AICAR (Acadesine)
Adenosine-regulating nucleoside (AICA riboside, acadesine), experimental AMPK activator; not a peptide; never approved; RED-CABG (3,080 patients) stopped for futility; WADA S4.4.1 (AMPK activators).
60-Second Scientific Briefing
AICAR (acadesine, AICA riboside) is a nucleoside that cells convert into an AMP mimic, which activates the energy-sensing enzyme AMPK; it is not a peptide. It is widely used in laboratory research, and a systematic review notes it also has important AMPK-independent effects. As a drug it was tested to protect the heart during bypass surgery: the large RED-CABG trial (3,080 patients) was stopped for futility with no benefit. It has never been approved, and WADA prohibits it at all times as an AMPK activator.
What is AICAR (Acadesine)?
Pharmacological Classification & Molecular IdentityAICAR (5-aminoimidazole-4-carboxamide ribonucleoside; acadesine) is an adenosine-regulating nucleoside. It is not a peptide. [1] JAMA, 2012 ↗
Verified Chemical & Regulatory Registry Identifiers
Mechanism of Action & Receptor Targets
Biological Pathway and Target BindingReceptor Selectivity: Inside cells it is converted to an AMP analogue that activates AMP-activated protein kinase (AMPK), the cell's energy sensor. A 2021 systematic review emphasises that many of its effects occur independently of AMPK, so laboratory findings cannot be attributed to AMPK alone. [1] Cells, 2021 ↗
Regulatory & FDA Approval Status
Legal and Regulatory ClassificationsNot approved by the US FDA or any other regulator. Its development as acadesine for heart protection in bypass surgery ended after the RED-CABG trial was stopped for futility (JAMA 2012). It is prohibited at all times by WADA under section S4.4.1 (AMPK activators). [1] World Anti-Doping Agency, 2024 ↗ [2] JAMA, 2012 ↗
AICAR (Acadesine) is not approved for commercial sale, prescription therapy, or compounded medication distribution. It exists strictly within authorized scientific and clinical research frameworks.
Human Evidence & Clinical Trials
Clinical Study Readouts and Evidence SynthesesRED-CABG (JAMA 2012): randomised, double-blind, placebo-controlled trial of perioperative acadesine in intermediate- to high-risk patients undergoing on-pump bypass surgery at 300 sites in 7 countries; stopped for futility after 3,080 of a planned 7,500 patients; the composite of death, non-fatal stroke or severe left ventricular dysfunction by day 28 occurred in 5.1% vs 5.0% with placebo (odds ratio 1.01), with no differences in key secondary end points. No human trial has tested it for exercise performance or weight. [1] JAMA, 2012 ↗
Clinical Evidence
RED-CABG (JAMA 2012): randomised, double-blind, placebo-controlled trial of perioperative acadesine in intermediate- to high-risk patients undergoing on-pump bypass surgery at 300 sites in 7 countries; stopped for futility after 3,080 of a planned 7,500 patients; the composite of death, non-fatal stroke or severe left ventricular dysfunction by day 28 occurred in 5.1% vs 5.0% with placebo (odds ratio 1.01), with no differences in key secondary end points. No human trial has tested it for exercise performance or weight.
Safety Profile & Clinical Limitations
Documented Adverse Events and Known UncertaintiesHuman safety data come from perioperative cardiac trials in hospital settings; no safety data exist for the uses promoted in sport or bodybuilding. [1] JAMA, 2012 ↗
Claims about endurance or fat loss come from laboratory and animal research; no human trial supports them. Its AMPK-independent effects make laboratory findings hard to interpret. It is prohibited in sport. [1] World Anti-Doping Agency, 2024 ↗ [2] Cells, 2021 ↗
Dose Approval Status
Commercial Dosing Status and Policy DirectivesNo dose is approved or established. It is prohibited at all times by WADA. Amounts used in the cardiac trials are described in the linked paper and are not a recommendation. [1] World Anti-Doping Agency, 2024 ↗
Under Egypt Peptides medical governance policies, no personal dosages, titration intervals, cycles, stacking recommendations, or self-injection instructions may be provided for unapproved investigational compounds. Clinical study protocols represent controlled experimental research parameters exclusively.
What is Known vs. What is Unknown
Evidence Comparison and Clinical Evidence Boundaries✓ Confirmed Scientific Evidence
- AICAR (5-aminoimidazole-4-carboxamide ribonucleoside; acadesine) is an adenosine-regulating nucleoside. It is not a peptide.
