Bkm120 (Not yet branded)
Other Medications
Description
BKM120 (buparlisib) is a pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor that has been tested in colorectal cancer patients, particularly those with advanced or metastatic disease. It targets the PI3K/AKT/mTOR signaling pathway, which is frequently dysregulated in colorectal tumors and contributes to treatment resistance. Clinical trials have evaluated BKM120 both as monotherapy and in combination with established colorectal cancer treatments like irinotecan and panitumumab, especially in RAS wild-type tumors.
Mechanism of Action
BKM120 inhibits all four class I PI3K isoforms ( , ?, ?, ?) by binding to the ATP-binding site of the kinase domain, blocking the conversion of PIP2 to PIP3 and subsequent activation of the AKT pathway. This inhibition disrupts critical cellular processes including proliferation, survival, and metabolism that are often hyperactivated in cancer cells. The drug is particularly relevant in colorectal cancer where PI3K pathway alterations can drive resistance to EGFR-targeted therapies.
Molecular Targets
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.