Idelalisib.
Cyproterone acetateThe serum concentration of Cyproterone acetate can be increased when it is combined with Idelalisib.
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Idelalisib.
DaclatasvirThe serum concentration of Daclatasvir can be increased when it is combined with Idelalisib.
DantroleneThe serum concentration of Dantrolene can be increased when it is combined with Idelalisib.
DapoxetineThe serum concentration of Dapoxetine can be increased when it is combined with Idelalisib.
DapsoneThe serum concentration of Dapsone can be increased when it is combined with Idelalisib.
DarifenacinThe serum concentration of Darifenacin can be increased when it is combined with Idelalisib.
DarunavirThe serum concentration of Darunavir can be increased when it is combined with Idelalisib.
DasatinibThe serum concentration of Dasatinib can be increased when it is combined with Idelalisib.
DeferasiroxThe serum concentration of Idelalisib can be decreased when it is combined with Deferasirox.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Idelalisib.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Idelalisib.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Idelalisib.
DienogestThe serum concentration of Dienogest can be increased when it is combined with Idelalisib.
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Idelalisib.
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Idelalisib.
DisopyramideThe serum concentration of Disopyramide can be increased when it is combined with Idelalisib.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Idelalisib.
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Idelalisib.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Idelalisib.
DoxazosinThe serum concentration of Doxazosin can be increased when it is combined with Idelalisib.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Idelalisib.
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Idelalisib.
DronedaroneThe serum concentration of Dronedarone can be increased when it is combined with Idelalisib.
DrospirenoneThe serum concentration of Drospirenone can be increased when it is combined with Idelalisib.
DutasterideThe serum concentration of Dutasteride can be increased when it is combined with Idelalisib.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Idelalisib.
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Idelalisib.
EnzalutamideThe serum concentration of Idelalisib can be decreased when it is combined with Enzalutamide.
EplerenoneThe serum concentration of Eplerenone can be increased when it is combined with Idelalisib.
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Idelalisib.
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Idelalisib.
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Idelalisib.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Idelalisib.
ErythromycinThe serum concentration of Erythromycin can be increased when it is combined with Idelalisib.
EscitalopramThe serum concentration of Escitalopram can be increased when it is combined with Idelalisib.
EstazolamThe serum concentration of Estazolam can be increased when it is combined with Idelalisib.
EszopicloneThe serum concentration of Eszopiclone can be increased when it is combined with Idelalisib.
EthosuximideThe serum concentration of Ethosuximide can be increased when it is combined with Idelalisib.
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Idelalisib.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Idelalisib.
FelbamateThe serum concentration of Felbamate can be increased when it is combined with Idelalisib.
FelodipineThe serum concentration of Felodipine can be increased when it is combined with Idelalisib.
FentanylThe serum concentration of Fentanyl can be increased when it is combined with Idelalisib.
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Idelalisib.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Idelalisib.
FludrocortisoneThe serum concentration of Fludrocortisone can be increased when it is combined with Idelalisib.
FlunisolideThe serum concentration of Flunisolide can be increased when it is combined with Idelalisib.
FlurazepamThe serum concentration of Flurazepam can be increased when it is combined with Idelalisib.
FlutamideThe serum concentration of Flutamide can be increased when it is combined with Idelalisib.
Fluticasone PropionateThe serum concentration of Fluticasone Propionate can be increased when it is combined with Idelalisib.
FosaprepitantThe serum concentration of Fosaprepitant can be increased when it is combined with Idelalisib.
FosphenytoinThe serum concentration of Idelalisib can be decreased when it is combined with Fosphenytoin.
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Idelalisib.
GuanfacineThe serum concentration of Guanfacine can be increased when it is combined with Idelalisib.
HalofantrineThe serum concentration of Halofantrine can be increased when it is combined with Idelalisib.
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Idelalisib.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Idelalisib.
Hydroxyprogesterone caproateThe serum concentration of Hydroxyprogesterone caproate can be increased when it is combined with Idelalisib.
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Idelalisib.
