Ibrutinib
Identification
- Summary
Ibrutinib is an antineoplastic agent used to treat chronic lymphocytic leukemia, mantle cell lymphoma, and Waldenstrom's Macroglobulinemia.
- Brand Names
- Imbruvica
- Generic Name
- Ibrutinib
- DrugBank Accession Number
- DB09053
- Background
Ibrutinib is a small molecule that acts as an irreversible potent inhibitor of Burton's tyrosine kinase. It is designated as a targeted covalent drug and it presents a very promising activity in B cell malignancies.4 Ibrutinib was developed by Pharmacyclics Inc and in November 2013 was FDA-approved for the treatment of mantle cell lymphoma. Later, in February 2014, ibrutinib was approved for the treatment of chronic lymphocytic leukemia and it is also indicated for the treatment of patients with Waldenström's Macroglobulinemia.13 Ibrutinib has also been approved by the EMA for the treatment of chronic lymphocytic leukemia and mantle cell lymphoma.4 Ibrutinib was approved for use in chronic graft versus host disease in August 2017 12.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Ibrutinib (DB09053)
- Weight
- Average: 440.507
Monoisotopic: 440.196074037 - Chemical Formula
- C25H24N6O2
- Synonyms
- 1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one
- Ibrutinib
- External IDs
- CRA-032765
- PC-32765
- PCI 32765
- PCI-32765
- PCI-32765-00
Pharmacology
- Indication
Ibrutinib acquired an accelerated approval for the treatment of mantle cell lymphoma who have received at least one prior therapy.Label Mantle cell lymphoma (MCL) is a B-cell non-Hodgkin lymphoma that develops in the outer edge of a lymph node. MCL is usually diagnosed at late stages and it is easily spread into bone marrow, spleen, liver and gastrointestinal tract.14
Ibrutinib is indicated for the treatment of chronic lymphocytic leukemia (CLL) who have at least one prior therapy.Label CLL is a type of cancer caused by an overproduction of lymphocytes by the bone marrow. Some of the symptoms include swollen lymph nodes and tiredness.15
Ibrutinib is indicated for the treatment of chronic lymphocytic leukemia (CLL) with 17p deletion.Label CLL with 17p is a type of leukemia in which a deletion in 17p disrupts the tumor suppressor p53 by deleting one allele of the TP53 gene. The remaining allele is mainly inactivated and thus, this type of leukemia is unresponsive to p53-dependent treatments.5
Ibrutinib is indicated for the treatment of patients with Waldenstrom's Macroglobulinemia (WM).Label WM, also called lymphoplasmacytic lymphoma, is a type of non-Hodgkin lymphoma in which the cancer cells make large amounts of macroglobulin. The macroglobulin is a monoclonal protein that corresponds to the type of IgM antibodies and the unrestricted formation of this protein causes typical symptoms such as excessive bleeding and effects in vision and nervous system.16
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
In vitro studies have shown an induction of CLL cell apoptosis even in presence of prosurvival factors. It has also been reported an inhibition of CLL cell survival and proliferation as well as an impaired in cell migration and a reduction in the secretion of chemokines such as CCL3 and CCL4. The latter effect has been shown to produce regression in xenograft mouse models.6
Clinical studies for relapsed/refractory CLL in phase I and II showed an approximate 71% of overall response rate.7,8. In the case of relapsed/refractory mantle cell lymphoma, approximately 70% of the tested patients presented a partial or complete response.7,9. In clinical trials for relapsed/refractory diffuse large B-cell lymphoma, a partial response was found in between 15-20% of the patients studied; while for patients with relapsed/refractory Waldenstrom's macroglobulinemia, a partial response was observed in over 75% of the patients tested. Finally, for patients with relapsed/refractory follicular lymphoma, a partial to complete response was obtained in approximately 54% of the patients.7
- Mechanism of action
