Table 2.
Drugs in clinical development against pathways identified in genomic/proteomic studies
| Receptor Tyrosine Kinases | ||
| Pan-ErbB receptors | ||
| CI-1033 | Pfizer | phase II[57,58] |
| BIBW-2992 | Boehringer Ingelheim | phase II[57,59] |
| Neratinib | Wyeth-Ayerst | phase III[60,61] |
| MET | ||
| MK-2461 | Merck | phase I/II[62] |
| XL184 | Exelixis | phase II/III[62] |
| MetMAb | Genentech | phase I[63] |
| FGFR | ||
| MK-2461 | Merck | phase I/II[62] |
| Brivanib | BMS | phase II[64] |
| K-RAS-RAF | ||
| PLX4032 | Plexxikon Inc/Roche | phase I[65] |
| PI3K-AKT Inhibitors-mTOR | ||
| Dual PI3K-mTOR | ||
| BEZ235 | Novartis | phase I/II[30,66,67] |
| XL765 | Exelixis | phase I[68] |
| SF1126 | Semafore | phase I/II[68,69] |
| BGT226 | Novartis | phase II[68] |
| PI3K Inhibitors | ||
| XL147 | Exelixis | phase I[68] |
| BKM120 | Novartis | phase I[68] |
| GDC0941 | Genentech | phase I[70,71] |
| AKT inhibitors | ||
| Perifosine | Keryx | phsae I/II[72-74] |
| GSK690693 | GSK | phase I[75-77] |
| MK2206 | Merck | phase I[68] |
| mTOR | ||
| OSI027 | OSI Pharmaceuticals | phase I[68] |
| AZD8055 | AstraZeneca | phase I/II[68] |
| MAPK inhibitors | ||
| MEK Inhibitors | ||
| CI-1040 | Pfizer | phase I/II[78,79] |
| AZD6244 | AstraZeneca | phase I/II[80,81] |
| XL518 | Genentech | phase I[71] |
| Cell Cycle | ||
| Flavopiridol | Sanofi-aventis | phase II/III[82] |
| SNS-032 | BMS | phase I/II[31] |
| R-547 | Roche | Phase I/II[83,84] |
| Seleciclib | Cyclacel Pharmaceuticals | Phase I/II[85] |
| Histone Deacetylase inhibitors | ||
| Vorinostat (SAHA) | Merck | Phase I/II[86] |
| Romidepsin | Gloucester Pharmaceuticals | Phase I/II[87,88] |
| MGCD0103 | MethylGene, Inc | phase I/II[89] |
| LBH589 | Novartis | phase I/II[90,91] |
| Demethylating agents | ||
| Azacitidine | Celgene | approved[92,93] |
| Decitabine | Eisai Pharmaceuticals | approved[94] |
| DNA repair | ||
| PARP | ||
| Olaparib | KuDOS Pharmaceuticals/AstraZeneca | phase II[95] |
| AG-014699 | Pfizer | phase II[96] |
| ATM | ||
| KU-55933 | KuDOS Pharmaceuticals | preclinical[97] |
| Matrix Metalloproteinases | ||
| Neovastat | Æterna Laboratories | phase III[98,99] |
| Prinomastat | Pfizer | phase III[98,100,101] |