| Category | Name | Targets | Uses |
| TKI | Dasatinib | BCR-ABL, SRC family, c-KIT, PDGFR | Chronic myeloid leukemia (CML), acute lymphocytic leukemia | Erlotinib | EGFR | Non-small-cell lung cancer (NSCLC), pancreatic cancer | Gefitinib | EGFR | NSCLC | Imatinib | BCR-ABL, c-KIT, PDGFR | Acute lymphocytic leukemia, CML, gastrointestinal stromal tumor | Lapatinib | HER2/neu, EGFR | Breast cancer | Sorafenib | BRAF, VEGFR, EGFR, PDGFR | Renal cell carcinoma (RCC), hepatocellular carcinoma (HCC) | Sunitinib | VEGFR, PDGFR, c-KIT, FLT3 | RCC, gastrointestinal stromal tumor | Temsirolimus | mTOR, VEGF | RCC | Pazopanib | VEGFR-1, VEGFR-2, VEGFR-3, PDGF-α/β, and c-KIT | RCC | Nilotinib | BCR-ABL | CML | Crizotinib | ALK, HGFR | NSCLC | Vemurafenib | BRAF | Late-stage melanoma | mAb | Alemtuzumab | CD52 | Chronic lymphocytic leukemia | Bevacizumab | VEGF | Colorectal cancer, NSCLC, RCC | Cetuximab | EFGR | Colorectal cancer, head and neck cancer | Gemtuzumab ozogamicin | CD33 | Relapsed acute myeloid leukemia | Ibritumomab tiuxetan | CD20 | Non-Hodgkin’s lymphoma (NHL) (with yttrium-90 or indium-111) | Panitumumab | EGFR | Colorectal cancer | Rituximab | CD20 | NHL | Tositumomab | CD20 | NHL (with iodine-131) | Trastuzumab | HER2/neu | Breast cancer with HER2/neu overexpression | Ipilimumab | CTLA-4 | Late-stage melanoma |
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