P29

Basic Information

• English Name: Tirzepatide
• Dosage Forms1: Subcutaneous injection (2.5 mg, 5 mg, 7.5 mg, 10 mg, 12.5 mg, 15 mg per 0.5 ml in single-dose pen)
• Brand Names1: Tirzepatide for type 2 diabetes, Tirzepatide for weight loss
• CAS Number2: 2023788-19-2
• Molecular Formula2: C₂₂₅H₃₄₈N₄₈O₆₈
• Molecular Weight2: 4813.45

Indications1

• Type 2 Diabetes: It is used to help lower blood sugar in adults with type 2 diabetes. It can be used as a single therapy or in combination with other diabetes medications like sulfonylureas, SGLT2 inhibitors, or metformin, along with diet and exercise.
• Weight Management: Approved for weight loss in adults with obesity or who are overweight and have weight-related medical problems, and should be combined with diet and exercise.

Mechanism of Action2

• Dual Receptor Activation: Tirzepatide is a GIP and GLP-1 receptor agonist. It activates both GIP (glucose-dependent insulinotropic polypeptide) and GLP-1 (glucagon-like peptide-1) hormone receptors.
• Insulin Secretion Promotion: It stimulates both the first and second phases of insulin secretion in a glucose-dependent manner, helping to lower blood sugar levels.
• Glucagon Reduction: Reduces the level of glucagon in the plasma, which further contributes to blood sugar control as glucagon promotes the release of glucose from the liver.
• Appetite Regulation: By activating GLP-1 receptors, it helps control appetite and calorie intake, and GIP is also thought to play a role in regulating food intake.
• Gastric Emptying Delay: Slows down the movement of food from the stomach into the small intestine, making people feel full more quickly and for a longer period, thus reducing food intake.

Clinical Trials

• SURMOUNT-1: In this trial with 2,539 overweight or obese adults (average weight 105 kg) without diabetes, after 72 weeks of treatment, participants in the 15 mg dose group had an average weight loss of 22.5%, or 24 kg.
• SURMOUNT-2: 938 diabetic obese or overweight patients (average weight 100.7 kg) participated. After 72 weeks, the 10 mg dose group had an average weight loss of 13.4% (13.5 kg), and the 15 mg dose group had an average weight loss of 15.7% (15.6 kg).
• SURMOUNT-3: In this trial, obese or overweight participants without diabetes had an average weight loss of 26.6% (29.2 kg) in the tirzepatide group over 84 weeks, compared to 3.8% (4.1 kg) in the placebo group.
• SURMOUNT-OSA: Over 72 weeks, patients in the tirzepatide treatment group had a significant average weight loss of 22.5%, compared to 3.1% in the placebo group.
• SURMOUNT-CN: Among 210 Chinese adult obese patients, at week 52, the 10 mg tirzepatide group had an average weight reduction of 13.6% (12.3 kg), and the 15 mg group had a reduction of 17.5% (16.1 kg), while the placebo group had only a 2.3% (2.1 kg) reduction.

Side Effects1

• Common Side Effects: Include abdominal pain, burping, constipation, diarrhea, dyspepsia, fatigue, gastroesophageal reflux disease, hair loss, hypersensitivity reactions, injection site reactions, nausea, and vomiting.
• Serious Side Effects: May include signs of an allergic reaction like hives, difficulty breathing, light-headedness, swelling of the face, lips, tongue, or throat; pancreatitis with severe upper stomach pain spreading to the back, nausea, and vomiting; severe stomach problems; eye side effects or vision changes; signs of a thyroid tumor such as swelling or a lump in the neck, trouble swallowing, hoarse voice, or shortness of breath; gallbladder problems; low blood sugar; and kidney problems.