Tyrosine Kinase Inhibitors (TKIs)

Question 1

Erlotinib
Gefitinib
Brigatinib

Answer 1

Type: EGFR TKI

MOA: blocks EGFR TK

AE:
1. Rash* (up to 75%)
2. Diarrhea*
3. Steven-Johnson Syndrome

*Class effects of EGF targeted therapies

Question 2

Lapatinib

Answer 2

Type: HER-2/EGFR TKI

MOA: blocks HER-2 (and EGFR) TK

AE:
1. Cardiotoxic (decreases LVEF)
2. Hepatotoxic

Question 3

Imatinib
Dasatinib
Nilotinib

Answer 3

Type: BCR-ABL TKI

MOA: blocks BCR-ABL TK

AE:
1. GI AE
2. Hepatotoxicity
3. QT prolongation (nilotinib) (BBW)

Question 4

Suntinib

Answer 4

Type: VEGFR TKI

MOA: blocks VEGFR TK

AE:
1. Hepatotoxicity (BBW)
2. HTN* –> VEGF stimulates NO Production
3. Thromboembolism*

*Class effects of VEGF targeted therapies