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

Table 3 Novel agents for GIST

Study Drug	Class of Drug	Disease	Dosage	Clinical Trial	No. of patients	Response	Reference
Everolimus	mTOR inhibitor	TKI resistant	Everolimus 2.5 mg/day with Imatinib	Phase 1/2	58	PFS 29%	[57]
Everolimus	mTOR inhibitor	Refractory GIST	10 mg/day	Phase 1/2	15	ORR27%	[59]
Sirolimus	mTOR inhibitor	TKI resistant with PDGFRA-D842V.	Sirolimus (2–3 mg/day) with a TKI.	Retrospective	3	Signs of antitumor activity.	[60]
Ganetespib	Hsp90 inhibitor	Following failure of prior therapy	200 mg/m2 IV qweek for 3 wks of a 28 day cycle.	Phase 2	26	SD 52%	[61]
Retaspimycin (IPI 504)	Hsp90 inhibitor	Following failure of TKIs	400 mg/m2 weekly for 2 doses in 21‒day cycles	Phase 3	47	Too toxic	[62]
Perifosine	Akt pathway inhibitor	Imatinib-resistant	2 doses of perifosine - 100 mg daily or 900 mg qweekly with daily imatnib	Phase 2	41	Minimal activity	[63]

Abbreviations: SD stable disease; PFS progression free survival; ORR overall response rate.

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