Pitavastatin: efficacy and safety in intensive lipid lowering.
Pitavastatin, (+)-monocalcium bis(3R,5S,6E)-7-(2-cyclopropyl-4-[4-fluorophenyl]-3-quinolyl-3,5-dihydroxy-6-heptenoate), is a totally synthetic statin developed in Japan with a molecular weight of 880.98. Pitavastatin achieves its potent pharmacologic action by strongly binding and inhibiting the active site of 3-hydroxy-3-methyl-glutaryl-CoA reductase, and has potent low-density lipoprotein-cholesterol-lowering effects similar to atorvastatin and rosuvastatin. One other characteristic of the agent is that pitavastatin is minimally metabolized by the cytochrome P450 isozymes; it undergoes glucuronidation and is converted to the inactive lactone form, and, therefore, the incidence of any drug interactions is reduced. Due to the promising results observed in clinical trials, it has the potential to be an excellent addition to the worldwide lipid management market.
Hayashi
Toshio
T
Nagoya University Graduate School of Medicine, Department of Geriatrics, 65 Tsuruma-cho, Showa-ku, Nagoya City, 466-8550, Japan. hayashi@med.nagoya-u.ac.jp
Yokote
Koutaro
K
Saito
Yasushi
Y
Iguchi
Akihisa
A
D000818:Animals; D000924:Anticholesteremic Agents / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use*; D006937:Hypercholesterolemia / Q000188:drug therapy* / Q000201:enzymology; D000960:Hypolipidemic Agents / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use; D011804:Quinolines / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use*
D000924:Anticholesteremic Agents; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D000960:Hypolipidemic Agents; D011804:Quinolines; C108475:pitavastatin