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AICAR

AICAR is a lab-made copy of a natural molecule from the pathway cells use to build purines, the A and G building blocks of DNA and RNA. It is not a peptide. Strictly, what is sold as AICAR is the nucleoside acadesine; cells add a phosphate to turn it into the nucleotide ZMP, which switches on the energy sensor AMPK. It was tested in hospitals as the IV drug acadesine, and sport banned it after a 2008 mouse study linked it to endurance.

Not approved · research onlyWADA Prohibited at all times (S4.4.1, AMPK activator)Checked October 2026
Open the AICAR calculatorSources

Approval status

Never approved. As the drug acadesine it reached large heart-surgery trials, but the last one (RED-CABG) was stopped early because it showed no benefit. The EMA gave acadesine orphan designation for B-cell chronic lymphocytic leukemia in 2005, which is not a marketing authorization. WADA bans AICAR at all times.5910

What it’s used or studied for

  • Human studies

    Given by IV during heart bypass surgery: early trials suggested fewer heart attacks, but a large trial of about 3,000 patients was stopped for lack of benefit.45

  • Human studies

    Tested by IV infusion in 24 people with relapsed chronic lymphocytic leukemia; this small study mainly assessed safety, and signs of effect varied.6

  • Human studies

    In healthy men, an IV infusion raised glucose uptake into muscle, with only a small effect on whole-body glucose use.7

  • Animal & lab only

    Raised running endurance in sedentary mice in a 2008 study; this finding led WADA to ban AMPK activators like AICAR.811

Each label shows how strong the evidence is: an approved use, human studies, animal or lab studies only, or a popular claim with no published studies. Being studied is not the same as being proven safe or effective.

Side effects

Common

  • Raised uric acid in the blood
  • Short-lived drop in red blood cells or platelets

Serious or rare

  • Kidney impairment (leukemia trial)
  • Low blood pressure during the infusion (leukemia trial)

From hospital IV trials of acadesine. In heart-surgery trials, side effects were similar to placebo apart from a short-lived rise in uric acid. Taken by mouth, less than 5% reached the bloodstream in a study of healthy men.346

Sources

  1. PubChem: Acadesine (AICA riboside, CID 17513)
  2. PubChem: AICA ribonucleotide (ZMP, CID 65110)
  3. Dixon R et al. AICA-riboside: safety, tolerance, and pharmacokinetics of a novel adenosine-regulating agent. J Clin Pharmacol. 1991
  4. Mangano DT. Effects of acadesine on myocardial infarction, stroke, and death following surgery: a meta-analysis of the 5 international randomized trials. JAMA. 1997
  5. Newman MF et al. Effect of acadesine on morbidity and mortality associated with coronary artery bypass grafting: the RED-CABG randomized controlled trial. JAMA. 2012
  6. Van Den Neste E et al. Acadesine for patients with relapsed/refractory chronic lymphocytic leukemia (CLL): a multicenter phase I/II study. Cancer Chemother Pharmacol. 2013
  7. Cuthbertson DJ et al. 5-aminoimidazole-4-carboxamide 1-beta-D-ribofuranoside acutely stimulates skeletal muscle 2-deoxyglucose uptake in healthy men. Diabetes. 2007
  8. Narkar VA et al. AMPK and PPARdelta agonists are exercise mimetics. Cell. 2008
  9. EMA: Orphan designation EU/3/05/280, acadesine for B-cell chronic lymphocytic leukaemia
  10. WADA 2026 Prohibited List
  11. Niederberger E et al. Activation of AMPK and its impact on exercise capacity. Sports Med. 2015

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