Ibrutinib is an inhibitor of Bruton’s tyrosine kinase (BTK). It forms a covalent bond with a cysteine residue in the active site of BTK (Cys481), leading to its inhibition. The inhibition of BTK plays a role in the B-cell receptor signaling and thus, the presence of ibrutinib prevents the phosphorylation of downstream substrates such as PLC-γ.6
Target Actions Organism ATyrosine-protein kinase BTK inhibitorHumans - Absorption
Ibrutinib is rapidly absorbed after oral administration and it presents a Cmax, tmax and AUC of approximately 35 ng/ml, 1-2 hour and 953 mg.h/ml respectively.11
- Volume of distribution
The volume of distribution at steady-state of ibrutinib is in approximately 10,000 L.11
- Protein binding
Irreversible plasma protein binding increases gradually over time and reaches 25% of the administered dose 8 hours after initial administration. From the plasma proteins, ibrutinib has been shown to be mainly bound to albumin and to bind to α1 AGP.3 The irreversible protein binding of ibrutinib to plasma proteins can account for 97.3% of the administered dose.11
- Metabolism
Three metabolic pathways have been identified according to the possible metabolites. These pathways are the hydroxylation of the phenyl group (M35), the opening of the piperidine with a reduction of the primary alcohol (M34) and the oxidation to a carboxylic acid and epoxidation of the ethylene followed by a hydrolysis to the formation of dihydrodiol (PCI-45227). The latter metabolite presents also 15 times lower inhibitory activity against BTK. The metabolism of ibrutinib is mainly performed by CYP3A5 and CYP3A4. and in a minor extent it is seen to be performed by CYP2D6.3
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- Route of elimination
The cumulative excretion of ibrutinib in urine is of about 7.8% of the administered dose and most of this excretion is found during the first 24 hours after administration. In feces, the cumulative excretion accounts for 80% of the administered dose and the excretion occurs within 48 hours of the initial administration. The total excretion of ibrutinib during the first 168 hours after initial administration accounts for 88.5% of the administered dose.3
- Half-life
The elimination half-life of ibrutinib is of approximately 4-6 hours.11
- Clearance
In patients with normal renal function, the clearance rate is in the range of 112-159 ml/min.3
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Ibrutinib was not showed to present a mutagenic potential in bacterial assays, nor clastogenic in chromosome aberration assays in mammalian cells or in bone marrow micronucleus assays in mice. Carcinogenicity or effects on fertility have not been determined.Label
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbaloparatide The therapeutic efficacy of Abaloparatide can be decreased when used in combination with Ibrutinib. Abametapir The serum concentration of Ibrutinib can be increased when it is combined with Abametapir. Abatacept The metabolism of Ibrutinib can be increased when combined with Abatacept. Abciximab The risk or severity of bleeding and hemorrhage can be increased when Ibrutinib is combined with Abciximab. Abiraterone The metabolism of Ibrutinib can be decreased when combined with Abiraterone. Acalabrutinib The metabolism of Ibrutinib can be decreased when combined with Acalabrutinib. Acebutolol The metabolism of Ibrutinib can be decreased when combined with Acebutolol. Acenocoumarol The risk or severity of bleeding and hemorrhage can be increased when Ibrutinib is combined with Acenocoumarol. Acetaminophen The metabolism of Ibrutinib can be decreased when combined with Acetaminophen. Acetazolamide The metabolism of Ibrutinib can be decreased when combined with Acetazolamide. 
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- Avoid grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of ibrutinib.
- Avoid St. John's Wort. This herb induces CYP3A4 and may reduce the serum concentration of ibrutinib.
- Take at the same time every day.
