This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact ­information

Endocrine/metabolic disease

Diabetes

Fibroblast growth factor receptor 1 (FGFR1; CD331); klotho-b (KLB); fibroblast growth factor 21 (FGF21)

In vitro and nonhuman primate studies identified an agonistic mAb of the FGFR1-KLB complex that could help treat type 2 diabetes. In vitro screening of antibodies from humanized mice identified an antibody that specifically bound to and agonized the FGFR1-KLB complex, which is a target of FGF21 expressed in adipocytes. In obese monkeys, the antibody decreased body weight, BMI, insulin resistance and triglyceride levels compared with vehicle. Next steps at Amgen Inc. include longer-term preclinical studies.
Ambrx Inc. and Bristol-Myers Squibb Co. have ARX618, a stabilized form of FGF21, in preclinical development for type 2 diabetes.
Roche's Genentech Inc. has an agonistic antibody that targets FGFR1 in preclinical development for the same indication.

SciBX 5(49); doi:10.1038/scibx.2012.1282
Published online Dec. 20, 2012

Patent application filed; licensing status undisclosed

Foltz, I.N. et al. Sci. Transl. Med.; published online Nov. 28, 2012;
doi:10.1126/scitranslmed.3004690
Contact: Yang Li, Amgen Inc., South San Francisco, Calif.
e-mail:

yangl@amgen.com