TABLE 4.
Tyrosine Kinase Inhibitors With KIT/PDGFRA Inhibitory Activity Tested in Advanced and Metastatic Gastrointestinal Stromal Tumor, But Without Regulatory Approval for This Indication
| Drug | Clinical Trial | Setting Treatment Line | ORR (%) | mPFS (mo) | Phase |
|---|---|---|---|---|---|
| Avapritinib | Kang (2021)78 | Third/fourth | 17 | 4.2 | III-R |
| Cabozantinib | Schöffski (2020)79 | Third | 14 | 5.5 | II |
| Dasatinib | Schuetze (2018)80 | Second or more | 4 | 2.9 | II |
| Dovitinib | Kang (2013)81 | Third or more | 3 | 3.6 | II |
| Joensuu (2017)82 | Third or more | 5 | 4.6 | II | |
| Masitinib | Adenis (2014)83 | Second | NA | 3.7 | II |
| Nilotinib | Montemurro (2009)84 | Third or more | 10 | 2.8 | II |
| Sawaki (2011)85 | Third | 3 | 3.7 | II | |
| Cauchi (2012)86 | Third or more | 0 | 2.0 | II | |
| Reichardt (2012)87 | Third | < 1 | 3.6 | III-R | |
| Pazopanib | Ganjoo (2014)88 | Second or more | 0 | 1.9 | II |
| Mir (2016)89 | Second or more | 0 | 3.4 | II-R | |
| Eriksson (2021)90 | Third/fourth | 3 | 4.5 | II | |
| Ponatinib* | George (2022)91 | Second or more | 8 | 4.3 | II |
| Sorafenib | Kindler (2011)92 | Second or more | 13 | 5.2 | II |
| Park (2012)93 | Third or more | 13 | 4.9 | II |
Abbreviations: ORR, overall response rate (complete and partial responses) determined by RECIST criteria; mPFS, median progression-free survival; NA, not available.
*
Data from patients with KIT exon 11 mutant gastrointestinal stromal tumor.