luspatercept   Click here for help

GtoPdb Ligand ID: 10538

Synonyms: ACE-536 | ACE536 | luspatercept-aamt | Reblozyl®
Approved drug
luspatercept is an approved drug (FDA (2019), EMA (2020))
Compound class: Peptide
Comment: Luspatercept (ACE-536) is a fusion protein comprising human ACVR2B (activin receptor type 2B) extracellular domain (which is mutated to reduce activin binding), fused with human immunoglobulin G1 Fc fragment [2]. Luspatercept was initially proposed as a ligand trap for growth/differentiation factor-11 (GDF11; and other TGFβ family ligands). Mechanistically, it reduces Smad2/3 activation, and promotes maturation of late-stage erythroid precursors, independently of the erythropoietin (EPO) pathway. In contrast, erythropoietin stimulates proliferation of early-stage erythrocyte precursors.
Using Gdf11 knockout, Guerra et al. (2019) disputed GDF11 as an important molecular target of luspatercept and its proposed inhibitory effect on late erythropoiesis [1].
Classification Click here for help
Compound class Peptide
Approved drug? Yes. FDA (2019)  |  EMA (2020)
International Nonproprietary Names Click here for help
INN number INN
9823 luspatercept
Synonyms Click here for help
ACE-536 | ACE536 | luspatercept-aamt | Reblozyl®
Database Links Click here for help
Specialist databases
IMGT/mAb-DB 487
Other databases
DrugBank Ligand DB12281
GtoPdb PubChem SID 387065620
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