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3yr
A phase 1, open-label, randomized drug-drug interaction study of zanubrutinib with moderate or strong CYP3A inhibitors in patients with B-cell malignancies - PubMed

A phase 1, open-label, randomized drug-drug interaction study of zanubrutinib with moderate or strong CYP3A inhibitors in patients with B-cell malignancies - PubMed

Source : https://pubmed.ncbi.nlm.nih.gov/36480811/

BTK inhibitor exposure increases significantly when coadministered with CYP3A inhibitors, which may lead to dose-related toxicities. This study explored the pharmacokinetics, efficacy, and safety of zanubrutinib when coadministered with moderate...



Conclusions: This study supports current United States Prescribing Information dose recommendations for the coadministration of reduced-dose zanubrutinib with moderate or strong CYP3A inhibitors and confirms the favorable efficacy and safety profile of zanubrutinib.

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3yr
A Preview of the 2022 American Society of Hematology Annual Meeting

The American Society of Hematology (ASH) Annual Meeting & Exposition is being held Dec. 10 to 13, 2022, in New Orleans. The event is being held in person and will be broadcast virtually.

Click to access a preview into the event and program highlights that caught the attention of our team of analysts.

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3yr
Design, synthesis and biological evaluation of novel pyrazolo-pyrimidin-amines as potent and selective BTK inhibitors

Design, synthesis and biological evaluation of novel pyrazolo-pyrimidin-amines as potent and selective BTK inhibitors

Source : https://www.sciencedirect.com/science/article/abs/pii/S0045206822006447?via=ihub

Author links open overlay panel Darshan Joshi a b Rajesh Bahekar Person a Envelope Show more * Structural optimization of first generation BTK inhibitors. * Bicyclic amine linkers and aromatic...

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Relevance: 14b was found to be potent, orally bioavailable and irreversible BTK inhibitor. 14b displayed robust efficacy in CIA and TMD8 xenograft models.


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3yr
Selective Inhibition of Bruton's Tyrosine Kinase by a Designed Covalent Ligand Leads to Potent Therapeutic Efficacy in Blood Cancers Relative to Clinically Used Inhibitors - PubMed

Selective Inhibition of Bruton's Tyrosine Kinase by a Designed Covalent Ligand Leads to Potent Therapeutic Efficacy in Blood Cancers Relative to Clinically Used Inhibitors - PubMed

Source : https://pubmed.ncbi.nlm.nih.gov/36407952/

Bruton's tyrosine kinase (BTK) is a member of the TEC-family kinases and crucial for the proliferation and differentiation of B-cells. We evaluated the therapeutic potential of a covalent inhibitor (JS25)...


Conclusions: JS25 was faster and more effective in decreasing tumor burden, producing superior therapeutic effects compared to ibrutinib. We expect JS25 to become therapeutically relevant as a BTK inhibitor and to find applications in the treatment of hematological cancers and other pathologies with unmet clinical treatment.


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3yr
Ibrutinib suppresses the activation of neutrophils and macrophages and exerts therapeutic effect on acute peritonitis induced by zymosan

Ibrutinib suppresses the activation of neutrophils and macrophages and exerts therapeutic effect on acute peritonitis induced by zymosan

Source : https://www.sciencedirect.com/science/article/pii/S1567576922009547?via=ihub

Ibrutinib inhibits the expression and secretion of inflammatory cytokines and chemokines in macrophages induced by multiple TLR agonists. * Ibrutinib selectively suppresses the activation, superoxide release, and calcium influx of...

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Conclusions: Conclusions/Relevance: Collectively, Ibrutinib can significantly inhibit the activation of neutrophils and macrophages by inhibiting BTK-PLCγ2-PKC signaling pathway, and has great potential to be developed into therapeutic drug for acute inflammatory diseases.