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Clinical-stage WADA prohibitedMetabolic / mitochondrial

AICAR

An AMPK-activating nucleoside studied medically for ischemia and known in exercise physiology as an "exercise mimetic." It failed a cardiac-surgery trial and is prohibited in sport.

CompoundAICAR
CategoryAMPK activator
ClassMetabolic and Mitochondrial Compounds
Evidence tierClinical-stage
WADA statusProhibited in sport (or falls under a prohibited class) — see the WADA reference table
Sold on this siteNo — this is a reference database

Overview

AICAR — a ampk activator — sits in the "Clinical-stage" tier of this catalog. This compound has completed or is undergoing formal human trials. Human safety and efficacy are being characterized, but no universal approval exists and results may still fail or be withdrawn.

An AMPK-activating nucleoside studied medically for ischemia and known in exercise physiology as an "exercise mimetic." It failed a cardiac-surgery trial and is prohibited in sport.

Mechanism of Action

AICAR is converted intracellularly to ZMP, which mimics AMP and activates AMPK — the master energy-sensor activated by exercise.

Research and Evidence

Human trials include cardiac-surgery contexts where outcomes were disappointing; animal exercise-mimicry data drove its WADA prohibition.

Evidence in context: the Metabolic and Mitochondrial Compounds class page collects the shared evidence themes and study-reading guidance for this category.

Safety and Side Effects

Documented effects include gastrointestinal complaints; long-term metabolic manipulation without medical indication is uncharacterized. Prohibited in sport.

Educational notice: this entry describes published research and, where they exist, regulator labels. It is not medical advice and not a recommendation for use. Research-grade compounds have no verified human-safety data.

Frequently Asked Questions

What is the evidence tier of AICAR?

AICAR is graded "Clinical-stage" on this site. This compound has completed or is undergoing formal human trials. Human safety and efficacy are being characterized, but no universal approval exists and results may still fail or be withdrawn.

Is AICAR an approved medicine?

No. Clinical-stage means the compound has not reached universal regulatory approval; the tier description above explains exactly what level of evidence exists.

Where can I read the primary studies for AICAR?

The references section at the end of this entry links the key primary sources — regulator labels, trial registrations, and peer-reviewed papers. Our "How to Read a Peptide Study" guide explains how to evaluate them.

References

  1. ClinicalTrials.gov — registered AICAR studies. [source]
  2. WADA Prohibited List. [source]
EM
Dr. Elena Marsh, PhDMolecular Pharmacology · Lead Editor

Written and maintained by the editorial team. Medically reviewed by Dr. James Okafor, MD (Internal Medicine).

Evidence tier: Clinical-stage · Last reviewed: 2026-09-05 · Sources cited below.

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