Tirzepatide
Dual-action GIP/GLP-1 therapy delivering the highest weight loss in clinical history.
From $349/mo
How It Works
Tirzepatide is a 39-amino acid linear peptide that acts as a dual agonist at both GIP and GLP-1 receptors. Its GIP receptor activity (approximately 5x native GIP potency) enhances fat metabolism in adipose tissue, improves insulin sensitivity in peripheral tissues, and may have direct effects on central appetite regulation through hypothalamic GIP receptors. Its GLP-1 receptor activity (comparable to native GLP-1) slows gastric emptying, promotes satiety through hypothalamic POMC neuron activation, and enhances glucose-dependent insulin secretion. The C20 fatty diacid moiety enables albumin binding, extending the half-life to approximately 5 days for once-weekly dosing. The dual mechanism produces additive effects on weight loss and glycemic control that exceed either pathway alone.
Key Benefits
Clinical Research
The SURMOUNT trial program evaluated tirzepatide across diverse populations. SURMOUNT-1 (n=2,539) demonstrated dose-dependent weight loss of 15.0% (5 mg), 19.5% (10 mg), and 22.5% (15 mg) vs 3.1% for placebo over 72 weeks in adults without diabetes. SURMOUNT-2 (n=938) in patients with type 2 diabetes showed 12.8-14.7% weight loss. SURMOUNT-3 (n=579) combined tirzepatide with intensive behavioral therapy, achieving 26.6% mean weight loss. SURMOUNT-4 (n=670) demonstrated that continuation beyond 36 weeks produced additional weight loss (total 25.3%), while withdrawal led to regain. The SURPASS diabetes trials (1-5) showed HbA1c reductions of 1.9-2.6% and weight loss of 5.4-12.9 kg across varied populations and comparators.
Dosage & Administration
Dosage
Treatment follows a structured dose escalation. Starting dose is 2.5 mg once weekly for 4 weeks, then 5.0 mg weekly for at least 4 weeks. Based on response and tolerability, the dose may be increased to 7.5 mg, then 10.0 mg, then 12.5 mg, and finally 15.0 mg weekly, with each step lasting at least 4 weeks. Many patients achieve excellent results at 10.0 mg without needing the maximum 15.0 mg dose. Your GetPepWell physician will determine the optimal maintenance dose based on your individual response and tolerance profile.
Administration
Administered as a subcutaneous injection once weekly, on the same day each week, at any time of day regardless of meals. Preferred injection sites include the abdomen (at least 2 inches from the navel), front of the thigh, or upper arm. Rotate injection sites weekly to prevent tissue irritation. Use a thin 30-31 gauge needle for minimal discomfort. If a dose is missed, administer within 4 days of the scheduled day; otherwise, skip and resume on the next scheduled day. Do not administer two doses within 3 days of each other.
Side Effects
- Nausea (most common, usually diminishes over 4-8 weeks)
- Diarrhea
- Decreased appetite (therapeutic but can be pronounced at higher doses)
- Vomiting, especially during dose escalation periods
- Constipation
- Abdominal pain or dyspepsia
- Injection site reactions
- Hair thinning (reported in some patients during rapid weight loss)
Contra-indications
- Personal or family history of medullary thyroid carcinoma (MTC)
- Multiple Endocrine Neoplasia syndrome type 2 (MEN 2)
- Known hypersensitivity to tirzepatide or its excipients
- History of pancreatitis or active gallbladder disease
- Pregnancy or planning to become pregnant (discontinue at least 2 months before)
- Breastfeeding
- Severe gastrointestinal disease or gastroparesis
- Diabetic retinopathy requiring active treatment (may worsen transiently)
Drug Interactions
- Insulin and sulfonylureas - significant hypoglycemia risk; dose reduction typically required
- Oral contraceptives - delayed gastric emptying may reduce bioavailability; use non-oral contraception
- Warfarin and other anticoagulants - monitor INR closely during initiation
- Oral medications with narrow therapeutic index - timing of absorption may be altered
- Acetaminophen - peak absorption delayed; clinical significance is minimal
Storage Info
Store unused vials refrigerated at 36-46 degrees F (2-8 degrees C). Do not freeze. After first use, the vial may be stored at room temperature (up to 86 degrees F / 30 degrees C) or refrigerated for up to 21 days. Protect from direct light. Discard 21 days after first puncture. Do not use if the solution is cloudy, discolored, or contains visible particles.
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