buparlisib + trastuzumab

Buparlisib + trastuzumab is a combination therapy consisting of buparlisib, an oral pan-class I phosphoinositide 3-kinase (PI3K) inhibitor, and trastuzumab, a monoclonal antibody targeting the human epidermal growth factor receptor 2 (HER2). This regimen has been investigated primarily in patients with HER2-positive advanced or metastatic breast cancer who have developed resistance to prior trastuzumab-based therapies. Buparlisib inhibits the PI3K/AKT/mTOR signaling pathway, which is often implicated in resistance to HER2-targeted treatments. Trastuzumab binds to the extracellular domain of HER2, inhibiting downstream signaling and mediating antibody-dependent cellular cytotoxicity. Clinical studies have shown that this combination has an acceptable safety profile but limited efficacy as a chemotherapy-free regimen in heavily pretreated populations; common adverse events include diarrhea, nausea, rash, hyperglycemia, and elevated liver enzymes[1][2][3]. The combination has also been explored with capecitabine for patients with brain metastases[1][3].

Other names

buparlisib and trastuzumabBKM120 and trastuzumabBKM-120 and trastuzumabBKM 120 and trastuzumab