IfosfamideThe serum concentration of the active metabolites of Ifosfamide can be reduced when Ifosfamide is used in combination with Idelalisib resulting in a loss in efficacy.
IloperidoneThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Idelalisib.
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Idelalisib.
ImidafenacinThe serum concentration of Imidafenacin can be increased when it is combined with Idelalisib.
IndinavirThe serum concentration of Idelalisib can be increased when it is combined with Indinavir.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Idelalisib.
IsavuconazoniumThe serum concentration of Isavuconazonium can be increased when it is combined with Idelalisib.
IsosorbideThe serum concentration of Isosorbide can be increased when it is combined with Idelalisib.
Isosorbide DinitrateThe serum concentration of Isosorbide Dinitrate can be increased when it is combined with Idelalisib.
Isosorbide MononitrateThe serum concentration of Isosorbide Mononitrate can be increased when it is combined with Idelalisib.
IsradipineThe serum concentration of Isradipine can be increased when it is combined with Idelalisib.
ItraconazoleThe serum concentration of Itraconazole can be increased when it is combined with Idelalisib.
IvabradineThe serum concentration of Ivabradine can be increased when it is combined with Idelalisib.
IvacaftorThe serum concentration of Ivacaftor can be increased when it is combined with Idelalisib.
IxabepiloneThe serum concentration of Ixabepilone can be increased when it is combined with Idelalisib.
KetamineThe serum concentration of Ketamine can be increased when it is combined with Idelalisib.
KetoconazoleThe serum concentration of Idelalisib can be increased when it is combined with Ketoconazole.
LacosamideThe serum concentration of Lacosamide can be increased when it is combined with Idelalisib.
LapatinibThe serum concentration of Lapatinib can be increased when it is combined with Idelalisib.
LeflunomideThe risk or severity of adverse effects can be increased when Idelalisib is combined with Leflunomide.
LercanidipineThe serum concentration of Lercanidipine can be increased when it is combined with Idelalisib.
LevobupivacaineThe serum concentration of Levobupivacaine can be increased when it is combined with Idelalisib.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Idelalisib.
LidocaineThe serum concentration of Lidocaine can be increased when it is combined with Idelalisib.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Idelalisib.
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Idelalisib.
LumefantrineThe serum concentration of Lumefantrine can be increased when it is combined with Idelalisib.
LurasidoneThe serum concentration of Lurasidone can be increased when it is combined with Idelalisib.
MacitentanThe serum concentration of MACITENTAN can be increased when it is combined with Idelalisib.
MaravirocThe serum concentration of Maraviroc can be increased when it is combined with Idelalisib.
Medroxyprogesterone acetateThe serum concentration of Medroxyprogesterone Acetate can be increased when it is combined with Idelalisib.
MefloquineThe serum concentration of Mefloquine can be increased when it is combined with Idelalisib.
MethadoneThe serum concentration of Methadone can be increased when it is combined with Idelalisib.
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Idelalisib.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Idelalisib.
MifepristoneThe serum concentration of Mifepristone can be increased when it is combined with Idelalisib.
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Idelalisib.
MitotaneThe serum concentration of Idelalisib can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Modafinil can be increased when it is combined with Idelalisib.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Idelalisib.
NatalizumabThe risk or severity of adverse effects can be increased when Idelalisib is combined with Natalizumab.
NateglinideThe serum concentration of Nateglinide can be increased when it is combined with Idelalisib.
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Idelalisib.
NelfinavirThe serum concentration of Idelalisib can be increased when it is combined with Nelfinavir.
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Idelalisib.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Idelalisib.
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Idelalisib.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Idelalisib.
NisoldipineThe serum concentration of Nisoldipine can be increased when it is combined with Idelalisib.
OlaparibThe serum concentration of Olaparib can be increased when it is combined with Idelalisib.
OspemifeneThe serum concentration of Ospemifene can be increased when it is combined with Idelalisib.
OxybutyninThe serum concentration of Oxybutynin can be increased when it is combined with Idelalisib.
OxycodoneThe serum concentration of Oxycodone can be increased when it is combined with Idelalisib.
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Idelalisib.
