Tirzepatide 1kits (10Vials)

Tirzepatide is a GIP/GLP-1 dual receptor agonist developed by Eli Lilly (the world's first), marketed under the brands Mounjaro (diabetes), Zepbound (weight loss), and Mufengda® 

Tirzepatide

Administration: Subcutaneous injection, once weekly (half-life approximately 5 days).

Core Function: Dual effect of lowering blood sugar and reducing weight; one of the first-line drugs for metabolic syndrome.

II. Mechanism of Action (Dual-Target Synergistic Effect)

Simultaneously activates two incretin receptors, 1+1>2:

GLP-1 Receptor Activation:

Glucose-dependent insulinotropic secretion → Lowering blood sugar.

Inhibition of glucagon, delaying gastric emptying → Enhancing satiety and reducing appetite.

GIP Receptor Activation:

Synergistically promotes insulin secretion and improves insulin sensitivity.

Reducing visceral fat, regulating lipid metabolism, and reducing nausea

III. Core Efficacy and Clinical Data

1. Blood Sugar Reduction (Type 2 Diabetes)

   HbA1c Reduction: 1.8%–2.0% (Superior to most single-target GLP-1 inhibitors).

Suitable for: Type 2 diabetes patients with poor diet and exercise control, and comorbid obesity/cardiovascular disease.

2. Effective Weight Loss (Obesity/Overweight)

   Weight Loss: 15%–21% (72 weeks, up to 24 kg), approaching the effect of bariatric surgery.

Suitable for:

BMI ≥30 kg/m² (Obesity);

BMI ≥27 kg/m² (Overweight) + at least 1 comorbidity (hypertension, dyslipidemia, diabetes, sleep apnea).

3. Comprehensive Metabolic Improvement

  Blood Lipids: Lowers triglycerides, increases high-density lipoprotein.

Blood Pressure: Average reduction of systolic blood pressure by 4–6 mmHg.

Fatty Liver: Significantly reduces liver fat content.

Cardiovascular: Reduces the risk of major adverse cardiovascular events.

4. Other Indications

 Obstructive Sleep Apnea (OSA): Improvement of OSA associated with moderate to severe obesity (National Health Insurance Administration).

IV. Dosage and Administration (Adults)

Initial: 2.5 mg once weekly for 4 weeks.

Regular: 5 mg → 7.5 mg → 10 mg → 12.5 mg → 15 mg (increases every 4 weeks).

Usually used maintenance: 5–15 mg/week (10–15 mg is commonly used for weight loss).

V. Common Side Effects and Contraindications

1. Common (mostly mild to moderate, lessening over time)

Gastrointestinal: Nausea, diarrhea, vomiting, constipation (incidence approximately 30%–50%).

Other: Headache, fatigue, hypoglycemia (when used in combination with hypoglycemic agents).

2. Contraindications

Personal/family history of medullary thyroid carcinoma (MTC).

Multiple endocrine neoplasia type 2 (MEN2).

Contraindications: Hypersensitivity to telpotrebide or any of its components.

Type 1 diabetes or diabetic ketoacidosis.

3. Contraindications for use with caution: History of pancreatitis, severe gastrointestinal disease, gallbladder disease, renal insufficiency.

VI. Comparison of Advantages (vs. smegglutide)

    Stronger weight loss: telpotrebide 15%–21%; smegglutide approximately 15%.

Comparable or better blood sugar control.

Slightly lower incidence of nausea (GIP receptors can alleviate GLP-1-related nausea).

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