Identification

Name
Idelalisib
Accession Number
DB09054
Type
Small Molecule
Groups
Approved
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 IDs
CAL 101 / CAL-101 / CAL101 / GS 1101 / GS-1101 / GS1101
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ZydeligTablet, film coated150 mgOralGilead Sciences Ireland Uc2014-09-18Not applicableEu
ZydeligTablet100 mgOralGilead Sciences2015-04-21Not applicableCanada
ZydeligTablet, film coated150 mg/1OralGilead Sciences, Inc.2014-07-23Not applicableUs
ZydeligTablet, film coated100 mgOralGilead Sciences Ireland Uc2014-09-18Not applicableEu
ZydeligTablet, film coated100 mg/1OralGilead Sciences, Inc.2014-07-23Not applicableUs
ZydeligTablet150 mgOralGilead Sciences2015-04-21Not applicableCanada
Categories
UNII
YG57I8T5M0
CAS number
870281-82-6
Weight
Average: 415.432
Monoisotopic: 415.155686391
Chemical Formula
C22H18FN7O
InChI Key
IFSDAJWBUCMOAH-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

Pharmacology

Indication

Idelalisib 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.

Associated Conditions
Pharmacodynamics
Not Available
Mechanism of action

Idelalisib 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.

TargetActionsOrganism
APhosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta isoform (P110δ)
inhibitor
Human
Absorption

Following oral administration, the median Tmax was observed at 1.5 hours.

Volume of distribution

23 L

Protein binding

Idelalisib 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.

Route of elimination

Following 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 life

The terminal elimination half-life is 8.2 hours.

Clearance

14.9 L/hr

Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Idelalisib.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Idelalisib.
2-MethoxyethanolThe risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Idelalisib.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Idelalisib.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be increased when combined with Idelalisib.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Idelalisib.
6-Deoxyerythronolide BThe metabolism of Idelalisib can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Idelalisib.
9-(N-methyl-L-isoleucine)-cyclosporin AThe risk or severity of adverse effects can be increased when Idelalisib is combined with 9-(N-methyl-L-isoleucine)-cyclosporin A.
AbataceptThe risk or severity of adverse effects can be increased when Abatacept is combined with Idelalisib.
Food Interactions
Not Available

