How does Ripretinib work?

How does ripretinib work at the molecular level?

Ripretinib is a kinase inhibitor designed to block the activity of specific KIT and PDGFRA proteins. It works by binding to these receptor tyrosine kinases in a way that prevents their abnormal signaling, which can drive tumor growth in cancers such as gastrointestinal stromal tumor (GIST) with KIT/PDGFRA mutations [1].

Why does it work even when tumors develop resistance?

Many resistant GIST tumors acquire new “activation” or “switch-control” mutations in KIT or PDGFRA that keep the signaling pathway turned on. Ripretinib is built to inhibit a broad set of KIT and PDGFRA variants, including switch-control mutations, helping it maintain drug activity across a range of resistant forms [1].

What does the drug change inside the cell?

By inhibiting KIT and PDGFRA kinase activity, ripretinib stops downstream pathways that would normally promote cell survival and proliferation. The practical effect is reduced signaling that supports tumor cell growth in mutation-driven settings [1].

What cancers use this mechanism?

Ripretinib is used for advanced GIST where the disease is driven by KIT and/or PDGFRA alterations, including settings involving prior therapy and resistant disease biology [1].

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Sources
[1] https://www.drugpatentwatch.com/p/ripretinib