Table 1.
Selected FDA Approved Targeted Oral Anticancer Medications.
| Generic Name | Trade Name | Year Approved* | Target Gene or Receptor | Indication |
|---|---|---|---|---|
| Dasatinib | Sprycell | 2006 | BCR-ABL | Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) |
| Imatinib | Gleevec | 2001 | BCR-ABL | Ph+ CML Gastrointestinal stromal tumors (GIST) |
| Nilotinib | Tasigna | 2007 | BCR-ABL | Ph+ CML |
| Bosutinib | Bosulif | 2012 | BCR-ABL, Src | Ph+ CML |
| Ponatinib | Iclusig | 2012 | BCR-ABL | ALL and CML |
| Vemurafenib | Zelboraf | 2012 | BRAF V600E | Melanoma |
| Vismodegib | Erivedge | 2012 | SMO | Basal cell carcinoma |
| Ruxolitinib | Jakafi | 2011 | JAK1/2 | Myelofibrosis |
| Gefinitib | Iressa | 2003 | EGFR | Non-small cell lung cancer (NSCLC) |
| Erlotinib | Tarceva | 2004 | EGFR | NSCLC and pancreatic cancer |
| Crizotinib | Xalkori | 2011 | EML4-ALK | NSCLC |
| Abiraterone | Zytiga | 2011 | CYP17A1 | Prostate cancer |
| Enzalutamide | Xtandi | 2012 | AR | Prostate cancer |
| Regorafenib | Stivarga | 2012 | VEGFR2-TIE2 | Colon cancer |
| Lenalidomide | Revlimid | 2006 | Anti-tumor, immunomodulatory | Multiple myeloma |
| Lapatinib | Tykerb | 2007 | EGFR, HER2/neu | Breast cancer |
| Sunitinib | Sutent | 2006 | PDGFR, VEGF, cKIT, RET, CSF-1R, flt3 | GIST Renal cell carcinoma (RCC) |
| Sorafenib | Nexavar | 2006 | VEGFR, PDGFR, C-Raf, B-Raf, MAP Kinase, cKIT | RCC Hepatocellular carcinoma |
| Pazopanib | Votrient | 2009 | VEGF, c-kit, PDGFR | RCC Soft tissue sarcoma |
| Axitinib | Inlyta | 2012 | VEGFR1–3, PDGFR, cKIT | RCC |
| Everolimus | Afinitor | 2009 | mTOR | Breast, RCC, soft tissue sarcoma and renal angiomyolipoma |
Abbreviations: BCR-ABL, fusion of Abelson (Abl) tyrosine kinase gene at chromosome 9 and break point cluster (Bcr) gene at chromosome 22; EGFR, epidermal growth factor receptor; EML4-ALK, rearrangement of echinoderm microtubule-associated protein-like 4anaplastic lymphoma kinase; HER2/neu, one of four membrane proteins in EGFR family; PDGFR, platelet-derived growth factor receptor; VEGFR, vascular endothelial growth factor receptor; RET, proto-oncogene, encodes receptor tyrosine kinase for the neurotrophic factor family; CSF-1R, colony stimulating factor 1; flt3, encodes receptor tyrosine kinase that regulates hematopoiesis; MAP Kinase, family of serine/threonine proteins responsible for regulating cellular activities, such as apoptosis; c-kit, tyrosine kinase stem cell factor receptor; SMO, Smoothened, a transmembrane protein involved in Hedgehog signal transduction; mTOR, mammalian target of rapamycin inhibitor; BRAF, gene encoding for B-Raf, member of Raf kinase family
year approved for initial indication.