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anastrozole + trastuzumab deruxtecan
- Development stage
- Unknown
- Lead developer
- Daiichi Sankyo
- Modality
- Nucleic Acid-Directed Small Molecules → Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Anastrozole + trastuzumab deruxtecan is an investigational combination therapy for breast cancer, specifically targeting HER2-low, hormone receptor–positive (HR+) subtypes. Anastrozole is a nonsteroidal aromatase inhibitor that reduces estrogen production, thereby inhibiting the growth of estrogen-dependent tumors. Trastuzumab deruxtecan (also known as T-DXd or by the brand name Enhertu) is an antibody-drug conjugate composed of a humanized anti-HER2 monoclonal antibody (trastuzumab) linked to the topoisomerase I inhibitor deruxtecan via a cleavable peptide linker. The antibody targets HER2-expressing tumor cells and delivers the cytotoxic payload directly into these cells after internalization, causing DNA damage and cell death. This combination has shown encouraging antitumor activity in clinical trials for patients with metastatic or early-stage HR+/HER2-low breast cancer who have not received prior chemotherapy[2][3][4][5][7].
- Brand names
- Enhertu
- Other names
- fam-trastuzumab deruxtecan-nxki + anastrozole
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)TOP1 (DNA Topoisomerase I)CYP19A1 (Aromatase)
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