Ibrutinib 140mg tablets
Requires a prescription from a doctor or prescriber
Ibrutinib is a small molecule that acts as an irreversible potent inhibitor of Burton's tyrosine kinase.
Official documents, adverse reaction reporting, and safety monitoring
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Official medicine documents
Safety monitoring data
Yellow Card reports
The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
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Suspected adverse reactions reported for Ibrutinib
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Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
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Suspected adverse reactions reported for Ibrutinib
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EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.
1 branded products available
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Imbruvica 140mg tablets
WHO defined daily dose (DDD)
420 mg
Not a recommended dose. The DDD is the assumed average maintenance dose per day for a drug used for its main indication in adults. It is a statistical measure used for research and comparison purposes only.
Source: WHO Collaborating Centre for Drug Statistics Methodology, distributed via NHS dm+d BNF mapping files. Contains public sector information licensed under the Open Government Licence v3.0.
Therapeutically similar medicines
Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
Clinical guidelines and formulary information
British National Formulary
Ibrutinib
Source: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
NICE clinical guidance(14)
Ibrutinib for treating Waldenstrom's macroglobulinaemia (TA795)
Ibrutinib with venetoclax for untreated chronic lymphocytic leukaemia (TA891)
Ibrutinib for treating relapsed or refractory mantle cell lymphoma (TA502)
Ibrutinib for previously treated chronic lymphocytic leukaemia and untreated chronic lymphocytic leukaemia with 17p deletion or TP53 mutation (TA429)
Ibrutinib with rituximab for treating Waldenstrom's macroglobulinaemia (terminated appraisal) (TA608)
Ibrutinib with rituximab for untreated chronic lymphocytic leukaemia (terminated appraisal) (TA703)
Ibrutinib with obinutuzumab for untreated chronic lymphocytic leukaemia and small lymphocytic lymphoma (terminated appraisal) (TA702)
Ibrutinib for untreated chronic lymphocytic leukaemia without a 17p deletion or TP53 mutation (terminated appraisal) (TA452)
Ibrutinib with bendamustine and rituximab for treating relapsed or refractory chronic lymphocytic leukaemia after systemic therapy (terminated appraisal) (TA437)
Acalabrutinib for treating chronic lymphocytic leukaemia (TA689)
Zanubrutinib for treating relapsed or refractory mantle cell lymphoma (TA1081)
Zanubrutinib for treating chronic lymphocytic leukaemia (TA931)
Venetoclax with rituximab for previously treated chronic lymphocytic leukaemia (TA561)
Zanubrutinib for treating Waldenstrom's macroglobulinaemia (TA833)
Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
Check stock at pharmacies and supply information
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Search for this medicine at major UK pharmacy chains. These links open the retailer's own website — results depend on their current online catalogue.
Supply & product information
Official product databases and supply status monitoring
Pharmacy links redirect to the retailer's own search and do not represent real-time stock levels. emc (electronic medicines compendium) is operated by Datapharm Ltd. Shortage information sourced from NHS Specialist Pharmacy Service (SPS), sps.nhs.uk.
Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
Browse tools
SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
81 found
Half-life
4-6 hours
Mechanism
Ibrutinib is an inhibitor of Bruton’s tyrosine kinase (BTK).
Food interactions
4 warnings
Human targets
1 target
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
35 ng/ml
Half-life
4-6 hours
Protein binding
25%
Volume of distribution
000 L
Metabolism
Elimination
7.8%
Clearance
112-159 ml/min
[A7663]
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Ibrutinib was approved by the EMA in October 2014 [L45884] and by Health Canada in November 2014.[L45889] It is currently approved for the treatment of various conditions, such as chronic lymphocytic leukemia (CLL), Waldenström's Macroglobulinemia, and chronic graft versus host disease (cGVHD) in August 2017.[L12228] Notably, ibrutinib became the first FDA-approved cGVHD treatment for children in August 2017.[L43020]
Chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL)
- In the US, it is used in adult patients with or without 17p deletion.
[L42980][L45884]
- In Europe and Canada, it is used as a single agent or combined with [rituximab], [obinutuzumab], or [venetoclax] in previously untreated CLL patients. In patients who have received at least one prior therapy, it is used as a single agent or in combination with [bendamustine] and [rituximab].
[L45884][L45889]
Waldenström's macroglobulinemia
- It is used alone [L42980][L45884][L45889] or with [rituximab].
[L45884][L45889]
- In Europe, it is approved for patients who have received at least one prior therapy or in first-line treatment for patients unsuitable for chemoimmunotherapy.
[L45884]
Chronic graft-versus-host disease (cGVHD)
- In the US, it is approved in patients aged one year and older after the prior failure of one or more lines of systemic therapy.
[L42980]
- In Canada, it is approved in adults with steroid-dependent or refractory cGVHD.
[L45889]
Mantle cell lymphoma (MCL)
- In Europe and Canada, ibrutinib is also indicated to treat relapsed or refractory MCL in adults.
[L45884][L45889]
Marginal zone lymphoma (MZL)
- In Canada, it is approved for adults who require systemic therapy and have received at least one prior anti-CD20-based therapy.
[L45889]
Known interactions with other medications. Always consult a healthcare professional.
