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. 2011 Jun 23;2011:678357. doi: 10.4061/2011/678357

Table 1.

Molecules used in preclinical and clinical trials as RET tyrosine kinase inhibitors.

Compound Trade name Structure Targets Clinical trials Refs
PP1 Zaleplon Pyrazolopyrimidine RET [50]
PP2

ZD6474 Vandetanib Anilinoquinazoline RET; VEGFR; EGFR Phase II [51]

RPI-1 Indolinone RET; MET [52]

SU5416 Sunitinib Butanedioic acid VEGFR-2; PDGFR; c-KIT; RET; CSF-1R Phase II [53, 54]
SU11248

ZD1839 Gefitinib Anilinoquinazoline EGFR Phase II [55, 56]

BAY43-9006 Sorafenib Bis-aryl urea RAF-1; BRAF; VEGFR-2/-3; PDGFR-B; Flt-3; c-KIT; RET Phase II [57, 58]

AMG706 Motesanib diphosphate Diphosphate salt VEGFR; PDGFR; KIT; RET Phase II [59, 60]

AG-013736 Axitinib Benzamide RET; VEGFR; PDGFR; c-KIT Phase II [61]

XL184/XL880 VEGFR2; RET and MET Phase III [***]

[***] Eder et al. [62]. LoRusso et al. [63]. Ross et al. [64]. Salgia et al. [65].