Drug intelligence / Profile preview

ado-trastuzumab emtansine + pyrotinib

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

Overview

Ado-trastuzumab emtansine + pyrotinib is a combination therapy consisting of two targeted anti-cancer agents used primarily in the treatment of HER2-mutated or HER2-positive advanced breast cancer. Ado-trastuzumab emtansine (T-DM1, marketed as Kadcyla) is an antibody-drug conjugate that links trastuzumab, a monoclonal antibody targeting human epidermal growth factor receptor 2 (HER2), to DM1, a potent microtubule inhibitor. Upon binding to HER2-expressing tumor cells, the conjugate is internalized and releases DM1 intracellularly, disrupting microtubules and inducing cell death[4][5]. Pyrotinib is an oral irreversible pan-ErbB tyrosine kinase inhibitor that targets multiple members of the ErbB family including HER1, HER2, and HER4[2]. The combination leverages dual mechanisms: direct cytotoxicity via T-DM1’s ADC action and broad inhibition of ErbB signaling pathways by pyrotinib. This regimen has shown promising efficacy in patients with advanced breast cancer harboring activating HER2 mutations who have progressed on prior therapies[1].

Brand names
Kadcyla
Other names
T-DM1 + pyrotinib
02

Targets

ERBB4 (Erb-b2 receptor tyrosine kinase 4)EGFR T790M (Epidermal growth factor receptor T790M mutant)TUBB (Tubulin (alpha and beta subunits))ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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