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Figitumumab (CP-751871) is a potent and fully human monoclonal anti–insulin-like growth factor 1 receptor (IGF1R) antibody. Figitumumab prevents IGF1 from binding to IGF1R with an IC50 of 1.8 nM[1]. | [in vivo]
Figitumumab (CP-751871) (31-125 μg/mouse; i.p.; once) induces the down-regulation of tumor associated IGF-1R in mice[2].
Figitumumab (62.5-500 μg/mouse; i.p.; once) inhibits the growth of s.c. xenografts derived from colon (Colo-205), breast (MCF7), and lung (H460) cancer cell lines in mice[2]. | Animal Model: | Female athymic mice (CD-1 nu/nu) bearing NIH3T3/IGF-1R tumors[2] | | Dosage: | 31 to 125 μg per mouse | | Administration: | Intraperitoneal injection, once | | Result: | Resulted in a serum Cmax between 12 and 24 hours. At 24 hours, there was a dose-dependent reduction of IGF-1R protein in tumors, with 50% reduction observed at a serum concentration of 15 μg/mL. Resulted in a down-regulation of IGF-1R from the tumor. The half-life in an athymic mouse was determined to be 4 to 6 days by longer-term studies. |
| Animal Model: | Female athymic mice (CD-1 nu/nu), human Colo-205 tumor xenograft model[2] | | Dosage: | 62.5 μg or 250 μg per mouse | | Administration: | Intraperitoneal injection, once | | Result: | Inhibited the tumor growth. |
| [References]
[1] Pavlicek A, et al. Molecular predictors of sensitivity to the insulin-like growth factor 1 receptor inhibitor Figitumumab (CP-751,871). Mol Cancer Ther. 2013 Dec;12(12):2929-39. DOI:10.1158/1535-7163.MCT-13-0442-T
[2] Cohen BD, et al. Combination therapy enhances the inhibition of tumor growth with the fully human anti-type 1 insulin-like growth factor receptor monoclonal antibody CP-751,871. Clin Cancer Res. 2005 Mar 1;11(5):2063-73. DOI:10.1158/1078-0432.CCR-04-1070 |
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