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.[6][7] Ibrutinib also binds to C-terminal Src Kinases. These are off-target receptors for the BTK inhibitor. 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.[8]
It is on the World Health Organization's List of Essential Medicines.[9]
^"Ibrutinib (Imbruvica) Use During Pregnancy". Drugs.com. 3 December 2019. Retrieved 28 March 2020.
^"Prescription medicines: registration of new chemical entities in Australia, 2015". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 10 April 2023.
^"Regulatory Decision Summary for Imbruvica". Drug and Health Products Portal. 4 August 2023. Retrieved 2 April 2024.
^"Imbruvica 140 mg Film-Coated Tablets - Summary of Product Characteristics (SmPC)". (emc). 16 January 2020. Retrieved 28 March 2020.
^Cite error: The named reference UKlabel2016 was invoked but never defined (see the help page).
^ abCite error: The named reference Imbruvica FDA label was invoked but never defined (see the help page).
^ ab"Imbruvica EPAR". European Medicines Agency (EMA). 8 July 2021. Retrieved 14 July 2021.
^Xiao L, Salem JE, Clauss S, Hanley A, Bapat A, Hulsmans M, et al. (December 2020). "Ibrutinib-Mediated Atrial Fibrillation Attributable to Inhibition of C-Terminal Src Kinase". Circulation. 142 (25): 2443–2455. doi:10.1161/CIRCULATIONAHA.120.049210. PMC 9661397. PMID 33092403.
^World Health Organization (2021). World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.
Ibrutinib, sold under the brand name Imbruvica among others, is a small molecule drug that inhibits B-cell proliferation and survival by irreversibly...
adverse effects relative to ibrutinib. In pre-clinical studies, it was shown to be more potent and selective than ibrutinib, the first-in-class BTK inhibitor...
acquire oncology firm Pharmacyclics and its treatment for blood cancers, ibrutinib; AstraZeneca had also been bidding to acquire Pharmacyclics. Under the...
inhibits BTK in a way that is different from the prototypical BTK inhibitor ibrutinib by binding in a different way that avoids a genetic change (mutation at...
well as potential for combination is expected from other drugs such as ibrutinib and idelalisib, both of which were also approved in 2014 to treat CLL...
first line treatments may be offered. As of 2021, BTK inhibitors such as ibrutinib and acalabrutinib are often recommended for first line treatment of CLL...
randomized, active control, open-label trial, comparing zanubrutinib and ibrutinib in participants with MYD88 L265P mutation (MYD88MUT) WM. Participants...
mechanistic step by many covalent inhibitor drugs. Cancer drugs such as ibrutinib, osimertinib, and rociletinib have an acrylamide functional group as a...
including two large global phase 3 clinical trials comparing zanubrutinib to ibrutinib between 2017 and 2023. BeiGene currently conducts global clinical trials...
by CHOP, produced responses in 75% cases. A phase 1 clinical trial of ibrutinib – an inhibitor of Bruton's tyrosine kinase – in 13 patients reported responses...
In January 2019, the US Food and Drug Administration (FDA) approved ibrutinib in combination with obinutuzumab for people with chronic lymphocytic leukemia/small...
CXCR4 WHIM mutations has been associated with clinical resistance to ibrutinib in patients with Waldenström's macroglobulinemia. While CXCR4's expression...
would acquire Pharmacyclics, as well as its lead anti-cancer compound ibrutinib (Imbruvica) for $21 billion. As part of the deal, AbbVie will pay $261...
Two Bruton tyrosine kinase inhibitors (BTKi), one In November 2013, ibrutinib (brand name Imbruvica, Pharmacyclics LLC) and one in October 2017, acalabrutinib...
January 19, 2017, the FDA approved the first ever targeted drug for MZL, ibrutinib. This drug works by inhibiting Bruton's tyrosine kinase (BKT), which is...
Woyach, Jennifer A. (1 October 2018). "The BTK Inhibitor ARQ 531 Targets Ibrutinib-Resistant CLL and Richter Transformation". Cancer Discovery. 8 (10): 1300–1315...
infused back into the donor patient); 3) Bruon's tyrosine kinase inhibitor, ibrutinib, to block the B-cell maturating actions of this kianase; 4) BCL inhibitor...
2018-08-27. Clinical trial number NCT03420183 for "A Study of Cirmtuzumab and Ibrutinib in Patients With B-Cell Lymphoid Malignancies" at ClinicalTrials.gov "1st...
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