Tirzepatide

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Tirzepatide API

Tirzepatide is a novel dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist. These dual GIP/GLP-1 agonists demonstrate improved glucose control and weight loss compared to a selective GLP-1 receptor agonist. Tirzepatide can activate both GLP-1 and GIP receptors simultaneously, which results in superior metabolic effects.

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Tirzepatide

Peptide Name: Tirzepatide
CAS Number: 2023788-19-2
Formula: C_₂₂₅H_₃₄₈N_₄₈O_₆₈
Molecular Weight: 4813g/mol
Sequence: YXEGT FTSDY SIXLD KIAQK AFVQW LIAGG PSSGA PPPS
Purity: 98%
Type: Drug Peptides, Synthetic peptide,

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Tirzepatide Description

Tirzepatide is a GIP analog and GLP-1 receptor agonist, it can improve glycemic control in adults with type 2 diabetes, and reduce weight in long-term for obesity and overweight. It is also approved for the treatment of moderate-to-severe obstructive sleep apnea in adults with obesity. However, tirzepatide is not indicated for patients with type 1 diabetes mellitus.

Chemical Structure

Tirzepatide is a linear polypeptide of 39 amino acids with chemical modification of lipidation, this improves its uptake into cells and its stability to metabolism.
Tirzepatide is a 39 amino acid linear synthetic peptide with conjugation of 1 C20 fatty diacid moiety. Its protein sequence is based on endogenous GIP, and its pharmacological action on GLP-1 receptors is comparable to endogenous GIP.
Tirzepatide conjugates a C20 fatty moiety through the hydrophilic linker at the lysine residue(Position 20). This binds highly to albumin in the plasma, and prolongs half-life. Therefore, it has the long half-life for once-weekly dosing.

Clinical Efficacy

Tirzepatide has extensive efficacy in clinical trials:

Blood Sugar Control: Tirzapatide achieves significant reduction in HbA1c levels, this surpasses other diabetes medications.
Weight Loss: Dual action of tirzapatide contributes to unparalleled results in weight loss. The level of weight loss is comparable to bariatric surgey, this is a significant advancement in non-surgical treatment options for obesity.
Cardiovascular Benefits:Tirzepatide has potential cardiovascular benefits like reduction in blood pressure and lipid levels.

Tirzepatide Reference

Mechanism of Action

Tirzepatide provides greater affinity to GIP receptors than to GLP-1 receptors, this dual agonist contribute to greater reductions of hyperglycemia. In signaling studies, tirzepatide mimics the action of natural GIP. While at GLP-1 receptor, it indicates bias toward cAMP generation rather than β-arrestin recruitment. This combination of preference increases insulin secretion. This dual-action mechanism involves several key processes:

Enhance Insulin Secretion: By activation of both GIP and GLP-1, tirzepatide stimulate insulin release significantly in response to high glucose level. This maintains glycemic control and minimizes the hypoglycemia.
Glucagon Suppression: GLP-1 receptor activation reduces glucagon release, it reduce hepatic glucagon production in the liver. This results in improved fasting and postprandial glucose levels.
Appetite Regulation: GLP-1 can slow gastric emptying, result in increased satiety and control of post-meal sugar spikes. The activation of GIP receptors enhance this effect by improving energy balance and fat metabolism.
Fat Metabolism for Weight Loss: GIP receptor activation can influence fat metabolism, it enhances the ability to break down stored fat for energy. This is the unique feature of tirzepatide different from GLP-1 only therapies.
Improve Insulin Sensitivity: Tirzepatide improves insulin sensitivity in peripheral tissues, contributes to effective glucose uptake and utilization. This is specially beneficial for individuals with insulin resistance(Type2 diabetes).