Frakefamide Explained

Frakefamide (INN) is a synthetic, fluorinated linear tetrapeptide with the amino acid sequence Tyr-D-Ala-(p-F)Phe-Phe-NH₂ which acts as a peripherally-specific, selective μ-opioid receptor agonist.^{[1] [2]} Despite its inability to penetrate the blood-brain-barrier and enter the central nervous system, frakefamide has potent analgesic effects and, unlike centrally-acting opioids like morphine, does not produce respiratory depression, indicating that its antinociceptive effects are mediated by peripheral μ-opioid receptors.^[3] It was under development for the treatment of pain by AstraZeneca and Shire but was shelved after phase II clinical trials.^{[4] [5]}

See also

• Casokefamide
• Metkefamide

Notes and References

1. Modalen ÅÖ, Quiding H, Frey J, Westman L, Lindahl S . A novel molecule (frakefamide) with peripheral opioid properties: the effects on resting ventilation compared with morphine and placebo . Anesthesia and Analgesia . 100 . 3 . 713–717 . March 2005 . 15728057 . 10.1213/01.ANE.0000145011.75545.C5 . 23249323 . free .
2. Book: Aronson JK . Jeffrey Aronson . Meyler's Side Effects of Analgesics and Anti-Inflammatory Drugs . 27 April 2012 . 30 November 2009 . Elsevier . 978-0-444-53273-2 . 84.
3. Modalen AO, Quiding H, Frey J, Westman L, Lindahl S . A novel molecule with peripheral opioid properties: the effects on hypercarbic and hypoxic ventilation at steady-state compared with morphine and placebo . Anesthesia and Analgesia . 102 . 1 . 104–109 . January 2006 . 16368813 . 10.1213/01.ANE.0000184254.85567.80 . 40297091 . free .
4. Book: Anderson NG . Introduction . Practical Process Research and Development: A Guide for Organic Chemists . https://books.google.com/books?id=I_nwhvhp1BAC&pg=PA4 . 27 April 2012 . 15 April 2012 . Academic Press . 978-0-12-386537-3 . 4.
5. Book: Schmidt WK . An overview of current and investigational drugs for the treatment of acute and chronic pain. Bountra C, Munglani R, Schmidt WK . Pain: Current Understanding, Emerging Therapies, And Novel Approaches To Drug Discovery . https://books.google.com/books?id=anRzslvfcUwC&pg=PA400 . 27 April 2012 . 13 May 2003 . CRC Press . 978-0-8247-8865-0 . 400.