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trastuzumab deruxtecan + paclitaxel
- Development stage
- Unknown
- Lead developer
- Daiichi Sankyo
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
This is a **combination therapy** of trastuzumab deruxtecan (an antibody-drug conjugate targeting HER2) and paclitaxel (a microtubule inhibitor). - **Trastuzumab deruxtecan** is a HER2-directed antibody-drug conjugate consisting of a humanized anti-HER2 IgG1 monoclonal antibody linked to deruxtecan, a potent topoisomerase I inhibitor, via a cleavable peptide linker. It binds to HER2-expressing cancer cells, is internalized, and releases deruxtecan to induce targeted DNA damage and apoptosis. - **Paclitaxel** is a classic antineoplastic agent that stabilizes microtubules, inhibiting their disassembly and thus blocking cell division at mitosis. Combination regimens are under investigation for HER2-positive metastatic breast and gastric cancers, as well as potentially other HER2-expressing solid tumors. The combination leverages both the targeted cytotoxicity of trastuzumab deruxtecan and the anti-mitotic effect of paclitaxel.
- Brand names
- Enhertu + paclitaxel
- Other names
- fam-trastuzumab deruxtecan-nxki + paclitaxelT-DXd + paclitaxel
02
Targets
TUBB (Tubulin (alpha and beta subunits))TOP1 (DNA Topoisomerase I)ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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