Drug intelligence / Profile preview

SHR-A1811 + pyrotinib

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

Overview

SHR-A1811 + pyrotinib is a combination therapy under investigation for the treatment of HER2-positive breast cancer. SHR-A1811 is a third-generation antibody-drug conjugate (ADC) composed of an anti-HER2 monoclonal antibody (trastuzumab), a cleavable linker, and a topoisomerase 1 inhibitor payload. It targets Human epidermal growth factor receptor 2 (HER2)-expressing tumor cells, delivering cytotoxic agents directly to these cells[3][4]. Pyrotinib is an irreversible pan-ErbB receptor tyrosine kinase inhibitor that blocks signaling from multiple members of the ErbB family, including Epidermal growth factor receptor (EGFR/HER1), Human epidermal growth factor receptor 2 (HER2), and Human epidermal growth factor receptor 4 (HER4)[6][8]. The combination has shown promising antitumor activity in phase II clinical trials as neoadjuvant therapy for patients with stage II–III HER2-positive breast cancer, with pathological complete response rates comparable to standard regimens. The most common grade ≥3 adverse events include neutropenia and diarrhea[2][4].

02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)EGFR (Epidermal growth factor receptor)ERBB4 (Erb-b2 receptor tyrosine kinase 4)TOP1 (DNA Topoisomerase I)

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