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SBT6050 + tucatinib + trastuzumab + capecitabine
- Development stage
- Unknown
- Lead developer
- ARS Pharmaceuticals
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous (SBT6050, Trastuzumab), Oral (tucatinib, Capecitabine)
01
Overview
A multi-agent combination regimen for HER2-positive advanced or metastatic malignancies, typically breast cancer. SBT6050 is a first-in-class antibody-drug conjugate targeting HER2 and functioning as a toll-like receptor 8 (TLR8) agonist to activate myeloid cells in the tumor microenvironment[3]. Tucatinib is a small molecule tyrosine kinase inhibitor selective for HER2, designed to inhibit downstream HER2 signaling and proliferation[4][6]. Trastuzumab is a monoclonal antibody binding HER2, blocking receptor activation, and engaging immune mechanisms including antibody-dependent cellular cytotoxicity (ADCC)[6]. Capecitabine is an orally active prodrug of 5-fluorouracil (5-FU), a chemotherapeutic antimetabolite interfering with DNA synthesis[2][4]. The combination is used in HER2-expressing solid tumors, frequently in heavily pretreated metastatic breast cancer patients, including those with brain metastases, improving survival and disease control compared to conventional therapies[4][6].
- Brand names
- Herceptin (trastuzumab)Xeloda (capecitabine)Tukysa (tucatinib)
- Other names
- SBT6050 + tucatinib + trastuzumab + capecitabine
02
Targets
TS (Thymidylate synthase)HER2 ECD subdomain II (Human epidermal growth factor receptor 2 dimerization interface)TLR8 (Toll-like receptor 8)
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