PalbociclibThe serum concentration of Palbociclib can be increased when it is combined with Idelalisib.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Idelalisib.
ParecoxibThe serum concentration of Parecoxib can be increased when it is combined with Idelalisib.
ParicalcitolThe serum concentration of Paricalcitol can be increased when it is combined with Idelalisib.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Idelalisib.
PhenobarbitalThe serum concentration of Idelalisib can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Idelalisib can be decreased when it is combined with Phenytoin.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Idelalisib.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Idelalisib.
PipotiazineThe serum concentration of Pipotiazine can be increased when it is combined with Idelalisib.
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Idelalisib.
PosaconazoleThe serum concentration of Idelalisib can be increased when it is combined with Posaconazole.
PranlukastThe serum concentration of Pranlukast can be increased when it is combined with Idelalisib.
PrasugrelThe serum concentration of the active metabolites of Prasugrel can be reduced when Prasugrel is used in combination with Idelalisib resulting in a loss in efficacy.
PraziquantelThe serum concentration of Praziquantel can be increased when it is combined with Idelalisib.
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Idelalisib.
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Idelalisib.
PrimidoneThe serum concentration of Idelalisib can be decreased when it is combined with Primidone.
PropafenoneThe serum concentration of Propafenone can be increased when it is combined with Idelalisib.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Idelalisib.
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Idelalisib.
QuinineThe serum concentration of Quinine can be increased when it is combined with Idelalisib.
RamelteonThe serum concentration of Ramelteon can be increased when it is combined with Idelalisib.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Idelalisib.
RegorafenibThe serum concentration of Regorafenib can be increased when it is combined with Idelalisib.
RepaglinideThe serum concentration of Repaglinide can be increased when it is combined with Idelalisib.
RetapamulinThe serum concentration of Retapamulin can be increased when it is combined with Idelalisib.
RifabutinThe serum concentration of Idelalisib can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Idelalisib can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Idelalisib can be decreased when it is combined with Rifapentine.
RilpivirineThe serum concentration of Rilpivirine can be increased when it is combined with Idelalisib.
RitonavirThe serum concentration of Idelalisib can be increased when it is combined with Ritonavir.
RoflumilastRoflumilast may increase the immunosuppressive activities of Idelalisib.
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Idelalisib.
RuxolitinibThe serum concentration of Ruxolitinib can be increased when it is combined with Idelalisib.
SalmeterolThe serum concentration of Salmeterol can be increased when it is combined with Idelalisib.
SaquinavirThe serum concentration of Idelalisib can be increased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be increased when it is combined with Idelalisib.
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Idelalisib.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Idelalisib.
SiltuximabThe serum concentration of Idelalisib can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Idelalisib.
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Idelalisib.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Idelalisib.
SirolimusThe serum concentration of Sirolimus can be increased when it is combined with Idelalisib.
SolifenacinThe serum concentration of Solifenacin can be increased when it is combined with Idelalisib.
SonidegibThe serum concentration of Sonidegib can be increased when it is combined with Idelalisib.
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Idelalisib.
SpiramycinThe serum concentration of Spiramycin can be increased when it is combined with Idelalisib.
St. John's WortThe serum concentration of Idelalisib can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Stiripentol can be increased when it is combined with Idelalisib.
SufentanilThe serum concentration of Sufentanil can be increased when it is combined with Idelalisib.
SunitinibThe serum concentration of Sunitinib can be increased when it is combined with Idelalisib.
SuvorexantThe serum concentration of Suvorexant can be increased when it is combined with Idelalisib.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Idelalisib.
TadalafilThe serum concentration of Tadalafil can be increased when it is combined with Idelalisib.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Idelalisib.
TamsulosinThe serum concentration of Tamsulosin can be increased when it is combined with Idelalisib.
TasimelteonThe serum concentration of Tasimelteon can be increased when it is combined with Idelalisib.
TelaprevirThe serum concentration of Telaprevir can be increased when it is combined with Idelalisib.
TelithromycinThe serum concentration of Telithromycin can be increased when it is combined with Idelalisib.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Idelalisib.
