Mechanism of Action

Specific targets

Generic Name (Brand Name), Year of FDA approval

Indication(s)

Anti-VEGF antibody

VEGF-A

Bevacizumab (Avastin®), 2004 [83]

Colorectal, non-small-cell lung cancer (NSCLC), glioblastoma multiforme, and epithelial ovarian cancer

VEGF inhibitor (trap mechanism)

VEGF-A, VEGF-B, PlGF

Ziv-aflibercept (Zaltrap®), 2012 [84]

Colorectal cancer

VEGFR antibody

VEGFR-2

Ramucirumab (Cyramza®), 2014 [85, 86]

Stomach cancer, gastroesophageal junction adenocarcinoma, NSCLC, and hepatocellular carcinoma

Tyrosine kinase inhibitor (TKI)

VEGFRs, PDGFRs, cKIT

Axitinib (Inlyta®), 2012 [87]

Renal cell carcinoma

TKI

VEGFRs cKIT, DDR2, FGFRs, FLT3, FMS, MUSK, cRAF,

PDGFRs, Ret, TAO2

Sorafenib (Nexavar®), 2005 [88]

Renal cell carcinoma and hepatocellular carcinoma

TKI

VEGFRs ARK5, CaMKIIs, CHK2,

cKIT, cRAF, FGFR1, Flt3,

FMS, Mer, PDGFR, Ret,

TrkA

Sunitinib (Sutent®), 2006 [89]

Renal cell carcinoma, gastrointestinal carcinoma and PNETs

TKI

VEGFRs, cKIT, FMS, FGFR2, FLT3,

MLK1, PDGFR

Pazopanib (Votrient®), 2009 [90, 91]

Renal cell carcinoma and advanced soft tissue sarcoma

TKI

VEGFRs PDGFRs, FGFRs, Tie2,

DDR2, Trk2A, Eph2A,

RAF-1, STK5

Regorafenib (Stivarga®), 2012 [92]

Colorectal cancer, gastrointestinal stromal tumor and hepatocellular carcinoma

TKI

VEGFRs, cMET, Ret, cKIT, Axl

Cabozantinib (Cometriq®), 2012 [86, 93]

Thyroid cancer, renal cell and hepatocellular carcinoma

TKI

VEGFRs EGFRs, Ret

Vandetanib (Caprelsa®), 2011 [94]

Thyroid cancer

bFGF inhibitor

FGF

Lenalidomide (Revlimid®) [95, 96]

Myeloma, mantle cell, follicular and marginal zone lymphoma

bFGF inhibitor

FGF

Thalidomide (Synovir, Thalomid®) [95-98]

Myeloma

mTOR inhibitor

mTOR

Everolimus (Afinitor®) [99]

Renal cell carcinoma, advanced breast cancer, pancreatic neuroendocrine tumors (PNETs), renal angiomyolipoma, and subependymal giant cell astrocytoma

mTOR inhibitor

mTOR

Temsirolimus (Torisel®) [99]

Renal cell carcinoma