AICAR

AICAR is the common name for acadesine, a nucleoside built from an imidazole carboxamide joined to a ribose sugar.

Educational summaryNon-peptide compound reference

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Dosing & scaling, explained

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Evidence context

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Storage, handling and interpretation

Product identity

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Storage & handling

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Prepared solutions

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Reported protocols for AICAR

What published studies and recent community write-ups report about amounts, timing and course length. 5 clinical, 1 preclinical and 3 community-reported rows, each linked to its source. These are descriptions of what others report, not instructions, and nothing here is medical advice.

ContextDoseFrequencyRouteCourseSource
Clinical5 rows
Pooled analysis of five cardiac surgery trials4,043 patients undergoing coronary artery bypass surgery at 81 centers in the United States, Canada and Europe0.1 mg/kg per minute, plus acadesine in the cardioplegia solutionOne continuous infusion per operationIntravenous, starting before surgery7 continuous hoursNot applicableJAMA (PubMed)1997
Pooling individual patient data from five randomized placebo-controlled trials, perioperative heart attacks were 27% lower and cardiac death through day 4 was 50% lower on acadesine. The only safety difference reported was a transient rise in serum uric acid, and this analysis is what motivated the much larger trial that followed.
RED-CABG phase 3 trial (stopped for futility)3,080 intermediate to high-risk adults, median age 66, having non-emergency on-pump bypass surgery at 300 sites in 7 countries42 mg/kg in 500 mL of saline, infused at 0.1 mg/kg per minute, plus 5 mcg/mL in the cardioplegia and bypass priming solutionsOne infusion, starting within about 30 minutes before anesthesiaIntravenousAbout 7 hoursNot applicableJAMA2012
The composite of death, non-fatal stroke or mechanical support for severe left ventricular dysfunction through day 28 occurred in 5.1% of the acadesine group and 5.0% on placebo, with no difference in secondary endpoints. A prespecified futility analysis stopped the trial at 3,080 of a planned 7,500 participants, and serious adverse events were closely matched between arms.
Phase 1/2 dose escalation in chronic lymphocytic leukemia24 adults with relapsed or refractory CLL who had already had at least one prior regimen50-315 mg/kg single doses; 210 mg/kg was the maximum tolerated and optimal biological doseSingle dose in part 1; two doses or five doses at 210 mg/kg in part 2Intravenous, as a 4-hour infusionOne infusion up to five infusionsNone describedCancer Chemotherapy and Pharmacology (PubMed)2013
Grade 2 or higher high uric acid was common but was managed with prophylactic allopurinol, and transient anemia, low platelets and renal impairment were also recorded. The authors classed transient infusion-related low blood pressure as the clinically significant adverse event, and efficacy signals were too variable to interpret in 24 patients.
Terminated myelodysplastic syndrome and AML trial5 of a planned larger cohort with higher-risk myelodysplastic syndrome, AML with 20-30% marrow blasts or chronic myelomonocytic leukemia type 2140 mg/kg per day, escalating to 210 and then 315 mg/kg per day, with a fallback to 85 mg/kg per day if two or more patients had toxicityDaily within each cycle, for up to 6 cyclesNot stated in the registry recordUp to 6 treatment cycles with response checks after cycles 2, 4 and 6Cycle-based; responders could continue at the same dose until progressionClinicalTrials.gov2013
This French academic study enrolled only five participants before being terminated, with the registry giving renal toxicity as the reason and posting no results. It is the only registered attempt at repeated daily dosing over months, and it stopped on a kidney signal.
Muscle glucose uptake infusion study22 men: 6 healthy and young, 8 older, and 8 with type 2 diabetes10 or 20 mg/kg per hourSingle session, infused from hour 3 to hour 6 of a 6-hour tracer infusionIntravenous3 hours of AICAR exposureNot applicableAmerican Journal of Physiology Endocrinology and Metabolism (PubMed)2009
Glucose uptake into muscle rose 2.9-fold in young men, 1.8-fold in older men and 1.6-fold in men with diabetes at 10 mg/kg per hour, and the authors concluded that the blunting tracks age rather than diabetes. Notably, muscle AMPK activity and phosphorylation were unchanged at 3 hours while ERK1/2 phosphorylation rose, so the effect was seen without the AMPK activation the compound is known for.
Preclinical1 row
Mouse exercise mimetic study, the source of the 44% figureSedentary 8-week-old male C57Bl/6J mice, 15 to 20 per group500 mg/kg per day in the endurance arm; a separate 6-day arm used 250 mg/kg per dayOnce dailyIntraperitoneal injection4 weeks (6 days in the gene expression arm)Not applicableCell (PubMed)2008
Untrained mice given AICAR for four weeks ran 44% farther on a treadmill than vehicle controls, with oxidative metabolism genes upregulated in quadriceps. The paper's abstract calls the compound orally active, but it was injected throughout, and the dose is hundreds of times larger per kilogram than anything given to a person.

How a course is commonly described

  1. Days 1-3Community-reported

    Community pages describe the first days as unremarkable or even flat, since the metabolic shift pushes toward fat oxidation and away from glycolytic output. Injection site redness is described as common, and anyone feeling tired past day four is advised to lower the dose or stop.