References

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]
  5. FDA Approval: Idelalisib Monotherapy for the Treatment of Patients with Follicular Lymphoma and Small Lymphocytic Lymphoma [File]
External Links
KEGG Drug
D10560
PubChem Compound
11625818
PubChem Substance
310264996
ChemSpider
9800565
BindingDB
50403068
ChEBI
82701
ChEMBL
CHEMBL2216870
HET
40L
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Idelalisib
ATC Codes
L01XX47 — Idelalisib
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
PDB Entries
4xe0
FDA label
Download (496 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentB-Cell Malignancies1
1Active Not RecruitingTreatmentChronic, recurrent Lymphoid Leukemia1
1CompletedTreatmentAgnogenic Myeloid Metaplasia1
1CompletedTreatmentAllergic Rhinitis (AR)1
1CompletedTreatmentChronic Lymphocytic Leukaemia (CLL) / Follicular Lymphoma (FL) / Indolent Non-Hodgkin's Lymphomas / Lymphoplasmacytic Lymphoma (With or Without Waldenstrom Macroglobulinemia) / Marginal Zone Lymphoma / Small Lymphocytic Lymphoma (SLL)1
1CompletedTreatmentChronic Lymphocytic Leukaemia (CLL) / Indolent Non-Hodgkin's Lymphomas / Mantle Cell Lymphoma (MCL)1
1CompletedTreatmentChronic Lymphocytic Leukaemia (CLL) / Leukemia Acute Myeloid Leukemia (AML) / Lymphoma, Non-Hodgkin (NHL) / Multiple Myeloma (MM)1
1CompletedTreatmentChronic Lymphocytic Leukaemia (CLL) / Non-Hodgkin's Lymphoma (NHL)1
1CompletedTreatmentFollicular Lymphoma (FL) / Follicular Lymphoma, Mantle Cell Lymphoma / Mantle Cell Lymphoma (MCL)1
1CompletedTreatmentRecurrent Follicular Lymphoma1
1CompletedTreatmentRelapsed/Refractory Mantle Cell Lymphoma1
1Not Yet RecruitingTreatmentChronic Lymphocytic Leukaemia (CLL) / Chronic Lymphocytic Leukemia (CLL) - Refractory / Relapsed Chronic Lymphocytic Leukemia1
1RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL) / Leukemia Acute Myeloid Leukemia (AML) / Untreated Adult Acute Myeloid Leukemia1
1RecruitingTreatmentB Cell Chronic Lymphocytic Leukemia / B Cells--Tumors / B Cells-Tumors / Follicular Lymphoma (FL) / Large B-Cell Diffuse Lymphoma of Bone (Diagnosis) / Lymphoma, Large B-Cell, Diffuse (DLBCL) / Mantle Cell Lymphoma (MCL)1
1RecruitingTreatmentChronic Lymphocytic Leukaemia (CLL) / Peripheral T-Cell Lymphoma (PTCL)1
1RecruitingTreatmentLymphoma, Large B-Cell, Diffuse (DLBCL) / Mediastinal B-cell Lymphoma1
1TerminatedTreatmentChronic Lymphocytic Leukaemia (CLL)1
1TerminatedTreatmentPancreatic Ductal Adenocarcinoma1
1, 2CompletedTreatmentFollicular Lymphoma (FL) / Indolent Non-Hodgkin's Lymphomas / Marginal Zone Lymphoma / Small Lymphocytic Lymphoma (SLL)1
1, 2RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL)1
1, 2RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Metastasis / Recurrences1
2Active Not RecruitingTreatmentChronic Lymphocytic Leukaemia (CLL) / Leukemia, Lymphocytic, Chronic, B-Cell / Small Lymphocytic Lymphoma (SLL)1
2Active Not RecruitingTreatmentWaldenström's Macroglobulinemia (WM)1
2CompletedTreatmentChronic Lymphocytic Leukaemia (CLL) / Indolent Non-Hodgkin's Lymphomas / Lymphoma, Large B-Cell, Diffuse (DLBCL) / Mantle Cell Lymphoma (MCL)1
2CompletedTreatmentFollicular Lymphoma (FL) / Lymphoplasmacytic Lymphoma / Marginal Zone Lymphoma / Small Lymphocytic Lymphoma (SLL)1
2CompletedTreatmentLymphoma, Hodgkins1
2RecruitingTreatmentAmyloidosis1
2RecruitingTreatmentChronic Lymphocytic Leucemia1
2RecruitingTreatmentChronic Lymphocytic Leukaemia (CLL)1
2RecruitingTreatmentChronic Lymphocytic Leukemia (CLL) - Refractory / Chronic, recurrent Lymphocytic Leukemia / Recurrent Extranodal Marginal Zone Lymphoma of Mucosa-Associated Lymphoid Tissue / Recurrent Grade 1 Follicular Lymphoma / Recurrent Grade 2 Follicular Lymphoma / Recurrent Grade 3 Follicular Lymphoma / Recurrent Lymphoplasmacytic Lymphoma / Recurrent Marginal Zone Lymphoma / Recurrent Nodal Marginal Zone Lymphoma / Recurrent Small Lymphocytic Lymphoma / Recurrent Splenic Marginal Zone Lymphoma / Refractory Extranodal Marginal Zone Lymphoma of Mucosa-Associated Lymphoid Tissue / Refractory Follicular Lymphoma / Refractory Lymphoplasmacytic Lymphoma / Refractory Nodal Marginal Zone Lymphoma / Refractory Small Lymphocytic Lymphoma / Refractory Splenic Marginal Zone Lymphoma / Richter's Syndrome / Waldenström's Macroglobulinemia (WM)1
2RecruitingTreatmentFollicular Lymphoma (FL) / Indolent Lymphoma / Lymphoma, B-Cell / Lymphoplasmacytic Lymphoma / Marginal Zone Lymphoma / Non Hodgkin Lymphoma (NHL) / Small Lymphocytic Lymphoma (SLL) / Transformed Lymphoma / Waldenström's Macroglobulinemia (WM)1
2RecruitingTreatmentLymphoma, Large B-Cell, Diffuse (DLBCL)1
2SuspendedTreatmentChronic Lymphocytic Leukaemia (CLL) / Small Lymphocytic Lymphoma (SLL)1
2TerminatedTreatmentB-cell Chronic Lymphocytic Leukemia (CLL) With 17p Deletion1
2TerminatedTreatmentChronic Lymphocytic Leukaemia (CLL) / Small Lymphocytic Lymphoma (SLL)1
2TerminatedTreatmentFollicular Lymphoma (FL) / Small Lymphocytic Lymphoma (SLL)1
2TerminatedTreatmentWaldenström's Macroglobulinemia (WM)1
2WithdrawnTreatmentChronic Lymphocytic Leukaemia (CLL)1
2WithdrawnTreatmentChronic Lymphocytic Leukaemia (CLL) / Chronic, recurrent Lymphocytic Leukemia / Leukemia, Prolymphocytic / Non-Hodgkin's Lymphoma (NHL) / Recurrent Non-Hodgkin Lymphoma / Recurrent Small Lymphocytic Lymphoma / Small Lymphocytic Lymphoma (SLL)1
3Active Not RecruitingTreatmentChronic Lymphocytic Leukaemia (CLL)1
3CompletedTreatmentChronic Lymphocytic Leukaemia (CLL)3
3RecruitingTreatmentChronic Lymphocytic Leukaemia (CLL)1
3RecruitingTreatmentFollicular Lymphoma (FL) / Small Lymphocytic Lymphoma (SLL)1
3TerminatedTreatmentChronic Lymphocytic Leukaemia (CLL)2
3TerminatedTreatmentIndolent Non-Hodgkin's Lymphomas2
4CompletedTreatmentLymphoid Malignancies1
Not AvailableApproved for MarketingNot AvailableChronic Lymphocytic Leukaemia (CLL)1
Not AvailableEnrolling by InvitationNot AvailableB-Cell Malignancies1
Not AvailableNot Yet RecruitingNot AvailableChronic Lymphocytic Leukaemia (CLL)1
Not AvailableRecruitingNot AvailableChronic Lymphocytic Leukaemia (CLL)1
Not AvailableRecruitingNot AvailableFollicular Non-Hodgkin's Lymphoma Refractory1
Not AvailableRecruitingBasic ScienceAbsence of Signs or Symptoms / B-cell Non-Hodgkin's Lymphomas / Chronic, recurrent Lymphocytic Leukemia / Digestive System Signs and Symptoms / Indolent Adult Non-Hodgkin Lymphoma / Recurrent B-Cell Non-Hodgkin Lymphoma / Recurrent Indolent Adult Non-Hodgkin Lymphoma / Recurrent Small Lymphocytic Lymphoma1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
TabletOral100 mg
TabletOral150 mg
Tablet, film coatedOral100 mg/1
Tablet, film coatedOral100 mg
Tablet, film coatedOral150 mg/1
Tablet, film coatedOral150 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6949535No2005-09-272021-04-24Us
US6800620No2004-10-052021-04-24Us
US8980901No2015-03-172025-05-12Us
US9149477No2015-10-062025-05-12Us
US8138195No2012-03-202021-04-24Us
USRE44599No2013-11-122025-07-21Us
US8865730No2014-10-212033-03-05Us
US8637533No2014-01-282021-04-24Us
USRE44638No2013-12-102025-08-05Us
US8492389No2013-07-232021-04-24Us
US9469643No2016-10-182033-09-02Us
US9492449No2016-11-152030-03-11Us

