fasinumab   Click here for help

GtoPdb Ligand ID: 8965

Synonyms: REGN475 | SAR164877
Compound class: Antibody
Comment: Fasinumab is an investigational, fully human IgG4κ monoclonal antibody targeting nerve growth factor (NGF).
Peptide sequence information for this antibody is available from its IMGT/mAb-DB record.
BLAST peptide sequence analysis reveals identical matches to peptide sequences submitted with patent US7988967 [4], with the preferred antibody being called REGN475 therein. REGN475 exhibits high specificity for human NGF, does not cross-react with closely related neurotrophin-3 (NT-3) and inhibits binding of NGF to its receptors TrkA (NTRK1) and p75 (NGFR) [4].
Bioactivity Comments
Fasinumab (REGN475) blocks NGF binding to its receptors TrkA and p75 with IC50 values of 20 and 22 pM respectively, and inhibits NGF-mediated TrkA/p75 signalling in PC12 cells with IC50 of 9.6pM [4]. A proof-of-concept study reported that fasinumab provided no clinical benefit in patients with acute sciatic pain [5].
Selectivity at ligand targets
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
NGF Primary target of this compound Hs Antibody Binding 12.7 pKd - 4
⤷ pKd 12.7 (Kd 1.8x10-13 M) [4]