Characteristics of tirzepatide1.
| Drug name | Tirzepatide |
|---|---|
| Alternate names | LY-3298176, twincretin |
| Trade names | Mounjaro, Zepbound |
| CAS-No. | 2023788-19-2 |
| Chemical class | Synthetic peptide (39 amino acids) with a C20 fatty acid diacid moiety attached, dual GIP/GLP-1 receptor agonist |
| Drug class | Antidiabetic agent (incretin-based therapy), GLP-1 receptor agonist |
| Molecular formula | C225H348N48O68 |
| Molecular mass | 4,813.527 g/mol |
| Appearance | Generally, a white to off-white powder (lyophilized peptide) |
| Melting point | Not well-defined (peptide typically denatures rather than exhibiting a true melting point) |
| pKa | Not well-defined (multiple ionizable amino acid residues) |
| Half-life | 5 days (varies slightly by individual and given concentration) |
| AUC brain/AUC plasma ratio | No publicly disclosed/unknown |
| B/P ratio | No publicly disclosed/unknown |
| Solubility in water | Soluble (typical for peptide therapeutics) |
| Soluble in DMSO | Yes, though actual solubility values are not extensively documented |
| Bioavailability | Information for subcutaneous administration suggests effective absorption; precise percentage not widely reported; the drug is highly bound to plasma albumin (99%) |
| Application | Treatment of type 2 diabetes mellitus and body weight reduction (investigational and off-label research for obesity and MASLD), administered subcutaneously once weekly |
| Dosage | 1.5–15 mg (for reduction of fasting serum glucose and body weight); the initial dosage for treatment initiation is 2.5 mg once weekly |
| Maximum observed drug concentration (Cmax, ng/mL)2 | 26.0 ng/mL (29) at dosage 0.25 mg to 874 ng/mL (19) at dosage 8.0 mg |
| Time of Cmax (h)3 | 24 (24, 72) at 5 mg; high individual variation at different concentrations |
| Apparent total body clearance of drug following subcutaneous administration (L/h)2 | 0.0416 (22)–0.0553 (15) |
| Apparent volume of distribution of drug during terminal phase following subcutaneous administration (L)2 | 6.76 (18)–9.80 (7) |
| Side effects | Dose-dependent gastrointestinal discomfort (vomiting, nausea, decreased appetite, diarrhoea, and abdominal distension), sinus tachycardia, acute kidney injury, likely secondary to dehydration from gastrointestinal losses, hypersensitivity reactions, pancreatitis, and hypoglycemia |
1: Part of the information was taken from [5, 6]; 2: data are given as geometric mean (coefficient of variability CV%); 3: Median (minimum, maximum). AUC: area under the curve; B/P ratio: blood/plasma ratio; GIP: glucose-dependent insulinotropic polypeptide; GLP-1: glucagon-like peptide-1; MASLD: metabolic dysfunction-associated steatotic liver disease.