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Preclinical characterization of pirtobrutinib, a highly selective, noncovalent (reversible) BTK inhibitor.

Author: AbadaPaolo B, AllerstonCharles K, BallardJoshua A, BrandhuberBarbara J, BrownNicholas E, CedervallE Peder, EbataKevin, GomezEliana B, GongXueqian, HansonLauren M, KuKarin S, LippincottIsabel, MoralesTony H, RanderiaHetal S, RosendahlMary S, StephensJennifer, WalgrenRichard A, WuWenjuan

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Overview

Pirtobrutinib, a novel, non-covalent BTK inhibitor, shows high selectivity and potent inhibition of BTK signaling in B-cell lymphoma cell lines, with potential for improved precision and tolerability in treating B-cell malignancies.
Paper Details　
Original Abstract of the Article :
Bruton tyrosine kinase (BTK), a nonreceptor tyrosine kinase, is a major therapeutic target for B-cell-driven malignancies. However, approved covalent BTK inhibitors (cBTKis) are associated with treatment limitations because of off-target side effects, suboptimal oral pharmacology, and development of...See full text at original site
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引用元：
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10651869/

データ提供：米国国立医学図書館（NLM）

Pirtobrutinib: A Promising New Approach to Treating B-Cell Driven Cancers

Bruton tyrosine kinase (BTK) is a key protein involved in the development and growth of certain types of B-cell cancers. This study focuses on pirtobrutinib, a novel BTK inhibitor, and explores its potential as a new treatment for B-cell driven malignancies. The study examines the preclinical profile of pirtobrutinib, highlighting its unique characteristics and potential advantages over existing BTK inhibitors.

Pirtobrutinib: A Unique Approach to Targeting BTK

The study emphasizes that pirtobrutinib is a highly selective, noncovalent (reversible) BTK inhibitor, meaning it binds to BTK without permanently altering its structure. This contrasts with existing BTK inhibitors, which are covalent and can lead to off-target side effects. The study also found that pirtobrutinib effectively inhibits both wild-type BTK and a commonly occurring resistance mutation, C481, suggesting its potential to overcome resistance to existing treatments.

A Potential for Improved Cancer Therapies: The Promise of Pirtobrutinib

This study highlights the promise of pirtobrutinib as a potential new treatment for B-cell driven cancers. The findings suggest that pirtobrutinib might offer a more targeted and effective approach, with the potential for fewer side effects and improved efficacy.

Dr.Camel's Conclusion

This research is like finding a hidden oasis in the vast desert of cancer research. The study reveals the potential of pirtobrutinib as a powerful new weapon in the fight against B-cell driven cancers, offering hope for a more targeted and effective treatment approach.

Date :
  1. Date Completed 2023-08-09
  2. Date Revised 2023-12-13
Further Info :

Pubmed ID

36796019

DOI: Digital Object Identifier

PMC10651869

SNS
PICO Info
in preparation
Languages

English

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