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.

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 Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
6.9K
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

1.4K
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
4.3K
M-Cdk Drives Transition Into Mitosis02:15

M-Cdk Drives Transition Into Mitosis

Checkpoints throughout the cell cycle serve as safeguards and gatekeepers, allowing the cell cycle to progress in favorable conditions and slow or halt it in problematic ones. This regulation is known as the cell cycle control system.
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...
5.3K
Clinical Trials: Overview01:11

Clinical Trials: Overview

Clinical development focuses on how the drug will interact with the human body and encompasses four key phases of clinical trials, each serving a specific purpose in assessing the safety and effectiveness of new drugs. These phases overlap and build upon one another. Phase I involves a small group of healthy volunteers (typically 20-80 individuals) or, in cases where significant toxicity is expected, patients with the targeted disease, such as cancer or AIDS. The volunteers are tested for...
4.6K
Pharmacogenomics: Identification of New Drug Targets01:29

Pharmacogenomics: Identification of New Drug Targets

Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...
113