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trastuzumab rezetecan + fulvestrant
- Development stage
- Unknown
- Lead developer
- Hengrui Pharmaceutical
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intramuscular, Intravenous
01
Overview
SHR-A1811 (trastuzumab rezetecan) is a third-generation antibody-drug conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2). It consists of a humanized anti-HER2 antibody linked via a cleavable linker to a topoisomerase I inhibitor payload. The drug is designed to deliver cytotoxic agents directly to HER2-expressing tumor cells, resulting in targeted cell death. SHR-A1811 has demonstrated promising antitumor activity and acceptable tolerability in patients with HER2-positive breast cancer and other advanced solid tumors expressing or harboring mutations in HER2. Fulvestrant is an estrogen receptor antagonist used primarily for hormone receptor–positive breast cancer; the combination aims to target both HER2 and estrogen signaling pathways for enhanced efficacy in certain breast cancers[1][3][4].
- Brand names
- Faslodex
- Other names
- trastuzumab rezetecan + fulvestrant
02
Targets
TOP1 (DNA Topoisomerase I)ESR1 (ERα)ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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