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taselisib + trastuzumab emtansine
- Development stage
- Unknown
- Lead developer
- Genentech
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Oral, Intravenous
01
Overview
Taselisib + trastuzumab emtansine is a combination therapy investigated for the treatment of advanced HER2-positive breast cancer. Taselisib is an α-selective potent oral inhibitor of phosphoinositide-3-kinase (PI3K), a protein that helps cancer cells grow. Trastuzumab emtansine (T-DM1) is an HER2-directed antibody-drug conjugate (ADC) designed to overcome trastuzumab resistance by using HER2 as a target for precision delivery of a cytotoxic agent to destroy cancer cells resistant to HER2 blockade. This combination was studied to potentially improve disease control in patients with advanced HER2+ breast cancer who developed acquired resistance to anti-HER2 therapies, which is often mediated through PI3K signaling.
- Other names
- taselisib + T-DM1
02
Targets
PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)ERBB2 (Erb-b2 receptor tyrosine kinase 2)TUBB (Tubulin (alpha and beta subunits))PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CD (Phosphatidylinositol 3-kinase delta)
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