- Targets & Selectivity: Inside cells it is converted to an AMP analogue that activates AMP-activated protein kinase (AMPK), the cell's energy sensor. A 2021 systematic review emphasises that many of its effects occur independently of AMPK, so laboratory findings cannot be attributed to AMPK alone.
- RED-CABG (JAMA 2012): randomised, double-blind, placebo-controlled trial of perioperative acadesine in intermediate- to high-risk patients undergoing on-pump bypass surgery at 300 sites in 7 countries; stopped for futility after 3,080 of a planned 7,500 patients; the composite of death, non-fatal stroke or severe left ventricular dysfunction by day 28 occurred in 5.1% vs 5.0% with placebo (odds ratio 1.01), with no differences in key secondary end points. No human trial has tested it for exercise performance or weight.
- Safety considerations: Human safety data come from perioperative cardiac trials in hospital settings; no safety data exist for the uses promoted in sport or bodybuilding.
? Unknown / Under Ongoing Investigation
- Claims about endurance or fat loss come from laboratory and animal research; no human trial supports them. Its AMPK-independent effects make laboratory findings hard to interpret. It is prohibited in sport.
Verified Questions & Answers
10 Verified scientific answers with permanent anchor keysAICAR (acadesine) is a nucleoside that activates the energy-sensing enzyme AMPK. It is not a peptide, has never been approved, and is prohibited in sport.
Cells convert it into an AMP analogue that activates AMPK. A 2021 systematic review stresses that many of its effects do not go through AMPK.
No. AICAR has never been approved. Its development for heart protection in bypass surgery ended after the RED-CABG trial was stopped for futility.
- The Prohibited List (World Anti-Doping Agency, 2024-01-01)
- Effect of adenosine-regulating agent acadesine on morbidity and mortality associated with coronary artery bypass grafting: the RED-CABG randomized controlled trial (JAMA, 2012-07-11)
RED-CABG (JAMA 2012, 3,080 bypass-surgery patients) found no reduction in death, stroke or severe heart dysfunction (5.1% vs 5.0%) and was stopped for futility. No human trial has tested it for endurance or fat loss.
RED-CABG (JAMA 2012) was a randomised, double-blind, placebo-controlled trial in intermediate- to high-risk patients (median age 66) undergoing non-emergency on-pump bypass surgery at 300 sites in 7 countries. Acadesine or placebo was started before anaesthesia and added to cardioplegic solutions. A prespecified futility analysis stopped the trial after 3,080 of 7,500 planned patients; the primary composite (death, non-fatal stroke or mechanical support for severe left ventricular dysfunction through day 28) occurred in 76 of 1,493 (5.1%) vs 75 of 1,493 (5.0%) on placebo (odds ratio 1.01, 95% CI 0.73–1.41), with no differences in key secondary end points.
Human safety data come only from hospital heart-surgery trials. No safety data exist for the uses promoted in sport or bodybuilding.
Endurance and fat-loss claims come from laboratory and animal research only; no human trial supports them. Its AMPK-independent effects make laboratory results hard to interpret.
- The Prohibited List (World Anti-Doping Agency, 2024-01-01)
- AICAr, a widely used AMPK activator with important AMPK-independent effects: a systematic review (Cells, 2021-05-01)
No dose is approved or established, and it is prohibited at all times by WADA. Amounts used in the cardiac trials are in the linked paper and are not a recommendation.
- The Prohibited List (World Anti-Doping Agency, 2024-01-01)
There is no approved product label, so no official storage instructions exist.
Yes. AICAR is prohibited at all times under section S4.4.1 (metabolic modulators: AMPK activators) of the 2026 WADA Prohibited List.
- WADA Prohibited List (World Anti-Doping Agency)
Egypt Peptides publishes reviewed scientific reference monographs for documentation and research. The site does not give individual medical advice, preparation or injection instructions, combination protocols or off-label use instructions. Decisions about any medicine belong to the treating physician.
Authoritative Sources & Literature Registry
Regulatory dossiers, clinical trial registries, and published studiesThe Prohibited List ↗
https://www.wada-ama.org/en/prohibited-list
AICAr, a widely used AMPK activator with important AMPK-independent effects: a systematic review ↗
https://pubmed.ncbi.nlm.nih.gov/34064363/
Effect of adenosine-regulating agent acadesine on morbidity and mortality associated with coronary artery bypass grafting: the RED-CABG randomized controlled trial ↗
https://pubmed.ncbi.nlm.nih.gov/22782417/