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Luspatercept (ACE-536) is a recombinant modified ActRIIB fusion protein that binds with transforming growth factor β superfamily ligands. Luspatercept increases the erythrocyte numbers and promotes maturation of erythroid precursors. Luspatercept binds with GDF11 and inhibits Smad2/3 signaling. Luspatercept can be used for the research of anemia[1]. | [in vivo]
Luspatercept (0.1-60 mg/kg, s.c.; 10 mg/kg, i.v.; twice weekly for 8 weeks) increases red blood cell (RBC) count, hemoglobin levels and hematocrit in mice, rats and monkeys[1].
Luspatercept (10 mg/kg; s.c., once) reduces erythroid burst forming units (BFU-Es) and erythroid colony-forming units (CFU-Es) from bone marrow and spleen of C57BL/6 mice[1].
Luspatercept (10 mg/kg; i.p., once) inhibits Smad2/3 phosphorylation in mouse spleen[1]. | Animal Model: | C57BL/6 mice[1] | | Dosage: | 0.1, 0.3, 1, 3 and 10 mg/kg | | Administration: | Subcutaneous injection and intravenous injection; 0.1-10 mg/kg (C57BL/6 mice, s.c.), 6-60 mg/kg (Sprague Dawley rats, s.c.), 0.4-30 mg/kg (cynomolgus monkeys, s.c.), 10 mg/kg, (cynomolgus monkeys, i.v.); twice weekly for 8 weeks | | Result: | Dose-dependently increased the level of RBC, hemoglobin and hematocrit in mice, rats and monkeys. |
| [References]
[1] Suragani RN, et al. Transforming growth factor-β superfamily ligand trap ACE-536 corrects anemia by promoting late-stage erythropoiesis. Nat Med. 2014 Apr;20(4):408-14. DOI:10.1038/nm.3512 |
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