Exploration of Targeted Anti-tumor Therapy

Table 1.

The half-life of the main drugs used in clinical practice to treat advanced thyroid cancer and the half-maximal inhibitory concentration (IC₅₀) of these drugs against the most common tyrosine kinase receptors

Drug	Half-life	RET	PDGFR	FGFR	EGFR	VEGFR	BRAF^V600E	NTRK	Other molecular targets
Lenvatinib	28 h	35 nM	39 nM	46 nM	-	22; 4; 5.2 nM*	-	-	c-KIT, KIF5B-RET, CCDC6-RET, NcoA4-RET
Sorafenib	25–48 h	47 μM	57 μM	-	-	9; 28; 7 μM *	38 μM	-	c-KIT, FLT3
Cabozantinib	55 h	4 nM	234 nM	-	-	12; 0.035; 6 nM*	-	-	c-KIT, MET, KIF5B-RET
Selpercatinib	32 h	0.4 nM	-	-	-	0.92–67.8 nM**	-	-	-
Vandetanib	19 days	130 nM	-	-	500 nM	40; 110 nM^#	-	-	RET-KIF5B
Pralsetinib	14.7 h	0.4 nM	-	-	-	35 nM°	-	-	KIF5B-RET, CCDC6-RET, FLT3
Entrectinib	20–40 h	-	-	-	-	-	-	0.002; 0.00057; 0.0011 nM^{^}	ROS, ALK
Larotrectinib	3 h	-	-	-	-	-	-	6.5; 8.1; 10.6 nM^{^}	-
Dabrafenib	8 h	-	-	-	-	-	0.5 nM	-	-
Trametinib	127 h	-	-	-	-	-	0.48 nM	-	MEK

Return to article view

RET: REarranged during Transfection receptor; PDGFR: platelet-derived growth factor receptor; FGFR: fibroblast growth factor receptor; EGFR: epidermal growth factor receptor; VEGFR: vascular endothelial growth factor receptor; BRAF^V600E: valine to the glutamic acid substitution of BRAF gene; NTRK: neurotrophic tyrosine receptor kinase; KIT: v-kit Hardy Zuckerman 4 feline sarcoma viral oncogene; KIF5B-RET, CCDC6-RET and NcoA4-RET: RET gene fusions; FLT3: Fms-like tyrosine kinase 3; MET: hepatocyte growth factor (HGF) receptor; MEK: mitogen-activated protein kinase; ROS: reactive oxygen species; ALK: anaplastic lymphoma kinase; - : no pharmacological action against these tyrosine kinase receptors. ^* respectively for VEGFR1, VEGFR2 and VEGFR3; ^** range of inhibition on VEGFR1 and VEGFR3; ^# respectively for VEGFR2 and VEGFR3; ° only for VEGFR2; ^ respectively for NTRK-1, NTRK-2 and NTRK-3