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In 2022, the World Health Organization reported that 2.5 billion adults worldwide were overweight, including 890 million classified as obese. Obesity, a chronic condition characterized by excessive body fat, is closely linked to type 2 diabetes—a connection supported by extensive research. As one of the most significant risk factors for diabetes, obesity contributes to serious health complications like heart disease and stroke.

New medications, such as tirzepatide, offer promising solutions by addressing both type 2 diabetes and obesity, enabling better management of these interconnected conditions. This makes tirzepatide a groundbreaking treatment option for individuals seeking effective solutions.

This guide provides insights into what is tirzepatide, covering its benefits, side effects, cost, and other essential details.

Key Takeaways

  • What it does: Tirzepatide, sold under the brand names Mounjaro and Zepbound, is a medicine that helps manage type 2 diabetes and supports long-term weight loss.
  • How it’s taken: It is administered as a once-weekly subcutaneous injection using a pre-filled pen.
  • It’s side effects: Some people may experience side effects like nausea or diarrhea, especially when starting or increasing the dose. These side effects typically improve over time.
  • How it works: Tirzepatide activates GIP and GLP-1 receptors, which help regulate blood sugar levels and increase insulin production in response to meals. It also reduces appetite, contributing to weight loss.
  • Results: Clinical studies show that tirzepatide can lower HbA1c levels by up to 2.3%. It also supports significant weight loss, with reductions of up to 20% in people with obesity or weight-related health conditions.
  • Better than semaglutide: Tirzepatide has been shown to outperform semaglutide in lowering blood sugar (HbA1c levels) and supporting greater weight loss.

What is tirzepatide used for?

Tirzepatide is a medication primarily used to help manage blood sugar levels in adults with type 2 diabetes. It is also prescribed to aid in weight loss for individuals with obesity or certain weight-related health conditions. Beyond these uses, studies suggest it may have potential benefits for other conditions, including:

    • Obstructive Sleep Apnea (OSA): The SURMOUNT-OSA Phase 3 trials demonstrated that tirzepatide significantly reduced the severity of OSA in individuals with obesity. It lowered the apnea-hypopnea index (AHI) by up to 62.8%, and in some cases, up to 52% of patients experienced complete resolution of symptoms.
    • Cardiovascular Risks and Heart Disease: The Phase 3 SUMMIT trial evaluated tirzepatide in adults with heart failure with preserved ejection fraction (HFpEF) and obesity. The medication reduced the risk of worsening heart failure events and cardiovascular death by 38%.
    • Metabolic Dysfunction-Associated Steatohepatitis (MASH): The SYNERGY-NASH Phase 2 study evaluated the efficacy and safety of tirzepatide at various doses in adults with biopsy-confirmed MASH, a progressive form of fatty liver disease previously referred to as NASH. Results showed that more than half of patients (73.3%) achieved improvement after 52 weeks.

Medical Insight

Dr. Rohit Loomba, a leading gastroenterologist, emphasized the significance of these findings, noting that MASH is the second most common cause of liver transplantation in the US and a growing public health concern.

    • Chronic Kidney Disease (CKD): A Phase 2 clinical trial, TREASURE-CKD, is underway, with results anticipated in 2026. This study aims to explore tirzepatide’s potential in addressing CKD in individuals with obesity, both with and without type 2 diabetes.

These findings highlight tirzepatide’s potential as a multifaceted treatment that addresses a range of health conditions.

How does tirzepatide work?

In people with type 2 diabetes, a natural process called the incretin effect doesn’t work as well as it should. This effect normally helps control blood sugar levels after eating, so when it’s impaired, blood sugar can stay too high after meals. Tirzepatide helps with this problem by activating the receptors of two incretins in the body.

1. Glucagon-like peptide-1 (GLP-1)

During digestion, GLP-1 is released from the gut to signal the pancreas to produce insulin. Insulin facilitates the movement of sugar (glucose) from the bloodstream into cells, where it is used for energy. GLP-1 also slows gastric emptying, leading to prolonged satiety after meals. This mechanism helps reduce overeating and maintain stable blood sugar levels.

2. Glucose-dependent insulinotropic polypeptide (GIP)

This hormone complements the effects of GLP-1 by influencing insulin release in response to rising blood sugar levels. Additionally, researchers have discovered its significant role in managing how the body processes and stores fat.

