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Tirzepatide

FDA Drug Information • Also known as: Mounjaro, Mounjaro Kwikpen, Zepbound, Zepbound Kwikpen

Brand Names
Mounjaro, Mounjaro Kwikpen, Zepbound, Zepbound Kwikpen
Dosage Form
POWDER
Product Type
BULK INGREDIENT

⚠ Boxed Warning (Black Box)

WARNING: RISK OF THYROID C-CELL TUMORS In both male and female rats, tirzepatide causes dose-dependent and treatment-duration-dependent thyroid C-cell tumors at clinically relevant exposures. It is unknown whether MOUNJARO causes thyroid C-cell tumors, including medullary thyroid carcinoma (MTC), in humans as human relevance of tirzepatide-induced rodent thyroid C-cell tumors has not been determined [see Warnings and Precautions ( 5.1 ) and Nonclinical Toxicology ( 13.1 )]. MOUNJARO is contraindicated in patients with a personal or family history of MTC or in patients with Multiple Endocrine Neoplasia syndrome type 2 (MEN 2) [see Contraindications ( 4 )] . Counsel patients regarding the potential risk for MTC with the use of MOUNJARO and inform them of symptoms of thyroid tumors (e.g., a mass in the neck, dysphagia, dyspnea, persistent hoarseness). Routine monitoring of serum calcitonin or using thyroid ultrasound is of uncertain value for early detection of MTC in patients treated with MOUNJARO [see Contraindications ( 4 ) and Warnings and Precautions ( 5.1 )]. WARNING: RISK OF THYROID C-CELL TUMORS See full prescribing information for complete boxed warning. Tirzepatide causes thyroid C-cell tumors in rats. It is unknown whether MOUNJARO causes thyroid C-cell tumors, including medullary thyroid carcinoma (MTC), in humans as the human relevance of tirzepatide-induced rodent thyroid C-cell tumors has not been determined ( 5.1 , 13.1 ). MOUNJARO is contraindicated in patients with a personal or family history of MTC or in patients with Multiple Endocrine Neoplasia syndrome type 2 (MEN 2). Counsel patients regarding the potential risk of MTC and symptoms of thyroid tumors ( 4 , 5.1 ).

Description

11 DESCRIPTION MOUNJARO (tirzepatide) injection, for subcutaneous use, contains tirzepatide, a once weekly GIP receptor and GLP-1 receptor agonist. Tirzepatide is based on the GIP sequence and contains 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 225 H 348 N 48 O 68 . Structural formula: MOUNJARO is a clear, colorless to slightly yellow, sterile 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. Each multi-dose vial or single-patient-use KwikPen contains 2.4 mL of solution, which provides 4 doses of 2.5 mg, 5 mg, 7.5 mg, 10 mg, 12.5 mg, or 15 mg of tirzepatide per 0.6 mL. Each dose contains the following excipients: benzyl alcohol (5.4 mg), glycerin (4.8 mg), phenol (1.08 mg), sodium chloride (1.05 mg), sodium phosphate dibasic heptahydrate (0.8 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 to 7.5. Each single-patient-use KwikPen contains additional volume to allow for device priming. Structural Formula

What Is Tirzepatide Used For?

1 INDICATIONS AND USAGE MOUNJARO ® is indicated as an adjunct to diet and exercise to improve glycemic control in adults and pediatric patients 10 years of age and older with type 2 diabetes mellitus. MOUNJARO ® is a glucose-dependent insulinotropic polypeptide (GIP) receptor and glucagon-like peptide-1 (GLP-1) receptor agonist indicated as an adjunct to diet and exercise to improve glycemic control in adults and pediatric patients 10 years of age and older with type 2 diabetes mellitus. ( 1 )

