PepTrackevidence-graded reference
Tirzepatide
fig.1 — stylized molecular motif
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.
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
1DailyMed Zepbound
＋PepTrack research dossier — iterations 1–4, 584 de-duplicated sources, adversarially verified.
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
← All peptides
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
A
FDA-approved RCTs
Status
FDA-approved
as of 2026-06
FDA approval
Approved
on-label use exists
Route
Subcutaneous
FDA label
Demand
#2
most-searched
WADA
Not listed
sport-legal
01

Dosing & protocol

FDA label. Dosing reference per the FDA label.
Typical — reference only

SC 5/10/15 mg once weekly (2.5 mg = initiation only; max 15 mg)

Worked reconstitution example

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.

Titration

2.5 mg x4 wks > 5 > 7.5 > 10 > 12.5 > 15 (>=4 wks/step)

Units are not milligrams. mg-vs-mcg confusion drives documented 5–1000× overdoses — always recompute for your own vial (use the calculator →).
02

Regulatory 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
StatusFDA-approved
503A bulksNot on the bulks list
Category 2 (2026)n/a; FDA proposed removal from 503B bulks ~Apr 2026 (opposite direction to the peptide reclassification)
PCAC reviewnone scheduled
WADANot listed
03

Evidence — the honest read

AFDA-approved RCTs

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.

04

Safety

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.

06

Sources

01DailyMed Zepbound
＋PepTrack research dossier — iterations 1–4, 584 de-duplicated sources, adversarially verified.
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