Catalog
Dual GIP / GLP-1 receptor agonist
Tirzepatide
aka Mounjaro · Zepbound
First dual incretin agonist — ~20% mean weight loss at 15 mg in obesity.
FDA-approvedGrade A — Clinically established
Target
GIPR + GLP-1R
Sequence / engineering
39 aa, C20 fatty-diacid lipidated. Imbalanced agonist (biased GIPR signaling).
Mechanism of action
Co-agonist of GIPR and GLP-1R. GIP arm augments insulin secretion and may modulate adipose lipid handling and central appetite circuits beyond GLP-1 alone. Net effect: superior glycemic and weight outcomes vs. selective GLP-1 RAs in head-to-head trials.
Pharmacokinetics
SC weekly. t½ ≈ 5 days. Steady state ~4 weeks.
Clinical context
T2D (Mounjaro); chronic weight management (Zepbound); SURMOUNT-OSA showed AHI reductions in obesity-related OSA.
Dosing
2.5 → 5 → 7.5 → 10 → 12.5 → 15 mg SC weekly, 4-week intervals.
Monitoring
- HbA1c
- Weight, BP
- Pancreatitis symptoms
- Gallbladder symptoms
Safety
Black-box warning
Thyroid C-cell tumor risk (rodent).
Contraindications
- MTC, MEN-2
- Hypersensitivity
Adverse effects
- GI (nausea, diarrhea, vomiting)
- Cholelithiasis
- Pancreatitis (rare)
- Hypoglycemia when combined with insulin/sulfonylurea
Relevant labs
Covered in modules
Key references
Related compounds
Generate prescriber-grade deep dive
Pull in expanded mechanism, PK/PD, dosing strategies for special populations, drug interactions, monitoring cadence, head-to-head differentials, prescriber pearls, and patient FAQs for Tirzepatide.
Educational reference. Not medical advice. Always verify against current FDA labeling and local regulatory guidance before prescribing or counseling.