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Mitochondria

AICAR Oral

The oral tablet form of the AMPK activator AICAR, with the same exercise-mimetic claim and the same thin human data.

1 min read 8 sources

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White tablet bottle with a black TPD label for AICAR Oral on a white podium, next to it a molecule model of blue and white glass spheres with two rings in a bright lab
Infusion up to phase 3, barely absorbed orally · not approved

Summary

At a glance

Sources checked on 26 Oct 2026

Absorption by mouth
<5 %

healthy men, taken as a solution, compared with an infusion2

Half-life (humans)
1.4 hours

after an infusion, levels fell quickly in two phases2

Running endurance (mice)
+44 %

untrained mice after four weeks of AICAR, injected into the abdominal cavity1

Sugar uptake into muscle
2.1 -fold

healthy men, AICAR as an infusion, cycling reached 4.7-fold3

Phase 3 without benefit
3,080 participants

bypass surgery, infusion, stopped after an interim analysis4

  • AICAR, known as the drug acadesine, activates the enzyme AMPK, the energy sensor of the cell. It became known as an exercise mimetic candidate.78
  • Untrained mice ran 44 percent longer after four weeks of AICAR. The animals received high doses, injected into the abdominal cavity.1
  • AICAR is barely absorbed by mouth: in humans less than 5 percent of a dose taken as a drink reached the blood and the half-life after an infusion was 1.4 hours.2
  • Acadesine was tested in humans as an infusion. In healthy men sugar uptake into muscle rose, a phase 3 trial in bypass surgery was stopped without benefit.34
  • There is no study of AICAR as a tablet for performance or metabolism. Everything here is research, not a recommendation.62
Profile

Updated May 2026

Class
AMPK activator

oral

Use
Oral

tablet

Half-life
short
Status
Tested as an infusion

acadesine, up to phase 3, no benefit; barely absorbed orally, not approved

Sizes
10 mg

1 size in the shop

Contents 13 sections
  1. At a glance
  2. What is AICAR Oral?
  3. How it works
  4. How to take it
  5. Dosing
  6. What the research shows
  7. Research status
  8. Side effects
  9. Storage
  10. Related compounds
  11. FAQ
  12. Glossary
  13. Sources

What is AICAR Oral?

AICAR Oral is the tablet form of the AMPK activator AICAR, which you also find as an injection in the lexicon. The principle is the same: an exercise-mimetic candidate meant to trigger part of the training signals without training.

Up front: AICAR has very poor bioavailability. Applied orally it is questionable how much works at all.

Comparison

Exercise mimetic candidates compared

Compounds from the TPD lexicon meant to mimic training signals, as described there. Tap a card to open its entry.

AMPK activator as a tablet AICAR Oral AMPK
AMPK activator for injection AICAR AMPK PPAR delta agonist Cardarine (GW-501516) PPAR-delta ERR agonist SLU-PP-332 ERR

Simplified: AICAR acts on AMPK, cardarine on the PPAR delta receptor. Both routes were tested in the 2008 mouse study. There is no comparison in humans. 1

How it works

Like the injectable form, AICAR activates the enzyme AMPK, the cell's energy sensor. Through AMPK it switches on programs for energy expenditure and endurance. Details on the mechanism are in the AICAR entry.

Where it acts

Where AICAR acted in studies

Tap a point or a card. Colour = AMPK, grey = observed. Only tested in humans as an infusion.

  1. Skeletal muscle

    More endurance in mice, more sugar uptake into muscle of healthy men (infusion)3

    AMPK
  2. Gut

    Barely absorbed: less than 5 percent of a dose taken as a drink in the blood2

    Observed in trials
  3. Blood

    Rapid uptake into red blood cells and conversion to the monophosphate2

    Observed in trials
  4. Heart

    No protection against complications in bypass surgery (phase 3)4

    Observed in trials
  5. Kidney

    Kidney problems with very high infusions in leukaemia studies5

    Observed in trials

Targets in the ChEMBL database7

Compound CHEMBL1551724 (Acadesin): one recorded mechanism, Activator according to ChEMBL.

AMP-activated protein kinase
Gene
PRKAA1, PRKAA2
UniProt
Q13131, P54646
ChEMBL
CHEMBL2096907
Action
Activator according to ChEMBL
Glass muscle fibres with orange glowing mitochondria, blue molecules dock onto a glass sensor shape and make it light up
AMPK as the energy sensor in muscle. Symbolic image.

