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SHR-A1811 + itraconazole
- 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 is a HER2-targeted antibody-drug conjugate (ADC) developed by Jiangsu Hengrui Pharmaceuticals. It consists of a humanized anti-HER2 monoclonal antibody (trastuzumab) covalently linked to a novel topoisomerase I inhibitor payload (SHR152852) via a cleavable linker. SHR-A1811 is designed to treat HER2-expressing or mutated solid tumors, including breast, gastric, and lung cancers. Itraconazole is a potent small molecule antifungal agent that also acts as a strong inhibitor of the cytochrome P450 3A4 (CYP3A4) enzyme and P-glycoprotein (P-gp). The combination of SHR-A1811 and itraconazole is primarily utilized in Phase 1 clinical pharmacology studies to evaluate the impact of CYP3A4 inhibition on the pharmacokinetics, safety, and tolerability of the ADC and its released payload, which is a critical step in understanding potential drug-drug interactions (DDI).
- Brand names
- Sporanox
- Other names
- trastuzumab-SHR152852 + itraconazole
02
Targets
TOP1 (DNA Topoisomerase I)CYP3A4 (Cytochrome P450 3A4)ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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