Bkm120 (Not yet branded)

Other Medications

US Experimental EU Experimental ES Not available Oral 5 Clinical Trials
PI3K alpha PI3K beta PI3K gamma PI3K delta

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

Hyperglycemia Mood alterations including depression and anxiety Diarrhea Decreased appetite Nausea Rash Fatigue Elevated liver enzymes

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT01591421 Phase 1
Archived
P13Kinase Inhibitor BKM120 in Combination With Panitumumab in Metastatic/Advanced RAS-Wild Type Colorectal Cancer.
Canada
NCT01576666 Phase 1
Archived
Phase Ib, Dose Escalation Study of Oral LDE225 in Combination With BKM120 in Patients With Advanced Solid Tumors
United States, Australia, Belgium, Canada, Germany, Italy, Spain, United Kingdom
NCT01571024 Phase 1
Archived
BKM120 + mFOLFOX6 in Advanced Solid Tumors With Expansion Cohort Pancreatic Cancer
United States
NCT01304602 Phase 1
Archived
A Trial of Irinotecan and BKM120 in Previously Treated Advanced Colorectal Cancer
United States
NCT01068483 Phase 1
Archived
Safety of BKM120 Monotherapy in Advanced Solid Tumor Patients
United States, Canada, Netherlands, Spain