3 Key Takeaways
Plain English Summary- 01Core Finding
We cover drug platforms, new targeting approaches, the expanding target spectrum, approvals and clinical trends.
- 02Study Evidence
Tested in a observational cohort study at the real-world cohort stage.
- 03Practical Meaning
Observational cohort findings reveal real-world links, though lifestyle or unmeasured factors cannot be fully ruled out without an RCT.
What This Means for You
Nevertheless, development remains highly concentrated around a small set of blockbuster kinase targets, such as EGFR. We also examine the features associated with successful kinase-targeting agents and causes of agent discontinuations and regulatory withdrawal.
The Discovery
In the past 25 years, kinase drug discovery has grown into one of the most thriving areas in pharmaceutical research and development. What began as a field dominated by ATP-competitive small molecules has diversified into a broad therapeutic landscape that includes allosteric and covalent inhibitors, activators, proximity-induced modulators, targeted protein degraders and antibody-based therapies, with more than 150 regulatory approvals so far worldwide. In this Review, we provide a comprehensive analysis of the current kinase therapeutic landscape, including more than 2,100 kinase-targeting agents that have entered clinical development in more than 23,000 clinical trials. We cover drug platforms, new targeting approaches, the expanding target spectrum, approvals and clinical trends. Nearly half of the canonical human protein kinases have at least one clinical-stage agent, placing kinases among the most intensively explored drug target classes.
How It Works, Simply
This pharmacology research focuses on antibodies. Researchers evaluated it using an observational cohort study at the real-world cohort stage of medical research.
3 Key Takeaways
Clinical Takeaways- 01Core Finding
We cover drug platforms, new targeting approaches, the expanding target spectrum, approvals and clinical trends.
- 02Study Evidence
Tested in a observational cohort study at the real-world cohort stage.
- 03Practical Meaning
Observational cohort findings reveal real-world links, though lifestyle or unmeasured factors cannot be fully ruled out without an RCT.
Biological Mechanism & Study Design
Study Design & Cohort
Observational cohort study
Observational cohort study · Real-World Cohort
Biological Pathway & Modality
Antibodies
Intervention: targeted protein degraders and antibody
Experimental Findings & Endpoints
In the past 25 years, kinase drug discovery has grown into one of the most thriving areas in pharmaceutical research and development.
What began as a field dominated by ATP-competitive small molecules has diversified into a broad therapeutic landscape that includes allosteric and covalent inhibitors, activators, proximity-induced modulators, targeted protein degraders and antibody-based therapies, with more than 150 regulatory approvals so far worldwide. In this Review, we provide a comprehensive analysis of the current kinase therapeutic landscape, including more than 2,100 kinase-targeting agents that have entered clinical development in more than 23,000 clinical trials.
We cover drug platforms, new targeting approaches, the expanding target spectrum, approvals and clinical trends. Nearly half of the canonical human protein kinases have at least one clinical-stage agent, placing kinases among the most intensively explored drug target classes.
Clinical Translation & Practice Context
Nevertheless, development remains highly concentrated around a small set of blockbuster kinase targets, such as EGFR.
We also examine the features associated with successful kinase-targeting agents and causes of agent discontinuations and regulatory withdrawal.
The Bottom Line · Clinical Pearl
“We also examine the features associated with successful kinase-targeting agents and causes of agent discontinuations and regulatory withdrawal.”
Published in Nature Reviews Drug Discovery · Current Stage: Real-World Cohort