Generic Name |
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---|---|---|
IND |
XL820 | |
Brand Name (US) |
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Manufacturer |
Exelixis | |
Drug Type |
Tyrosine Kinase Inhibitor | |
Delivery |
Oral | |
Approval Status |
Phase 2 | |
Indications |
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Overall Strategy |
KIT Protein Based | |
Strategy |
Block KIT | |
Drug Category |
KIT/PDGFRA inhibitor |
XL820 is a novel small molecule inhibitor of the receptor tyrosine kinases KIT, VEGFR2, and PDGFR-α and -β. In preclinical studies, XL820 potently inhibited the resistance-associated activation loop mutations in KIT, and mutations in the ATP binding region of KIT including those in the juxtamembrane domain.
XL820 has been investigated in two Phase 1 studies (XL820-001 and XL820-002), and is being evaluated in a multi-center Phase 2 study (XL820-201) of subjects with advanced gastrointestinal stromal tumors (GIST) resistant to or intolerant of imatinib and/or sunitinib.
We understand the phase II trial has stopped and the trial status is "withdrawn".