What is AICAR?

A research compound that activates AMPK, nicknamed the “exercise pill”; prohibited in sport and not approved for human use.

AICAR in the library · Metabolic & Weight Peptides · Human Trials · What are peptides?

4 registered trials · 16 indexed papers · 283 human / 1459 animal studies

From the PeptideWhiz library entry. "As described" sections summarize claims made in the sources; they are not PeptideWhiz endorsements.

What it is

AICAR (5-aminoimidazole-4-carboxamide ribonucleoside) is described as a research compound that activates AMP-activated protein kinase (AMPK). It earned the nickname “exercise pill” after studies in which sedentary animals given AICAR showed large endurance improvements.

It is described as prohibited in sports (WADA classifies it as a metabolic modulator) and as not approved for therapeutic use in humans.

Overview (as described)

Research interest is described as activating AMPK pathways to mimic exercise-like metabolic effects.

Registered human trials (4)

Trial	Phase	Status	Year	Enrolled
GFM-Acadesine: A Phase I-II Trial of Acadesine	Phase 1/Phase 2	terminated	2013	5
The Effect Of Acadesine On Reducing Cardiovascular and Cerebrovascular Adverse Events In Coronary Artery Bypass Graft (CABG) Surgery (Study P05633 AM1)(TERMINATED)	Phase 3	terminated	2009	3080
Safety and Tolerability Open Label Dose Escalation Study of Acadesine in B-CLL Patients	Phase 1/Phase 2	completed	2007	40
Contraction (Exercise) Mediated Glucose Uptake as a Therapeutic Target in Type 2 Diabetes		completed	2002	40

Peer-reviewed studies (16)

Paper	Authors	Journal	Year	Type
Urine levels of 5-aminoimidazole-4-carboxamide riboside (AICAR) in patients with type 2 diabetes	Mendler M et al.	Acta diabetologica	2018	Clinical Trial
Predictors of contemporary coronary artery bypass grafting outcomes	Weisel RD et al.	The Journal of thoracic and cardiovascular surgery	2014	Randomized Controlled Trial
Acadesine for patients with relapsed/refractory chronic lymphocytic leukemia (CLL): a multicenter phase I/II study	Van Den Neste E et al.	Cancer chemotherapy and pharmacology	2013	Clinical Trial, Phase II
Effect of adenosine-regulating agent acadesine on morbidity and mortality associated with coronary artery bypass grafting: the RED-CABG randomized controlled trial	Newman MF et al.	JAMA	2012	Randomized Controlled Trial
Intra-arterial AICA-riboside administration induces NO-dependent vasodilation in vivo in human skeletal muscle	Bosselaar M et al.	American journal of physiology. Endocrinology and metabolism	2009	Controlled Clinical Trial
Intravenous AICAR administration reduces hepatic glucose output and inhibits whole body lipolysis in type 2 diabetic patients	Boon H et al.	Diabetologia	2008	Clinical Trial
5-aminoimidazole-4-carboxamide 1-beta-D-ribofuranoside acutely stimulates skeletal muscle 2-deoxyglucose uptake in healthy men	Cuthbertson DJ et al.	Diabetes	2007	Controlled Clinical Trial
Post-reperfusion myocardial infarction: long-term survival improvement using adenosine regulation with acadesine	Mangano DT et al.	Journal of the American College of Cardiology	2006	Randomized Controlled Trial
Effect of acadesine on myocardial ischaemia in patients with coronary artery disease	de Jonge R et al.	European journal of pharmacology	1997	Controlled Clinical Trial
Electrocardiographic and hemodynamic changes and their association with myocardial infarction during coronary artery bypass surgery. A multicenter study. Multicenter Study of Perioperative Ischemia (McSPI) Research Group	Jain U et al.	Anesthesiology	1997	Clinical Trial
Acadesine inhibits neutrophil CD11b up-regulation in vitro and during in vivo cardiopulmonary bypass	Mathew JP et al.	The Journal of thoracic and cardiovascular surgery	1995	Randomized Controlled Trial
Effects of acadesine on the incidence of myocardial infarction and adverse cardiac outcomes after coronary artery bypass graft surgery. Multicenter Study of Perioperative Ischemia (McSPI) Research Group		Anesthesiology	1995	Randomized Controlled Trial
Acadesine: a new drug that may improve myocardial protection in coronary artery bypass grafting. Results of the first international multicenter study. Multinational Acadesine Study Group	Menasché P et al.	The Journal of thoracic and cardiovascular surgery	1995	Randomized Controlled Trial
Effect of acadesine, a new metabolic agent, on exercise-induced myocardial ischemia in chronic stable angina	Holdright DR et al.	Cardiovascular drugs and therapy	1994	Randomized Controlled Trial
An initial multicenter, randomized controlled trial on the safety and efficacy of acadesine in patients undergoing coronary artery bypass graft surgery. SPI Research Group	Leung JM et al.	Anesthesia and analgesia	1994	Randomized Controlled Trial
AICA-riboside: safety, tolerance, and pharmacokinetics of a novel adenosine-regulating agent	Dixon R et al.	Journal of clinical pharmacology	1991	Randomized Controlled Trial

More cited research

Specific features of L-histidine production by Escherichia coli concerned with feedback control of AICAR formation and inorganic phosphate/metal transport (2018, human observational)
Anti-Tumorigenic Potential of a Novel Orlistat-AICAR Combination in Prostate Cancer Cells (2017, human observational)
Determination of ¹³C/¹² C ratios of endogenous urinary 5-amino-imidazole-4-carboxamide 1β-D-ribofuranoside (AICAR) (2014, human observational)
Synergistic anti-tumor activity of acadesine (AICAR) in combination with the anti-CD20 monoclonal antibody rituximab in in vivo and in vitro models of mantle ce (2014, human trial (non-randomized))
Administration of AICAR, an AMPK Activator, Prevents and Reverses Diabetic Polyneuropathy (DPN) by Regulating Mitophagy (2024, animal)
AICAR Ameliorates Non-Alcoholic Fatty Liver Disease via Modulation of the HGF/NF-κB/SNARK Signaling Pathway and Restores Mitochondrial and Endoplasmic Reticular (2023, animal)
AICAR decreases acute lung injury by phosphorylating AMPK and upregulating heme oxygenase-1 (2021, animal)
AICAR, an AMP-Activated Protein Kinase Activator, Ameliorates Acute Pancreatitis-Associated Liver Injury Partially Through Nrf2-Mediated Antioxidant Effects and (2021, animal)

Conditions researched

Related compounds

FAQ

What is AICAR?

A research compound that activates AMPK, nicknamed the “exercise pill”; prohibited in sport and not approved for human use.

How many registered human trials study AICAR?

The PeptideWhiz trial index lists 4 registered trials for AICAR, the most recent from 2013.

How much published research exists on AICAR?

The PeptideWhiz paper index links 16 PubMed papers to AICAR; by study type, 283 human and 1459 animal studies.

Which conditions is AICAR researched for?

Atherosclerosis, cardiovascular disease & high blood pressure, Concussion, traumatic brain injury & stroke recovery, Heart repair: after heart attack, heart failure & enlarged heart, Insulin resistance, prediabetes & type 2 diabetes, Post-surgical inflammation and surgery recovery.

Research and education only. Not medical advice. No dosing guidance. Data: ClinicalTrials.gov registry and PubMed via the PeptideWhiz index (204,289 studies).

Reported dosing ranges from research