Table I.
Approved agents targeting important cancer-related genes or their pathways.
| Agent | Target(s) | FDA-approved indication(s) |
|---|---|---|
| Cetuximab (Erbitux) | EGFR (HER1/ERBB1) | Colorectal cancer (KRAS wild-type), squamous cell cancer of the head and neck |
| Panitumumab (Vectibix) | EGFR (HER1/ERBB1) | Colorectal cancer (KRAS wild-type) |
| Regorafenib (Stivarga) | KIT, PDGFRβ, RAF, RET, VEGFR1/2/3 | Colorectal cancer, gastrointestinal stromal tumors |
| Crizotinib (XALKori) | ALK, MET, ROS1 | Non-small cell lung cancer (with ALK fusion or ROS1 gene alteration) |
| Alectinib (Alecensa) | ALK | Non-small cell lung cancer (with ALK fusion) |
| Ceritinib (Zykadia) | ALK | Non-small cell lung cancer (with ALK fusion) |
| Gefitinib (Iressa) | EGFR (HER1/ERBB1) | Non-small cell lung cancer [with EGFR exon 19 deletions or exon 21 substitution (L858R) mutations] |
| Afatinib (Gilotrif) | EGFR (HER1/ERBB1), HER2 (ERBB2/neu) | Non-small cell lung cancer [with EGFR exon 19 deletions or exon 21 substitution (L858R) mutations] |
| Erlotinib (Tarceva) | EGFR (HER1/ERBB1) | Non-small cell lung cancer [with EGFR exon 19 deletions or exon 21 substitution (L858R) mutations], pancreatic cancer |
| Osimertinib (Tagrisso) | EGFR | Non-small cell lung cancer (with EGFR T790M mutation) |
| Necitumumab (Portrazza) | EGFR (HER1/ERBB1) | Squamous non-small cell lung cancer |
| Ponatinib (Iclusig) | ABL, FGFR1-3, FLT3, VEGFR2 | Chronic myelogenous leukemia, acute lymphoblastic leukemia (Philadelphia chromosome-positive) |
| DaBRAFenib (Tafinlar) | BRAF | Melanoma (with BRAF V600 mutation) |
| Vemurafenib (Zelboraf) | BRAF | Melanoma (with BRAF V600 mutation) |
| Vandetanib (Caprelsa) | EGFR (HER1/ERBB1), RET, VEGFR2 | Medullary thyroid cancer |
| Cabozantinib [Cabometyx (tablet), Cometriq (capsule)] | FLT3, KIT, MET, RET, VEGFR2 | Medullary thyroid cancer, renal cell carcinoma |
| Ado-trastuzumab emtansine (Kadcyla) | HER2 (ERBB2/neu) | Breast cancer (HER2+) |
| Pertuzumab (Perjeta) | HER2 (ERBB2/neu) | Breast cancer (HER2+) |
| Trastuzumab (Herceptin) | HER2 (ERBB2/neu) | Breast cancer (HER2+), gastric cancer (HER2+) |
| Lapatinib (Tykerb) | HER2 (ERBB2/neu), EGFR (HER1/ERBB1) | Breast cancer (HER2+) |
| Cobimetinib (Cotellic) | MEK | Melanoma (with BRAF V600E or V600K mutation) |
| Trametinib (Mekinist) | MEK | Melanoma (with BRAF V600 mutation) |
| Everolimus (Afinitor) | mTOR | Pancreatic, gastrointestinal, or lung origin neuroendocrine tumor, renal cell carcinoma, breast cancer (HR+, HER2−), non-resectable subependymal giant cell astrocytoma associated with tuberous sclerosis |
| Temsirolimus (Torisel) | mTOR | Renal cell carcinoma |
| Sorafenib (Nexavar) | VEGFR, PDGFR, KIT, RAF | Hepatocellular carcinoma, thyroid carcinoma, renal cell carcinoma |
The information listed in this table was retrieved from MyCancer Genome Site (www.mycancergenome.org/).