Journal
EXPERT OPINION ON THERAPEUTIC PATENTS
Volume 26, Issue 11, Pages 1257-1272Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/13543776.2016.1216977
Keywords
Statins; HMG-R; sterols; terpenoids; new chemical entities; formulations; cardiovascular diseases
Categories
Funding
- European Union (FEDER funds) [POCI/01/0145/FEDER/007728]
- National Funds (FCT/MEC, Fundacao para a Ciencia e Tecnologia and Ministerio da Educacao e Ciencia) [UID/MULTI/04378/2013]
- Norte Portugal Regional Operational Programme (NORTE), under the PORTUGAL Partnership Agreement [NORTE-01-0145-FEDER-000024]
- European Regional Development Fund ( ERDF)
- Fundacao para a Ciencia e a Tecnologia (FCT) [EXCL-II/QEQ-COM/0394/2012]
- [PTDC/QUI-QUI/102760/2008]
- [SFRH/DB/84922/2012]
- [SFRH/BD/77625/2011]
- [SFRH/BPD/94883/2013]
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Introduction: Statins are remarkably safe and efficient medications that are the mainstay of hypercholesterolemia treatment and have proven to be an invaluable tool to lower the risk of acute cardiovascular events. These compounds are inhibitors of 3-hydroxy-methylglutaryl CoA reductase (HMG-R), the rate-limiting enzyme in cholesterol biosynthesis. In spite of their success, they present undesirable side effects and are now loosing patent protection, which provides a great opportunity for the development of new and improved statins. Areas covered: This review summarizes the new patents for HMG-R inhibitors for the 2011-2015 period. Combinations of existing statins with other drugs are also addressed, as well as novel applications of existing statins. Expert opinion: Recent efforts for the discovery of HMG-CoA-R inhibitors has resulted in several new molecules. Most of these are based on commercially available statins, including sterol and terpenoid derivatives. A few peptides have also been patented. However, the origin of the side effects caused by previous statins continues to be, to a large extent, unknown. Although the patents published in the past 5 years are promising, and might result in new drugs, there is still no way to know if they will present reduced toxicity. Only future clinical trials will answer this question.
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