Drug intelligence / Profile preview

trastuzumab emtansine + docetaxel + pertuzumab

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

Overview

This combination drug regimen includes **trastuzumab emtansine** (an antibody-drug conjugate targeting HER2, also known as T-DM1 or Kadcyla), **docetaxel** (a cytotoxic taxane chemotherapy agent, known as Taxotere), and **pertuzumab** (a monoclonal antibody targeting HER2 dimerization, known as Perjeta). It is used in the treatment of **HER2-positive breast cancer**, both metastatic and locally advanced types. - **Trastuzumab emtansine** delivers the cytotoxic agent DM1 specifically to HER2-overexpressing cells via a monoclonal antibody, inhibiting cell proliferation and inducing apoptosis. - **Docetaxel** promotes cell death by inhibiting microtubule depolymerization, disrupting mitosis. - **Pertuzumab** binds to a distinct epitope on HER2, blocking HER2 dimerization (especially with HER3) and preventing downstream signaling that promotes cell growth. Clinical studies demonstrate enhanced antitumor activity for dual and triple combinations in both preclinical and early-phase clinical trials, with efficacy as measured by response rates and progression-free survival in HER2-positive breast cancer[1][2][3].

Brand names
Kadcyla + Taxotere + Perjeta
Other names
T-DM1 + docetaxel + pertuzumabado-trastuzumab emtansine + docetaxel + pertuzumab
02

Targets

TUBB (Tubulin (alpha and beta subunits))ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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