Table 2. Common Genomic Alterations in Breast Cancer and Existing Therapeutic Options.
PI3-Kinase Pathway | ERBB2/ HER2 |
Fibroblast Growth Factor |
Insulin-Like Growth Factor |
Estrogen Receptor |
BRCA Mutation |
c-MET | ||||
---|---|---|---|---|---|---|---|---|---|---|
| ||||||||||
PIK3CA (34%), PIK3R1 (2%), AKT1 (2%) | ERBB2 (14%) | FGFR1 (13%), FGFR2 (3%), FGFR3 (2%) |
IGF1R (6%), IGF2R (3%), IGF1 (1%) |
ESR1 (4%) | BRCA1 (4%), BRCA2 (4%) |
MET (2%) | ||||
| ||||||||||
Inhibitors | PI3K Inhibitors | mTOR inhibitors | AKT inhibitors | PI3K/mTOR Inhibitors | PARP Inhibitors | |||||
Buparlisib (BKM120) | Everolimus | GDC-0068 | BGT226 | Trastuzumab | AZD4547 | BMS-754807 | Tamoxifen | Olaparib | SGX523 | |
Pictilisib (GDC-0941) | Temsirolimus | MK2206 | GDC-0980 | T-DM1 | BGJ398 | Cixutumumab | Toremifene | Veliparib | INC280 | |
BYL120 | AZD8055 | GSK2141795 | PKI-587 | Pertuzumab | Dovitinib | Dalotuzumab | Anastrazole | Rucaparib | Tivantinib | |
GDC-0032 | INK128 | XL765 | Lapatinib | Lucitinib (E-3810)** | Figitumumab | Letrozole | BMN-673 | PF-02341066* | ||
INK1117 | Afatinib | HGS1036 | Ganitumab | Exemestane | CEP-9722 | Cabozantinib** | ||||
PF-04691502 | Canertinib | BAY1163877 | Linsitinib | Fulvestrant | E7016 | GSK1363089 | ||||
PX-866 | Dacomitinib | GSK3052230 | MEDI-573 | INO-1001 | ARQ197 | |||||
XL147 | Neratinib | MK4827 | ||||||||
MM-121 |
Also inhibits ALK
Also inhibits VEGFR