Sitravatinib
Multikinase inhibitor / Immuno-oncology agent / Sitravatinib is a broad spectrum receptor tyrosine kinase inhibitor. Its targets include Axl, c-Met, PDGFR, VEGFR, Ephrin receptor family, and FLT3 among others at nanomolar levels.1 Sitravatinib has been tested in mouse models of sarcoma and showed better efficacy than both imatinib and crizotinib. Because of its unique kinase inhibition profile (especially that of TAM receptors), it has been used to restore response to anti-PD-1 therapy (nivolumab) in NSCLC patients.2 Sitravatinib was able to significantly alter the immunosuppressive tumor microenvironment in three preclinical tumor models to enhance the effects of PD-1 blockade therapy.3
Biochemicals & reagents
1123837-84-2
MGCD516
1) Parag et al. (2016) Significant blockade of multiple receptor kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma; Oncotarget 7 4093 2) Leal et al. (2017) Evidence of clinical activity of sitravatinib in combination with nivolumab in NSCLC patients progressing on prior checkpoint inhibitors; J.Thorac.Oncol. 12 S1803 3) Du et al. (2018); Sitravatinib potentiates immune checkpoint blockade in refractory cancer models; JCI Insight 3 124184
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TARGET: Kinase -- RESEARCH AREA: Immunology -- DISEASE AREA: Cancer