Dosage and Administration

2 DOSAGE AND ADMINISTRATION The recommended starting dosage is 2.5 mg injected subcutaneously once weekly. ( 2.1 ) After 4 weeks, increase to 5 mg injected subcutaneously once weekly. ( 2.1 ) If additional glycemic control is needed, increase the dosage in 2.5 mg increments after at least 4 weeks on the current dose. ( 2.1 ) Maximum dosage ( 2.1 ): Adults: 15 mg subcutaneously once weekly. Pediatric patients 10 years of age and older: 10 mg subcutaneously once weekly. Administer once weekly at any time of day, with or without meals. ( 2.2 ) Inject subcutaneously in the abdomen, thigh, or another person should inject in the back of the upper arm. Rotate injection sites with each dose. ( 2.2 ) Refer to the Full Prescribing Information for additional important administration instructions about MOUNJARO presentations. ( 2.2 ) 2.1 Recommended Dosage The recommended starting dosage of MOUNJARO is 2.5 mg injected subcutaneously once weekly [see Dosage and Administration ( 2.2 )] . Follow the dosage escalation below to reduce the risk of gastrointestinal adverse reactions [see Warnings and Precautions ( 5.6 ) and Adverse Reactions ( 6.1 )] . The 2.5 mg dosage is for treatment initiation and is not intended for glycemic control. After 4 weeks, increase the dosage to 5 mg injected subcutaneously once weekly. If additional glycemic control is needed, increase the dosage in 2.5 mg increments after at least 4 weeks on the current dose. The maximum dosage of MOUNJARO is: 15 mg injected subcutaneously once weekly in adults. 10 mg injected subcutaneously once weekly in pediatric patients. If a dose is missed, instruct patients to administer MOUNJARO as soon as possible within 4 days (96 hours) after the missed dose. If more than 4 days have passed, skip the missed dose and administer the next dose on the regularly scheduled day. In each case, patients can then resume their regular once weekly dosing schedule. The day of weekly administration can be changed, if necessary, as long as the time between the two doses is at least 3 days (72 hours). 2.2 Important Administration Instructions Inform patients and their caregiver(s) which MOUNJARO presentation (e.g., vial, pre-filled single-dose pen, single-patient-use KwikPen) they will receive and ensure they receive training appropriate for that specific presentation. If the prescribed MOUNJARO presentation changes, ensure patients and caregivers receive appropriate training and instruct them to consult the Instructions for Use for the newly prescribed presentation. Prior to initiation, train patients and their caregiver(s) on proper injection technique for the prescribed MOUNJARO presentation [see Instructions for Use] . After training, a patient may self-inject MOUNJARO if the healthcare provider determines that it can be properly administered, except for the following: MOUNJARO KwikPen is not recommended for self-administration by pediatric patients. MOUNJARO KwikPen is not recommended for self-administration by...

Side Effects (Adverse Reactions)

6 ADVERSE REACTIONS The following serious adverse reactions are described below or elsewhere in the prescribing information: Risk of Thyroid C-cell Tumors [see Warnings and Precautions ( 5.1 )] Acute Pancreatitis [see Warnings and Precautions ( 5.2 )] Hypoglycemia with Concomitant Use of Insulin Secretagogues or Insulin [see Warnings and Precautions ( 5.3 )] Hypersensitivity Reactions [see Warnings and Precautions ( 5.4 )] Acute Kidney Injury Due to Volume Depletion [see Warnings and Precautions ( 5.5 )] Severe Gastrointestinal Adverse Reactions [see Warnings and Precautions ( 5.6 )] Diabetic Retinopathy Complications in Patients with a History of Diabetic Retinopathy [see Warnings and Precautions ( 5.7 )] Acute Gallbladder Disease [see Warnings and Precautions ( 5.8 )] Pulmonary Aspiration During General Anesthesia or Deep Sedation [see Warnings and Precautions ( 5.9 )] The most common adverse reactions, reported in ≥5% of patients treated with MOUNJARO are nausea, diarrhea, decreased appetite, vomiting, constipation, dyspepsia, and abdominal pain. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Eli Lilly and Company at 1-800-LillyRx (1-800-545-5979) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Adverse Reactions in the Clinical Trials of Adults with Type 2 Diabetes Mellitus Pool of Two Placebo-Controlled Clinical Trials in Adults The data in Table 1 are derived from 2 placebo-controlled trials [1 monotherapy trial (SURPASS-1) and 1 trial in combination with basal insulin with or without metformin (SURPASS-5)] in adult patients with type 2 diabetes mellitus [see Clinical Studies ( 14.2 , 14.4 )] . These data reflect exposure of 718 patients to MOUNJARO and a mean duration of exposure to MOUNJARO of 36.6 weeks. The mean age of patients was 58 years, 4% were 75 years or older and 54% were male. The population was 57% White, 27% Asian, 13% American Indian or Alaska Native, and 3% Black or African American; 25% identified as Hispanic or Latino ethnicity. At baseline, patients had type 2 diabetes mellitus for an average of 9.1 years with a mean HbA1c of 8.1%. As assessed by baseline fundoscopic examination, 13% of the population had retinopathy. At baseline, eGFR was ≥90 mL/min/1.73 m 2 in 53%, 60 to 90 mL/min/1.73 m 2 in 39%, 45 to 60 mL/min/1.73 m 2 in 7%, and 30 to 45 mL/min/1.73 m 2 in 1% of patients. Pool of Seven Controlled Clinical Trials Adverse reactions were also evaluated in a larger pool of adult patients with type 2 diabetes mellitus participating in seven controlled clinical trials which included two placebo-controlled trials (SURPASS-1 and -5), three trials of MOUNJARO in combination with metformin, sulfonylureas, and/or SGLT2 Inhibitors (SURPASS-2, -3, -4) [see Clinical Studies ( 14.3 )] and two additional trials conducted in Japan. In this pool, a total of 5119 adult patients with type 2 diabetes mellitus were treated with MOUNJARO for a mean duration of 48.1 weeks. The mean age of patients was 58 years, 4% were 75 years or older and 58% were male. The population was 65% White, 24% Asian, 7% American Indian or Alaska Native, and 3% Black or African American; 38% identified as Hispanic or Latino ethnicity. At baseline, patients had type 2 diabetes mellitus for an average of 9.1 years with a mean HbA1c of 8.3%. As assessed by baseline fundoscopic examination, 15% of the population had retinopathy. At baseline, eGFR was ≥90 mL/min/1.73 m 2 in 52%, 60 to 90 mL/min/1.73 m 2 in 40%, 45 to 60 mL/min/1.73 m 2 in 6%, and 30 to 45 mL/min/1.73 m 2 in 1% of patients. Common Adverse Reactions Table 1 shows common adverse reactions, not including hypoglycemia, associated with the use of MOUNJARO in the pool of...

