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megestrol acetate + trastuzumab deruxtecan
- Development stage
- Unknown
- Lead developer
- Daiichi Sankyo
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Oral, Intravenous
01
Overview
Megestrol acetate + trastuzumab deruxtecan is a combination regimen being investigated for the management of treatment-related fatigue in patients with advanced breast cancer. Trastuzumab deruxtecan (T-DXd) is a HER2-directed antibody-drug conjugate (ADC) composed of a humanized anti-HER2 monoclonal antibody (trastuzumab) covalently linked to a topoisomerase I inhibitor payload (deruxtecan) via a cleavable tetrapeptide-based linker. Megestrol acetate is a synthetic derivative of progesterone used primarily as an appetite stimulant and for the treatment of advanced breast and endometrial cancers; in this context, it is being evaluated for its ability to prevent and alleviate T-DXd-related fatigue. The combination is currently being studied in a Phase III clinical trial led by Sun Yat-sen University to determine if early intervention with megestrol acetate can improve the quality of life for patients undergoing ADC therapy.
- Brand names
- Megace
- Other names
- T-DXdTrastuzumab deruxtecan-nxki
02
Targets
PR (Progesterone receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)TOP1 (DNA Topoisomerase I)
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