Table 7.
Targets | Molecular alterations | Molecularly targeted agents |
---|---|---|
KIT, ABL 1/2, RET | Activating mutation† or amplification* | Imatinib 400 mg qd PO |
PI3KCA, AKT1 AKT2, 3, mTOR, RAPTOR, RICTOR PTEN STK11 INPP4B |
Activating mutation or amplification Amplification Amplification Homozygous deletion or heterozygous deletion + inactivating mutation or heterozygous deletion + IHC confirmation Homozygous deletion or heterozygous deletion + inactivating mutation Homozygous deletion |
Everolimus 10 mg qd PO |
BRAF | Activating mutation or amplification Abirterone 1000 mg qd PO | Vemurafenib 960 mg bid PO |
PDGFRA/B, FLT3 | Activating mutation or amplification | Sorafenib 400 mg bid PO |
EGFR | Activating mutation or amplification | Erlotinib 150 mg qd PO |
ERBB2/HER2 | Activating mutation or amplification |
Lapatinib 1000 mg qd PO + Trastuzumab 8 mg/kg IV followed by 6 mg/kg IV q3w |
SRC EPHA2, LCK, YES1 |
Activating mutation or amplification Amplification |
Dasatinib 70 mg bid PO |
ER, PR | Protein expression > 10% |
Tamoxifen 20 mg qd PO (or letrozole 2–5 mg qd PO if contraindicated) |
AR | Protein expression > 10% | Abiraterone 1000 mg qd PO |