Global InformationAcadesine information
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| ECHA InfoCard | 100.018.271 |
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| Formula | C9H14N4O5 |
| Molar mass | 258.234 g·mol−1 |
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Acadesine (INN), also known as 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside, AICA-riboside, and AICAR, is an AMP-activated protein kinase activator[1] which is used for the treatment of acute lymphoblastic leukemia[2] and may have applications in treating other disorders such as diabetes.[3] AICAR has been used clinically to treat and protect against cardiac ischemic injury.[4] The drug was first used in the 1980s as a method to preserve blood flow to the heart during surgery.[5]
Acadesine is an adenosine regulating agent developed by PeriCor Therapeutics and licensed to Schering-Plough in 2007 for phase III studies. The drug is a potential first-in-class agent for prevention of reperfusion injury in CABG surgery. Schering began patient enrollment in phase III studies in May 2009. The trial was terminated in late 2010 based on an interim futility analysis.[6]
- ^ Favero CB, Mandell JW (September 2007). "A pharmacological activator of AMP-activated protein kinase (AMPK) induces astrocyte stellation". Brain Research. 1168: 1–10. doi:10.1016/j.brainres.2007.06.087. PMC 2000700. PMID 17706943.
- ^ Cronstein BN, Kamen BA (December 2007). "5-aminoimidazole-4-carboxamide-1-beta-4-ribofuranoside (AICA-riboside) as a targeting agent for therapy of patients with acute lymphoblastic leukemia: are we there and are there pitfalls?". Journal of Pediatric Hematology/Oncology. 29 (12): 805–7. doi:10.1097/MPH.0b013e31815bbb83. PMID 18090925.
- ^ Cuthbertson DJ, Babraj JA, Mustard KJ, Towler MC, Green KA, Wackerhage H, et al. (August 2007). "5-aminoimidazole-4-carboxamide 1-beta-D-ribofuranoside acutely stimulates skeletal muscle 2-deoxyglucose uptake in healthy men". Diabetes. 56 (8): 2078–84. doi:10.2337/db06-1716. PMID 17513706.
- ^ Cite error: The named reference
Corton_1995was invoked but never defined (see the help page). - ^ Galiñanes M, Bullough D, Mullane KM, Hearse DJ (August 1992). "Sustained protection by acadesine against ischemia- and reperfusion-induced injury. Studies in the transplanted rat heart". Circulation. 86 (2): 589–97. doi:10.1161/01.cir.86.2.589. PMID 1638724.
- ^ "Research and Development Update". Merck & Co., Inc. 30 June 2010.
In the third quarter of 2010, the Company terminated the internal clinical development program for acadesine, an adenosine regulating agent for ischemia reperfusion injury in patients undergoing heart bypass surgery. Merck has decided to follow the recommendation of the independent Data Safety Monitoring Board ("DSMB") to stop enrollment of the RED-CABG trial based upon the DSMB's review of a pre-specified interim futility analysis which showed a low probability of the trial meeting its primary efficacy endpoint.