Drug intelligence / Profile preview

pertuzumab + taselisib + trastuzumab emtansine

Development stage
Phase 1
Lead developer
Genentech
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen of three targeted therapies for HER2-positive breast cancer: - **Pertuzumab** is a monoclonal antibody that binds to the HER2 receptor at subdomain II, inhibiting dimerization with other HER family members and blocking downstream signaling pathways involved in cell proliferation. - **Taselisib** is an investigational small molecule inhibitor of phosphoinositide 3-kinase (PI3K), specifically targeting the PI3K pathway, which plays a key role in cancer cell growth and survival. - **Trastuzumab emtansine** (T-DM1) is an antibody-drug conjugate consisting of trastuzumab linked to DM1, a cytotoxic agent. Trastuzumab targets the HER2 receptor on tumor cells, delivering DM1 directly into these cells to inhibit microtubule assembly and induce apoptosis. This combination has been studied in phase Ib clinical trials for patients with advanced or metastatic HER2-positive breast cancer who have progressed on prior anti-HER2 therapies. The rationale for this regimen is to simultaneously block multiple pathways critical for tumor growth and resistance mechanisms—HER2 signaling via two antibodies plus PI3K inhibition—while delivering targeted cytotoxicity through T-DM1[1][4][5].

Other names
T-DM1T-DM-1T-DM 1GDC-0032GDC0032GDC 0032
02

Targets

HER2 ECD subdomain II (Human epidermal growth factor receptor 2 dimerization interface)PIK3CD (Phosphatidylinositol 3-kinase delta)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CA (Phosphoinositide 3-kinase alpha)

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