| | Drug (brand name, company) | Target | Approved | Clinical trials with single treatment | Indication |
| | Bevacizumab (Avastin, Genentech/Roche) | Monoclonal antibody against VEGFA | mCRC, mRCC, NSCLC, metastatic HER2-negative breast cancer, glioblastoma | Phase I, II | Multiple solid tumors (e.g., RCC, BC, pancreatic, prostate, ovarian, brain cancers) and hematologic malignancies (e.g., MM) |
| | Sunitinib, SU11248 (Sutent, Pfizer) | TKI of VEGFR 1–3, PDGFRα/β, c-Kit, Flt3, RET, CSF-1R | mRCC, GIST | Phase I | Multiple solid tumors (e.g., RCC, BC, melanoma, lung) |
| | Pazopanib (Votrient, GlaxoSmithKline) | TKI of VEGFR 1–3, PDGFRα/β, c-kit tyrosine kinases | mRCC | Phase I, II | Multiple solid tumors (e.g., BC, RCC, ovarian, lung) and others (e.g., lymphoma) |
| | Sorafenib, BAY43-9006 (Nexavar, Bayer) | TKI of Multiple cell surface kinases (VEGFR 1–3, RET, PDGFRβ, Flt-3, c-Kit, CSF-1) and intracellular kinases (CRAF, BRAF, mutant BRAF) | mRCC, unresectable hepatocellular carcinoma | Phase I, II | Multiple solid tumors (e.g., RCC, BC, melanoma, lung cancers) and hematologic malignancies (e.g., MM) |
| | Vandetanib, ZD6474 (Zactima, AstraZeneca) | TKI of VEGFR, EGFR and RET | Metastatic medullary thyroid cancer | Phase I, II | NSCLC, RCC, glioblastoma |
| | Bortezomib, PS-341 (Velcade, Millennium Pharmaceuticals) | 26S proteasome inhibitor | MM, relapsed mantle cell lymphoma | Phase I, II | MM, lymphoma, leukemia and multiple solid tumors (e.g., RCC, BC, lung, prostate) |
| | Temsirolimus (Torisel, Wyeth) | mTOR inhibitor | mRCC | Phase I, II | Multiple solid tumors (e.g., RCC, BC, melanoma, prostate, liver cancers) and hematologic malignancies (e.g., lymphoma) |
| | Everolimus, RAD001 (Afinitor, Novartis) | mTOR inhibitor | Advanced renal cell carcinoma | Phase I, II | Multiple solid tumors (e.g., BC, pancreatic, gastric cancers) and lymphoma |
| | Thalidomide (Thalomid, Celgene) | Angiogenesis inhibitor, multiple | MM |
*
| MM |
| | Lenalidomide, CC-5013 (Revlimid, Celgene) | Angiogenesis inhibitor, Thalidomide derivative | MM | Phase I, II | MM, lymphoma, chronic lymphocytic leukemia, and multiple solid tumors (e.g., CRC, ovarian) |
| | Pomalidomide, CC-4047 (Actimid, Celgene) | Angiogenesis inhibitor, Thalidomide derivative | No yet approved | Phase I | MM, Lymphoma |
| | Aflibercept, VEGF-trap (ZALTRAP, Sanofi-Aventis and Regeneron) | Decoy receptor for all VEGF-A isoforms | No yet approved |
*
| mCRC, RCC, Ovarian, NSCLC, prostate cancers, lymphoma, leukemia |
| | Axitinib, AG-013736 (Pfizer) | TKI of VEGFR 1–3, PDGFRβ, c-KIT and CSF-1 | No yet approved | Phase I | mRCC, BC, NSCLC, metastatic pancreatic cancer, GIST, lung cancer, thyroid cancer |
| | Icrucumab, IMC-18F1 (ImClone) | Monoclonal antibody against VEGFR-1 | No yet approved | Phase I | Advanced solid tumors, (e.g., CRC, BC, carcinoma of urinary tract) |
| | Ramucirumab, IMC-1121b (ImClone) | Monoclonal antibody against VEGFR-2 | No yet approved |
*
| CRC, BC, mRCC, Advanced liver, gastric, prostate, ovarian, and NSCL cancers, melanoma |
| | Vatalanib, PTK787 (Novartis) | TKI of VEGFR 1–3, PDGFRα/β, and c-KIT | Not yet approved |
*
| Multiple solid tumors (e.g., CRC, glioblastoma, NSCLCs) and hematologic malignancies (e.g., leukemia) |
| | Enzastaurin, LY317615.HCl (Eli Lilly) | PKC inhibitor | Not yet approved |
*
| BC, mCRC, Brain tumor, advanced NSCL, glioblastoma, lymphoma |
| | Cediranib, AZD2171 (Recentin, AstraZeneca) | TKI of VEGFR 1–3 | Not yet approved | Phase I | RCC, CRC, BC, ovarian, prostate cancer, lung, brain, head and neck cancers, glioblastoma, melanoma |
| | Vectibix, panitumumab (Amgen) | EGFR | mCRC | Phase I, II | mCRC, pancreatic, HNSCC, NSCLC, lung |
| | Erbitux, cetuximab, (Imclone, Bristol-Myers Squibb) | EGFR | mCRC | Phase I, II | mCRC, HSNCC, brain, MM, lung, pancreatic, liver |
| | Trastuzumab, herceptin (Genentech) | HER2 receptor | Gastric cancer, HER2 positive BC | Phase I, II | BC, gastric |
| | Tykerb, lapatinib (GlaxoSmithKline) | EGFR and HER2 receptor | BC | Phase I, II | BC, CRC, lung, HNSCC, pancreatic, melanoma |
| | Tamoxifen, Novadex, Istubal, Valodex (AstraZeneca) | Estrogen receptor | BC | Phase I, II | BC, bladder, melanoma, prostate |
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