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Metabolic & GLP-1PeptideEvidence A2 cited

Tirzepatide

Dual GIP/GLP-1 Receptor Agonist

aka Mounjaro · Zepbound · LY3298176

A dual GIP/GLP-1 receptor agonist that research associates with substantial body weight reduction and improved glycaemic control.

Molecular wt
4813.53g/mol
Formula
C225H348N48O68
CAS
2023788-19-2
Half-life
5 days
established
Tmax
1 day
PubChem
166567236

Sequence

One-letter26 residues

Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS-NH2

Three-letter

Tyr-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-Aib-Leu-Asp-Lys-Ile-Ala-Gln-Lys-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2

Read this before quoting the sequence
39-residue dual GIP/GLP-1 receptor agonist. FDA label: tirzepatide 'is based on the GIP sequence and contains aminoisobutyric acid (Aib) in positions 2 and 13, a C-terminal amide, and Lys residue at position 20 that is attached to 1,20-eicosanedioic acid via a linker.' The FDA GSRS registry gives the proteinogenic backbone as YAEGTFTSDYSIGLDKIAQKAFVQWLIAGGPSSGAPPPS, with Ala2 and Gly13 replaced by Aib; the C20 fatty diacid on Lys20 confers albumin binding and the ~5-day half-life. Cannot be written in plain one-letter code because Aib is non-proteinogenic.
Source ↗

Mechanism of action

Tirzepatide is a dual agonist that targets both the GLP-1 and GIP receptors. By activating these receptors, it enhances insulin secretion and reduces glucagon levels in a glucose-dependent manner. This leads to improved glycemic control and promotes weight loss by reducing appetite and increasing energy expenditure.

What the evidence actually shows

Grade A

Multiple human trials, including the SURMOUNT series, have demonstrated significant weight loss and improved glycemic control with tirzepatide. These studies show consistent results across diverse populations, but long-term safety data is still being gathered.

Regulatory status

Status
Approved. Marketed in the United States by Eli Lilly under two brand names with separate indications.
Approved as
MOUNJARO (tirzepatide) injection - adjunct to diet and exercise to improve glycaemic control in adults and paediatric patients 10 years and older with type 2 diabetes; 2.5 mg SC weekly starting dose, maximum 15 mg weekly in adults (10 mg weekly in paediatrics). ZEPBOUND (tirzepatide) injection - chronic weight management.
Clinical stage
Approved, with an extensive ongoing SURPASS/SURMOUNT trial programme.
WADA
Not named on the WADA 2026 Prohibited List; no GLP-1 or GIP receptor agonist appears on it.
UK
prescription_only

Tirzepatide is approved for use in the UK as a prescription-only medication for the treatment of type 2 diabetes.

Source ↗

Pharmacokinetics

Half-life
5 days
Tmax
1 day
Absorption
subcutaneous
Elimination
both
Washout
35 days
Titration
2.5mg x4wk then 5mg x4wk ramp
Low-confidence pharmacokinetics
These figures are recorded as established rather than measured in a published PK study. Treat them as an order of magnitude. Anything downstream of them — accumulation, steady state, washout — inherits that uncertainty.

Dosing — what backs each figure

Tirzepatide has fully established, FDA-labelled human dosing: 2.5 mg subcutaneously once weekly to start, titrated in 2.5 mg steps at intervals of at least 4 weeks to a maximum of 15 mg once weekly, across type 2 diabetes (MOUNJARO) and obesity/OSA (ZEPBOUND). It is chronic maintenance therapy, not a cycled compound.

ClinicalApproved labelling or a published human trial

  • Start 2.5 mg subcutaneously once weekly; after 4 weeks increase to 5 mg once weekly; increase in 2.5 mg increments after at least 4 weeks on the current dose; maximum 15 mg once weekly (10 mg in paediatric patients)

    Adults and paediatric patients 10 years and older with type 2 diabetes mellitus · subcutaneous (abdomen, thigh or upper arm; rotate sites)

    FDA label, MOUNJARO (tirzepatide) injection, 2026 revision ↗

  • Start 2.5 mg subcutaneously once weekly for 4 weeks, then 5 mg once weekly; increase in 2.5 mg increments after at least 4 weeks; maintenance 5, 10 or 15 mg once weekly; maximum 15 mg once weekly

    Adults with obesity, or overweight with at least one weight-related comorbidity · subcutaneous

    FDA label, ZEPBOUND (tirzepatide) injection, 2026 revision ↗

  • Maintenance 10 mg or 15 mg subcutaneously once weekly (same 2.5 mg starting dose and titration)

    Adults with obesity and moderate-to-severe obstructive sleep apnea · subcutaneous

    FDA label, ZEPBOUND (tirzepatide) injection, 2026 revision ↗

Handling and storage

Lyophilized
Not applicable - tirzepatide is supplied as a ready-to-use sterile solution, not a lyophilised powder. Label: 'Store ZEPBOUND single-dose pen and single-dose vial in a refrigerator at 2 C to 8 C (36 F to 46 F).'
Reconstituted
No reconstitution step. In-use limits from the label: single-dose pen or vial may be stored unrefrigerated at up to 30 C for a total of 21 days, then discarded. Unopened multi-dose vial or KwikPen: refrigerated until expiry, or 30 days if kept at room temperature. Opened multi-dose vial or KwikPen: discard after 30 days at room temperature, 30 days after first use, or after 4 weekly doses, whichever comes first.

Label verbatim: 'Do not freeze ZEPBOUND. Do not use ZEPBOUND if frozen. Protect ZEPBOUND from heat and light. Store ZEPBOUND in the original carton to protect from light.' Freezing is an absolute disqualifier - there is no freeze-thaw tolerance.

Source ↗
→ Reconstitution walkthrough→ Reconstitution calculator

Safety

Commonly reported
  • ·Nausea
  • ·Diarrhea
  • ·"Decreased appetite"
Rarely reported
  • ·Pancreatitis
  • ·"Thyroid tumors"
Contraindications
  • ·Personal or family history of medullary thyroid carcinoma
  • ·Multiple Endocrine Neoplasia syndrome type 2
Drug interactions
  • ·Sulfonylureas: Increased risk of hypoglycemia due to enhanced insulin secretion

Nausea, diarrhoea, decreased appetite, injection-site reactions

Reported combinations

Reported as synergistic
  • ·Metformin: May enhance glycemic control effects
Reported as antagonistic
  • ·Corticosteroids: May counteract glycemic control effects

Combination claims in this dataset are largely unsourced and should be treated as folk knowledge until a citation appears beside them.

References (2)

Data provenance

Chemistry and citations on this page were checked against primary sources on 2026-08-14. Values that could not be verified were left blank rather than filled with a plausible guess.

Research use only
This profile is educational reference material. It is not medical advice, not a prescription, and not an endorsement of self-administration. Compounds discussed here are research chemicals and most are not approved for human therapeutic use.

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