Limitations: Small phase 2 completer analysis; no multiplicity adjustment. DXA lean mass is not muscle function; exploratory function showed no notable difference. Eight weeks after stopping both drugs, the lean-mass difference narrowed to 0.9 kg.
Uses, doses and availability depend on the formulation, indication and country. Study doses below describe research; they are not prescribing instructions.
The active peptide and its covalent lipid/linker modifications, reproduced from the official product label.
Shown: Active peptide; formulation excipients excluded.
Official two-dimensional structural formula. The letters denote amino-acid residues; the lipid side chain and linkers are included. This is not an experimental three-dimensional conformation.
Eli Lilly prescribing information via DailyMed/NLM
A next milestone is not summarized for this therapy. This does not mean development has ended.
Development history13 selected milestones
Tirzepatide · compound history across indications
Selected clinical milestones from the documented 2016 phase 1 study through diabetes approval and later indications. A precise discovery date and a complete list of studies have not been established here.
Study start
Phase 1 human study begins (LY3298176)
NCT02759107 began testing safety, pharmacokinetics and early glucose effects in healthy participants and people with type 2 diabetes. LY3298176 is the development code for tirzepatide.
Discovery and phase 1 proof-of-concept paper published
The paper describes preclinical characterization and the phase 1 human study. This is its online publication date, not the date the molecule was discovered or first tested in people.
The randomized 26-week dose-ranging study reported glycemic efficacy and safety in The Lancet. This is the online publication date; the print issue followed in November.
NCT03730662 began comparing tirzepatide with insulin glargine in adults with type 2 diabetes and increased cardiovascular risk. SURPASS trial numbers do not indicate their chronological order.
The head-to-head diabetes trial against semaglutide 1 mg was published online in NEJM. This is the study supplying the tirzepatide endpoint in the HbA1c plot; its results preceded Mounjaro approval.
Lilly reported submission of the tirzepatide new drug application for type 2 diabetes, using a priority review voucher. This dates the announcement; the release does not establish the exact submission day.
Tirzepatide versus higher-dose semaglutide comparison depends on estimand
A new comparison uses separate SURMOUNT-1 and STEP UP trials, not randomization between tirzepatide and semaglutide 7.2 mg. Adjusted for sex, age, initial weight and A1c; residual cross-trial differences remain. Credible intervals are not confidence intervals. This indirect comparison does not establish head-to-head superiority.
