Molecular basis and management of gastrointestinal stromal tumors

Table 4 Novel agents being developed for GIST therapy

Agent	Molecular target	Clinical benefit in pilot studies
Kinase inhibitors
Nilotinib	KIT, PDGFRs, bcr-abl	46%-77%[69,70]
Sorafenib	Raf, KIT, PDGFR-B, VEGFR, FLT3, RET	71%[71]
Dasatinib	Src, ABL, KIT, PDGFRs	Phase II ongoing in advanced sarcomas and accepting patients
AZD2171	VEGFR, KIT, PDGFRs	Phase II ongoing, not recruiting
OSI-930	VEGFR, KIT	Phase I ongoing, not recruiting
PTK787	VEGFR, KIT, PDGFRs	67%[74]
XL820	KIT, PDGFR-B, VEGFR	Phase II ongoing, not recruiting
AMG706	VEGFR, KIT, PDGFRs, RET	24%-27%[75,76]
mTOR and AKT inhibitors
Perifosine	AKT	Phase II ongoing in combination with imatinib
Everolimus	mTOR	26%[73]
Temsirolimus	mTOR	Phase II ongoing, closed recruitment
Others
IPI-504	Hsp90	78%[72], phase III ended due to safety concerns
Flavopiridol	Transcription inhibitor	Phase I ongoing in combination with doxorubicin

Clinical benefit is defined as complete or partial response or stable disease.