Manjaro is prescribed through online medical consultations. Special campaign ongoing!
Order OnlineWhat is Mounjaro?
"Mounjaro" is the latest "sustained GIP/GLP-1 receptor agonist" that acts not only on GLP-1, which is well-known in medical weight loss, but also on the GIP hormone receptor. Clinical trial results have shown that GIP/GLP-1 receptor agonists have stronger appetite suppression and weight loss effects than GLP-1 receptor agonists, with the assistance of GIP. The impactful image above shows the results of weight loss effects from a clinical trial (SURMOUNT-1) using a placebo and Mounjaro. For more details, please refer to the clinical trial section below.
Mechanism of Action of Mounjaro (Tirzepatide, GIP/GLP-1 Receptor Agonist)
GIP and GLP-1 are hormones called incretins, secreted from different cells in the small intestine. GIP and GLP-1 are secreted after meals, promoting insulin secretion from the pancreas in a glucose-dependent manner, and having the effect of suppressing appetite and slowing down gastrointestinal movement, making it harder to feel hungry. This effect naturally reduces food intake and leads to weight loss.
In addition, incretin hormones are also said to act on various other organs, with effects such as improving fatty liver and reducing cardiovascular risk.
Furthermore, GIP, which has been newly added, has many beneficial effects on adipose tissue.
- GIP increases blood flow in abdominal adipose tissue.
- GIP effectively breaks down and metabolizes lipids (triglycerides) in adipose tissue, thus reducing fat accumulation.
- In obese individuals, the increase in adipose tissue blood flow due to meals and GIP is blunted, but it has been reported that this partially recovers with weight loss.
- GIP directly promotes lipogenesis in adipocytes.
- In human adipocytes cultured in vitro, GIP promotes the activation of lipoprotein lipase, an enzyme involved in lipid breakdown and uptake of circulating free fatty acids.
- In isolated rat adipocytes, GIP promotes insulin sensitivity, glucose uptake, de novo lipogenesis, and lipolysis.
- In mice and non-human primates, impaired GIP function has been reported to reduce adipose tissue accumulation and lower the risk of diet-induced obesity.
With the synergistic effect of GIP in addition to GLP-1, Mounjaro is said to be effective for weight loss.
How is Mounjaro superior to previous GLP-1 receptor agonists (Ozempic)?
Previous GLP-1 receptor agonists (such as Ozempic, Saxenda, and Rybelsus) worked only on "GLP-1," as their name suggests. However, Mounjaro, which has just been released, is a GIP/GLP-1 receptor agonist, meaning it works on both GIP and GLP-1.
The figure below compares GIP receptor agonists, GLP-1 receptor agonists (Saxenda, Rybelsus, Ozempic, etc.), and GIP/GLP-1 receptor agonists. Previous research showed that GIP alone did not demonstrate much weight loss effect. However, it was concluded that with GIP assisting the action of GLP-1, GIP/GLP-1 receptor agonists were superior to GLP-1 receptor agonists in terms of weight loss, food intake, and fat mass.
(From top: GIP receptor agonist, GLP-1 receptor agonist, GIP/GLP-1 receptor agonist)
Mounjaro's Weight Loss Effects: Clinical Study Introduction
SURMOUNT-1 Study (Mounjaro vs. Placebo)
The SURMOUNT-1 clinical trial compared "Mounjaro (tirzepatide) with a placebo." This trial included 2,539 individuals with a BMI of 30 or greater than 27, and co-morbidities other than diabetes, who were administered the drug for 72 weeks. The figure above demonstrates the remarkable efficacy of Mounjaro compared to the placebo. (Gray: placebo, Blue from lightest: Mounjaro 5mg/10mg/15mg) Significant weight loss was observed even with Mounjaro 5mg, not just the maximum dose (average weight loss: -16kg).
SURMOUNT-2 Study (Mounjaro VS Ozempic)
The SURMOUNT-2 clinical trial compared "Mounjaro (tirzepatide) with Ozempic (semaglutide/GLP-1 receptor agonist)." This clinical trial involved 1,878 individuals with an average BMI of 34.2, type 2 diabetes (on metformin), who were administered the drug for 40 weeks. The figure above shows the remarkable efficacy of Mounjaro compared to Ozempic 1mg. (Gray: Ozempic 1mg, Blue from lightest: Mounjaro 5mg/10mg/15mg) It is surprising that Mounjaro 5mg showed a higher weight loss effect than the maximum dose of Ozempic 1.0mg.