  2. Days 4-14Community-reported

    This is the whole of the described cycle. Guides suggest a uric acid check around day 7 for anyone at 25 mg or more and treat day 14 as a stopping point tied to kidney load rather than any measured effect. No human study has dosed daily for two weeks, so nothing confirms or refutes this window.

  3. Washout, 6-8 weeksCommunity-reported

    Community sources place the washout at 6 to 8 weeks and frame it as time for uric acid and kidney function to normalize rather than for any receptor to recover. One guide caps use at three cycles a year on the same reasoning.

  4. Clinical comparisonClinical

    Human exposure has essentially one shape: a single 7-hour intravenous infusion at 0.1 mg/kg per minute during heart surgery, tested in roughly 7,000 patients across two eras that gave opposite answers. The longest repeated schedule in any registered study was five doses in a leukemia trial.

  • No human study has measured exercise capacity after AICAR, and the 44% endurance figure belongs to sedentary mice injected with 500 mg/kg per day for four weeks. Community flat doses of 10-50 mg work out to a fraction of a milligram per kilogram.
  • Uric acid rises with administration because the molecule is a purine, and this was the only safety difference in the pooled cardiac surgery analysis. Renal impairment was recorded in the leukemia trial, and a later academic trial was terminated with renal toxicity given as the reason.
  • Intravenous dosing in healthy men gave a terminal half-life of about 1.4 hours and oral bioavailability in solution under 5%, so oral and sublingual community doses have no pharmacokinetic support.
  • AICAR has been on the WADA prohibited list since 2009 and appears in the 2026 list at S4.4.1 among AMPK activators, prohibited at all times in and out of competition. It is not an approved medicine in any country.
Sources for this section (10)
  1. Effects of acadesine on myocardial infarction, stroke, and death following surgery: a meta-analysis of the 5 international randomized trialsJAMA (PubMed)1997Clinical
  2. Effect of Adenosine-Regulating Agent Acadesine on Morbidity and Mortality Associated With Coronary Artery Bypass Grafting: The RED-CABG Randomized Controlled TrialJAMA2012Clinical
  3. RED-CABG Trial Registration and Posted Results (NCT00872001)ClinicalTrials.gov2009Clinical
  4. Acadesine for patients with relapsed/refractory chronic lymphocytic leukemia (CLL): a multicenter phase I/II studyCancer Chemotherapy and Pharmacology (PubMed)2013Clinical
  5. A Phase I-II Trial of Acadesine in Higher-Risk Myelodysplastic Syndrome, AML and CMML Type 2 (NCT01813838)ClinicalTrials.gov2013Clinical
  6. Blunting of AICAR-induced human skeletal muscle glucose uptake in type 2 diabetes is dependent on age rather than diabetic statusAmerican Journal of Physiology Endocrinology and Metabolism (PubMed)2009Clinical
  7. AMPK and PPARdelta agonists are exercise mimeticsCell (PubMed)2008Preclinical

Plus 3 community resources (dosing guides, forum threads and vendor write-ups), reported above but not linked.

Overview

AICAR is the common name for acadesine, a nucleoside built from an imidazole carboxamide joined to a ribose sugar. Cells take it up through adenosine transporters and phosphorylate it to ZMP, which mimics AMP and activates AMP-activated protein kinase, so it is often described as an exercise mimetic. Several thousand people have received it intravenously, almost all of them during coronary artery bypass surgery, where an early pooled analysis suggested fewer heart attacks and the much larger RED-CABG trial then found no benefit at all. It is not an approved medicine anywhere, has been on the WADA prohibited list since 2009 and sits in the 2026 list at S4.4.1 among AMPK activators, and no registered human study has ever measured exercise capacity.

What researchers are exploring

These themes organize the educational information currently available. Individual claims remain under source review and are not treatment claims.

  • 1

    Effects

    AICAR's effects on insulin resistance, inflammation, and cancer research

  • 2

    Anti-inflammatory Properties

    AICAR's role in combating cellular-level inflammation and inflammatory conditions

  • 3

    Research and the Heart

    AICAR's effects on cardiovascular health and atherosclerosis prevention

  • 4

    Research and Fertility

    AICAR's potential effects on sperm motility and fertility research

What is known and what still needs verification

Available context is organized without assigning unsupported study models or evidence grades.

  • Not graded

    Effects

    AICAR's effects on insulin resistance, inflammation, and cancer research

  • Not graded

    Anti-inflammatory Properties

    AICAR's role in combating cellular-level inflammation and inflammatory conditions

Chemistry identifiers

Sequence, synonyms and registry identifiers as recorded in PubChem, the National Library of Medicine's open chemistry database. Formula, mass and CAS number are summarized at the top of the page.

Also listed as

Acadesine, AICA riboside, 5-Aminoimidazole-4-carboxamide ribonucleoside, ARA-100, GP-1-110, NSC-105823, UNII 53IEF47846, CHEBI:28498

InChIKey

RTRQQBHATOEIAF-UUOKFMHZSA-N

IUPAC name

5-amino-1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]imidazole-4-carboxamide

Limitations and unknowns

Important limitations

  • Individual claims and source links have not yet completed editorial verification.
  • Evidence level, applicable study model, formulation, route and population remain unassigned.

Sources

1 link carried over from the earlier page, awaiting verification.

  1. Source link (pmc.ncbi.nlm.nih.gov)Verification pendingNot graded