Introduction
Tyrosine kinases
Tumor angiogenesis
Agent | Target | Clinical activity and/or study | Phase of development | Refs |
---|---|---|---|---|
Sunitinib (SU11248; Sutent) | VEGFR-1, -2, -3, PDGFR, KIT, FLT3, CSF-1R, RET | Kidney, breast, prostate, lung, liver, ovarian, colorectal, thyroid, head and neck, gastric, bladder, cervical and pancreatic cancer, GIST, melanoma, glioblastoma, myeloma, lymphoma | Approved for kidney cancer and GIST, phase II or III for other cancers | |
Sorafenib (BAY439006; Nexavar) | VEGFR-2, -3, PDGFR, Raf, KIT | Kidney, liver, breast, prostate, lung, ovarian, colorectal, thyroid, head and neck, gastric and pancreatic cancer, GIST, melanoma, glioblastoma, lymphoma, leukemia | Approved for kidney and liver cancer, phase II or III for other cancers | |
Pazopanib (GW786034; Votrient) | VEGFR-1, -2, -3, PDGFR, KIT | Kidney, breast, lung, cervical, liver, thyroid, prostate and colorectal cancer, melanoma, glioblastoma | Approved for kidney cancer, phase II or III for other cancers | |
Vandetanib (ZD6474; Zactima) | VEGFR-2, EGFR, KIT, RET | Lung, kidney, thyroid, head and neck, prostate, ovarian, breast and colorectal cancer, glioma, neuroblastoma | Phase II or III | |
Axitinib (AG013736) | VEGFR-1, -2, -3, PDGFR-β, KIT | Kidney, lung, thyroid, pancreatic, colorectal and breast cancer, melanoma | Phase II or III | |
Cediranib (AZD2171; Recentin) | VEGFR-1, -2, -3, PDGFR-β, KIT | Kidney, breast, lung, liver, ovarian, head and neck, prostate and colorectal cancer, GIST, glioblastoma, melanoma | Phase II | |
Vatalanib (PTK787; ZK222584) | VEGFR-1, -2, -3, PDGFR-β, KIT | Prostate, colorectal, kidney and pancreatic cancer, melanoma, lymphoma, leukemia | Phase II or III | |
Motesanib (AMG706) | VEGFR-1, -2, -3, PDGFR, KIT, RET | Lung, thyroid, gallbladder, breast and colorectal cancer, GIST | Phase II or III |