Tirzepatide
Profil Związku

Tirzepatide

Dual GIP/GLP-1 receptor agonist studied for type 2 diabetes and obesity

Znany również jako: LY3298176 · Mounjaro · Zepbound · twincretin

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Chemistry data
Class
dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist
Molecular weight
4813.5 g/mol
Sequence
YAibEGTFTSDVSSYLEEQAAKEFIAWLVKGRG-OH (39 amino acids; Aib = aminoisobutyric acid at position 2; C-20 fatty diacid conjugated to lysine at position 20)
Half-life
approximately 5 days (subcutaneous)
Routes
subcutaneous
Studied doses
subcutaneous 2.5 mg, 5 mg, 10 mg, 15 mg once weekly

Status Regulacyjny

Stany Zjednoczone
fda_approved
Unia Europejska
ema_approved
Wielka Brytania
mhra_approved

Jak to działa

  • Dual agonism at GIP and GLP-1 receptors with imbalanced biased signaling favoring GIPR engagement, enhancing insulin secretion in a glucose-dependent manner
  • Suppression of glucagon secretion via GLP-1 receptor activation on pancreatic alpha cells during hyperglycemia
  • Slowing of gastric emptying contributing to postprandial glucose reduction and increased satiety
  • Central appetite suppression via brainstem circuits, modulated by GIP receptor activation attenuating GLP-1-induced nausea
  • GIPR-mediated weight-independent insulin sensitization and adipocyte nutrient metabolism modulation

Wyniki badań

Kontekst dawkowania

  • Drogi Podania
    subcutaneous
    Zakres
    2.5 mg, 5 mg, 10 mg, 15 mg once weekly

    FDA-approved dosing: 2.5 mg starting dose titrated to 5 mg, 10 mg, or 15 mg once weekly for type 2 diabetes (Mounjaro) and obesity (Zepbound)

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Efekty uboczne: kontekst badań

  • nausea
  • diarrhea
  • decreased appetite
  • vomiting
  • constipation
  • dyspepsia
  • abdominal pain
  • injection site reactions

Pełne podsumowanie badań wkrótce. Tymczasem zajrzyj do danych naukowych i referencji PubMed powyżej.

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