Drug Interactions

7 DRUG INTERACTIONS MOUNJARO delays gastric emptying and has the potential to impact the absorption of concomitantly administered oral medications. ( 7.2 ) 7.1 Concomitant Use with an Insulin Secretagogue (e.g., Sulfonylurea) or with Insulin When initiating MOUNJARO, consider reducing the dose of concomitantly administered insulin secretagogues (e.g., sulfonylureas) or insulin to reduce the risk of hypoglycemia [see Warnings and Precautions ( 5.3 )]. 7.2 Oral Medications MOUNJARO delays gastric emptying and thereby has the potential to impact the absorption of concomitantly administered oral medications. Caution should be exercised when oral medications are concomitantly administered with MOUNJARO. Monitor patients on oral medications dependent on threshold concentrations for efficacy and those with a narrow therapeutic index (e.g., warfarin) when concomitantly administered with MOUNJARO. Advise patients using oral hormonal contraceptives to switch to a non-oral contraceptive method or add a barrier method of contraception for 4 weeks after initiation and for 4 weeks after each dose escalation with MOUNJARO. Hormonal contraceptives that are not administered orally should not be affected [see Use in Specific Populations ( 8.3 ) and Clinical Pharmacology ( 12.2 , 12.3 )].

Contraindications

4 CONTRAINDICATIONS MOUNJARO is contraindicated in patients with: A personal or family history of medullary thyroid carcinoma (MTC) or in patients with Multiple Endocrine Neoplasia syndrome type 2 (MEN 2) [see Warnings and Precautions ( 5.1 )] . Known serious hypersensitivity to tirzepatide or any of the excipients in MOUNJARO. Serious hypersensitivity reactions, including anaphylaxis and angioedema, have been reported with MOUNJARO [see Warnings and Precautions ( 5.4 )] . Personal or family history of medullary thyroid carcinoma or in patients with Multiple Endocrine Neoplasia syndrome type 2. ( 4 ) Known serious hypersensitivity to tirzepatide or any of the excipients in MOUNJARO. ( 4 )

