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pictilisib + ado-trastuzumab emtansine
- Development stage
- Preclinical
- Lead developer
- Genentech
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Oral, Intravenous
01
Overview
Pictilisib + ado-trastuzumab emtansine is an investigational combination therapy for cancer, primarily explored in metastatic or locally recurrent breast cancer. **Pictilisib** is an oral small molecule inhibitor that targets class I phosphoinositide 3-kinase (PI3K), a key component in the PI3K/AKT/mTOR pathway involved in tumor growth and survival. **Ado-trastuzumab emtansine** (also known as T-DM1 or Kadcyla) is an antibody-drug conjugate combining trastuzumab (a HER2-targeted monoclonal antibody) with DM1 (a cytotoxic microtubule inhibitor). Trastuzumab emtansine binds HER2-overexpressing cells, is internalized, and releases DM1 intracellularly to disrupt microtubules, providing cytotoxic activity specifically against HER2-positive tumor cells. This combination is rationally designed to address tumors with both HER2 overexpression and aberrant PI3K pathway activity.
- Brand names
- Kadcyla
- Other names
- pictilisib + T-DM1pictilisib + trastuzumab emtansinepictilisib + ado-trastuzumab emtansine
02
Targets
PIK3CA (Phosphoinositide 3-kinase alpha)TUBB (Tubulin (alpha and beta subunits))
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