| Compound (code or generic name) | Class | Target(s) | Mechanism of action | Highest Phase |
| Erlotinib | Kinase inhibitor | EGFR | EGFR Inhibitor | Launched-2004 |
| Lapatinib | Kinase inhibitor | EGFR, HER2 | EGFR and HER2 Inhibitor | Launched-2007 |
| PHA-665752 | Kinase inhibitor | c-MET | c-MET Inhibitor | Preclinical |
| PF-2341066 | Kinase inhibitor | c-MET, ALK | c-MET and ALK Inhibitor | Launched-2011 |
| TAE684 | Kinase inhibitor | ALK | ALK Inhibitor | Preclinical |
| Vandetanib | Kinase inhibitor | Abl, EGFR, Flt3, C-KIT, RET, VEGFR-1, KDR, FLT4 | Multi-kinase inhibitor | Launched-2011 |
| Nilotinib | Kinase inhibitor | Abl/Bcr-Abl | Abl Inhibitor | Launched-2007 |
| AZD0530 | Kinase inhibitor | Src, Abl/Bcr-Abl, EGFR | Src and Abl inhibitor | Phase II |
| Sorafenib | Kinase inhibitor | Flt3, C-KIT, PDGFRbeta, RET, Raf kinase B, Raf kinase C, VEGFR-1, KDR, FLT4 | Multi-kinase inhibitor | Launched-2005 |
| TKI258 | Kinase inhibitor | EGFR, FGFR1, PDGFRbeta, VEGFR-1, KDR | Multi-kinase inhibitor | Phase III |
| PD-0332991 | Kinase inhibitor | CDK4/6 | CDK4/6 Inhibitor | Phase II |
| AEW541 | Kinase inhibitor | IGF-1R | IGF-1R Inhibitor | Preclinical |
| RAF265 | Kinase inhibitor | Raf kinase B, KDR | Raf kinase B and KDR Inhibitor | Phase I |
| PLX4720 | Kinase inhibitor | RAF | Raf kinase B Inhibitor | Preclinical |
| PD-0325901 | Kinase inhibitor | MEK | MEK1 and MEK2 Inhibitor | Discontinued |
| AZD6244 | Kinase inhibitor | MEK | MEK1 and MEK2 Inhibitor | Phase II |
| Nutlin-3 | Other targeted therapies | MDM2 | MDM2 Inhibitor | Preclinical |
| LBW242 | Other targeted therapies | IAP | Inhibitor of Apoptosis Proteins (IAP) Inhibitor | Preclinical |
| 17-AAG | Other targeted therapies | HSP90 | Heat Shock Protein 90 (hsp90) Inhibitor | Phase III |
| L-685458 | Other targeted therapies | Gamma Secretase | gamma-Secretase Inhibitor | Preclinical |
| Panobinostat | Other targeted therapies | HDAC | Histone Deacetylase (HDAC) Inhibitor | Pre-Registered |
| Paclitaxel | Cytotoxic | beta-tubulin | Microtubule-Stabilizing Agents | Launched-1993 |
| Irinotecan | Cytotoxic | Topoisomerase I | DNA Topoisomerase I Inhibitor | Launched-1994 |
| Topotecan | Cytotoxic | Topoisomerase I | DNA Topoisomerase I Inhibitor | Launched-1996 |
