Related Experiment Video
Updated: Oct 1, 2025

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
Recent development of BTK-based dual inhibitors in the treatment of cancers
Fansheng Ran1, Yun Liu1, Zhongyuan Xu1
1School of Pharmacy and Jiangsu Province Key Laboratory for Inflammation and Molecular Drug Target, Nantong University, Nantong, 226001, China.
Abstract:
Bruton's tyrosine kinase (BTK) is a promising target in the treatment of various cancers. Despite the early success of BTK inhibitors in the clinic, these single-target drug therapies have limitations in their clinical applications, such as drug resistance. Several alternative strategies have been developed, including the use of dual inhibitors, to maximize the therapeutic potential of anticancer drugs. In this review, we highlight the scientific background and theoretical basis for developing BTK-based dual inhibitors, as well as the status of these agents in preclinical and clinical studies, and discuss further options in this field. We posit that these advances in BTK-based dual inhibitors confirm their feasibility for the treatment of refractory tumors, including those with drug resistance, and provide a framework for future drug design in this field. Accordingly, we anticipate increasingly rapid progress in the development of novel potent dual inhibitors and advanced clinical research on BTK-based dual inhibitors.
Insights
Dual inhibitors targeting Bruton
Area of Science:
- Oncology
- Pharmacology
- Drug Discovery
Background:
- Bruton's tyrosine kinase (BTK) is a key target for cancer therapy.
- Current BTK inhibitors show promise but face challenges like drug resistance.
- Dual inhibitors offer a strategy to overcome limitations of single-target therapies.
Purpose of the Study:
- To review the scientific rationale and development of BTK-based dual inhibitors.
- To summarize the current status of these agents in preclinical and clinical research.
- To discuss future directions for BTK-based dual inhibitor drug design.
Main Methods:
- Literature review of scientific background and theoretical basis for BTK dual inhibitors.
- Analysis of preclinical and clinical study data for BTK-based dual agents.
- Discussion of emerging trends and future research opportunities.
Main Results:
- BTK-based dual inhibitors are a feasible strategy for treating refractory and drug-resistant tumors.
- Advances in this field provide a foundation for future drug development.
- Significant progress is anticipated in novel dual inhibitor design and clinical trials.
Conclusions:
- BTK-based dual inhibitors represent a promising therapeutic approach for challenging cancers.
- Further research and development are expected to yield potent new treatments.
- This strategy holds potential for overcoming drug resistance in various malignancies.
More Related Videos
13:22Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
10:33Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
Published on: October 26, 2015
Related Concept Videos
Targeted Cancer Therapies
There are several types of targeted therapies against...
Inhibition of Cdk Activity
Combination Therapies and Personalized Medicine
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
Tumor Immunotherapy
Treatment Resistant Cancers
The Intrinsic Apoptotic Pathway