Table 3.
Tyrosine kinase inhibitors used in Mast Cell Disorders.
| Drug | Drug Target | Dosing | Comments |
|---|---|---|---|
| Midostaurin * | Multi-kinase inhibitor of KIT, VEGFR, FLT3, PDGFR | 100 mg PO BID | Multi-kinase inhibitor with activity against KIT-D816V |
| Avapritinib * | Selective KIT-D816V inhibitor | 200 mg PO daily | Selective KIT-D816V inhibition; Effective in patients having received prior Midostaurin therapy |
| Imatinib | Multi-kinase inhibitor of KIT, PDGFR, Bcr-Abl | 400 mg PO daily | Resistance observed in KIT-D816V |
| Masitinib | Multi-kinase inhibitor of KIT, PDGFR, Lyn, FGFR3 | 6 mg/kg PO divided into two daily doses | Resistance observed in KIT-D816V |
| Dasatinib | Multi-kinase inhibitor of KIT, PDGFR, Bcr-Abl, Src | 140 mg PO daily | Limited therapeutic activity in SM |
| Nilotinib | Multi-kinase inhibitor of KIT, PDGFR, Bcr-Abl | 400 mg PO BID | Limited therapeutic activity in SM |
Abbreviations: PO, per oral; BID, twice daily; mg, milligrams; kg, kilograms; SM, Systemic Mastocytosis. * FDA approval for treatment of Systemic Mastocytosis.