Tirzepatide

Summary

Tirzepatide is a synthetic 39‑amino‑acid peptide administered subcutaneously once weekly for treatment of type 2 diabetes and chronic weight management.

Mechanism of Action

Agonist of glucose‑dependent insulinotropic polypeptide (GIP) and glucagon‑like peptide‑1 (GLP‑1) receptors, enhancing glucose‑dependent insulin secretion, suppressing glucagon, delaying gastric emptying and reducing appetite.

Routes of Administration

Goals & Uses

• Chronic Weight ManagementObesityHigh
• Cardiovascular risk reductionCardiovascularModerate
• Non-alcoholic fatty liver disease (MASH/NASH)Hepatic / MetabolicModerate
• Reduction of obstructive sleep apnea severityPulmonary / SleepModerate
• Appetite suppression and satietyNeurological / BehavioralHigh
• Weight loss / obesity managementMetabolicHigh
• Glycemic control in type 2 diabetesMetabolicHigh
• Type 2 diabetes mellitusMetabolicHigh

Contraindications

• Personal or family history of medullary thyroid carcinoma (MTC)OncologicHigh
• Multiple endocrine neoplasia syndrome type 2 (MEN2)OncologicHigh
• Medullary thyroid carcinoma (MTC)OncologyHigh
• PregnancyPopulationModeratePotential fetal risk or insufficient safety data
• Type 1 diabetes mellitusEndocrineHigh
• Multiple endocrine neoplasia type 2 (MEN 2)OncologyHigh
• Hypersensitivity to tirzepatide or excipientsImmunologicalHigh

Adverse Effects

• PancreatitisGastrointestinalRareInflammation of the pancreas
• HypoglycemiaMetabolicUncommonAbnormally low blood glucose
• Injection site reactionsLocalCommon
• ConstipationGastrointestinalCommonReduced bowel frequency or difficulty passing stool
• NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
• VomitingGastrointestinalCommonForceful expulsion of stomach contents
• Injection site reactionLocalCommonRedness, swelling, itching, bruising, or pain at the injection site
• DiarrheaGastrointestinalCommonLoose or frequent stools

Drug Interactions

• Insulin and insulin secretagogues (e.g., sulfonylureas)High
• Oral contraceptivesLowDelayed gastric emptying may affect absorption timing
• InsulinModerateMay increase risk of low blood sugar
• WarfarinModerate
• CyclosporineModerate
• SulfonylureasModerateMay increase risk of low blood sugar

Population Constraints

• PregnancyReproductive SafetyAbsolute
• Pediatric patients (<18 years)AgeRelative
• Lactation / BreastfeedingReproductiveRelative
• Pediatric patientsAgeAbsolute
• Severe renal impairment / End-stage renal diseaseRenalRelative
• History of pancreatitisGastrointestinalRelative
• Severe renal impairment (eGFR <30 mL/min/1.73 m²)RenalRelative
• Severe gastrointestinal diseaseGastrointestinalRelative

Regulatory Status

• European UnionApprovedApproved: type 2 diabetes mellitus, obesityEMA approval for diabetes (2022) and obesity (2023).
• United StatesApprovedApproved: type 2 diabetes mellitus, chronic weight managementFDA approved under brand Mounjaro.
• United KingdomApprovedApproved: type 2 diabetes mellitus, obesityMHRA approval aligned with EMA.

FDA approved (2022) for type 2 diabetes; FDA approved (2023) for chronic weight management under the brand Mounjaro. EMA approval for diabetes (2022) and obesity (2023).

Evidence & Sources

No sources recorded yet.

Frequently Asked Questions