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alpelisib + trastuzumab emtansine
- Development stage
- Unknown
- Lead developer
- Novartis
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Oral, Intravenous
01
Overview
Alpelisib + trastuzumab emtansine is a combination therapy consisting of alpelisib, an alpha-specific PI3K inhibitor that selectively inhibits the PI3K alpha isoform, and trastuzumab emtansine (T-DM1), an antibody-drug conjugate that combines the HER2-targeting properties of trastuzumab with the cytotoxic agent DM1 (emtansine). This combination targets two key pathways in HER2-positive breast cancer: the PI3K pathway, which is often activated in trastuzumab-resistant tumors, and HER2 signaling. The combination has shown promising results in clinical trials for patients with HER2-positive metastatic breast cancer who have developed resistance to trastuzumab-based therapies.
- Other names
- alpelisib + T-DM1BYL-719 + T-DM1alpelisib + ado-trastuzumab emtansine
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)TUBB (Tubulin (alpha and beta subunits))PIK3CA (Phosphoinositide 3-kinase alpha)
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