Active in Trastuzumab-resistant, HER2+ breast cancer; crosses the BBB and suppresses CNS metastasis used in combination with Capecitabine for HER2+ MBC
Inhibits HER2 autophosphorylation and suppresses downstream signalling; active in HER2+ patients with and without Trastuzumab pretreatment; not currently approved for MBC
Antiangiogenic therapy; FDA-approved for renal cell carcinoma and Gleevec-resistant gastrointestinal stromal tumours; effective as a single agent for metastatic breast cancer (phase II study)
Anti-angiogenic therapy; FDA-approved for renal cell carcinoma; combination with Lapatinib has superior activity as the first-line treatment for MBC (phase II study)