Drug intelligence / Profile preview

HS-10516 + lenvatinib

Development stage
Phase 2
Lead developer
Hansoh Pharmaceutical Group
Modality
Small Molecules
Administration
Oral
01

Overview

HS-10516 + lenvatinib is a combination of HS-10516, a small molecule drug in clinical investigation, and lenvatinib, a well-established multikinase inhibitor[2][4]. The combination is currently being studied in advanced clear cell renal cell carcinoma (ccRCC) after progression on prior systemic therapy[2]. HS-10516's precise mechanism has not been fully disclosed, but it targets neoplasms and renal cell carcinoma[4]. Lenvatinib acts by inhibiting multiple receptor tyrosine kinases, including vascular endothelial growth factor receptors (VEGFR1, VEGFR2, VEGFR3), fibroblast growth factor receptors (FGFR1–4), platelet-derived growth factor receptor alpha (PDGFRα), RET, and KIT, leading to inhibition of tumor angiogenesis and proliferation[1]. The rationale for combination therapy is to leverage potential synergistic antitumor effects: HS-10516 is under dose exploration and proof-of-concept phases in ccRCC, while lenvatinib provides established kinase-inhibiting effects.

Other names
HS-10516 + lenvatinib
02

Targets

FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)EPAS1 (Hypoxia-inducible factor 2-alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)RET (Rearranged during transfection receptor tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)

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