TeniposideThe serum concentration of Teniposide can be increased when it is combined with Idelalisib.
TerfenadineThe serum concentration of Terfenadine can be increased when it is combined with Idelalisib.
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Idelalisib.
TiagabineThe serum concentration of Tiagabine can be increased when it is combined with Idelalisib.
TicagrelorThe serum concentration of the active metabolites of Ticagrelor can be reduced when Ticagrelor is used in combination with Idelalisib resulting in a loss in efficacy.
TocilizumabThe serum concentration of Idelalisib can be decreased when it is combined with Tocilizumab.
TofacitinibThe serum concentration of Tofacitinib can be increased when it is combined with Idelalisib.
TolterodineThe serum concentration of Tolterodine can be increased when it is combined with Idelalisib.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Idelalisib.
ToremifeneThe risk or severity of adverse effects can be increased when Idelalisib is combined with Toremifene.
TrabectedinThe serum concentration of Trabectedin can be increased when it is combined with Idelalisib.
TramadolThe serum concentration of Tramadol can be increased when it is combined with Idelalisib.
TrastuzumabTrastuzumab may increase the neutropenic activities of Idelalisib.
Trastuzumab emtansineThe serum concentration of ado-trastuzumab emtansine can be increased when it is combined with Idelalisib.
TrazodoneThe serum concentration of Trazodone can be increased when it is combined with Idelalisib.
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Idelalisib.
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Idelalisib.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Idelalisib.
VardenafilThe serum concentration of Vardenafil can be increased when it is combined with Idelalisib.
VemurafenibThe serum concentration of Vemurafenib can be increased when it is combined with Idelalisib.
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Idelalisib.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Idelalisib.
VilazodoneThe serum concentration of Vilazodone can be increased when it is combined with Idelalisib.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Idelalisib.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Idelalisib.
VindesineThe serum concentration of Vindesine can be increased when it is combined with Idelalisib.
VinorelbineThe serum concentration of Vinorelbine can be increased when it is combined with Idelalisib.
VorapaxarThe serum concentration of Vorapaxar can be increased when it is combined with Idelalisib.
VoriconazoleThe serum concentration of Idelalisib can be increased when it is combined with Voriconazole.
ZolpidemThe serum concentration of Zolpidem can be increased when it is combined with Idelalisib.
ZonisamideThe serum concentration of Zonisamide can be increased when it is combined with Idelalisib.
ZopicloneThe serum concentration of Zopiclone can be increased when it is combined with Idelalisib.
ZuclopenthixolThe serum concentration of Zuclopenthixol can be increased when it is combined with Idelalisib.
Food InteractionsNot Available

Targets

1. Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta isoform (P110δ)
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
Inhibitor

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Xanthine dehydrogenase activity
Specific Function:
Oxidase with broad substrate specificity, oxidizing aromatic azaheterocycles, such as N1-methylnicotinamide and N-methylphthalazinium, as well as aldehydes, such as benzaldehyde, retinal, pyridoxal, and vanillin. Plays a key role in the metabolism of xenobiotics and drugs containing aromatic azaheterocyclic substituents. Participates in the bioactivation of prodrugs such as famciclovir, catalyz...
Gene Name:
AOX1
Uniprot ID:
Q06278
Molecular Weight:
147916.735 Da
2. Cytochrome p450 3A subfamily
Kind
Protein group
Organism
Human
Pharmacological action
no
Actions
substrateinhibitor
3. UDP-glucuronosyltransferase 1A4
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
4. UDP-glucuronosyltransferase 1A1
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
inhibitor
Kind
Protein
Organism
Human
Pharmacological action
no
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
Kind
Protein
Organism
Human
Pharmacological action
no
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
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
inducer
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
inducer
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

Transporters

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrateinhibitor
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
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Molecular Weight:
76447.99 Da
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B3
Uniprot ID:
Q9NPD5
Molecular Weight:
77402.175 Da
Comments
comments powered by Disqus
Drug created on May 08, 2015 13:47 / Updated on July 30, 2016 01:53