GIP helps the body use fat tissue more efficiently to prevent fat from “spilling over” into other parts of the body, like the liver, muscles, heart, or pancreas. This type of fat accumulation, known as ectopic fat, is linked to serious conditions such as:

    • Insulin resistance
    • Fatty liver disease
    • Heart problems

This is particularly beneficial because type 2 diabetes is closely connected to these diseases. These conditions often contribute to each other’s progression, creating a vicious cycle where one worsens the others over time.

Fun Fact!

Unlike most diabetes medications that focus on a single pathway, tirzepatide stands out as the first-ever “twincretin,” combining the actions of two key hormones into a single treatment. This innovative dual-action approach marks a significant medical breakthrough, setting it apart from traditional therapies.

What are the side effects of tirzepatide?

The side effects of tirzepatide can vary but are generally divided into common and serious effects. The common side effects include:

    • Nausea 
    • Diarrhea
    • Vomiting
    • Constipation
    • Decreased appetite
    • Abdominal pain
    • Dyspepsia
    • Injection site reactions
    • Fatigue
    • Hypersensitivity reactions
    • Burping/belching
    • Hair loss
    • Gastroesophageal reflux disease (GERD)

Serious side effects may include:

Serious side effects reported in clinical trials Signs and symptoms to monitor
Pancreatitis Severe abdominal pain that may radiate to the back, nausea, or vomiting
Hypoglycemia (low blood sugar) Dizziness, sweating, confusion, shakiness
Serious hypersensitivity reactions Rash, itching, difficulty breathing, or swelling of the face, lips, or throat
Acute kidney injury Decreased urine output, swelling in the legs, ankles, or feet (edema), feeling unusually tired or weak
Severe gastrointestinal adverse reactions Persistent nausea or vomiting that prevents eating or drinking, diarrhea lasting several days, dehydration
Progression of diabetic retinopathy (in patients with a history of the condition) Blurred or fluctuating vision, difficulty seeing in low-light conditions, dark spots or floaters in vision
Acute gallbladder disease Pain in the upper right abdomen, fever, or jaundice
Pulmonary aspiration during general anesthesia or deep sedation Coughing or choking during or after the procedure, difficulty breathing, wheezing, feeling of something “stuck” in the throat or chest
Suicidal behavior and ideation Persistent feelings of hopelessness or worthlessness, intense sadness or depression, extreme mood swings or irritability, fatigue or lack of energy, changes in sleep patterns
Thyroid Tumors (seen in animal studies only) Lump in the neck, hoarseness, or difficulty swallowing

What is the brand name for tirzepatide?

Tirzepatide is marketed under two brand names:

The FDA approved Mounjaro on May 13, 2022, to treat type 2 diabetes. Later, on November 8, 2023, Zepbound was approved to help with long-term weight loss for people who are obese or overweight and have a related health condition.

Both brands are available as single-dose pens for a weekly injection, offered in the following strengths:

    • 2.5 mg
    • 5 mg
    • 7.5 mg 
    • 10 mg
    • 2.5 mg
    • 15 mg

Tirzepatide for Weight Loss (Zepbound)

The SURMOUNT clinical trial program evaluated the efficacy and safety of tirzepatide for weight management in adults with obesity or overweight. The longest trial was SURMOUNT-4, which lasted a total of 88 weeks.

The design of the study involved a 36-week period where all participants received tirzepatide, followed by a 52-week phase where participants were randomized to continue tirzepatide or switch to a placebo.

Participants who completed the 36-week lead-in phase saw an average weight loss of 20.9%. From week 36 to week 88, participants who continued on tirzepatide lost an additional 5.5% of their weight, while those who switched to placebo regained 14%.

By week 88, 89.5% of those taking tirzepatide maintained at least 80% of their weight loss from the lead-in period, compared to only 16.6% in the placebo group. The tirzepatide group achieved a total average weight reduction of 25.3% by week 88, compared to 9.9% with placebo. The most common side effects were mild to moderate gastrointestinal issues, which occurred more often with tirzepatide than placebo.

Zepbound, tirzepatide for weight loss

Tirzepatide for Type 2 Diabetes (Mounjaro)

Across all SURPASS clinical trials, tirzepatide significantly reduced HbA1c (a measure of long-term blood sugar control) in people with type 2 diabetes and consistently outperformed comparator treatments.

For instance, in the SURPASS-2 trial (tirzepatide vs semaglutide for type 2 diabetes), tirzepatide achieved greater reductions in HbA1c, ranging from 2.01% to 2.30%, compared to 1.86% with semaglutide. Additionally, up to 92% of participants on tirzepatide reached HbA1c levels below 7%, demonstrating superior efficacy. It also resulted in more weight loss, with reductions ranging from approximately 17.2 lbs to 27.3 lbs, compared to 13.7 lbs with semaglutide.