- Take with a full glass of water.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Imbruvica Tablet, film coated 560 mg/1 Oral Pharmacyclics LLC 2018-02-16 Not applicable US 
Imbruvica Tablet, film coated 140 mg Oral Janssen Cilag International Nv 2021-02-10 Not applicable EU 
Imbruvica Tablet, film coated 560 mg Oral Janssen Cilag International Nv 2021-02-11 Not applicable EU Imbruvica Tablet 560 mg Oral Janssen Pharmaceuticals Not applicable Not applicable Canada 
Imbruvica Tablet, film coated 140 mg/1 Oral Pharmacyclics LLC 2018-02-16 Not applicable US Imbruvica Capsule 140 mg Oral Janssen Cilag International Nv 2016-09-08 Not applicable EU Imbruvica Tablet 140 mg Oral Janssen Pharmaceuticals Not applicable Not applicable Canada Imbruvica Tablet, film coated 280 mg Oral Janssen Cilag International Nv 2021-02-10 Not applicable EU Imbruvica Tablet, film coated 420 mg/1 Oral Pharmacyclics LLC 2018-02-16 Not applicable US Imbruvica Tablet 420 mg Oral Janssen Pharmaceuticals Not applicable Not applicable Canada
Categories
- ATC Codes
- L01XE27 — Ibrutinib
- Drug Categories
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- Cancer immunotherapy
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 Substrates
- Immunosuppressive Agents
- Immunotherapy
- Kinase Inhibitor
- Myelosuppressive Agents
- Protein Kinase Inhibitors
- Tyrosine Kinase Inhibitors
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as diphenylethers. These are aromatic compounds containing two benzene rings linked to each other through an ether group.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Diphenylethers
- Direct Parent
- Diphenylethers
- Alternative Parents
- Diarylethers / Phenylpyrazoles / Pyrazolo[3,4-d]pyrimidines / N-acylpiperidines / Phenol ethers / Phenoxy compounds / Aminopyrimidines and derivatives / Imidolactams / Heteroaromatic compounds / Tertiary carboxylic acid amides show 8 more
- Substituents
- Acrylic acid or derivatives / Amine / Amino acid or derivatives / Aminopyrimidine / Aromatic heteropolycyclic compound / Azacycle / Azole / Carbonyl group / Carboxamide group / Carboxylic acid derivative show 24 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- aromatic ether, N-acylpiperidine, aromatic amine, pyrazolopyrimidine, acrylamides (CHEBI:76612)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 1X70OSD4VX
- CAS number
- 936563-96-1
- InChI Key
- XYFPWWZEPKGCCK-GOSISDBHSA-N
- InChI
- InChI=1S/C25H24N6O2/c1-2-21(32)30-14-6-7-18(15-30)31-25-22(24(26)27-16-28-25)23(29-31)17-10-12-20(13-11-17)33-19-8-4-3-5-9-19/h2-5,8-13,16,18H,1,6-7,14-15H2,(H2,26,27,28)/t18-/m1/s1
- IUPAC Name
- 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one
- SMILES
- NC1=NC=NC2=C1C(=NN2[C@@H]1CCCN(C1)C(=O)C=C)C1=CC=C(OC2=CC=CC=C2)C=C1
References
- General References
