Tirzepatide

Metabolic

aka Mounjaro · Zepbound · LY3298176

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Formula

MW (Da)

Half-life

~5 days

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Overview

Tirzepatide is the active ingredient in Mounjaro and Zepbound. It is an FDA-approved synthetic peptide that activates both GIP and GLP-1 receptors. The current Zepbound label covers chronic weight management and moderate-to-severe obstructive sleep apnea in adults with obesity; Mounjaro is approved for type 2 diabetes. Tirzepatide products were first approved in the U.S. in 2022.

Mechanism

Tirzepatide is described in primary pharmacology as an imbalanced and biased dual agonist. It binds and signals more like native GIP at GIPR, while showing lower relative affinity and biased signaling at GLP-1R with preference for cAMP generation over β-arrestin recruitment and receptor internalization. Clinically, delayed gastric emptying contributes to satiety and to drug-interaction effects on absorption of co-administered medications, including reduced oral-contraceptive efficacy for ~4 weeks after initiation and after each dose escalation.

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Reported benefits

About 20.9% weight loss at 15 mg in SURMOUNT-1

In SURMOUNT-1, mean body-weight change at 72 weeks was about -15.0% with 5 mg, -19.5% with 10 mg, and -20.9% with 15 mg, versus -3.1% with placebo. The biggest weight-loss numbers in the FDA-approved incretin class.

[tirze-zepbound-label]

clinical

FDA approval for obstructive sleep apnea in obesity

Zepbound is also approved for moderate-to-severe OSA in adults with obesity, with labeled trials showing statistically significant reductions in apnea-hypopnea index at week 52 alongside about 17.7% to 19.6% weight loss at the maximum tolerated tirzepatide dose.

[tirze-zepbound-label]

clinical

Type 2 diabetes glycemic control

Mounjaro is FDA-approved for glycemic control in adults with type 2 diabetes alongside diet and exercise. The dual GIP/GLP-1 mechanism produces meaningful A1C reductions and weight loss compared with GLP-1-only comparators.

[tirze-fda-label]

clinical

Reported side effects

Boxed warning: rodent thyroid C-cell tumors
clinical
Tirzepatide carries a boxed warning for thyroid C-cell tumors observed in rodents. It is contraindicated in patients with MEN2 or a personal or family history of medullary thyroid carcinoma.
Dose-related severe GI events
clinical
In pooled Zepbound weight-loss trials, severe GI adverse reactions occurred in 1.7% at 5 mg, 2.5% at 10 mg, and 3.1% at 15 mg, versus ~1% with placebo. Nausea, vomiting, and diarrhea are the most common GI events overall.
Pancreatitis, gallbladder disease, AKI, hypoglycemia, aspiration risk
clinical
Labeled risks include pancreatitis, gallbladder disease, AKI from dehydration, hypersensitivity, hypoglycemia when combined with insulin or sulfonylureas, retinopathy worsening in type 2 diabetes, and aspiration risk around anesthesia due to delayed gastric emptying.
Oral contraceptive effectiveness reduced for 4 weeks after dose changes
clinical
Oral contraceptive efficacy may be reduced for 4 weeks after initiation and after each dose escalation; a non-oral or backup method is advised during these windows.

Dosing notes

Zepbound starts at 2.5 mg subcutaneously once weekly for 4 weeks, then 5 mg, with further 2.5 mg increments after at least 4 weeks on each dose. Recommended maintenance: 5, 10, or 15 mg weekly for weight management and 10 or 15 mg weekly for OSA. Maximum labeled dose 15 mg weekly. Do not coadminister with other tirzepatide-containing products or any GLP-1 receptor agonist. Counsel on oral-contraceptive interaction for 4 weeks after initiation and after each escalation.

Research use only. Information on this page is editorial reference, not medical or dosing advice. Always consult qualified medical guidance before use.

Storage

Single-dose pens and vials are stored at 2-8°C, protected from light, and may be kept unrefrigerated below 30°C for up to 21 days. Multi-dose vials and the single-patient KwikPen are refrigerated before use, can sit at room temperature for up to 30 days, and once opened are discarded after 30 days, after 4 weekly doses, or after a total of 30 days at room temperature, whichever comes first. Do not freeze.

Vendors carrying Tirzepatide

No approved vendors are listing this peptide yet. Check back later or browse the full vendor directory.

Discussion

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References

[tirze-zepbound-label]
Zepbound (tirzepatide) U.S. Prescribing Information
Eli Lilly · Eli Lilly / FDA
Source
[tirze-fda-label]
FDA approved label (tirzepatide, 217806s003)
U.S. FDA · FDA
Source
[tirze-mech]
Tirzepatide as an imbalanced and biased dual GIP and GLP-1 receptor agonist
Willard FS et al. · PubMed Central
Source

Reported benefits

About 20.9% weight loss at 15 mg in SURMOUNT-1

FDA approval for obstructive sleep apnea in obesity

Type 2 diabetes glycemic control

Boxed warning: rodent thyroid C-cell tumors

Dose-related severe GI events

Pancreatitis, gallbladder disease, AKI, hypoglycemia, aspiration risk

Oral contraceptive effectiveness reduced for 4 weeks after dose changes

Discussion