How to Use Mounjaro
This medication is administered once a week. Initially, you start with 2.5mg/dose, and after 4 weeks (from the 5th dose), you increase to 5mg/dose. The usual maintenance dose of Mounjaro is 5mg. The dose can be adjusted as needed, and if 5mg is not effective enough, the dose can be increased by 2.5mg, with an interval of at least 4 weeks. However, the maximum dose is 15mg.
How to Administer Mounjaro
Usage is just 3 steps!
- Remove the cap
- Place the base against your skin and unlock
- Press the injection button and wait 10 seconds
For detailed precautions, please refer to the separate sheet included with the medication or the diagram below.
If you forget to administer Mounjaro
Whether it's less than 72 hours or more than 72 hours from the scheduled administration date, it differs as follows.
If you are concerned, please contact the clinic!
Is it really only necessary to administer Mounjaro once every 7 days?
The blood concentration of tirzepatide in Mounjaro changes as shown in this figure, and the half-life of the drug is approximately 5 to 6 days, allowing it to act for a long period. Administration once a week is possible, reducing the burden of injections on patients. Since it is a long-acting drug, please be sure to adhere to the administration period of once a week, and never administer it daily or every other day, as it could be dangerous.
Individuals Who Cannot Use Mounjaro or for Whom it is Not Recommended
The following individuals cannot be prescribed by our clinic:
・Individuals with a history of allergic reactions to this medication
・Individuals with a BMI of 23 or less (due to precautions in the official package insert)
・Individuals with severe gastrointestinal disorders (e.g., severe gastroparesis) (gastrointestinal symptoms may worsen even without prior experience)
・Individuals with a history of pancreatitis or thyroid disease
・Patients or conditions with a risk of hypoglycemia
- Individuals engaging in intense physical exercise
- Individuals with excessive alcohol intake
・Pregnant women
・Breastfeeding women
・Elderly individuals
・Individuals taking birth control pills or Warfarin (blood-thinning medication) (not contraindicated, but may weaken the effect of the medication)
Common Side Effects of Mounjaro
The side effects of Mounjaro are basically the same as those of GLP-1 receptor agonists, and the frequency is said to be similar (gastrointestinal symptoms are reported slightly more often than with GLP-1 receptor agonists).
In clinical trials, the following gastrointestinal symptoms were reported as side effects in more than 5% of patients: nausea, vomiting, diarrhea, constipation.
As shown in the figure below, gastrointestinal side effects can be alleviated by reducing meal portions, avoiding fried foods, and stopping eating when feeling full.
Furthermore, attention must be paid to the following serious side effects:
- Hypoglycemia (caution required when used in combination with other drugs): If symptoms such as those shown in the figure below appear, please consume sugar.
- Acute pancreatitis (less than 0.1%): Although rare, if you experience sudden abdominal pain, discontinue administration and seek medical attention immediately.
When will Mounjaro (tirzepatide) be released in Japan?
Mounjaro received approval in the United States in May 2022 and sales began in June. It recently also received approval from the European Medicines Agency. In Japan, Mounjaro 2.5mg and 5mg are the latest GIP/GLP-1 receptor agonists, which became available for sale in April 2023.
Mounjaro (tirzepatide) Insurance Coverage
In Japan, as of April 2023, Mounjaro is only approved as a "treatment for type 2 diabetes." Prescriptions for weight loss purposes are self-pay. However, it has shown clear weight loss effects in clinical trials, generating significant interest and expectations as an obesity treatment.
Where can I buy Mounjaro (Tirzepatide)? Is it safe?
If you'd like to learn more about Mounjaro (tirzepatide) or other medicines from a doctor or specialist, please schedule a free online consultation at Mona Aoyama Clinic!
Manjaro is prescribed through online medical consultations. Special campaign ongoing!
Order OnlineReferences
https://www.nature.com/articles/s41574-022-00783-3
Eli Lilly｜Mounjaro® (Tirzepatide)
N Engl J Med. 2021;385(6):503-15.
Lancet. 2021;398(10295):143-55.
https://www.sciencedirect.com/science/article/pii/S0168822723005338
