Table 2 |
||||
|
Targeted therapeutic agents in NSCLC |
||||
|
Class |
Agent |
Target |
Company |
Stage of development in NSCLC |
|
|
||||
|
First Generation TKI |
||||
|
|
||||
|
Gefitinib |
EGFR (reversable) |
AstraZeneca |
Approved for a restricted group of patients |
|
|
|
||||
|
Erlotinib |
EGFR (reversable) |
OSI, Genentec and Roche |
Approved |
|
|
|
||||
|
Second Generation TKI |
||||
|
|
||||
|
EKB-569 |
EGFR (irreversible) |
Wyeth |
Phase II |
|
|
|
||||
|
CL-387,785 |
EGFR (irreversible) |
Wyeth |
Preclinical |
|
|
|
||||
|
Multi-Targeted TKI |
||||
|
|
||||
|
HKI-272 |
EGFR, HER2 (irreversible) |
Wyeth |
Phase I/II |
|
|
|
||||
|
Canertinib |
EGFR, HER2, HER4 (irreversible) |
Pfizer Inc. |
Phsae II |
|
|
|
||||
|
BIBW 2992 |
EGFR, HER2 (irreversible) |
Boehringer Ingelheim |
Phase I/II |
|
|
|
||||
|
HKI-357 |
EGFR, HER2 (irreversible) |
Wyeth |
Preclinical |
|
|
|
||||
|
Vandetanib, ZD-6474 |
EGFR, HER2, FLT1, KDR (reversible) |
AtraZeneca |
Phase III |
|
|
|
||||
|
XL647 |
EGFR, HER2, KDR, EPHB4 (reversible) |
Exelexis |
Phase II |
|
|
|
||||
|
HER2 Heterodimerization |
||||
|
|
||||
|
BMS-599626 |
EGFR, HER2 |
Bristol-Myers Squibb |
Phase I |
|
|
|
||||
|
Macrolide Derivatives |
||||
|
|
||||
|
RAD001 |
mTOR |
Novartis Pharma AG |
Phase II |
|
|
|
||||
|
CCI-779 |
mTOR |
Wyeth |
Phase II |
|
|
|
||||
|
AP23573 |
mTOR |
Ariad Pharmaceuticals |
Phase I |
|
|
|
||||
|
Monoclonal Antibodies |
||||
|
|
||||
|
Cetuximab |
EGFR (chimeric mAB) |
ImClone/Merk KGaA Bristol-Myers Squibb |
Approved |
|
|
|
||||
|
Matuzumab |
EGFR (humanized mAb) |
Merck KgaA |
Phase II |
|
|
|
||||
|
Panitumumab |
EGFR (humanized mAb) |
Abgenix |
Phase II/III, |
|
|
|
||||
|
Trastuzumab |
HER2 (humanized mAb) |
Genentech/Roche |
Approved |
|
|
|
||||
|
Bevacizumab |
VEGF-A |
Genentech |
Approved |
|
|
|
||||
|
VEGF Inhibitors |
||||
|
|
||||
|
Sorafenib |
VEGFR2, FLT3, PDGFR, fibroblast growth factor receptor-1 |
Bayer HealthCare Pharmaceuticals and Onyx Pharmaceuticals |
Phase III |
|
|
|
||||
|
Sunitinib |
c-kit, VEGFR1-3, PDGFRa, PDGFRb, Flt-3, CSF-1R, ret |
Pfizer Inc. |
Phase II/III |
|
|
|
||||
|
Axitinib AG013736 |
VEGF 1-3, PDGFR, cKIT |
Pfizer Inc. |
phase II |
|
|
|
||||
|
Regeneron |
VEGF-Trap |
Phase I |
||
|
|
||||
|
Non VEGF Angiogenesis inhibitors |
||||
|
|
||||
|
Celecoxib |
COX-2 |
Pfizer Inc. |
Phase II |
|
|
|
||||
|
Proteasome Inhibitors |
||||
|
|
||||
|
Bortezomib |
Inhibits 26S proteasome |
Millennium Pharmaceuticals, Inc. |
Phase II |
|
|
|
||||
|
Retinoic Acid Receptor |
||||
|
|
||||
|
Bexarotene |
Retinoid × receptor |
Eisai Inc. |
Phase III |
|
|
|
||||
|
Katzel et al. Journal of Hematology & Oncology 2009 2:2 doi:10.1186/1756-8722-2-2 |
||||
