Drug intelligence / Profile preview

DP303c + simmitinib

Development stage
Unknown
Lead developer
CSPC ZhongQi Pharmaceutical Technology
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous, Oral
01

Overview

**DP303c + simmitinib** is a combination regimen investigated in clinical trials for the treatment of HER2-positive gastric adenocarcinoma or gastroesophageal junction adenocarcinoma that has progressed after at least one line of systemic therapy. **DP303c** is an antibody-drug conjugate (ADC) consisting of an anti-HER2 monoclonal antibody linked to the cytotoxic payload monomethyl auristatin E (MMAE), employing an enzyme-specific cleavable linker. DP303c inhibits HER2 signaling, induces antibody-dependent cellular cytotoxicity (ADCC), and delivers the microtubule-disrupting MMAE to HER2-expressing tumor cells. **Simmitinib** is a small molecule tyrosine kinase inhibitor; while its precise kinase target profile is not explicitly stated in trial documentation, it suggests activity relevant to synergize with HER2-targeted therapy. The combination is being studied for its safety and antitumor efficacy in patients resistant to previous systemic chemotherapy, including platinum- and fluorouracil-based regimens.

02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)FGFR3 (Fibroblast growth factor receptor 3)CSF1R (Macrophage colony-stimulating factor receptor)TUBB (Tubulin (alpha and beta subunits))FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)VEGFR2 (Vascular endothelial growth factor receptor 2)

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