Drug name
Last update: Jul 2026Tirzepatide
Developer(s)
Drug information
Tirzepatide
Mounjaro; Zepbound
Biotherapeutic
Not provided
Tirzepatide, a therapeutic protein with a molecular weight of 4810.52 Da, functions as a glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) agonist. It is used to treat type 2 diabetes (T2DM). The half-life is around 5 days, with peak concentrations ranging from 8 to 72 hours. Tirzepatide mimics native GIP at the GIP receptor, but at the GLP-1 receptor, it favors cAMP generation over β-arrestin recruitment, resulting in a lower ability to stimulate GLP-1 receptor internalization compared to GLP-1. Additionally, patients administered tirzepatide experience substantial weight reduction.
Tirzepatide, in various strengths has been approved in more than 40 countries, for use in one or more indications.
Mounjaro and Zepbound are approved by several regulatory authorities globally
Therapeutic area(s)
- Diabetes : "Also investigated in Type 1 diabetes"
- Obesity / Weight Management
- Cardiovascular : "Heart Failure with Preserved Ejection Fraction (HFpEF) and cardiovascular mortality reduction (investigational)"
- Obstructive sleep apnea
- Metabolic Dysfunction-Associated Steatohepatitis (MASH/NASH) : "investigational"
- Treatment
- Prevention
Administration route
Subcutaneous
Associated long-acting platforms
Solution
Use of drug
- Administered by a community health worker
- Administered by a nurse
- Administered by a specialty health worker
- Self-administered
- Weekly
Dosage
2.5 mg/0.5 ml; 5 mg/0.5 ml; 7.5 mg/0.5 ml; 10 mg/0.5 ml; 12.5 mg/0.5 ml; 15 mg/0.5 ml
15 mg SC Q1W (once weekly)
Initial Dose: 2.5 mg SC Q1W Maintenance dose: After 4 weeks, increase to 5 mg SC Q1W, then every 4 weeks, increase the dose by 2.5 mg increments.
Inject the tirzepatide prefilled injection subcutaneously in the abdomen, thigh, or upper arm
Associated compounds, formulations and regimens
Not provided
Associated technologies
Not provided
Additional information
Developer(s)
Eli Lilly
Colonel Eli Lilly created Eli Lilly and Company, also known as Lilly, an American international pharmaceutical firm with headquarters in Indianapolis, Indiana, and offices in 18 countries, in 1876. The company researches, develops, produces, and markets medicinal products, with a focus on therapeutic areas such as diabetes, oncology, immunology, and neuroscience.
Drug structure
Scale-up and manufacturing prospects
Investment in Tirzepatide API production has risen to 9 million USD in 2024 by the innovator.
Plug-Flow Reactors (PFRs), PTFE tubing and inline mixers, temperature-controlled baths, surge vessels, nanofiltration systems with ceramic membranes, high-pressure pumps, glass-lined or stainless-steel reactors, cooling systems, MTBE precipitation tanks, filtration units, and vacuum dryers.
Tirzepatide is manufactured in an ISO 8/7 room using a hybrid SPPS/LPPS strategy. Four peptide fragments are first synthesized via SPPS, then coupled in solution using continuous flow reactors with real-time HPLC monitoring. Step 1: Join fragments 2 and 3 in DMSO/ACN with PyOxim and iPr₂NEt, followed by Fmoc removal and nanofiltration. Step 2: Couple the product with fragment 4 under similar conditions, then solvent-swap to DMF. Step 3: Join fragment 5 using HATU at 0°C, followed by precipitation. Step 4: Remove 19 protecting groups using TFA/TIPS/DTT, resulting in crude tirzepatide.
1. HPLC (High-Performance Liquid Chromatography)/ PATROL HPLC 2. Mass Spectrometry (MS)
Excipients & delivery device(s)
No proprietary excipient used
Sodium chloride (NaCl), sodium phosphate dibasic heptahydrate (Na₂HPO₄·7H₂O), water for injection (WFI), HCL solution, and/or NaOH solution.
No residual solvent used
No delivery device
Safety, Efficacy and Evidence Summary
Not provided
Not provided
Not provided
Not provided