Drug intelligence / Profile preview

XL092 + atezolizumab

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

Overview

XL092 + atezolizumab is a combination regimen of two drugs under investigation for the treatment of metastatic colorectal cancer (mCRC), specifically in patients with microsatellite stable (MSS) or microsatellite instability–low (MSI-L) disease who have progressed on or are intolerant to standard-of-care therapies[1][3][5]. - **XL092 (zanzalintinib)** is an orally-administered small molecule multi-kinase inhibitor that targets MET, VEGFR2, and the TAM kinases (AXL and MER, as well as TYRO3 in preclinical data)[2][4][5]. These kinases are involved in tumor growth, metastasis, angiogenesis, and immunosuppression. - **Atezolizumab (Tecentriq)** is an intravenously administered monoclonal antibody immune checkpoint inhibitor that binds PD-L1, blocking its interaction with PD-1 and B7.1, thereby restoring anti-tumor immune response. The combination is being evaluated in the phase 3 STELLAR-303 trial (NCT05425940), where XL092 is administered as 100 mg oral daily and atezolizumab as 1200 mg IV every 3 weeks[1][3][5]. The intended mechanism is the synergistic action of VEGFR2 multi-kinase inhibition and immune modulation by both agents for enhanced antitumor efficacy and immunomodulation.

Brand names
Tecentriq
Other names
XL092 plus atezolizumabXL-092 plus atezolizumabXL 092 plus atezolizumab
02

Targets

AXL (AXL receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)VEGFR2 (Vascular endothelial growth factor receptor 2)CD274 (Programmed cell death protein 1 ligand 1)

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