Related Experiment Video
Updated: Apr 22, 2026

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
Advances in kinase targeting: current clinical use and clinical trials
Mathias Rask-Andersen1, Jin Zhang2, Doriano Fabbro3
1Department of Neuroscience, Division of Functional Pharmacology, Uppsala University, Biomedicinska Centrum (BMC), Uppsala 751 24, Sweden.
Abstract:
Phosphotransferases, also known as kinases, are the most intensively studied protein drug target category in current pharmacological research, as evidenced by the vast number of kinase-targeting agents enrolled in active clinical trials. This development has emerged following the great success of small-molecule, orally available protein kinase inhibitors for the treatment of cancer, starting with the introduction of imatinib (Gleevec®) in 2003. The pharmacological utility of kinase-targeting has expanded to include treatment of inflammatory diseases, and rapid development is ongoing for kinase-targeted therapies in a broad array of indications in ophthalmology, analgesia, central nervous system (CNS) disorders, and the complications of diabetes, osteoporosis, and otology. In this review we highlight specifically the kinase drug targets and kinase-targeting agents being explored in current clinical trials. This analysis is based on a recent estimate of all established and clinical trial drug mechanisms of action, utilizing private and public databases to create an extensive dataset detailing aspects of more than 3000 approved and experimental drugs.
Insights
Kinases are key drug targets, with many agents in clinical trials for cancer and other diseases. This review focuses on current kinase drug targets and therapies in development.
Area of Science:
- Pharmacological Research
- Drug Discovery
- Biochemistry
Background:
- Kinases (phosphotransferases) are a major focus in drug development.
- The success of imatinib (Gleevec®) in cancer treatment spurred further research.
- Kinase inhibitors are now explored for inflammatory, ophthalmological, CNS, and metabolic disorders.
Purpose of the Study:
- To review kinase drug targets and agents in current clinical trials.
- To analyze the landscape of kinase-targeted therapies across various indications.
- To provide an overview of the development of kinase inhibitors.
Main Methods:
- Analysis of established and clinical trial drug mechanisms of action.
- Utilization of private and public databases for drug information.
- Compilation of a dataset detailing over 3000 approved and experimental drugs.
Main Results:
- A vast number of kinase-targeting agents are in active clinical trials.
- Kinase inhibitors have expanded beyond cancer to other therapeutic areas.
- Significant ongoing development in kinase-targeted therapies for diverse diseases.
Conclusions:
- Kinases remain a highly significant target class in pharmaceutical research.
- Clinical trials showcase a broad spectrum of kinase inhibitors under investigation.
- The therapeutic potential of kinase-targeting drugs continues to expand rapidly.
Related Concept Videos
Targeted Cancer Therapies
There are several types of targeted therapies against...
Targeted Cancer Therapies
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
M-Cdk Drives Transition Into Mitosis
Cyclin-dependent kinases, or Cdks, work in concert with cyclins to control cell cycle transitions. M-Cdk, a complex of Cdk1 bound to M cyclin, is a well-known example of this coordinated control that drives the transition from the G2 to the M phase.
M cyclin...
Clinical Trials: Overview
Pharmacogenomics: Identification of New Drug Targets

