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disitamab vedotin + tucatinib
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous, Oral
01
Overview
**Disitamab vedotin + tucatinib** is a combination therapy under clinical investigation for the treatment of locally advanced or metastatic solid tumors that express human epidermal growth factor receptor 2 (HER2), including breast cancer and gastric cancer. Disitamab vedotin is an antibody-drug conjugate (ADC) targeting HER2, composed of a humanized anti-HER2 antibody (hertuzumab), a cathepsin-cleavable valine-citrulline linker, and the cytotoxic microtubule inhibitor monomethyl auristatin E (MMAE). DV binds to HER2 on tumor cells, becomes internalized, and releases MMAE to induce targeted cytotoxicity and a bystander effect. Tucatinib is a small molecule, HER2-selective tyrosine kinase inhibitor approved for HER2-positive breast cancer. The combination leverages targeted immune-mediated destruction with ADC delivery and intracellular HER2 signaling blockade[1][2][4][5][6][7][9][10].
- Other names
- disitamab vedotintucatinib
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)TUBB (Tubulin (alpha and beta subunits))
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