- Bagcchi S: Ibrutinib in pretreated Waldenstrom's macroglobulinaemia. Lancet Oncol. 2015 May;16(5):e204. doi: 10.1016/S1470-2045(15)70185-3. Epub 2015 Apr 16. [Article]
- Kim ES, Dhillon S: Ibrutinib: a review of its use in patients with mantle cell lymphoma or chronic lymphocytic leukaemia. Drugs. 2015 May;75(7):769-76. doi: 10.1007/s40265-015-0380-3. [Article]
- Scheers E, Leclercq L, de Jong J, Bode N, Bockx M, Laenen A, Cuyckens F, Skee D, Murphy J, Sukbuntherng J, Mannens G: Absorption, metabolism, and excretion of oral (1)(4)C radiolabeled ibrutinib: an open-label, phase I, single-dose study in healthy men. Drug Metab Dispos. 2015 Feb;43(2):289-97. doi: 10.1124/dmd.114.060061. Epub 2014 Dec 8. [Article]
- Berglof A, Hamasy A, Meinke S, Palma M, Krstic A, Mansson R, Kimby E, Osterborg A, Smith CI: Targets for Ibrutinib Beyond B Cell Malignancies. Scand J Immunol. 2015 Sep;82(3):208-17. doi: 10.1111/sji.12333. [Article]
- Sellner L, Denzinger S, Dietrich S, Glimm H, Merkel O, Dreger P, Zenz T: What do we do with chronic lymphocytic leukemia with 17p deletion? Curr Hematol Malig Rep. 2013 Mar;8(1):81-90. doi: 10.1007/s11899-012-0143-0. [Article]
- Davids MS, Brown JR: Ibrutinib: a first in class covalent inhibitor of Bruton's tyrosine kinase. Future Oncol. 2014 May;10(6):957-67. doi: 10.2217/fon.14.51. [Article]
- Advani RH, Buggy JJ, Sharman JP, Smith SM, Boyd TE, Grant B, Kolibaba KS, Furman RR, Rodriguez S, Chang BY, Sukbuntherng J, Izumi R, Hamdy A, Hedrick E, Fowler NH: Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765) has significant activity in patients with relapsed/refractory B-cell malignancies. J Clin Oncol. 2013 Jan 1;31(1):88-94. doi: 10.1200/JCO.2012.42.7906. Epub 2012 Oct 8. [Article]
- Byrd JC, Furman RR, Coutre SE, Flinn IW, Burger JA, Blum KA, Grant B, Sharman JP, Coleman M, Wierda WG, Jones JA, Zhao W, Heerema NA, Johnson AJ, Sukbuntherng J, Chang BY, Clow F, Hedrick E, Buggy JJ, James DF, O'Brien S: Targeting BTK with ibrutinib in relapsed chronic lymphocytic leukemia. N Engl J Med. 2013 Jul 4;369(1):32-42. doi: 10.1056/NEJMoa1215637. Epub 2013 Jun 19. [Article]
- Wang ML, Rule S, Martin P, Goy A, Auer R, Kahl BS, Jurczak W, Advani RH, Romaguera JE, Williams ME, Barrientos JC, Chmielowska E, Radford J, Stilgenbauer S, Dreyling M, Jedrzejczak WW, Johnson P, Spurgeon SE, Li L, Zhang L, Newberry K, Ou Z, Cheng N, Fang B, McGreivy J, Clow F, Buggy JJ, Chang BY, Beaupre DM, Kunkel LA, Blum KA: Targeting BTK with ibrutinib in relapsed or refractory mantle-cell lymphoma. N Engl J Med. 2013 Aug 8;369(6):507-16. doi: 10.1056/NEJMoa1306220. Epub 2013 Jun 19. [Article]
- Authors unspecified: Ibrutinib. Aust Prescr. 2015 Oct;38(5):178-80. Epub 2015 Jun 15. [Article]
- Bronson J., Black A., Dhar M., Ellsworth B. and Merritt R. (2014). Annual reports in medicinal chemistry. Elsevier.
