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Therapeutic uses of melatonin and melatonin derivatives: a patent review (2012 - 2014)
Silvia Rivara1, Daniele Pala, Annalida Bedini
1Università degli Studi di Parma, Dipartimento di Farmacia , Parco Area delle Scienze 27/A, I-43124 Parma , Italy +39 0521 905061 ; +39 0521 905006 ; silvia.rivara@unipr.it.
Introduction:
Melatonin is a neurohormone involved in the regulation of circadian rhythms, with potent antioxidant activity. It has a wide functional repertoire, with effects almost on all tissues and organs. It is mainly used as a dietary supplement for sleep regulation and re-synchronization of disrupted circadian rhythms. Melatonin has very low toxicity, but some pharmacokinetic issues, such as limited oral bioavailability and short half-life, limit its tissue availability.
Areas Covered:
Patents and patent applications from 2012 to September 2014 in which melatonin or synthetic analogues are claimed for the prevention or treatment of pathological conditions.
Expert Opinion:
Melatonin is considered a valuable substance that can be safely administered for the prevention and treatment of many diverse diseases. A major trend in 2012 - 2014 patents is the co-administration of melatonin with other drugs to increase the efficacy of the treatment and reduce side-effects. Two different actions have been combined in hybrid ligands (e.g., melatonin-tamoxifen and melatonin-tacrine derivatives). Further experimental evidence is needed to support the usefulness of these approaches. The number of new melatonin analogues has shown a marked decrease in the past 3 years, with claimed applications mainly as hypnotic or antioxidant agents.
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