Table 1.
Summary of approved treatments for advanced GIST.
| Imatinib | Sunitinib | Regorafenib | Ripretinib | Avapritinib | |
|---|---|---|---|---|---|
| Indication for advanced GIST | 1st line | 2nd line | 3rd line | 4th line | PDGFRA Exon 18 mutant (including D842V) |
| MOA | Type II a | Type II a | Type II a | Type II a | Type I b |
| Competitive ATP-binding site inhibitor | Competitive ATP-binding site inhibitor | Competitive ATP-binding site inhibitor | Switch-pocket inhibitor | Competitive ATP-binding site inhibitor | |
| Efficacy | |||||
| mPFS (mo) | 18 | 5.6 | 4.8 | 6.3 | 34 c |
| ORR (%) | 50 | 7 | 4.5 | 9.4 | 91 c |
a
Binds the inactive confirmation.
b
Binds the active confirmation.
c
D842V patients only.
GIST, gastrointestinal stromal tumor; mo, months; MOA, mechanism of action; mPFS, median progression-free survival; ORR, overall response rate; PDGFRA, platelet-derived growth factor receptor a.