How to take it

Oral, one to two tablets (10-20mg) per day with some water.

White tablet bottle with a black TPD label for AICAR Oral, a glass of water and a few white tablets on a white tray
Tablet with water, absorption by mouth is very low. Symbolic image.

Dosing

Dosing

Dosing, titration and syringe

Loading the dosing information …

  • Getting started and stepping up, drawn as a staircase
  • Units on the U-100 syringe for every step
  • How long one vial lasts

What the research shows

The well-known study (Narkar, 2008) showed in mice that AICAR increased endurance performance, a classic exercise-mimetic result, but with high, mostly injected doses. AICAR is also on the WADA list.

In humans AICAR, under the name acadesine, was mainly tested as an infusion, up to a phase 3 study in heart bypass surgery (RED-CABG, Newman 2012). It was stopped early because no benefit was expected. Taken orally, less than 5 percent reached the blood in healthy men (Dixon, 1991). So the basis for oral use is missing.

Study results

What the trials measured

Interactive: switch tabs, tap points, show or hide arms. Arms are named relative to each other, no dosing advice.

Running endurance of untrained mice after four weeks1

Change compared with mice without AICAR, in percent

Treadmill running endurance1
Without AICAR (comparison) 0%
With AICAR 44%

Value from the abstract, dosing into the abdominal cavity according to the full text. The mice did not train, AICAR switched on metabolic genes in muscle. The animals received high doses. Mouse model, not tested in humans.

Sugar uptake into muscle of healthy men3

Rise after three hours compared with baseline, as a multiple

Uptake of labelled sugar3
Acadesine as infusion 2.1-fold
Cycling (comparison) 4.7-fold

Values from the abstract, 29 healthy men. AICAR was given as an infusion into a vein, not as a tablet. Whole-body glucose disposal rose by only 7 percent and AMPK activity in muscle did not change measurably.

Death, stroke or severe heart failure up to day 284

Share of participants in percent, 1,493 per group

Primary endpoint4
Placebo 5.0%
Acadesine as infusion 5.1%

Values from the abstract. The trial was stopped after 3,080 of a planned 7,500 participants because an interim analysis made a benefit unlikely. The key secondary endpoints showed no difference either.

Glass display case with a glass bundle of muscle fibres full of orange glowing mitochondria, a white running shoe below it
Endurance effect only shown in mice so far. Symbolic image.

Research status

Where the research stands

The registry lists five trials with AICAR or acadesine, all using the compound as an infusion or lab tool, none with tablets for performance. Shown are the three acadesine trials with a start and end date in the registry. As of 26 Oct 2026. 6

  1. Preclinical Cell assays and mouse models, exercise mimetic study 2008
  2. Phase 1 no registered trial
  3. Phase 2 2 trials, 1 completed, 1 stopped early
  4. Phase 3 1 trial, 0 completed, 1 stopped early
  5. Approval not yet
3,080 participants in phase 3 Not approved. As an infusion, development ended after phase 3 without benefit. As a tablet, AICAR was only tested in an early pharmacokinetic study.6
Show all 3 phase 2 and 3 trials on a timelineHide timeline 1 completed 0 running 2 stopped early 2 with results
Phase 2
Phase 3

Bar: start to primary endpoint (planned for running trials). Green = completed, blue = progress until 26 Oct 2026, grey = stopped early.

Side effects

  • Solid human data are largely missing.
  • Banned in official competition.

Storage

Store dry, cool and protected from light, out of reach of children. Keep the original container closed and mind the expiry date.

Three white bottles on a bright shelf next to a folded light blue towel
Store dry, cool and out of reach of children. Symbolic image.

Related

Related compounds

Blends with AICAR Oral or a different path: all in the TPD lexicon.

AICAR Oral
AICAR The same compound for injection Cardarine (GW-501516) PPAR delta agonist, tested in the same mouse study SLU-PP-332 ERR agonist, also an exercise mimetic candidate MOTS-c Peptide from the mitochondria, a different metabolic approach SR9009 (Stenabolic) Rev-erb agonist, a different route Metformin (Glucophage) Biguanide, a different metabolic approach

FAQ

Common questions about AICAR Oral

Short answers, each backed by the sources below.

