Drug intelligence / Profile preview

XL092 + avelumab

Development stage
Phase 1
Lead developer
Exelixis
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

**XL092 + avelumab** is an investigational combination therapy of XL092, a small molecule multi-targeted receptor tyrosine kinase inhibitor, and avelumab, a monoclonal antibody immune checkpoint inhibitor directed against PD-L1. XL092 inhibits MET, VEGFR2, AXL, and MER kinases, impacting tumor growth, angiogenesis, and the tumor microenvironment. Avelumab blocks PD-L1, resulting in immune activation against tumor cells. This combination is being evaluated primarily in advanced solid tumors, including renal cell carcinoma (clear cell and non-clear cell), hormone receptor–positive breast cancer, metastatic castration-resistant prostate cancer, and urothelial carcinoma. The therapy is being studied in phase 1 trials for safety, tolerability, pharmacokinetics, and preliminary antitumor activity[1][2][3][4][5].

02

Targets

AXL (AXL receptor tyrosine kinase)FcγR (Low affinity immunoglobulin gamma Fc region receptor II-c)MET (Mesenchymal-epithelial transition factor receptor)CD274 (Programmed cell death protein 1 ligand 1)VEGFR2 (Vascular endothelial growth factor receptor 2)MERTK (MER proto-oncogene, tyrosine kinase)

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