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Lapaquistat
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| Systematic (IUPAC) name | |
| 1-{[(3R,5S)-1-(3-hydroxy-2,2-dimethylpropyl)-7-chloro-5-(2,3-dimethoxyphenyl) -2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepin-3-yl]acetyl}piperidine-4-acetic acid | |
| Identifiers | |
| CAS number | |
| ATC code | ? |
| PubChem | ? |
| Chemical data | |
| Formula | C31H39ClN2O8 |
| Mol. mass | 603.103 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | ? |
Lapaquistat (TAK-475) is a cholesterol-lowering drug. Unlike statins which inhibit HMG-CoA reductase, lapaquistat metabolites inhibit squalene synthase which is further downstream in the synthesis of cholesterol. It is hoped that side effects can be reduced by not disturbing the mevalonate pathway which is important for other biochemical molecules besides cholesterol. However, there is increasing evidence that statins (which inhibit the mevalonate pathway) may be clinically useful because they affect these other molecules (including protein prenylation)[1].
On March 28, 2008, Takeda halted further development of lapaquistat.[2]
References
- ^ Greenwood J, Steinman L, Zamvil SS (May 2006). "Statin therapy and autoimmune disease: from protein prenylation to immunomodulation". Nat. Rev. Immunol. 6 (5): 358–70. doi:. PMID 16639429.
- ^ Takeda Pharmaceutical Company Limited press release - Discontinuation of Development of TAK-475, A Compound for Treatment of Hypercholesterolemia
- Davidson MH (Jan 2007). "Squalene synthase inhibition: a novel target for the management of dyslipidemia". Curr Atheroscler Rep 9 (1): 78–80. doi:. PMID 17169251.
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Wikipedia content modification information:
- This page was last modified on 28 August 2008, at 15:21.
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