Imatinib (Gleevec)

Tyrosine kinase inhibitor (KIT, BCR-ABL, PDGFR)

Response rate
Effective in non-D816V cases; ineffective in D816V+ SM
Onset
Weeks–months
Route
Oral 400mg daily
Line
1st
IgM effect
N/A

Evidence summary

FDA-approved (2006) for ASM without D816V or unknown KIT status. Inhibits wild-type KIT and select non-codon 816 mutants (e.g., K509I, F522C). D816V causes conformational resistance. Effective in well-differentiated SM (WDSM), which typically lacks D816V. Long-term remissions reported in non-D816V patients.

Sources (3)

DetailsAkin C et al. (2017) Imatinib in systemic mastocytosis: a phase IV clinical trial in patients lacking exon 17 KIT mutations · HaematologicaDOI ↗
DetailsLim KH et al. (2009) Phase II study of imatinib mesylate as therapy for patients with systemic mastocytosis · BloodDOI ↗
DetailsFrost MJ et al. (2020) Systemic Mastocytosis: Following the Tyrosine Kinase Inhibition Roadmap · Front PharmacolDOI ↗