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Association details:
| Biomarker: | PDGFRA H845Y |
|---|---|
| Cancer: | Melanoma |
| Drug: | crenolanib (ARO-002) (FLT3 inhibitor, PDGFR α inhibitor, PDGFR β inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
Large-scale analysis of PDGFRA mutations in melanomas and evaluation of their sensitivity to tyrosine kinase inhibitors imatinib and crenolanib
Excerpt:
Thirteen mutations were not reported before, and five (P577S, V658A, R841K, H845Y, and G853D) of them resulted in strong autophosphorylation of PDGFRA. Crenolanib showed higher potency than imatinib in inhibiting the kinase activity of PDGFRA. Except that V658A mutation was imatinib-resistant, all the other mutations were sensitive to both imatinib and crenolanib.
DOI:
10.1158/1078-0432.CCR-13-1266