- FDA: Ibrutinib cGVHD approval [Link]
- FDA approved drugs [Link]
- Canadian cancer society [Link]
- National Cancer Institute [Link]
- American Cancer Society [Link]
- External Links
- KEGG Drug
- D10223
- PubChem Compound
- 24821094
- PubChem Substance
- 310264995
- ChemSpider
- 26637187
- BindingDB
- 50357312
- 1442981
- ChEBI
- 76612
- ChEMBL
- CHEMBL1873475
- ZINC
- ZINC000035328014
- PharmGKB
- PA166121346
- PDBe Ligand
- 1E8
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Ibrutinib
- PDB Entries
- 4ifg / 4rz7 / 5p9i / 5yu9 / 6l8l / 6yg2 / 6yz4
- FDA label
- Download (579 KB)
- MSDS
- Download (24.9 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Waldenström's Macroglobulinemia (WM) 1 4 Enrolling by Invitation Treatment B Cell Leukemias / B Cell Lymphoma (BCL) / Graft Versus Host Disease (cGvHD) / Non-Hodgkin's Lymphoma (NHL) / Tumors, Solid 1 4 Recruiting Other B-Cell Chronic Lymphocytic Leukemia (B-CLL) / Mantle Cell Lymphoma (MCL) 1 3 Active Not Recruiting Treatment Anemia / Chronic Lymphocytic Leukemia (CLL) / Small Lymphocytic Lymphoma 1 3 Active Not Recruiting Treatment B-Cell Chronic Lymphocytic Leukemia (B-CLL) 1 3 Active Not Recruiting Treatment Chronic Lymphocytic Leukemia (CLL) 3 3 Active Not Recruiting Treatment Chronic Lymphocytic Leukemia (CLL) / Small Lymphocytic Lymphoma 3 3 Active Not Recruiting Treatment Follicular Lymphoma ( FL) 1 3 Active Not Recruiting Treatment Graft Versus Host Disease (cGvHD) 2 3 Active Not Recruiting Treatment Malignant Lymphomas 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule Oral Capsule Oral 140 mg/1 Capsule Oral 70 mg/1 Tablet Oral 140 mg Tablet Oral 280 mg Tablet Oral 420 mg Tablet Oral 560 mg Tablet, film coated Oral 140 mg/1 Tablet, film coated Oral 140 MG Tablet, film coated Oral 280 mg/1 Tablet, film coated Oral 280 MG Tablet, film coated Oral 420 mg/1 Tablet, film coated Oral 420 MG Tablet, film coated Oral 560 MG Tablet, film coated Oral 560 mg/1 Capsule, coated Oral 140 mg Capsule Oral 140 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8476284 No 2013-07-02 2026-12-28 US US8703780 No 2014-04-22 2026-12-28 US US8754090 No 2014-06-17 2031-06-03 US US8497277 No 2013-07-30 2026-12-28 US US9125889 No 2015-09-08 2031-06-03 US US8999999 No 2015-04-07 2031-06-03 US US8697711 No 2014-04-15 2026-12-28 US US8754091 No 2014-06-17 2026-12-28 US US9181257 No 2015-11-10 2026-12-28 US US8957079 No 2015-02-17 2026-12-28 US US8008309 No 2011-08-30 2026-12-28 US US8735403 No 2014-05-27 2026-12-28 US US9296753 No 2016-03-29 2033-10-30 US US7514444 No 2009-04-07 2026-12-28 US US9540382 No 2017-01-10 2033-08-18 US US8952015 No 2015-02-10 2026-12-28 US US9725455 No 2017-08-08 2033-06-03 US US9713617 No 2017-07-25 2033-06-03 US US9795604 No 2017-10-24 2034-10-24 US US9801883 No 2017-10-31 2031-06-03 US US9801881 No 2017-10-31 2031-06-03 US US9814721 No 2017-11-14 2031-06-03 US US8563563 No 2013-10-22 2027-04-26 US US9655857 No 2017-05-23 2036-03-03 US US10004746 No 2018-06-26 2031-06-03 US US10016435 No 2018-07-10 2031-06-03 US US10010507 No 2018-07-03 2036-03-03 US US10106548 No 2018-10-23 2033-06-03 US US10125140 No 2018-11-13 2033-06-03 US US10213386 No 2019-02-26 2036-03-03 US US10294232 No 2019-05-21 2033-06-03 US US10294231 No 2019-05-21 2033-06-03 US US10463668 No 2019-11-05 2034-10-24 US US10478439 No 2019-11-19 2031-06-03 US US10653696 No 2020-05-19 2031-06-03 US US10695350 No 2020-06-30 2034-10-24 US US10752634 No 2020-08-25 2033-06-03 US US10751342 No 2020-08-25 2031-06-03 US US10828259 No 2020-11-10 2036-03-03 US US10961251 No 2021-03-30 2033-06-03 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 149-158ºC FDA Imbruvica review. (2013) water solubility 0.003 mg/ml FDA Imbruvica review. (2013) logP 3.97 FDA Imbruvica review. (2013) pKa 3.74 FDA Imbruvica review. (2013) - Predicted Properties
Property Value Source Water Solubility 0.0203 mg/mL ALOGPS logP 2.76 ALOGPS logP 3.63 ChemAxon logS -4.3 ALOGPS pKa (Strongest Acidic) 19.7 ChemAxon pKa (Strongest Basic) 6.58 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 5 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 99.16 Å2 ChemAxon Rotatable Bond Count 5 ChemAxon Refractivity 138.07 m3·mol-1 ChemAxon Polarizability 47.84 Å3 ChemAxon Number of Rings 5 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Protein tyrosine kinase activity
- Specific Function
- Non-receptor tyrosine kinase indispensable for B lymphocyte development, differentiation and signaling. Binding of antigen to the B-cell antigen receptor (BCR) triggers signaling that ultimately le...
