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Table 2 New TKIs for GIST

From: Recent advances and novel agents for gastrointestinal stromal tumor (GIST)

Study drug Disease Dosage Clinical Trial Number of patients Results Reference
Regorafenib Imatinib and Sunitinib Resistant 160 mg/day orally day 1–21 of 28  day cycle. Phase 2 33 SD 86% [52]
Masitinib First line therapy 7.5 mg/kg/day Phase 2 30 PFS 41 m [53]
Crenolanib Selective for D842V mutation - In vitro - Blocks the kinase activity of PDGFRA D842V mutants. [54]
PTK787/ZK222584 Imatinib resistant 1,250 mg o.d Phase 2 15 ORR 67% [44]
AMG 706 Imatinib-resistant 600 mg daily Phase 2 138 ORR33% [48]
  1. Abbreviations:SD stable disease; PFS progression free survival; ORR overall response rate.