buparlisib + lapatinib

This is a combination therapy of two small molecule inhibitors: - **Buparlisib (BKM120)** is an oral pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor that targets both wild-type and mutant PI3K p110 isoforms. It inhibits the PI3K/AKT/mTOR pathway, which is frequently activated in HER2-positive breast cancer and implicated in resistance to trastuzumab. - **Lapatinib** is an oral dual tyrosine kinase inhibitor targeting both the human epidermal growth factor receptor 2 (HER2/ERBB2) and epidermal growth factor receptor (EGFR/ERBB1). It blocks downstream signaling pathways involved in cell proliferation and survival. The combination has been investigated primarily for HER2-positive, trastuzumab-resistant advanced or metastatic breast cancer. Clinical studies have shown feasibility with preliminary antitumor activity but also notable toxicities such as diarrhea, nausea, skin rash, asthenia, depression/anxiety, transaminase elevation, vomiting, stomatitis and hyperglycemia[6][4][1]. The recommended phase II dose was determined as buparlisib 80 mg plus lapatinib 1000 mg daily[6].

Brand names

Tykerb

Other names

BKM120 + lapatinibbuparlisib + lapatinib