Drug |
Class |
Mechanism (Cellular Targets) |
Year of Approval |
Indications |
Dosages |
Bevacizumab (Avastin) |
Anti-VEGF mAB |
VEGF |
2004 |
First- and second-line metastatic CRC |
5 mg/kg IV q2wk + bolus IFL; 10 mg/kg IV q2wk + FOLFOX4 |
|
|
|
2006 |
First-line NSCLC |
15 mg/kg IV q3wk + carboplatin/paclitaxel |
|
|
|
2009
2009
2013 |
Second-line GBM
Metastatic RCC
Second-line metastatic CRC (after prior bevacizumabcontaining regimen) |
10 mg/kg IV q2wk
10 mg/kg IV q2wk + IFN
5 mg/kg IV q2wk or 7.5 mg/kg IV q3wk + fluoropyrimidine-irinotecan or fluoropyrimidineoxaliplatin-based regimen |
Ziv-aflibercept (Zaltrap, VEGF Trap) |
Anti-VEGF mAB |
VEGFA, VEGFB, PlGF1, PlGF2 |
2012 |
Metastatic CRC (after prior oxaliplatin-containing regimen) |
4 mg/kg IV q2wk (1-hr infusion) |
Sorafenib (Nexavar, BAY439006) |
Small-molecule TKI |
VEGFR2, VEGFR3, PDGFR, FLT3, c-Kit |
2005
2007
2013 |
Advanced RCC
Unresectable HCC
RAI-refractory DTC |
400 mg PO bid (w/o food)
400 mg PO bid (w/o food)
400 mg PO bid (w/o food) |
Sunitinib (Sutent, SU11248) |
Small-molecule TKI |
VEGFR1, VEGFR2, VEGFR3, PDGFR, FLT3, c-Kit, RET |
2006 |
Imatinib-resistant or -intolerant GIST |
50 mg PO qd, 4 wk on/2 wk off |
|
2006
2011 |
Advanced RCC
Advanced pNET |
50 mg PO qd, 4 wk on/2 wk off
37.5 mg PO qd |
Pazopanib (Votrient) |
Small-molecule TKI |
VEGFR1, VEGFR2, VEGFR3, PDGFR, Itk, Lck, c-Fms |
2009
2012 |
Advanced RCC
Advanced soft tissue sarcoma |
800 mg PO qd (w/o food)
800 mg PO qd (w/o food) |
Vandetanib (Caprelsa) |
Small molecule TKI |
RET, VEGFR, EGFR, BRK, TIE2 |
2011 |
Advanced MTC |
300 mg PO qd |
Axitinib (Inlyta) |
Small molecule TKI |
VEGFR1, VEGFR2, VEGFR3 |
2012 |
Advanced RCC (after failure of prior therapy) |
5 mg PO bid |
Cabozantinib (XL184, Cometriq) |
Small molecule TKI |
MET, VEGFR2, RET, KIT, AXL, FLT3 |
2012 |
Progressive, metastatic MTC |
140 mg PO qd (w/o food) |
Regorafenib (Stivarga) |
Small molecule TKI |
RET, VEGFR1, VEGFR2, VEGFR3, TIE2, KIT, PDGFR |
2012 |
Previously treated metastatic CRC |
160 mg PO qd × 21days (q28-day cycle) |
|
2013 |
GIST |
160 mg PO qd × days 1-21 (q28-day cycle) |
Temsirolimus (Torisel) |
mTOR inhibitor |
mTOR |
2007 |
Advanced RCC |
25 mg IV qwk (infused over 30-60 min) |
Everolimus (Afinitor, RAD-001)a |
mTOR inhibitor |
mTOR |
2009 |
Second-line advanced RCC (after VEGFR TKI failure) |
10 mg PO qd |
|
|
2010
2011
2012 |
SEGA associated w/TSC
pNET
Advanced HR+, HER2- breast cancer |
4.5 mg/m2 PO qd
10 mg PO qd
10 mg PO qd |
|
|
|
2012 |
AML associated w/TSC |
10 mg PO qd |
a Afinitor Disperz (everolimus tablets for oral suspension) was approved in 2012 for children aged 1 and older who have SEGA + TSC. mAB, monoclonal antibody; CRC, colorectal cancer; IV, intravenous; IFL, irinotecan, 5-fluorouracil, and leucovorin; FOLFOX4, 5-flourouracil, leucovorin, and oxaliplatin; NSCLC, non-small-cell lung cancer; GBM, glioblastoma multiforme; RCC, renal cell carcinoma; VEGFA, vascular endothelial growth factor A; PlGF, placental growth factor; TKI, tyrosine-kinase inhibitor; VEGFR, VEGF receptor; PDGFR, platelet-derived growth factor receptor; FLT, Fms-like tyrosine kinase; c-Kit, stem cell factor receptor; HCC, hepatocellular carcinoma; RAI, radioactive iodine; DTC, differentiated thyroid carcinoma; PO, orally; RET, glial cell line-derived neurotrophic factor receptor; pNET, pancreatic neuroendocrine tumor; GIST, gastrointestinal stromal tumor; qd, every day; Itk, interleukin-2 receptor inducible T-cell kinase; Lck, leukocyte-specific protein tyrosine kinase; c-Fms, transmembrane glycoprotein receptor tyrosine kinase; bid, twice daily; EGFR, epidermal growth factor receptor; BRK, protein tyrosine kinase 6; MTC, medullary thyroid cancer; mTOR, mammalian target of rapamycin; SEGA, subependymal giant cell astrocytoma; TSC, tuberous sclerosis complex; HR, hormone receptor; HER2, human epidermal growth factor receptor 2; AML, angiomyolipoma. | |