Pregnancy and Breastfeeding

8.1 Pregnancy Risk Summary Available data with MOUNJARO use in pregnant women are insufficient to evaluate for a drug-related risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy (see Clinical Considerations) . Based on animal reproduction studies, there may be risks to the fetus from exposure to tirzepatide during pregnancy. MOUNJARO should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. In pregnant rats administered tirzepatide during organogenesis, fetal growth reductions and fetal abnormalities occurred at clinical exposure in maternal rats based on AUC. In rabbits administered tirzepatide during organogenesis, fetal growth reductions were observed at clinically relevant exposures based on AUC. These adverse embryo/fetal effects in animals coincided with pharmacological effects on maternal weight and food consumption (see Data) . The estimated background risk of major birth defects is 6–10% in women with pre-gestational diabetes with an HbA1c >7% and has been reported to be as high as 20–25% in women with an HbA1c >10%. The estimated background risk of miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2–4% and 15–20%, respectively. Clinical Considerations Disease-Associated Maternal and/or Embryo/Fetal Risk Poorly controlled diabetes in pregnancy increases the maternal risk for diabetic ketoacidosis, pre-eclampsia, spontaneous abortions, preterm delivery, and delivery complications. Poorly controlled diabetes increases the fetal risk for major birth defects, stillbirth, and macrosomia-related morbidity. Data Animal Data In pregnant rats given twice weekly subcutaneous doses of 0.02, 0.1, and 0.5 mg/kg tirzepatide (0.03-, 0.07-, and 0.5-fold...

Overdosage

10 OVERDOSAGE In the event of an overdosage, consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdosage management recommendations. Initiate appropriate supportive treatment according to the patient's clinical signs and symptoms. A period of observation and treatment for these symptoms may be necessary, taking into account the half-life of tirzepatide of approximately 5 days.

How Supplied

16 HOW SUPPLIED/STORAGE AND HANDLING 16.1 How Supplied MOUNJARO is a clear, colorless to slightly yellow solution available in cartons containing 4 pre-filled single-dose pens, 1 single-dose vial, 1 multi-dose vial, or 1 Single-Patient-Use KwikPen as follows: Single-Dose Vial and Prefilled Pen Strength 4 pack Single-dose Pen NDC 1 pack Single-dose Vial NDC 2.5 mg/0.5 mL 0002-1506-80 0002-1152-01 5 mg/0.5 mL 0002-1495-80 0002-1243-01 7.5 mg/0.5 mL 0002-1484-80 0002-2214-01 10 mg/0.5 mL 0002-1471-80 0002-2340-01 12.5 mg/0.5 mL 0002-1460-80 0002-2423-01 15 mg/0.5 mL 0002-1457-80 0002-3002-01 Multi-Dose Vial Doses per Vial Strength 1-pack Multi-dose Vial NDC 4 doses of 2.5 mg/0.6 mL 10 mg/2.4 mL (4.17 mg/mL) 0002-4052-11 4 doses of 5 mg/0.6 mL 20 mg/2.4 mL (8.33 mg/mL) 0002-4103-11 4 doses of 7.5 mg/0.6 mL 30 mg/2.4 mL (12.5 mg/mL) 0002-4210-11 4 doses of 10 mg/0.6 mL 40 mg/2.4 mL (16.7 mg/mL) 0002-4304-11 4 doses of 12.5 mg/0.6 mL 50 mg/2.4 mL (20.8 mg/mL) 0002-4523-11 4 doses of 15 mg/0.6 mL 60 mg/2.4 mL (25 mg/mL) 0002-4612-11 Single-Patient-Use KwikPen (with four weekly doses) Doses per KwikPen Strength 1-pack Single-Patient-Use KwikPen NDC 4 doses of 2.5 mg 10 mg/2.4 mL (4.17 mg/mL) 0002-3466-11 4 doses of 5 mg 20 mg/2.4 mL (8.33 mg/mL) 0002-3455-11 4 doses of 7.5 mg 30 mg/2.4 mL (12.5 mg/mL) 0002-3444-11 4 doses of 10 mg 40 mg/2.4 mL (16.7 mg/mL) 0002-3433-11 4 doses of 12.5 mg 50 mg/2.4 mL (20.8 mg/mL) 0002-3422-11 4 doses of 15 mg 60 mg/2.4 mL (25 mg/mL) 0002-3411-11 16.2 Storage and Handling Do not freeze MOUNJARO. Do not use MOUNJARO if frozen. Protect MOUNJARO from heat and light. Store MOUNJARO in the original carton to protect from light. MOUNJARO Single-dose Pen and Single-dose Vial Store MOUNJARO single-dose pen and single-dose vial in a refrigerator at 2°C to 8°C (36°F to 46°F). If needed, each single-dose pen or single-dose vial can be stored unrefrigerated at temperatures not to exceed 30°C (86°F) for up to 21 days. MOUNJARO Multi-dose Vial or...

About This Information

This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.

What are side effects?

Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.

What are drug interactions?

Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.