TABLE 1 Molecular-targeted therapies discussed in this Review and their targets.
From the following article:
Drug Insight: gastrointestinal and hepatic adverse effects of molecular-targeted agents in cancer therapy
Yohann Loriot, Gabriel Perlemuter, David Malka, Frédérique Penault-Lorca, Valérie Boige, Eric Deutsch, Christophe Massard, Jean Pierre Armand and Jean-Charles Soria
BACK TO ARTICLE| Drug | Development phase | Main area of development | Class of agent | Molecular target |
|---|---|---|---|---|
Abbreviations: GIST, gastrointestinal stromal tumors; HER, human epidermal growth factor receptor; MBC, metastatic breast cancer; mTOR, mammalian target of rapamycin; PDGFR, platelet-derived growth factor receptor; VEGFR, vascular endothelial growth factor receptor. | ||||
| Erlotinib (Tarceva®, OSI Pharmaceuticals, Inc., Melville, NY) | Approved | Non-small-cell lung cancer | Kinase inhibitor | HER1 |
| Gefitinib (Iressa®, AstraZeneca, London, UK) | Phase III | Non-small-cell lung cancer | Kinase inhibitor | HER1 |
| Cetuximab (Erbitux®, ImClone Systems Incorporated, New York, NY) | Approved | Colorectal and head and neck cancer | Monoclonal antibody | HER1 |
| Pertuzumab (Omnitary®, Genentech Inc.) | Phase II | Breast cancer | Monoclonal antibody | HER2 |
| Lapatinib (Tykerb®, GlaxoSmithKline, Carrigaline, Ireland) | Approved for MBC HER2+; Phase III | Breast, prostate, and esophageal cancer | Kinase inhibitor | HER1 and HER2 |
| HKI 272 (Wyeth Pharmaceuticals) | Phase II | Non-small-cell lung cancer | Kinase inhibitor | HER1 and HER2 |
| Trastuzumab (Herceptin®, Genentech, Inc., South San Francisco, CA) | Approved | Breast cancer | Monoclonal antibody | HER2 |
| Sorafenib (Nexavar®, Bayer Aktiengesellschaft, Leverkusen-Bayerwerk, Germay) | Approved | Renal cell carcinoma | Kinase inhibitor | VEGFR3, RAF, PDGFR  |
| Sunitinib (Sutent®, Pharmacia and Upjohn Company, Morris Plains, NJ) | Approved; Phase III | Renal cell carcinoma and GIST resistant to imatinib | Kinase inhibitor | VEGFR3, RAF, PDGFR |
| Vatalanib (PTK 787, Novartis Pharmaceuticals, East Hanover, NJ) | Phase II | Prostate and pancreatic cancer | Kinase inhibitor | VEGFR1–3, PDGFR |
| Bevacizumab (Avastin®, Genentech, Inc.) | Approved; Phase III | Lung, breast, and colorectal cancer | Monoclonal antibody | VEGF |
| Everolimus (Certican®, Novartis AG Aktiengesellschaft, Basel, Switzerland) | Phase II | Lung, breast, and colorectal cancer | Kinase inhibitor | mTOR |
| Temsirolimus (CCI-779; Torisel®, Wyeth, Madison, NJ) | Phase III | Lymphoma, breast cancer, melanoma, lung cancer, and renal cell carcinoma | Kinase inhibitor | mTOR |
| Imatinib (Gleevec®, Novartis) | Approved | GIST and chronic myelogenous leukemia | Kinase inhibitor | BCR–ABL, KIT, PDGFR  |
| Nilotinib (Tasigna®, Novartis) | Phase III | Chronic myelogenous leukemia | Kinase inhibitor | BCR–ABL |
| Tipifarnib (Zarnestra®, Johnson & Johnson, New Brunswick, NJ) | Phase III | Leukemia and breast cancer | Kinase inhibitor | Farnesyltransferase |
| Alvocidib (flavopiridol) | Phase II | Leukemia and pancreatic cancer | Kinase inhibitor | Cyclin-dependent kinase |
| Gemtuzumab (Mylotarg®, Wyeth Pharmaceuticals) | Approved | Acute myeloid leukemia | Monoclonal antibody | CD33 |
| Bortezomib (Velcade®, Millenium Pharmaceuticals, Inc., Cambridge, MA) | Approved | Multiple myeloma | Proteasome inhibitor | Proteasomes |