Description
Prexasertib (LY2606368) is a selective checkpoint kinase 1 (CHK1) inhibitor that disrupts DNA damage response pathways in cancer cells. In colorectal cancer, it is being evaluated in combination with other targeted agents like ralimetinib (a p38 MAPK inhibitor) and various chemotherapy regimens. The drug targets tumors with defective DNA repair mechanisms, particularly those with PIK3CA mutations that may render cells more vulnerable to checkpoint inhibition.
Mechanism of Action
Prexasertib selectively inhibits checkpoint kinase 1 (CHK1), a critical enzyme in the DNA damage response pathway that normally prevents cells from progressing through the cell cycle when DNA is damaged. By blocking CHK1 function, the drug forces cancer cells with existing DNA repair defects to proceed through cell division despite having damaged DNA, ultimately leading to cell death through replication catastrophe.
Molecular Targets
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.
Clinical Trials
Quick Info
| Brand Name | Not yet branded |
| Category | Other Medications |
 Status | Experimental |
| Administration | IV |
| Clinical Trials | 2 |
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Medical Disclaimer
This information is for educational purposes only and should not replace professional medical advice. Always consult your healthcare team before making treatment decisions.