THERAPY DOSSIER · th-d53fade96eb2

AICAR (5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside), an AMPK agonist

Drug · AMP-activated protein kinase (AMPK) activator (ACTIVATOR); direct interaction, disease efficacy true. ATC C01EB13. Max phase 3, never approved (first_approval null); USAN 1992.

Not approved Suggest a correction

Evidence & regulatory context

Mechanism: AMP-activated protein kinase (AMPK) activator (ACTIVATOR); direct interaction, disease efficacy true. ATC C01EB13. Max phase 3, never approved (first_approval null); USAN 1992.
Target: CHEMBL2096907
Injury models: Other · TBI
Reported indication: Not recorded
First approval: Not recorded
Development stage: In trials, not approved
ChEMBL record: CHEMBL1551724 ↗
ChEMBL max phase: 3 / 4 (development scale, not regulatory approval)
Synonyms: AICAR; AICA riboside; Acadesina; GP-1-110; NSC-105823
Note: Not recorded

Clinical trials 5

0 linked trials carry an injury-indication flag. These flags support record-level exploration and sit alongside the stringent aggregate counts described in Methods.

NCT00872001 ↗PHASE3terminated

RED-CABG: Acadesine on adverse CV/cerebrovascular events in high-risk CABG

Coronary Artery Bypass · Myocardial Infarction · Ventricular Dysfunction, Left · Stroke · Cardiopulmonary Bypass

Enrolment: 3080 · Results not recorded

NCT00004314 ↗PHASE2completed

Phase II pilot of AICAR for Lesch-Nyhan disease

Lesch-Nyhan Syndrome

Enrolment: 2 · Results not recorded

NCT00559624 ↗PHASE1/PHASE2completed

Phase I/II dose escalation of acadesine in B-cell CLL

Leukemia, B-Cell, Chronic

Enrolment: 40 · Results not recorded

NCT01813838 ↗PHASE1/PHASE2terminated

Phase I-II acadesine in high/int-2 MDS, AML, CMML type 2

Myelodysplastic Syndrome

Enrolment: 5 · Results not recorded

NCT00168519 ↗NAcompleted

Contraction-mediated glucose uptake in type 2 diabetes (AICAR infused)

Diabetes Mellitus, Type 2

Enrolment: 40 · Results not recorded

Preclinical evidence 2

2 studies reported at therapy level; 2 evidence entries itemised.

PMID 30632675 ↗2018Reported benefit

Activation of AMPK alleviates cardiopulmonary bypass-induced cardiac injury via ameliorating acute cardiac glucose metabolic disorder.

RatOtherSprague-DawleyMalePretreatment at the beginning of cardiopulmonary bypass

Model: Rat model of cardiopulmonary bypass causing cardiac injury and acute glucose metabolic disorder

AICAR pretreatment activated AMPK, increased AS160 phosphorylation and membrane GLUT4, improved myocardial glucose uptake and reduced markers of cardiac injury after bypass, with the benefit abolished by mutant AS160-4P.

Extraction: extract · Supplied extraction confidence: 0.55. Machine-extracted fields require source verification.

PMID 27379837 ↗2016Mixed findings

Traumatic brain injury decreases AMP-activated protein kinase activity and pharmacological enhancement of its activity improves cognitive outcome.

MixedTBIControlled cortical impactSprague-Dawley (rat); C57BL/6 (mouse)MaleAcute administration after injury

Model: Electromagnetic controlled cortical impact traumatic brain injury

Traumatic brain injury reduced AMPK phosphorylation at Thr172 and altered phosphorylation of downstream targets S6 and AS160. Post-injury treatment with AICAR or metformin did not affect spatial learning but significantly improved spatial memory, supporting a contribution of reduced AMPK activity t…

Extraction: extract · Subtype source: rule · Supplied extraction confidence: 0.6. Machine-extracted fields require source verification.

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