Abemaciclib: CDK6 Inhibitor

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Cyclin-dependent kinases (CDKs) are proteins are involved in the regulation of the cell cycle. Many human cancers involve mutations in CDKs or the proteins which regulate CDKs. This contributes to sustained proliferative signalling, which is one of the hallmarks of cancer. Therefore, CDK inhibition is an attractive therapeutic target for the treatment of cancer because it can decelerate cell proliferation and hence reduce tumour growth. The specificity of CDK inhibitors is an important factor in minimising the off-target effects of these drugs. Abemaciclib is a CDK inhibitor which is specific to CDK4, CDK6 and CDK9. However, despite this specificity, abemaciclib also inhibits other cellular protein kinases, leading to gastrointestinal toxicity. This is explored in the above diagram, which depicts the interactions between abemaciclib and CDK6.