Metabolic
Tirzepatide
Mounjaro · Zepbound
Fastest-growing blockbuster: Mounjaro $8.7B + Zepbound $4.1B in Q1 2026; 42% of endocrinologists first-line; SURMOUNT-5 beat semaglutide.
Evidence
AFDA-approved RCTs
Status
FDA-approvedas of 2026-06
Approval
FDA-approved
Category
Metabolic
Route
Subcutaneous
Demand rank
#2 most-searched
01Dosing & Protocol
Typical · reference only
SC 5/10/15 mg once weekly (2.5 mg = initiation only; max 15 mg)
Titration
2.5 mg x4 wks > 5 > 7.5 > 10 > 12.5 > 15 (>=4 wks/step)
Reconstitution — illustrative, not a recommendation
Compounded (illustrative): 30 mg vial + 3 mL BAC = 10 mg/mL; 5 mg = 50 U. 12.5 mg (125 U) & 15 mg (150 U) EXCEED a 100-U syringe -> split or larger syringe. Ready-to-use pens/vials must NOT be diluted.
Reconstitution calculatorlive tool
50units
on a U-100 syringedraw to the 50 mark
Concentration10 mg/mL
Draw volume0.5 mL
Illustrative, not a recommendation. mg vs mcg confusion drives 5–1000× overdoses — always recompute for your own vial and syringe.
Units are not milligrams. mg-vs-mcg confusion drives documented 5–1000× overdoses — always recompute for your own vial.
02Regulatory Status
Removal from Category 2 ≠ legal to compound ≠ FDA-approved. Compounded tirzepatide winding down; not part of the 503A peptide reclassification.
Pre-clinical
Phase 1
Phase 2
Phase 3
Approved
Status
FDA-approved
503A bulks
Not on the bulks list
Category 2
n/a; FDA proposed removal from 503B bulks ~Apr 2026 (opposite direction to the peptide reclassification)
PCAC review
none scheduled
WADA
Not listed
03Evidence — the honest read
What the evidence actually shows
Strongest dataset of any catalog peptide (SURPASS-CVOT n=13,299: non-inferior, NOT superior to dulaglutide; superiority P=0.09). +OSA approval Dec 2024.
04Safety
Contraindications
- MTC/MEN-2hard stop
- Pregnancyhard stop
- Severe gastroparesis
- Pancreatitis history (relative)
Key interactions
- Oral contraceptives -> reduced efficacy (WARNING; switch to non-oral OR add barrier for 4 wks after start AND each escalation; Cmax drop ~55-66%)
- Insulin/sulfonylureas -> hypoglycemia (warning)
- Anesthesia -> aspiration (warning)
Serious signals
- Pancreatitis
- Dehydration/AKI
- Megadosing >15 mg -> documented ICU hypoglycemia
Monitoring
Glucose; contraception counseling at start/each escalation; renal function if GI losses.
05Related in Metabolic
Semaglutide
FDA-approved RCTs
grade A →Retatrutide
human trials
grade B →Cagrilintide / CagriSema
human trials
grade B →MOTS-c
animal-only
grade D →06Sources
The primary sources behind this monograph — each opens the registry so you can verify the claim yourself. Last verified 2026-06-13.
FDA labelFDA label — ZepboundFDA-approved label — dosing & safety · DailyMed SPLHow we source & verify — the full method →Beyond these primaries, every monograph is distilled from TrackurStack’s research dossier — 584 de-duplicated sources across 4 research iterations, adversarially verified against primary sources.
Not medical or legal advice. Educational / harm-reduction reference. Regulatory and dosing claims in this field move monthly — re-verify against primary sources (FDA docket FDA-2025-N-6895, DailyMed, ClinicalTrials.gov) before acting.
Last reviewed — 2026-06-13 · confidence: high