Drug intelligence / Profile preview

GQ1001

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

Overview

GQ1001 is a next-generation, HER2-targeted antibody-drug conjugate (ADC) designed for the treatment of HER2-positive advanced solid tumors. It consists of a monoclonal antibody targeting human epidermal growth factor receptor 2 (HER2/ErbB2), specifically trastuzumab, conjugated via a unique site-specific open-ring linker to the cytotoxic maytansinoid mertansine (DM1). This design improves homogeneity and stability compared to earlier ADCs such as T-DM1, resulting in markedly reduced non-specific cytotoxicity and lower systemic exposure to free DM1. The mechanism of action involves targeted delivery of DM1 to HER2-expressing tumor cells, leading to inhibition of tubulin polymerization, mitotic arrest, and apoptosis. Preclinical studies demonstrated robust antitumor activity in multiple HER2+ models with favorable pharmacokinetics and safety profiles. Phase Ia/Ib clinical trials have shown that GQ1001 is well tolerated with promising efficacy in heavily pretreated patients with HER2-positive advanced solid tumors including breast cancer, gastric/gastroesophageal junction cancer, salivary gland cancer, biliary cancer, and other solid tumors[3][4][5][6].

Other names
anti-HER2-DM1 antibody-drug conjugate GQ1001anti-HER-2-DM1 antibody-drug conjugate GQ1001anti-HER 2-DM1 antibody-drug conjugate GQ1001Toxin-DM1-trastuzumab-conjugateToxin-DM-1-trastuzumab-conjugateToxin-DM 1-trastuzumab-conjugate
02

Targets

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

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