Efinopegdutide
Efinopegdutide (MK-6024, formerly JNJ-64565111 / HM12525A) is a once-weekly dual agonist at the GLP-1 and glucagon receptors, developed by Hanmi and Merck. It has been studied for obesity and notably for metabolic liver disease (MASH/NAFLD); a phase-2 trial showed greater liver-fat reduction than semaglutide. Investigational, not approved.
Mechanism of action
Efinopegdutide is an oxyntomodulin-derived peptide acting as a dual agonist at the GLP-1 and glucagon receptors with a relative potency of approximately 2:1 (GLP-1 to glucagon). The GLP-1 component mediates glucose-dependent insulin secretion and modulation of satiety; the glucagon component increases energy expenditure and hepatic fat oxidation, which is proposed to contribute to the observed reduction in liver fat. Conjugation to an IgG4 fragment prolongs the half-life and enables weekly administration.
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Wat de studies laten zien
Waar studies elkaar tegenspreken
Does the greater liver-fat reduction versus semaglutide translate into a relevant clinical benefit in MASH?
Farmacokinetiek
Theoretische concentratiecurve bij een halfwaardetijd van 115 h. Puur farmacokinetisch model — geen doseringsaanbeveling.
Open in PK tool →Veiliger gebruik & risico's
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Interacties & combinaties
Anekdotische waarnemingen
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Reconstitutie-calculator
Peptiden komen als droog poeder. Eenmaal opgelost in een vloeistof (reconstitutie) beantwoordt deze calculator één enkele vraag: hoeveel stof zit er daarna in één milliliter oplossing?
- 1Voer de hoeveelheid stof van de flacon in (staat op het etiket).
- 2Voer in hoeveel oplosmiddel je toevoegt.
- 3Resultaat = concentratie in mg per mL.
Studieregister
A phase IIa active-comparator-controlled study to evaluate the efficacy and safety of efinopegdutide in patients with non-alcoholic fatty liver disease
Efficacy and safety of glucagon-like peptide-1/glucagon receptor co-agonist JNJ-64565111 in individuals with obesity without type 2 diabetes mellitus: A randomized dose-ranging study
Efficacy and safety of glucagon-like peptide-1/glucagon receptor co-agonist JNJ-64565111 in individuals with type 2 diabetes mellitus and obesity: A randomized dose-ranging study
Bronnen & methode
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