Nonclinical Pharmacokinetics, Disposition, and Drug-Drug Interaction Potential of a Novel d-Amino Acid Peptide Agonist of the Calcium-Sensing Receptor AMG 416 (Etelcalcetide)

AMG 416 (etelcalcetide) is a novel synthetic peptide agonist of the calcium-sensing receptor composed of a linear chain of seven d-amino acids (referred to as the d-amino acid backbone) with a d-cysteine linked to an l-cysteine via a disulfide bond. AMG 416 contains four basic d-arginine residues an...

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Veröffentlicht in:	Drug metabolism and disposition 2016-08, Vol.44 (8), p.1319-1331
Hauptverfasser:	Subramanian, Raju, Zhu, Xiaochun, Kerr, Savannah J., Esmay, Joel D., Louie, Steven W., Edson, Katheryne Z., Walter, Sarah, Fitzsimmons, Michael, Wagner, Mylo, Soto, Marcus, Pham, Roger, Wilson, Sarah F., Skiles, Gary L.
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Intravenous Animals Biotransformation Calcimimetic Agents - administration & dosage Calcimimetic Agents - blood Calcimimetic Agents - pharmacokinetics Calcimimetic Agents - toxicity Cytochrome P-450 Enzyme System - metabolism Dogs Drug Interactions Female HEK293 Cells Humans Kidney - metabolism Liver - metabolism Male Membrane Transport Proteins - genetics Membrane Transport Proteins - metabolism Molecular Structure Peptides - administration & dosage Peptides - blood Peptides - pharmacokinetics Peptides - toxicity Protein Binding Rats, Inbred BN Receptors, Calcium-Sensing - agonists Receptors, Calcium-Sensing - chemistry Receptors, Calcium-Sensing - metabolism Renal Elimination Risk Assessment Serum Albumin - metabolism Structure-Activity Relationship Tissue Distribution Transfection
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