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Synonyms: eflapegrastim-xnst | HM-10460A | HM10460A | rolontis | Rolvedon® | SPI-2012 | SPI2012
eflapegrastim is an approved drug (FDA (2022))
Compound class:
Peptide or derivative
Comment: Eflapegrastim (SPI-2012) is a long-acting, human granulocyte colony-stimulating factor (G-CSF) recombinant peptide. Structurally it consists of a recombinant G-CSF (1-174) peptide monomer and an IgG4 Fc dimer, that are joined by a PEG-derived linker molecule. G-CSF stimulates neutrophil progenitor proliferation and differentiation, a molecular mechanism that is exploited to reduce the incidence and severity of chemotherapy-induced neutropenia. The Fc fragment increases the drug's half-life (reduces clearance) and overall efficacy by improving uptake into the bone marrow via binding to Fc receptors on the endothelial cells [1].
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| References |
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1. Barrett JA, Choi J, Lakshmikanthan S, Kim YY, Greene D, Kolli P, Song TH, Choi IY, Kim YH, Lebel F. (2020)
Eflapegrastim's enhancement of efficacy compared with pegfilgrastim in neutropenic rats supports potential for same-day dosing. Exp Hematol, 92: 51-61. [PMID:33002567] |
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2. Schwartzberg LS, Bhat G, Peguero J, Agajanian R, Bharadwaj JS, Restrepo A, Hlalah O, Mehmi I, Chawla S, Hasal SJ et al.. (2020)
Eflapegrastim, a Long-Acting Granulocyte-Colony Stimulating Factor for the Management of Chemotherapy-Induced Neutropenia: Results of a Phase III Trial. Oncologist, 25 (8): e1233-e1241. [PMID:32476162] |
