TKI Targets/Indications

Question 1

Sorafenib

Answer 1

Nexavar, Bayer

Targets: VEGFR1-3, TIE2, PDGFR, FGFR, BRAF, CRAF, KIT, FLT-3

Renal Cell Carcinoma (2005)
Hepatocellular Carcinoma (2007)
Differentiated Thyroid Cancer (2013)

Question 2

Sunitinib

Answer 2

Sutent, Pfizer Inc

Targets: VEGFR-1–2, PDGFR, FLT3, KIT

GIST after disease progression on or intolerance to imatinib
(2006)
mRCC (2006)
unresectable or metastatic pancreatic neuroendocrine tumor (2011)
Adjuvant treatment for RCC (2017)

Question 3

Vandetanib

Answer 3

Caprelsa, AstraZeneca

EGFR, VEGFR2-3, RET

Unresectable or metastatic MTC (2011)

Question 4

Regorafenib

Answer 4

Stivarga, Bayer

VEGFR1-3, TIE2, PDGFR, FGFR, BRAF, KIT, RET

Recurrent or metastatic CRC (2012)

Locally advanced/unresectable or metastatic GIST previously treated with imatinib and sunitinib (2013)

Advanced HCC who has been previously treated with sorafenib (2017)

Question 5

Lenvatinib

Answer 5

Lenvima, Eisai Inc

VEGFR1-3, PDGFR, FGFR 1–4, RET, KIT

Radioactive iodine refractory DTC (2015)
2L combined with everolimus for mRCC (2016)
1L unresectable HCC (2018)
Combined with pembrolizumab for certain types of endometrial cancer (2019)
1L combined with pembrolizumab for advanced RCC (2021)

Question 6

Cabozantinib

Answer 6

Cometriq/Cabometyx, Exelixis Inc

VEGFR1-3, MET, ROS1, RET, AXL, NTRK, KIT

Progressive metastatic MTC (COMETRIQ capsules 2012)

1L mRCC + nivolumab (2017)
HCC who has been previously treated with sorafenib (2019)
DTC that has progressed following prior VEGFR-targeted therapy (2021)

Question 7

Axitinib

Answer 7

Inlyta, Pfizer Inc
VEGFR1-3, PDGFR, KIT, FLT-3

2L advanced RCC (2012)

1L combined with pembrolizumab for advanced RCC (2019)

1L combined with avalumab (BAVENCIO) for advanced RCC (2019)

Question 8

Pazopanib

Answer 8

Votrient, GlaxoSmithKline

VEGFR, PDGFR, KIT

Advanced RCC (2009)

 Advanced soft tissue sarcoma (STS) who has previously received chemotherapy (2012)