Table 2.

Summary of single-agent antitumor efficacy of axitinib in nonclinical models

Disease typeDescriptionDose (mg/kg)RegimenSize at start of dosing (mm3)Dosing period (d)TGI (%)
Colon carcinomaDose-dependent TGI in MV522 model1orally twice daily1701618.3
315.2
1063.9
3061.1
10080.3
15094.6
20096.3
Dose response TGI in HT29 model10orally twice daily1101651
3076
10099
15099
TGI in orthotopic HTC-116 GFP model30orally twice daily1 d after implant10Unevaluable
1787
2880
LungDose-dependent efficacy in LLC model1orally twice daily<501833
349
1075
3068
10069
300Not tolerated
TGI and antimetastasis activity and survival assessment in LLC model100orally twice dailyProphylactic dose (s.c. model)3863
orally twice dailyTail vein implanted tumorsSurvival∼11 d median survival vs control
TGI in KIT+ NCI-H526 SCLC model30orally twice daily1801347
10061
MelanomaTGI in established A375 melanoma10orally twice daily3361238
3059
Dose-dependent TGI in activating mutant b-Raf A2058 melanoma model3orally twice daily1501536
1057
3065
10083
Renal carcinomaTGI in orthotopically implanted SN12C GFP human renal carcinoma model10orally twice daily2 d after implant4154
107261
304156
307274
1004163
1007270
GliomaDose-dependent efficacy in U87 glioma model10orally twice daily46-721744
3069
6074
NHLEfficacy in human lymphoma model Namalwa (time course)50orally twice daily1 d after implant14Significant reduction in i.p. tumor burden as indicated by reduction in body weights
5022
5023
  • NOTE: TGI (%) was calculated according to the equation: [1 - ΔTreat/ΔControl] × 100, where ΔTreat and ΔControl are changes of tumor volume between the end of the dosing and the beginning of the dosing for a treated group and a control group, respectively.