Showing 50 of 1125 interactions
[L12228]
Clinical studies for relapsed/refractory CLL in phase I and II showed an approximate 71% of overall response rate.[A32308][A32309]. In the case of relapsed/refractory mantle cell lymphoma, approximately 70% of the tested patients presented a partial or complete response.[A32308][A32310]. 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.[A32308]
How the body processes this drug — absorption, distribution, metabolism, and elimination
[A7663]
The irreversible protein binding of ibrutinib to plasma proteins can account for 97.3% of the administered dose.T148
The metabolism of ibrutinib is mainly performed by CYP3A5 and CYP3A4. and in a minor extent it is seen to be performed by CYP2D6.
[A7663]
[A7663]
[A7663]
Proteins and enzymes this drug interacts with in the body
PMID:19290921
Binding of antigen to the B-cell antigen receptor (BCR) triggers signaling that ultimately leads to B-cell activation .
PMID:19290921
After BCR engagement and activation at the plasma membrane, phosphorylates PLCG2 at several sites, igniting the downstream signaling pathway through calcium mobilization, followed by activation of the protein kinase C (PKC) family members .
PMID:11606584
PLCG2 phosphorylation is performed in close cooperation with the adapter protein B-cell linker protein BLNK .
PMID:11606584
BTK acts as a platform to bring together a diverse array of signaling proteins and is implicated in cytokine receptor signaling pathways .
PMID:16517732 PMID:17932028
Plays an important role in the function of immune cells of innate as well as adaptive immunity, as a component of the Toll-like receptors (TLR) pathway .
PMID:16517732
The TLR pathway acts as a primary surveillance system for the detection of pathogens and are crucial to the activation of host defense .
PMID:16517732
Especially, is a critical molecule in regulating TLR9 activation in splenic B-cells .
PMID:16517732 PMID:17932028
Within the TLR pathway, induces tyrosine phosphorylation of TIRAP which leads to TIRAP degradation .
PMID:16415872
BTK also plays a critical role in transcription regulation .
PMID:19290921
Induces the activity of NF-kappa-B, which is involved in regulating the expression of hundreds of genes .
PMID:19290921
BTK is involved on the signaling pathway linking TLR8 and TLR9 to NF-kappa-B .
PMID:19290921
Acts as an activator of NLRP3 inflammasome assembly by mediating phosphorylation of NLRP3 .
PMID:34554188
Transiently phosphorylates transcription factor GTF2I on tyrosine residues in response to BCR .
PMID:9012831
GTF2I then translocates to the nucleus to bind regulatory enhancer elements to modulate gene expression .
PMID:9012831
ARID3A and NFAT are other transcriptional target of BTK .
PMID:16738337
BTK is required for the formation of functional ARID3A DNA-binding complexes .
PMID:16738337
There is however no evidence that BTK itself binds directly to DNA .
PMID:16738337
BTK has a dual role in the regulation of apoptosis .
PMID:9751072
Plays a role in STING1-mediated induction of type I interferon (IFN) response by phosphorylating DDX41 PMID:25704810
Enzymes involved in drug metabolism — important for understanding drug interactions
Proteins that carry this drug through the body
PMID:19021548
Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity).
Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity).
Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli .
PMID:6234017
Does not prevent iron uptake by the bacterial siderophore aerobactin PMID:6234017
Appears to function in modulating the activity of the immune system during the acute-phase reaction
ATC L01EL01
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Ibrutinib
Additional database identifiers
Drugs Product Database (DPD)
22542
ChemSpider
26637187
BindingDB
50357312
PDB
1E8
ZINC
ZINC000035328014
HUGO Gene Nomenclature Committee (HGNC)
HGNC:1133
GenAtlas
BTK
GeneCards
BTK
GenBank Gene Database
X58957
GenBank Protein Database
312467
Guide to Pharmacology
1948
UniProt Accession
BTK_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2637
GenAtlas
CYP3A4
GeneCards
CYP3A4
GenBank Gene Database
M18907
Guide to Pharmacology
1337
UniProt Accession
CP3A4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2638
GenAtlas
CYP3A5
GeneCards
CYP3A5
GenBank Gene Database
J04813
GenBank Protein Database
181346
Guide to Pharmacology
1338
UniProt Accession
CP3A5_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2625
GenAtlas
CYP2D6
GeneCards
CYP2D6
GenBank Gene Database
M20403
GenBank Protein Database
181350
Guide to Pharmacology
1329
UniProt Accession
CP2D6_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:399
GenAtlas
ALB
GeneCards
ALB
GenBank Gene Database
V00494
GenBank Protein Database
28590
UniProt Accession
ALBU_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:8498
GenAtlas
ORM1
GeneCards
ORM1
GenBank Gene Database
X02544
GenBank Protein Database
757907
UniProt Accession
A1AG1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:8499
GeneCards
ORM2
GenBank Gene Database
BC015964
GenBank Protein Database
16359000
UniProt Accession
A1AG2_HUMAN
Patent information
43 active patents
Source: DrugBank · CC BY-NC 4.0. Patent data sourced from national patent offices. Expiry dates may not reflect extensions, regulatory exclusivity periods, or legal challenges.
DrugBank citations
If you use DrugBank data in your research, please cite the following publications: