Modimelanotide

Modimelanotide
Systematic (IUPAC) name
N2-acetyl-L-lysyl-L-lysyl-L-lysyl-L-lysyl-L-lysyl-L-lysyl-L-seryl-L-tyrosyl-L-seryl-L-methionyl-L-alpha-glutamyl-L-histidyl-L-phenylalanyl-L-arginyl-L-tryptophylglycyl-L-lysyl-L-prolyl-L-valinamide
Identifiers
CAS Number 926277-68-1
ATC code None
PubChem CID 72941953
ChemSpider 34988374
Synonyms Acetylhexa-L-lysyl-α-MSH
Chemical data
Formula C113H181N33O25S
Molar mass 2433.945 g/mol

Modimelanotide (INN) (code names AP-214, ABT-719, ZP-1480) is a melanocortinergic peptide drug derived from α-melanocyte-stimulating hormone (α-MSH) which was under development by, at different times, Action Pharma, Abbott Laboratories, AbbVie, and Zealand for the treatment of acute kidney injury.[1][2] It acts as a non-selective melanocortin receptor agonist, with IC50 values of 2.9 nM, 1.9 nM, 3.7 nM, and 110 nM at the MC1, MC3, MC4, and MC5 receptors.[3] Modimelanotide failed clinical trials for acute kidney injury despite showing efficacy in animal models,[4][5] and development was not further pursued.[1][2]

See also

References

  1. 1 2 Ramos, Adrián M; González-Guerrero, Cristian; Sanz, Ana; Sanchez-Niño, María Dolores; Rodríguez-Osorio, Laura; Martín-Cleary, Catalina; Fernández-Fernández, Beatriz; Ruiz-Ortega, Marta; Ortiz, Alberto (2015). "Designing drugs that combat kidney damage". Expert Opinion on Drug Discovery 10 (5): 541–556. doi:10.1517/17460441.2015.1033394. ISSN 1746-0441.
  2. 1 2 Montero-Melendez, Trinidad (2015). "ACTH: The forgotten therapy". Seminars in Immunology. doi:10.1016/j.smim.2015.02.003. ISSN 1044-5323.
  3. "Renal-Urologic drugs". Drug Data Reports (Prous Science) 29 (1): 42. 2007. ISSN 0379-4121.
  4. Doi, K; Hu, X; Yuen, P S T; Leelahavanichkul, A; Yasuda, H; Kim, S M; Schnermann, J; Jonassen, T E N; Frøkiær, J; Nielsen, S; Star, R A (2008). "AP214, an analogue of α-melanocyte-stimulating hormone, ameliorates sepsis-induced acute kidney injury and mortality". Kidney International 73 (11): 1266–1274. doi:10.1038/ki.2008.97. ISSN 0085-2538.
  5. Simmons, Matthew N.; Subramanian, Vairavan; Crouzet, Sebastien; Haber, Georges-Pascal; Colombo, Jose R.; Ukimura, Osamu; Neilsen, Søren; Gill, Inderbir S. (2010). "α-Melanocyte Stimulating Hormone Analogue AP214 Protects Against Ischemia Induced Acute Kidney Injury in a Porcine Surgical Model". The Journal of Urology 183 (4): 1625–1629. doi:10.1016/j.juro.2009.12.007. ISSN 0022-5347.

External links


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