Properties

State
Solid
Experimental Properties
Not 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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Imidazopyrimidines
Sub Class
Purines and purine derivatives
Direct Parent
6-alkylaminopurines
Alternative Parents
Quinazolines / Secondary alkylarylamines / Pyrimidones / Aminopyrimidines and derivatives / Aryl fluorides / Benzene and substituted derivatives / Imidolactams / Vinylogous halides / Heteroaromatic compounds / Imidazoles
show 7 more
Substituents
6-alkylaminopurine / Diazanaphthalene / Quinazoline / Aminopyrimidine / Pyrimidone / Secondary aliphatic/aromatic amine / Aryl fluoride / Aryl halide / Monocyclic benzene moiety / Pyrimidine
show 20 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
organofluorine compound, secondary amino compound, aromatic amine, purines, quinazolines (CHEBI:82701)

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...
Gene Name
AOX1
Uniprot ID
Q06278
Uniprot Name
Aldehyde oxidase
Molecular Weight
147916.735 Da
2. UDP-glucuronosyltransferase 1A4
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
3. 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 un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Backman JT, Filppula AM, Niemi M, Neuvonen PJ: Role of Cytochrome P450 2C8 in Drug Metabolism and Interactions. Pharmacol Rev. 2016 Jan;68(1):168-241. doi: 10.1124/pr.115.011411. [PubMed:26721703]
  2. Lumacraftor Australian Prescribing Information [File]
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 im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
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 un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Idelalisib FDA Label [File]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
Inhibitor
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Drug Interactions & Labeling - FDA [Link]
  2. FDA reports [Link]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
Inhibitor
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 un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
Inhibitor
General Function
Monooxygenase activity
Specific Function
Exhibits low testosterone 6-beta-hydroxylase activity.
Gene Name
CYP3A43
Uniprot ID
Q9HB55
Uniprot Name
Cytochrome P450 3A43
Molecular Weight
57669.21 Da
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
Inhibitor
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 un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 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 fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
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
Uniprot Name
Multidrug resistance protein 1
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, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
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), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da

Drug created on May 08, 2015 13:47 / Updated on November 20, 2018 00:58