Targeting Bruton’s Tyrosine Kinase Across B-Cell Malignancies

Cunha‐Bang, Caspar da; Niemann, Carsten Utoft

doi:10.1007/s40265-018-1003-6

Cited by 37 publications

(19 citation statements)

References 74 publications

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“…Subsequently, to overcome offtarget side effects and the emerging resistances of ibrutinib, some selective second-generation BTK inhibitors were developed. Acalabrutinib, also known as ACP-196, is a novel second-generation BTK inhibitor, which was designed by Acerta Pharma [12]. Similar to ibrutinib, Harrington et al elected a canine model of B-cell NHL to evaluate the pharmacodynamic effects of acalabrutinib in vitro and vivo [13].…”

Section: History Of the Discovery And Characteristics Of Btk Inhibitorsmentioning

confidence: 99%

Inhibitors targeting Bruton’s tyrosine kinase in cancers: drug development advances

et al. 2020

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Bruton’s tyrosine kinase (BTK) inhibitor is a promising novel agent that has potential efficiency in B-cell malignancies. It took approximately 20 years from target discovery to new drug approval. The first-in-class drug ibrutinib creates possibilities for an era of chemotherapy-free management of B-cell malignancies, and it is so popular that gross sales have rapidly grown to more than 230 billion dollars in just 6 years, with annual sales exceeding 80 billion dollars; it also became one of the five top-selling medicines in the world. Numerous clinical trials of BTK inhibitors in cancers were initiated in the last decade, and ~73 trials were intensively announced or updated with extended follow-up data in the most recent 3 years. In this review, we summarized the significant milestones in the preclinical discovery and clinical development of BTK inhibitors to better understand the clinical and commercial potential as well as the directions being taken. Furthermore, it also contributes impactful lessons regarding the discovery and development of other novel therapies.

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Section: History Of the Discovery And Characteristics Of Btk Inhibitorsmentioning

confidence: 99%

Inhibitors targeting Bruton’s tyrosine kinase in cancers: drug development advances

et al. 2020

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“…In a preclinical study, ibrutinib treatment successfully reprogrammed macrophages for increasing CD8+ T cells to assist with tumour control in PC (125). Moreover, the synergistic activity of ibrutinib with ICIs has also been described in preclinical models, including regulating tumour-induced immune tolerance by enhancing the activity of tumour-infiltrating cells and reducing the secretion of immunosuppressive cytokines (126). A recent phase Ib/II study evaluated ibrutinib plus durvalumab, a PD-L1-targeting antibody, in patients with relapsed or refractory solid tumours (127).…”

Section: Bruton Tyrosine Kinasementioning

confidence: 99%

Targeting the Stroma in the Management of Pancreatic Cancer

2021

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Pancreatic cancer (PC) presents extremely aggressive tumours and is associated with poor survival. This is attributed to the unique features of the tumour microenvironment (TME), which is known to create a dense stromal formation and poorly immunogenic condition. In particular, the TME of PC, including the stromal cells and extracellular matrix, plays an essential role in the progression and chemoresistance of PC. Consequently, several promising agents that target key components of the stroma have already been developed and are currently in multiple stages of clinical trials. Therefore, the authors review the latest available evidence on novel stroma-targeting approaches, highlighting the potential impact of the stroma as a key component of the TME in PC.

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“…Ibrutinib is used to treat cGVHD and indolent B-cell malignancies [ 103 ]. A study conducted in an animal model revealed the potential protective effect of Ibrutinib on lung injury, pulmonary inﬂammatory cytokines, and death [ 40 ].…”

Section: The Role Of Btk Inhibitors In the Treatment Of Covid-19mentioning

confidence: 99%

Bruton tyrosine kinase inhibitors as potential therapeutic agents for COVID-19: A review

Kifle¹

2021

Metabolism Open

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Coronavirus disease 2019 (COVID-19) is first detected in December 2019 in Wuhan, China which is a new pandemic caused by SARS-COV-2 that has greatly affected the whole world. Bruton tyrosine kinase (BTK) inhibitors are drugs that are used for the management of cancer, and are being repurposed for COVID-19. BTK regulates macrophage and B cell activation, development, survival, and signaling. Inhibition of BTK has revealed an ameliorative effect on lung injury in patients with severe COVID-19. Thus, this review aimed to summarize evidence regarding the role of Bruton tyrosine kinase inhibitors against COVID-19. To include findings from diverse studies, publications related to BTK inhibitors and Covid-19 were searched from the databases such as SCOPUS, Web of Science, Medline, Google Scholar, PubMed, and Elsevier, using English key terms. Both experimental and clinical studies suggest that targeting excessive host inflammation with a BTK inhibitor is a potential therapeutic strategy in the treatment of patients with severe COVID-19. Currently, BTK inhibitors such as ibrutinib and acalabrutinib have shown a protective effect against pulmonary injury in a small series group of COVID-19 infected patients. Small molecule inhibitors like BTK inhibitors, targeting a wide range of pro-inﬂammatory singling pathways, may a key role in the management of COVID-19.

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Targeting Bruton’s Tyrosine Kinase Across B-Cell Malignancies

Cited by 37 publications

References 74 publications

Inhibitors targeting Bruton’s tyrosine kinase in cancers: drug development advances

Inhibitors targeting Bruton’s tyrosine kinase in cancers: drug development advances

Targeting the Stroma in the Management of Pancreatic Cancer

Bruton tyrosine kinase inhibitors as potential therapeutic agents for COVID-19: A review

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