Drug intelligence / Profile preview

garsorasib + benmelstobart + anlotinib

Development stage
Phase 2
Lead developer
Chia Tai-Tianqing Pharmaceutical Group
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

This combination therapy consists of garsorasib (also known as goselasib or D-1553), benmelstobart (TQB2450), and anlotinib (AL3818). It is currently being investigated as a first-line treatment for patients with KRAS G12C-mutant locally advanced or metastatic non-small cell lung cancer (NSCLC). Garsorasib is a potent and selective small-molecule inhibitor of the KRAS G12C mutation, which locks the protein in its inactive GDP-bound state to inhibit downstream oncogenic signaling. Benmelstobart is a humanized monoclonal antibody targeting programmed cell death ligand 1 (PD-L1), designed to block the PD-1/PD-L1 pathway and restore T-cell-mediated anti-tumor immunity. Anlotinib is a multi-targeted tyrosine kinase inhibitor that primarily inhibits VEGFR1/2/3, FGFR1/2/3/4, PDGFR alpha/beta, and c-Kit, thereby suppressing tumor angiogenesis and growth. The triple combination aims to provide a synergistic therapeutic effect by simultaneously targeting the driver mutation, the immune microenvironment, and tumor vascularization.

Other names
Goselasib + Benmelstobart + Anlotinib
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)KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)CD274 (Programmed cell death protein 1 ligand 1)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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