Does AICAR work as a tablet?

That is questionable. In the only study with oral dosing, less than 5 percent of the dose taken as a drink reached the blood in healthy men. What was in the blood disappeared quickly after an infusion, with a half-life of 1.4 hours.2

Where does the exercise mimetic reputation come from?

From a 2008 mouse study: untrained mice ran 44 percent longer after four weeks of AICAR and their muscles switched on metabolic genes. The animals received high doses, injected into the abdominal cavity. This cannot be transferred to tablets in humans.1

Has AICAR been tested in humans?

Yes, as an infusion under the name acadesine. A phase 3 trial in bypass surgery was stopped after 3,080 participants: death, stroke or severe heart failure occurred in 5.1 percent, as often as with placebo at 5.0 percent. There were also small studies in blood cancer.45

What happens in human muscle?

In 29 healthy men an AICAR infusion raised sugar uptake into muscle 2.1-fold after three hours, cycling reached 4.7-fold. Whole-body glucose disposal rose by only 7 percent and AMPK activity in muscle did not change measurably.3

Which side effects are known?

Healthy men tolerated AICAR well in the early study, with mild and short-lived complaints. With very high infusions in a leukaemia study raised uric acid, temporary blood count changes, kidney problems and drops in blood pressure occurred. There are no solid data for tablets.25

Glossary

Terms explained briefly

Dotted words in the text open these explanations directly.

Acadesine
The drug name of AICAR. Clinical development as an infusion ran under this name.
AMPK
The energy sensor of the cell. When energy runs short, AMPK switches the cell to burning sugar and fat.
Bioavailability
The share of a substance that actually reaches the blood after intake.
Bypass surgery
Heart surgery in which narrowed coronary arteries are bridged with a piece of vessel.
Exercise mimetic
A substance meant to trigger part of the signals of training without any training.
Half-life
The time until the amount in the blood has fallen by half.
Infusion
Giving a solution directly into a vein over a longer time. This bypasses absorption in the gut.
Interim analysis
A planned look at the data before a trial is finished. If it shows no prospect of benefit, the trial is stopped.
Uric acid
The end product of purine breakdown. The body largely breaks AICAR down into it.

Evidence

Sources

Show all 8 sourcesHide sources 5 Studies1 Trial registry2 Database checked 26 Oct 2026

Studies

  1. AMPK and PPAR delta agonists as exercise mimetics (mice)

    Narkar et al., Cell, 2008

    DOI 10.1016/j.cell.2008.06.051 PMID 18674809
    Checked 26 Oct 2026 via doi.org, Crossref, PubMed, PMC (Volltext)
  2. Safety and pharmacokinetics in healthy men, infusion and oral

    Dixon et al., Journal of Clinical Pharmacology, 1991

    DOI 10.1002/j.1552-4604.1991.tb03715.x PMID 2037706
    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  3. AICAR infusion and muscle sugar uptake in healthy men

    Cuthbertson et al., Diabetes, 2007

    DOI 10.2337/db06-1716 PMID 17513706
    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  4. RED-CABG: acadesine in bypass surgery, phase 3

    Newman et al., JAMA, 2012

    DOI 10.1001/jama.2012.7633 PMID 22782417
    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  5. Acadesine in chronic lymphocytic leukaemia, phase 1/2

    Van Den Neste et al., Cancer Chemotherapy and Pharmacology, 2013

    DOI 10.1007/s00280-012-2033-5 PMID 23228986
    Checked 26 Oct 2026 via doi.org, Crossref, PubMed

Trial registry

  1. Trials with acadesine on ClinicalTrials.gov

    ClinicalTrials.gov, U.S. National Library of Medicine

    Checked 26 Oct 2026 via ClinicalTrials.gov API v2

Database

  1. Acadesine in ChEMBL (mechanism and highest phase)

    ChEMBL, EMBL-EBI (CHEMBL1551724)

    Checked 26 Oct 2026 via ChEMBL
  2. Structure of AICAR (acadesine) in PubChem

    PubChem, U.S. National Library of Medicine (CID 17513)

    Checked 26 Oct 2026 via PubChem

In the shop

AICAR Oral in the catalog

Sizes, prices and shipping times are on the product page.

To the product