ChemicalBook Product Catalog API Nervous system drugs Drug Metabolism in Human Brain Elezanumab

Elezanumab

Product NameElezanumab
CAS1791416-49-3
MF
MW0
EINECS
MOL FileMol File

Chemical Properties

form	Liquid
color	Colorless to light yellow

Usage And Synthesis

Uses

Elezanumab (ABT-555; AE12-1Y-QL) is a human monoclonal antibody that selectively targets repulsive guidance molecule A (RGMa). Elezanumab potently inhibited RGMa mediated BMP signalling via the SMAD1/5/8 pathway, with an IC50 around 97 pM. Elezanumab promotes neuroregeneration and neuroprotection in neuronal injury and demyelination models binds N-terminal RGMa, blocks BMP signaling and lacks RGMc cross-reactivity. elezanumab has neuroregenerative and neuroprotective activities without impact on iron metabolism[1][2].

in vivo

Elezanumab (ABT-555; AE12-1Y-QL; 1-10 mg/kg; IV; once a week for 5 doses) promotes axonal regeneration and prevents retinal nerve fiber layer degeneration in the optic nerve crush and optic neuritis models (female Lewis rats)^[1].
Elezanumab (0.01, 0.1, 1, 10 mg/kg; IV; once a week for 3 doses ) promotes axonal regeneration and remyelination, decreases inflammatory lesion area and improves functional recovery in the spinal targeted experimental autoimmune encephalomyelitis (EAE) model (female Lewis rats)^[1].

Animal Model:	Female Lewis rat optic neuritis models^[1]
Dosage:	1, 3, or 10 mg/kg
Administration:	IV; once a week for 5 doses
Result:	Protected against the optic nerve inflammationinduced RNFL degeneration. Showed significant protection of the RNFL, as demonstrated by decreased reduction in RNFL thickness measured by optical coherence tomography (OCT) with 10 mg/kg

References

[1] Lili Huang, et al. Elezanumab, a clinical stage human monoclonal antibody that selectively targets repulsive guidance molecule A to promote neuroregeneration and neuroprotection in neuronal injury and demyelination models. Neurobiol Dis. 2021 Nov;159:105492. DOI:10.1016/j.nbd.2021.105492
[2] Peer B Jacobson, et al. Elezanumab, a human anti-RGMa monoclonal antibody, promotes neuroprotection, neuroplasticity, and neurorecovery following a thoracic hemicompression spinal cord injury in non-human primates. Neurobiol Dis. 2021 Jul;155:105385. DOI:10.1016/j.nbd.2021.105385

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