- Gene Name
- BTK
- Uniprot ID
- Q06187
- Uniprot Name
- Tyrosine-protein kinase BTK
- Molecular Weight
- 76280.71 Da
References
- Kim ES, Dhillon S: Ibrutinib: a review of its use in patients with mantle cell lymphoma or chronic lymphocytic leukaemia. Drugs. 2015 May;75(7):769-76. doi: 10.1007/s40265-015-0380-3. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
- Scheers E, Leclercq L, de Jong J, Bode N, Bockx M, Laenen A, Cuyckens F, Skee D, Murphy J, Sukbuntherng J, Mannens G: Absorption, metabolism, and excretion of oral (1)(4)C radiolabeled ibrutinib: an open-label, phase I, single-dose study in healthy men. Drug Metab Dispos. 2015 Feb;43(2):289-97. doi: 10.1124/dmd.114.060061. Epub 2014 Dec 8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Scheers E, Leclercq L, de Jong J, Bode N, Bockx M, Laenen A, Cuyckens F, Skee D, Murphy J, Sukbuntherng J, Mannens G: Absorption, metabolism, and excretion of oral (1)(4)C radiolabeled ibrutinib: an open-label, phase I, single-dose study in healthy men. Drug Metab Dispos. 2015 Feb;43(2):289-97. doi: 10.1124/dmd.114.060061. Epub 2014 Dec 8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Scheers E, Leclercq L, de Jong J, Bode N, Bockx M, Laenen A, Cuyckens F, Skee D, Murphy J, Sukbuntherng J, Mannens G: Absorption, metabolism, and excretion of oral (1)(4)C radiolabeled ibrutinib: an open-label, phase I, single-dose study in healthy men. Drug Metab Dispos. 2015 Feb;43(2):289-97. doi: 10.1124/dmd.114.060061. Epub 2014 Dec 8. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Scheers E, Leclercq L, de Jong J, Bode N, Bockx M, Laenen A, Cuyckens F, Skee D, Murphy J, Sukbuntherng J, Mannens G: Absorption, metabolism, and excretion of oral (1)(4)C radiolabeled ibrutinib: an open-label, phase I, single-dose study in healthy men. Drug Metab Dispos. 2015 Feb;43(2):289-97. doi: 10.1124/dmd.114.060061. Epub 2014 Dec 8. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Not Available
- Specific Function
- Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
Components:
References
- Scheers E, Leclercq L, de Jong J, Bode N, Bockx M, Laenen A, Cuyckens F, Skee D, Murphy J, Sukbuntherng J, Mannens G: Absorption, metabolism, and excretion of oral (1)(4)C radiolabeled ibrutinib: an open-label, phase I, single-dose study in healthy men. Drug Metab Dispos. 2015 Feb;43(2):289-97. doi: 10.1124/dmd.114.060061. Epub 2014 Dec 8. [Article]
Drug created on May 07, 2015 19:33 / Updated on October 19, 2021 07:39