Tirzepatide

Tirzepatide is a novel dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist. Approved by the FDA in 2022 for T2DM and 2023 for obesity, it represents the first dual incretin therapy. The SURPASS clinical program demonstrated superior glycemic control and weight loss compared to semaglutide in head-to-head trials.

PubMed results: 1,808 · Human studies: 988 · Animal studies: 1,045

Ranges reflect protocols studied in published research and animal-model extrapolation. Presented for research purposes only, not a recommendation or instruction for human use.

FDA-approved dosing with 4-week titration schedule

• Subcutaneous Injection — standard range 5-15 mg weekly, Once weekly. Start at 2.5 mg, increase by 2.5 mg every 4 weeks

~5 days (high confidence)

• Superior HbA1c reduction (Strong human clinical data): SURPASS trials showed HbA1c reductions up to 2.5%, superior to semaglutide
• Weight loss exceeding 20% (Strong human clinical data): SURMOUNT trials demonstrated 20.9% mean weight loss at 15 mg dose

• Nausea — Mild-Moderate, Common (12-18%)

• Personal or family history of medullary thyroid carcinoma (MTC) (Established): GLP-1 receptor agonists carry a boxed warning based on rodent C-cell tumor findings; dual GIP/GLP-1 agonism inherits this class restriction for individuals with personal or family history of MTC.
• Multiple Endocrine Neoplasia syndrome type 2 (MEN2) (Established): MEN2 confers elevated MTC risk; product labeling contraindicates use in patients with MEN2 given the GLP-1 receptor agonist class concern for thyroid C-cell neoplasia.

Lyophilized (powder): Refrigerated (2-8°C), Up to manufacturer-labeled shelf life (multi-dose pens typically refrigerated until first use). Light sensitive: yes, store dark

Reconstituted (solution): Refrigerated (2-8°C), Prefilled pens: refrigerate until first use; after first use, follow pen-specific labeling (often room temperature or refrigerated for a limited number of days). Solvent: Bacteriostatic water

• NCT07349641 — A Study of Weight Loss Intervention With Tirzepatide and Progestin Intrauterine Device to Treat Endometrial Hyperplasia and Grade 1 Endometrial Cancer (PHASE2), status: NOT_YET_RECRUITING. Indications: Endometrial Atypical Hyperplasia/Endometrioid Intraepithelial Neoplasia, FIGO Grade 1 Endometrial Endometrioid Adenocarcinoma
• NCT07128082 — The Long COVID Treatment Trial (PHASE2), status: ACTIVE_NOT_RECRUITING. Indications: Long COVID
• NCT06605703 — A Randomized Controlled Trial Comparing the Effectiveness of Different Treatment Options for Weight Management After Discontinuation of Semaglutide and Tirzepatide (GLP1 Transition Trial) (PHASE4), status: ACTIVE_NOT_RECRUITING. Indications: Obesity, Overweight
• NCT07115069 — Comparison of Body Composition Changes With Weight Loss Interventions, status: RECRUITING. Indications: Obesity
• NCT06890611 — A Study of Bimagrumab Alone (LY3985863) and Bimagrumab With Tirzepatide (LY900042) in Healthy Participants (PHASE1), status: COMPLETED. Indications: Healthy
• NCT04004988 — A Study of Tirzepatide Administered by Two Different Devices in Healthy Participants (PHASE1), status: COMPLETED. Indications: Healthy
• NCT06009653 — Effects of Tirzepatide Plus Intensive Lifestyle Therapy on Body Weight and Metabolic Health in Latinos With Obesity (PHASE4), status: WITHDRAWN. Indications: Obesity, Metabolic Disease
• NCT06345066 — A Study of LY3841136 in Overweight and Obese Participants (PHASE1), status: COMPLETED. Indications: Obesity, Overweight
• NCT06727331 — Study of Tirzepatide for Recovery and Alcohol Use Management (PHASE2), status: RECRUITING. Indications: Alcohol Use Disorder (AUD)
• NCT03482024 — A Study of Tirzepatide (LY3298176) in Participants With Impaired Kidney Function (PHASE1), status: COMPLETED. Indications: Renal Insufficiency, End Stage Renal Disease
• NCT06657209 — Normal-weight Diabetes: Adipocyte-directed Therapy with Pioglitazone or Tirzepatide (PHASE4), status: NOT_YET_RECRUITING. Indications: Diabetes Mellitus, Type 2
• NCT06779929 — Comparative Study of Tirzepatide Versus Dulaglutide (SURPASS CVOT) or Semaglutide on Major Cardiovascular Events in Participants With Type 2 Diabetes, status: ACTIVE_NOT_RECRUITING. Indications: Type 2 Diabetes
• NCT03951753 — A Study of Tirzepatide in Participants With Type 2 Diabetes Mellitus (T2DM) (PHASE1), status: COMPLETED. Indications: Diabetes Mellitus, Type 2
• NCT03730662 — A Study of Tirzepatide (LY3298176) Once a Week Versus Insulin Glargine Once a Day in Participants With Type 2 Diabetes and Increased Cardiovascular Risk (PHASE3), status: COMPLETED. Indications: Type 2 Diabetes Mellitus
• NCT04093752 — A Study of Tirzepatide (LY3298176) in Participants With Type 2 Diabetes on Metformin With or Without Sulfonylurea (SURPASS-AP-Combo) (PHASE3), status: COMPLETED. Indications: Type 2 Diabetes
• NCT05751720 — Effect on Non-Alcoholic Fatty Liver Disease in Patients With Type 2 Diabetes Mellitus With Gastric Inhibitory Polypeptide/Glucagon Like Peptide-1 Analogue (PHASE1 / PHASE2), status: UNKNOWN. Indications: Non-Alcoholic Fatty Liver Disease, Non-alcoholic Steatohepatitis, Type 2 Diabetes, Liver Fat
• NCT07228741 — Resistance Exercise and Incretin Mimetic for Cardiometabolic Health in Survivors of ALL With Obesity (PHASE2), status: NOT_YET_RECRUITING. Indications: Acute Lymphoblastic Leukemia, Obesity
• NCT06897475 — A Study of LY3457263 Compared With Placebo in Participants With Type 2 Diabetes on a Stable Dose of Semaglutide or Tirzepatide (PHASE2), status: RECRUITING. Indications: Type 2 Diabetes
• NCT07262762 — Spartina® (Tirzepatide) Effectiveness and Safety Evaluation, status: RECRUITING. Indications: Obesity & Overweight
• NCT06976853 — Moving Beyond Inflammation as a Therapeutic Target for Crohn's Disease (PHASE2), status: RECRUITING. Indications: Crohn Disease (CD)