Tirzepatide 10Vials/box

 

Basic Information

 

Generic Name: Tirzepatide

 

Brand Names: Mounjaro, Zepbound (for weight loss)

 

Developed/Marketed by: Eli Lilly; FDA approved in 2022 (diabetes), FDA approved in 2023 (weight loss), approved in China in 2024

 

Molecular Type: Peptide, GIP/GLP-1 dual receptor agonist

 

Specifications: Multi-dose pen, containing 2.5mg, 5mg, 10mg, and 15mg doses

 

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

 

1. GLP-1 Receptor Activation

 

Blood Sugar Reduction: Glucose-dependent insulin secretion stimulation, glucagon inhibition, reduced hepatic glucose output

 

Weight Loss: Delayed gastric emptying, increased satiety, central appetite suppression

 

2. GIP Receptor Activation

 

Improved insulin sensitivity, improved β-cell function

 

Promoted lipolysis, reduced visceral fat, protected muscle mass

 

Relief of GLP-1 Common gastrointestinal reactions to monotherapy, such as nausea and vomiting.

 

III. Indications (Clinically Approved)

 

Type 2 Diabetes in Adults: Can be used alone or in combination for patients with poor control through diet/exercise/monotherapy.

 

Long-term weight management in obese/overweight adults.

 

Obesity: BMI ≥ 28 kg/m²

 

Overweight: BMI ≥ 24 kg/m² at least one weight-related complication (hypertension, hyperlipidemia, OSA, cardiovascular disease, etc.)

 

Moderate to severe obstructive sleep apnea (OSA) in obese adults.

 

IV. Dosage and Administration (Standard Regimen)

 

Starting dose: 2.5 mg once weekly for 4 weeks (adaptation period)

 

Increase dose: 2.5 mg every 4 weeks, up to a maximum of 15 mg/week

 

Maintenance:

Diabetes/Weight Loss: 5 mg, 10 mg, 15 mg (as needed)

 

OSA: 10 mg, 15 mg

 

V. Core Clinical Efficacy

 

1. Blood Glucose Reduction

Significantly reduces HbA1c, with a maximum reduction of... 2.0%+, superior to single-target GLP-1 receptor agonists

Extremely low risk of hypoglycemia (glucose-dependent onset)

 

2. Weight loss (milestone)

15mg/week, 52 weeks: Average weight loss 16-22kg (17%-22% of initial body weight)

Chinese population: 15mg group, average weight loss 16.1kg (17.5%) over 52 weeks, 87.7% achieved ≥5% weight loss

Weight loss approaching the effect of partial bariatric surgery, superior to smegglutide

 

3. Metabolic improvement

Lowering triglycerides, increasing… HDL, improves blood pressure, reduces waist circumference

Improves non-alcoholic fatty liver disease (NAFLD), reduces liver fat, and lowers the risk of liver fibrosis

Reduces the risk of major cardiovascular adverse events (myocardial infarction, stroke)

VI. Adverse Reactions (mostly mild to moderate, mostly transient)

Common (30%-40%)

Gastrointestinal: nausea, diarrhea, vomiting, constipation, decreased appetite (significant in the initial stage of treatment, alleviates with adaptation)

Rare / Caution Required

Pancreatitis, gallbladder disease (incidence not significantly different from placebo)

Hypoglycemia (dosage reduction required when used in combination with insulin/sulfonylureas)

 

VII. Contraindications and Cautions

Absolute Contraindications

Medullary thyroid carcinoma (MTC)

Personal/family history

MEN 2 type multiple endocrine adenoma syndrome (MEN 2)

Severe hypersensitivity to telpolide or excipients

Pregnancy/ Use with caution during lactation. Contraindicated in patients with a history of pancreatitis, severe gastrointestinal disease, moderate to severe renal insufficiency, severe hepatic insufficiency, or at risk of diabetic retinopathy.

VIII. Storage and Handling

Unopened: Refrigerate at 2-8℃, protected from light, do not freeze.

Opened pen: Store at room temperature ≤30℃ for 28 days, or refrigerate at 2-8℃.

 

Note: Remaining medication in the pen should not be reused.

IX. Combination Therapy (Commonly Used Clinically)

Diabetes: Tepalpitide Metformin / SGLT-2 Inhibitor

Weight Loss Metabolic Ailment: Tepalpitide Diet Control Exercise

OSA: Tepalpitide Continuous Positive Airway Pressure (CPAP)

NAFLD: Tepalpitide Lifestyle Intervention