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Uses
Evinacumab (REGN1500) is a human anti-ANGPTL3 (angiopoietin-like protein 3) monoclonal antibody (IgG4 class antibody). Evinacumab reduces plasma lipids in dyslipidemic mice by blocking ANGPTL3. Evinacumab can be used in studies of homozygous familial hypercholesterolaemia (HoFH), refractory hypercholesterolaemia (both familial and non-familial) and severe hypertriglyceridaemia[1].
in vivo
Evinacumab (REGN1500) (10 mg/kg; s.c.; single) lowers serum TGs in normolipidemic C57Bl/6 mice and increases postheparin plasma LPL activity[1].
Evinacumab (25 mg/kg; s.c.; once weekly for 8 weeks) lowers serum TG and cholesterol levels in dyslipidemic C57Bl/6 mice[1].
Evinacumab (10 mg/kg; s.c.; single) lowers serum HDL-C by an EL-dependent mechanism in Lipg-/- mice[1].
| Animal Model: | Male C57Bl/6 mice (8-week-old)[1]. |
| Dosage: | 10 mg/kg |
| Administration: | Subcutaneous injection, single. |
| Result: | Caused a rapid reduction in TG levels with the maximal mean level of serum TG 55% lower than control group, and reduced 26% levels of TC. Significantly reduced VLDL-TG, VLDL-cholesterol, and HDL-C levels. Increased postheparin plasma LPL and improved lipid tolerance. |
| Animal Model: | Male C57Bl/6 mice (8-week-old; on a high-fat high-cholesterol diet)[1]. |
| Dosage: | 25 mg/kg |
| Administration: | Subcutaneous injection, once weekly for 8 weeks. |
| Result: | Led to a marked and sustained reduction in circulating TG levels (up to 53%). Significantly reduced levels of TC (up to 35%) and LDL-C (up to 45%). |
| Animal Model: | Lipg-/- mice[1]. |
| Dosage: | 10 mg/kg |
| Administration: | Subcutaneous injection, single. |
| Result: | Blocked the inhibitory action of ANGPTL3 on EL with an IC50 value of 96 nM. |
References
[1] Gusarova V, et al. ANGPTL3 blockade with a human monoclonal antibody reduces plasma lipids in dyslipidemic mice and monkeys. J Lipid Res. 2015 Jul;56(7):1308-17. DOI:10.1194/jlr.M054890
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