G-Protein-linked Receptor Interactions

Glucagon-like Peptide-1 (GLP-1) Agonists

GLP-1 Receptor Agonist

Glucose-dependent Insulinotropic Polypeptide Receptor Agonist

Diabetes Mellitus, Type 2

<section class="Section" data-sectioncode="34089-3"><a name="s51"></a><a name="section-10"></a><p></p><h1>11 DESCRIPTION</h1><p class="First">MOUNJARO (tirzepatide) injection, for subcutaneous use, contains tirzepatide, a once weekly GIP receptor and GLP-1 receptor agonist. It is a 39-amino-acid modified peptide based on the GIP sequence. Tirzepatide contains 2 non-coded amino acids (aminoisobutyric acid, Aib) in positions 2 and 13, a C-terminal amide, and Lys residue at position 20 that is attached to 1,20-eicosanedioic acid via a linker. The molecular weight is 4813.53 Da and the empirical formula is C<span class="Sub">225</span>H<span class="Sub">348</span>N<span class="Sub">48</span>O<span class="Sub">68</span>.</p><p>Structural formula:</p><div class="Figure"><a name="f01"></a><img alt="Structural Formula
" src="moun-uspi-chem-struc.jpg"/></div><p>MOUNJARO is a clear, colorless to slightly yellow, sterile, preservative-free solution for subcutaneous use. Each single-dose pen or single-dose vial contains a 0.5 mL solution of 2.5 mg, 5 mg, 7.5 mg, 10 mg, 12.5 mg, or 15 mg of tirzepatide and the following excipients: sodium chloride (4.1 mg), sodium phosphate dibasic heptahydrate (0.7 mg), and water for injection. Hydrochloric acid solution and/or sodium hydroxide solution may have been added to adjust the pH. MOUNJARO has a pH of 6.5 – 7.5.</p></section>

MOUNJARO

tirzepatide

Mounjaro

0.5 ML tirzepatide 10 MG/ML Auto-Injector

0.5 ML tirzepatide 10 MG/ML Auto-Injector [Mounjaro]

0.5 ML tirzepatide 30 MG/ML Auto-Injector

0.5 ML tirzepatide 30 MG/ML Auto-Injector [Mounjaro]

0.5 ML tirzepatide 5 MG/ML Auto-Injector

0.5 ML tirzepatide 5 MG/ML Auto-Injector [Mounjaro]

0.5 ML tirzepatide 20 MG/ML Auto-Injector

0.5 ML tirzepatide 20 MG/ML Auto-Injector [Mounjaro]

0.5 ML tirzepatide 25 MG/ML Auto-Injector

0.5 ML tirzepatide 25 MG/ML Auto-Injector [Mounjaro]

0.5 ML tirzepatide 15 MG/ML Auto-Injector

0.5 ML tirzepatide 15 MG/ML Auto-Injector [Mounjaro]

0.5 ML tirzepatide 15 MG/ML Injection

0.5 ML tirzepatide 15 MG/ML Injection [Mounjaro]

0.5 ML tirzepatide 10 MG/ML Injection

0.5 ML tirzepatide 10 MG/ML Injection [Mounjaro]

0.5 ML tirzepatide 5 MG/ML Injection

0.5 ML tirzepatide 5 MG/ML Injection [Mounjaro]

0.5 ML tirzepatide 30 MG/ML Injection

0.5 ML tirzepatide 30 MG/ML Injection [Mounjaro]

0.5 ML tirzepatide 25 MG/ML Injection

0.5 ML tirzepatide 25 MG/ML Injection [Mounjaro]

0.5 ML tirzepatide 20 MG/ML Injection

0.5 ML tirzepatide 20 MG/ML Injection [Mounjaro]

Psoriasis (PsO)

Psoriatic Arthritis (PsA)

Ankylosing Spondylitis (AS)

Nonradiographic Axial Spondyloarthritis

Taltz

Juvenile Idiopathic Arthritis

Hidradenitis Suppurativa (HS)

Cosentyx

Siliq

Tremfya

Crohn's Disease (CD)

Ulcerative Colitis (UC)

Stelara

Skyrizi

Ilumya

Migraine

Cluster Headache

Migraine Prevention

Emgality

Qulipta

Acute Migraine

Ubrelvy

Nurtec ODT

Vyepti

Aimovig

Ajovy

Breast Cancer: HR+ (HER2-)

Verzenio

Ibrance

Kisqali

Atopic Dermatitis (Eczema)

Cibinqo

Eucrisa

Asthma (injectable)

Asthma OCS Dependent

Nasal Polyposis

Eosinophilic Esophagitis (EoE)

Prurigo Nodularis

Dupixent

Opzelura

Adbry

NSCLC ALK+ OR ROS1+ Disease

Lorbrena

Alecensa

Alunbrig

NSCLC cMET Mutation

Xalkori

Rheumatoid Arthritis (RA)

Xeljanz

Uveitis

Graft Versus Host Disease (GVHD)

Orencia

COVID-19 Treatment

Alopecia Areata

Olumiant

Multiple Sclerosis (MS)

Secondary Progressive Multiple Sclerosis

Zeposia

Rinvoq

Entyvio

Mounjaro (tirzepatide) is prescribed for adults with type 2 diabetes to effectively lower blood sugar levels (blood glucose). Administered as a once-weekly injection, Mounjaro is an integral component of a comprehensive approach that includes dietary adjustments and regular physical activity. 

The mechanism of Mounjaro involves a multifaceted approach to blood sugar reduction. It enhances insulin production, decreases sugar production by the liver, and retards the pace at which food moves through the digestive system, thereby prolonging the sensation of fullness. This intricate interplay is facilitated through the activation of the body's innate receptors for GIP and GLP-1, which are natural incretin hormones.

Type 2 diabetes arises when the body fails to adequately produce or utilize insulin, causing blood sugar levels (HbA1c) to become excessively elevated. Over time, heightened blood sugar levels can lead to serious health complications, including cardiovascular disease, impaired vision, and kidney dysfunction.

Distinguished as the pioneer GIP/GLP-1 receptor agonist, Mounjaro acts on two vital receptors: the glucose-dependent insulinotropic polypeptide (GIP) receptors and the glucagon-like peptide-1 (GLP-1) receptors.

It is important to emphasize that Mounjaro is unsuitable for individuals with type 1 diabetes. Furthermore, the use of this medication in individuals with a history of pancreatitis remains uncertain.

Mounjaro achieved FDA approval on May 13, 2022, for the purpose of enhancing blood sugar (glucose) control in adults diagnosed with type 2 diabetes mellitus. Its effectiveness is maximized when integrated into a comprehensive strategy involving dietary modifications and regular physical exercise.