Sunitinib: a novel tyrosine kinase inhibitor. A brief review of its therapeutic potential in the treatment of renal carcinoma and gastrointestinal stromal tumors (GIST)

Figures & data

Figure 1 Mechanism of action of sunitinib.

Abbreviations: FLT3, fetal liver tyrosine kinase receptor 3; KIT, stem cell factor receptor; PDGF, platelet-derived growth factor; PDGFR, platelet-derived growth factor receptors; SCF stem-cell factor; VEGF, vascular endothelial growth factor;VEGER, vascular endothelial growth factor receptors.

Table 1 Efficacy of sunitinib in trials with patients treated for renal cell carcinoma and GIST

	RCC			GIST
	Supportive (Motzer, Michaelson, et al 2006) (n = 63)	Pivotal (Motzer, Rini, et al 2006) (n = 106)	Phase III (Motzer, Hutson, et al 2006) (n = 374)	Phase I/II (Maki et al 2005) (n = 97)	Phase III (Demetri et al 2005) (n = 207)
ORR	25 (40%)	46 (34%)	103 (31%)	8 (8%)	17 (8%)
SD	18 (28%)	24 (29%)	160 (48%)	36 (37%)	37 (18%)
TTP	8.7 months	8.3 months	11 months	7.8 months	6.3 months
OS	16.4 months	NR	NR	19.8 months	NR

Abbreviations: GIST, gastrointestinal stromal tumors; NR, not reached; ORR, overall response rate; OS, overall survival; RCC, renal cell carcinoma; SD, stable disease;TTP, time to progression.

Table 2 Grade 3 or 4 toxicity of sunitinib in trials with patients treated for renal cell carcinoma and GIST

	RCC			GIST
	Supportive (Motzer, Michaelson, et al 2006) (n = 63)	Pivotal (Motzer, Rini, et al 2006) (n = 106)	Phase III (Motzer, Hutson, et al 2006) (n = 374)	Phase I/II (Maki et al 2005) (n = 97)	Phase III (Demetri et al 2005) (n = 207)
Nonhematological
Fatigue	11%	8%	7%	10%	7%
Diarrhea	3%	3%	5%	7%	4%
Nausea	3%	0%	3%	4%	1%
Dermatitis	2%	5%	5%	7%	5%
Stomatitis	2%	5%	1%	3%	NA
Asymptomatic lipase increase	21%	15%	4%	13%	NA
Hypertension	2%	6%	8%	17%	4%
Hematological
Neutropenia	13%	13%	11%	NA	8%
Anemia	10%	6%	3%	NA	4%
Thrombocytopenia	0%	6%	8%	NA	5%

Abbreviations: GIST, gastrointestinal stromal tumor; NA, not available; RCC, renal cell carcinoma.

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