Evidence review: Open Peptide Project (verified against primary PubMed, ClinicalTrials.gov & FDA records) · Last checked 2026-10-26. ← Back to Evidence Library

AICAR (acadesine): what the evidence says

Name: AICAR (acadesine)
Published: 2026-10-26

At a glance

What it is: a small molecule (5-aminoimidazole-4-carboxamide riboside), not a peptide. It is a natural purine intermediate that switches on the energy sensor AMPK, and it was developed as the drug acadesine. ^{R1, R2}

What the evidence says: in mice, 4 weeks of AICAR raised running endurance 44% without exercise. ^R3 In people, the large RED-CABG heart-surgery trial was stopped for futility with no benefit. ^R2 A small leukemia study set a maximum tolerated amount. ^R4 No human trial tested endurance or fat loss.

Biggest risks: high uric acid, anemia, low platelets, kidney impairment and low blood pressure during IV infusion in cancer patients. ^R4

Rating


Human Human evidence	Not effective for bypass surgery (RCT, n = 3,080) ^R2 · Very limited for CLL (24 patients) ^R4 · No data for endurance or body composition
Animal Animal / lab evidence	Mouse endurance and many cell studies; many effects are not AMPK-driven ^{R3, R1}
Regulatory	Never approved · not on FDA's 503A or 503B bulk-substance category lists and not on FDA's compounding safety-risk page · WADA 2026: prohibited at all times (S4.4.1, AMPK activators) ^{R5, R6, R7, R8}
Established human dose	None. Study details lists what studies used

Evidence verdict: Heart protection in bypass surgery: Not effective (3,080-patient RCT) · Blood cancer (CLL): Very limited (phase 1/2) · Endurance in people: No human data (mouse only)

This page reports what studies used. It is not dosing advice.

Legend: HUMAN data · ANIMAL / LAB data · UNKNOWN · UNVERIFIED: not yet confirmed against a primary source

About the evidence: the human trials gave AICAR by IV drip in hospitals, not as gray-market injections. A systematic review warns that many AICAR effects once credited to AMPK are AMPK-independent. ^{R2, R4, R1}

What is it?

AICAR is made in the body during purine synthesis and is found in normal urine. As a drug it was tested to protect the heart during surgery and against leukemia. The 2008 "exercise in a pill" mouse paper made it popular in sport. ^{R9, R3} Related pages: SLU-PP-332, MOTS-c, 5-Amino-1MQ.

Does it work?

Human Bypass surgery (RED-CABG, 2012): 3,080 patients; primary outcome 5.1% vs 5.0% placebo (odds ratio 1.01). Stopped for futility. ^{R2, R10}
Human Relapsed CLL: 24 patients; variable drops in leukemia cells and lymph nodes. ^R4
Animal Mice: sedentary mice ran 44% longer after 4 weeks. ^R3
Unknown No human endurance, fat-loss or longevity trial.

Is it safe?

Human CLL study (IV): hyperuricemia common; transient anemia and low platelets; kidney impairment; infusion-related low blood pressure. ^R4
Human RED-CABG: no difference in key safety outcomes vs placebo at surgical amounts. ^R2
Unknown No data on repeated injections in healthy people.

Gray-market "research use only" AICAR: extra risks

A gray-market vial has no quality control and no guarantee of identity, strength or sterility. We test retail vials blind under the Open Peptide Standard; see /tests/. A passing test covers one batch on one date and does not mean the compound is safe. Because the body makes AICAR, anti-doping labs use urine reference ranges and carbon-isotope tests to tell added AICAR from natural levels. ^R9

What we don't know

Unknown Whether it improves endurance or metabolism in people
Unknown Safety of long-term non-medical use

Is it legal?

US (FDA): not approved; not on FDA's 503A or 503B bulk-substance category lists and not on FDA's compounding safety-risk page. ^{R5, R6, R7}
Athletes: WADA 2026 S4.4.1 names AICAR among AMPK activators; prohibited at all times. ^R8

Study details

These are amounts researchers used, not recommendations.

Study	People / model	Route	Amount used	Follow-up	Reported	Citation
RED-CABG (Newman 2012)	3,080 bypass patients	IV infusion	0.1 mg/kg per minute for 7 hours	28 days	No benefit	PMID 22782417
Van Den Neste 2013	24 patients with CLL	IV, 4-hour infusion	50–315 mg/kg single; 210 mg/kg was the maximum tolerated	Weeks	Safety profile set	PMID 23228986
Narkar 2008	Sedentary C57BL/6J mice	Intraperitoneal	500 mg/kg per day	4 weeks	Endurance +44%	PMID 18674809

Full reference list (PubMed, CT.gov, FDA and WADA checked Oct 26, 2026)

^R1 Višnjić D, et al. Cells. 2021. PMID 34064363
^R2 Newman MF, et al. JAMA. 2012. PMID 22782417
^R3 Narkar VA, et al. Cell. 2008. PMID 18674809
^R4 Van Den Neste E, et al. Cancer Chemother Pharmacol. 2013. PMID 23228986
^R5 FDA, 503A bulk drug substances categories list (updated May 14, 2026). https://www.fda.gov/media/94155/download
^R6 FDA, 503B bulk drug substances categories list (updated Mar 21, 2025). https://www.fda.gov/media/94164/download
^R7 FDA, Certain bulk drug substances for use in compounding that may present significant safety risks (content current Apr 22, 2026). https://www.fda.gov/drugs/human-drug-compounding/certain-bulk-drug-substances-use-compounding-may-present-significant-safety-risks
^R8 WADA. The 2026 Prohibited List, S4.4.1. https://www.wada-ama.org/sites/default/files/2025-09/2026list_en_final_clean_september_2025.pdf
^R9 Thomas A, et al. Anal Bioanal Chem. 2010. PMID 20225061
^R10 ClinicalTrials.gov NCT00872001, RED-CABG, Merck, terminated (CT.gov API v2, checked Oct 26, 2026). https://clinicaltrials.gov/study/NCT00872001

Disclaimer

This page is for education and harm reduction, not medical advice or a recommendation to use AICAR (acadesine). Talk to a clinician you trust, especially if you have gout or kidney disease, are pregnant, or are a tested athlete. Report problems to FDA MedWatch (https://www.fda.gov/safety/medwatch).