Drug intelligence / Profile preview

GQ1001 + pyrotinib

Development stage
Phase 2
Lead developer
GeneQuantum Biosciences
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

GQ1001 + pyrotinib is a combination therapy under investigation for the treatment of HER2-positive metastatic breast cancer, particularly in patients who have failed previous anti-HER2 treatments. GQ1001 is a next-generation HER2-targeted antibody-drug conjugate (ADC) created by conjugating trastuzumab to DM1 via a unique linker using enzymatic site-specific conjugation technology, which enhances drug homogeneity and stability. It exerts its effect by targeting the HER2 receptor and delivering the cytotoxic agent DM1 to tumor cells, leading to cell death. Pyrotinib is an irreversible pan-HER tyrosine kinase inhibitor that blocks autophosphorylation of HER family receptors (HER1/EGFR, HER2, and HER4), thereby inhibiting downstream signaling pathways essential for tumor growth. Preclinical studies have shown that this combination has synergistic anti-tumor activity in models of breast and gastric cancer. Clinical trials are ongoing to evaluate safety, pharmacokinetics, and efficacy in patients with advanced or metastatic HER2-positive breast cancer[1][2][3][5].

02

Targets

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

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