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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.