KIT mutants bind ripretinib

Stable Identifier
R-HSA-9681382
Type
Reaction [binding]
Species
Homo sapiens
Compartment
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Ripretinib is a member of a new class of inhibitor that binds to the switch pocket domain of KIT. Switch pocket inhibitors are type II tyrosine kinase inhibitors that force the activation loop (AL) into an inactive conformation, and are therefore active against AL mutants of KIT that are otherwise only sensitive to type I TKIs. Ripretinib is active against mutations affecting extracellular, juxtamembrane, ATP-binding pocket and activation loop domains and is thus the first inhibitor with pan-KIT inhibitory activity. Ripretinib has been successfully studied in TKI-refractory GIST (Smith et al, 2019).

Literature References
PubMed ID Title Journal Year
31085175 Ripretinib (DCC-2618) Is a Switch Control Kinase Inhibitor of a Broad Spectrum of Oncogenic and Drug-Resistant KIT and PDGFRA Variants

Smith, BD, Kaufman, MD, Lu, WP, Gupta, A, Leary, CB, Wise, SC, Rutkoski, TJ, Ahn, YM, Al-Ani, G, Bulfer, SL, Caldwell, TM, Chun, L, Ensinger, CL, Hood, MM, McKinley, A, Patt, WC, Ruiz-Soto, R, Su, Y, Telikepalli, H, Town, A, Turner, BA, Vogeti, L, Vogeti, S, Yates, K, Janku, F, Abdul Razak, AR, Rosen, O, Heinrich, MC, Flynn, DL

Cancer Cell 2019
Participants
Participant Of
Normal reaction
Disease
Name Identifier Synonyms
gastrointestinal stromal tumor 9253 GANT, GIST, Stromal tumor of gastrointestinal tract
cancer 162 malignant tumor, malignant neoplasm, primary cancer
Authored
Reviewed
Created
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