Table 3 Clinical trials of the drugs targeting KIT expression in GIST
Drug | Category | Combination | Phase | Status | Sponsor location | NCT Number |
|---|---|---|---|---|---|---|
Entacapone | FTO demethylation inhibitor | Imatinib | 1 | Active, not recruiting | China | 04006769 |
BBI503 | BRD4 | / | 2 | Terminated | Canada | 02232620 |
BBI503 | BRD4 | / | 1 | Completed | US | 02354898 |
BIIB021 | HSP90 inhibitor | / | 2 | Completed | US | 00618319 |
IPI-504 | HSP90 inhibitor | / | 1 | Completed | US | 00276302 |
Pimitespib | HSP90 inhibitor | Imatinib | 1 | Recruiting | Japan | 05245968 |
AT13387 | HSP90 inhibitor | Imatinib | 2 | Completed | US | 01294202 |
Ganetespib | HSP90 inhibitor | / | 2 | Completed | US | 01039519 |
AUY922 | HSP90 inhibitor | / | 2 | Unknown | Taiwan, China | 01389583 |
AUY922 | HSP90 inhibitor | / | 2 | Completed | US | 01404650 |
IPI-504 | HSP90 inhibitor | / | 3 | Terminated | US | 00688766 |
BKM120 | PI3K inhibitor | Imatinib | 1 | Completed | US | 01468688 |
BYL719 | PI3Kα inhibitor | Imatinib | 1 | Completed | US | 01735968 |
Copanlisib | PI3K inhibitor | BAY1895344 | 1 | Not recruiting | US | 05010096 |
Perifosine | AKT inhibitor | Imatinib | 2 | Completed | US | 00455559 |
Perifosine | AKT inhibitor | Sunitinib | 1 | Completed | Canada | 00399152 |
RAD001 (Everolimus) | mTOR inhibitor | Imatinib | 1/2 | Completed | US | 01275222 |
RAD001 (Everolimus) | mTOR inhibitor | / | / | Available | / | 03493152 |
Temsirolimus | mTOR inhibitor | / | / | Recruiting | Germany | 00700258 |
RAD001 (Everolimus) | mTOR inhibitor | / | 2 | Completed | Germany | 00767819 |
MEK162 (Binimetinib) | MEK inhibitor | Ripretinib | 1/2 | Withdrawn | US | 05080621 |
MEK162 (Binimetinib) | MEK inhibitor | Pexidartinib | 1 | Completed | US | 03158103 |
MEK162 (Binimetinib) | MEK inhibitor | Imatinib | 1/2 | Active, not recruiting | US | 01991379 |
MEK162 (Binimetinib) | MEK inhibitor | Ripretinib | 1/2 | Withdrawn | Unknown | 05080621 |
Trametinib | MEK inhibitor | Pazopanib | 2 | Withdrawn | US | 02342600 |
Selumetinib (AZD6244) | MEK inhibitor | / | 2 | Withdrawn | US | 03109301 |
Sorafenib | Raf inhibitor | / | 2 | Completed | Korea | 01091207 |
Sorafenib Tosylate | Raf inhibitor | / | 2 | Active, not recruiting | US | 00265798 |
THE-630 | Pan-KIT inhibitor | / | 1/2 | Recruiting | US | 05160168 |
Linsitinib | IGF-1R inhibitor | / | 2 | Completed | US | 01560260 |
BGJ398 | Pan-FGFR inhibitor | Imatinib | 1b | Completed | US | 02257541 |
Vismodegib | Hedgehog inhibitor | / | 1/2 | Completed | US | 01154452 |
Arsenic trioxide | GI1/2 | / | 1 | Completed | US | 00124605 |
Arsenic trioxide | GI1/2 | / | 1 | Completed | US | 00003630 |
XL820 | GLIPR1 inhibitor | / | 2 | Completed | US | 00570635 |
Vorinostat | HDACI | / | 2 | Completed | Germany | 00918489 |
LBH589 | HDACI | / | 2 | Completed | France | 01136499 |
Selinexor | Selective inhibitor of Nuclear Export | Imatinib | 1/2 | Recruiting | Spain | 04138381 |
BLU-263 | KIT Exon17 D816V | / | 2/3 | Recruiting | US | 04910685 |
Bezuclastinib | KIT exons 9, 11, 17, and 18, including D816V | / | 2 | Recruiting | US | 04996875 |
Bezuclastinib | KIT exons 9, 11, 17, and 18, including D816V | / | 2/3 | Recruiting | US | 05186753 |
Bezuclastinib | KIT exons 9, 11, 17, and 18, including D816V | Pexidartinib/ Sunitinib | 1b/2a | Completed | US | 02401815 |