ibrutinib
Sign in to saveAlso known as Imbruvica®, PCI-32765, PCI 32765, PCI32765, 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, sold under the brand name Imbruvica among others, is a small molecule drug that inhibits B-cell proliferation and survival by irreversibly binding the protein Bruton's tyrosine kinase (BTK). Blocking BTK inhibits the B-cell receptor pathway, which is often aberrantly active in B cell cancers. Ibrutinib is therefore used to treat such cancers, including mantle cell lymphoma, chronic lymphocytic leukemia, and Waldenström's macroglobulinemia. Ibrutinib also binds to C-terminal Src Kinases, which are off-target receptors for the BTK inhibitor. This binding inhibits the kinase from promo
Key facts
- Drug.image
- Ibrutinib.svg
- Drug.image_class
- skin-invert-image
- Drug.width
- 200
- Drug.tradename
- Imbruvica, others
- Drug.MedlinePlus
- a614007
- Drug.DailyMedID
- Ibrutinib
- Drug.pregnancy_AU
- D
- Drug.routes_of_administration
- By mouth
- Drug.ATC_prefix
- L01
- Drug.ATC_suffix
- EL01
- Drug.legal_AU
- S4
- Drug.legal_CA
- Rx-only
- Drug.legal_UK
- POM
- Drug.legal_US
- Rx-only
- Drug.legal_EU
- Rx-only
- Drug.legal_status
- Rx-only
- Drug.protein_bound
- 97.3%
- Drug.metabolism
- Hepatic (CYP3A & CYP2D6)
via Wikipedia infobox
Wikidata facts
- Has part
- carbon
- Mass
- 440.196
- Has use
- medication
Show 9 more facts
- medical condition treated
- diffuse large B-cell lymphoma
- chemical formula
- C₂₅H₂₄N₆O₂
- Commons category
- Ibrutinib
- isomeric SMILES
- C=CC(=O)N1CCC[C@H](C1)N2C3=C(C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=NC=N3)N
- canonical SMILES
- C=CC(=O)N1CCCC(C1)N2C3=C(C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=NC=N3)N
- World Health Organisation international non-proprietary name
- ibrutinib
- subject has role
- protein kinase inhibitors
- physically interacts with
- Bruton's tyrosine kinase
- significant drug interaction
- idelalisib
via Wikidata · CC0
~9 min read
Encyclopedic overview
10 sectionsContents
- Medical uses
- Adverse effects
- Pharmacology
- Mechanism
- History
- Society and culture
- Economics
- References
- Further reading
- External links
Ibrutinib, sold under the brand name Imbruvica among others, is a small molecule drug that inhibits B-cell proliferation and survival by irreversibly binding the protein Bruton's tyrosine kinase (BTK). Blocking BTK inhibits the B-cell receptor pathway, which is often aberrantly active in B cell cancers. Ibrutinib is therefore used to treat such cancers, including mantle cell lymphoma, chronic lymphocytic leukemia, and Waldenström's macroglobulinemia. Ibrutinib also binds to C-terminal Src Kinases, which are off-target receptors for the BTK inhibitor. This binding inhibits the kinase from promoting cell differentiation and growth. Ibrutinib binds to these receptors and inhibits the kinase from promoting cell differentiation and growth. This leads to many different side effects like left atrial enlargement and atrial fibrillation during the treatment of Chronic Lymphocytic Leukemia.
It is on the World Health Organization's List of Essential Medicines.
Excerpted from Wikipedia’s “ibrutinib” article, available under the CC BY-SA 4.0 licence.