The most common side effects were related to the digestive system and were usually mild to moderate. These included nausea, diarrhea, and vomiting. Low blood sugar was rare, occurring in 0.6–1.7% of tirzepatide users, depending on the dose, and in 0.4% of those taking semaglutide. Serious side effects were reported in 5–7% of tirzepatide users and 3% of semaglutide users.

Mounjaro, tirzepatide for type 2 diabetes

What is the cost of tirzepatide?

The cost of tirzepatide depends on several factors, including insurance coverage and location. Without insurance, it can be quite expensive. For example, the list price for Zepbound is $1,059.87 per month (four pens), while Mounjaro is slightly higher at $1,069.08 for the same supply.

The list price is the manufacturer’s suggested price before any discounts, insurance adjustments, or pharmacy markups. However, the actual amount charged at pharmacies—the retail price—can be significantly higher due to factors like supply and demand, geographic location, and additional pharmacy fees. Retail prices can climb as high as $1,500.

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Wrap-up

Losing weight and managing diabetes can be challenging, but it is achievable with the help of tirzepatide. Clinical trials have shown significant benefits, including weight loss and improvements in cardiovascular health. Although it may cause mild gastrointestinal side effects, tirzepatide is considered a highly effective treatment option. It is essential to consult a healthcare provider before starting tirzepatide to determine if it is the right treatment choice.

Frequently Asked Questions

Tirzepatide belongs to the incretin mimetic drug class, specifically a dual GIP/GLP-1 receptor agonist. This class of drugs mimics the effects of incretin hormones, which help regulate blood sugar levels and appetite.

The main difference between semaglutide and tirzepatide is that semaglutide is a GLP-1 receptor agonist that mimics the GLP-1 hormone. In contrast, tirzepatide is a dual agonist, mimicking both the GLP-1 and GIP hormones.

Tirzepatide is generally considered more effective than semaglutide for weight loss. In a large study, patients taking tirzepatide were more likely to achieve significant weight loss (5%, 10%, or 15%) than those on semaglutide. Over 12 months, tirzepatide users experienced more substantial reductions in weight at each time point. Both treatments had similar rates of gastrointestinal side effects. Moreover, in a clinical study of patients with type 2 diabetes, tirzepatide demonstrated clear superiority over semaglutide in reducing glycated hemoglobin (HbA1c) levels. After 40 weeks, tirzepatide at all doses (5 mg, 10 mg, and 15 mg) showed more significant reductions in HbA1c compared to semaglutide.

Compounded tirzepatide is a custom formulation created by pharmacies to meet specific patient needs, such as adjusting dosages in response to previous shortages. The safety and efficacy of these compounded versions are not guaranteed like those of the original formulations. Compounding was more common when tirzepatide was on the FDA’s shortage list, but it is no longer on that list, making compounding unnecessary at this time.

Tirzepatide has a half-life of approximately five days, meaning it takes about five days for half of the drug to be eliminated from the body. If an individual discontinues tirzepatide, it is typically cleared from their system within about 30 days. This extended half-life enables a convenient once-weekly dosing schedule.

If tirzepatide is not refrigerated, it may lose its effectiveness. It can be stored at room temperature (up to 30°C or 86°F) for up to 21 days. After 21 days, it should be discarded if unused.

Retatrutide and tirzepatide both show effectiveness in managing diabetic kidney disease (DKD), blood glucose, and body weight. However, retatrutide outperforms tirzepatide in improving kidney function and body weight, while tirzepatide is more effective at controlling blood glucose. Overall, both drugs have significant benefits, with their specific strengths depending on the desired outcome.

Yes, tirzepatide can potentially cause depression as a side effect, although this is uncommon. Individuals experiencing mood changes, such as anxiety, anger, restlessness, or depression, should consult their doctor. Healthcare providers can assess the situation and monitor symptoms effectively.

The potential link between tirzepatide and cancer is still controversial. Some studies suggest that tirzepatide could promote cancers of the pancreas, thyroid, breast, liver, and colon, but current short-term data isn’t enough to confirm these risks. Long-term exposure to tirzepatide may cause cancer progression in target tissues, but more research is needed to fully understand the potential risks. Ongoing clinical trials and long-term follow-up are necessary to evaluate tirzepatide’s safety and any possible links to cancer.

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