生物活性

• 描述HMG-CoA reductase, the rate-limiting enzyme in the process of cholesterol synthesis in liver cells, catalyzes the production of mevalonate. Inhibiting HMG-CoA reductase inhibits cholesterol synthesis. Mevastatin reversibly inhibits HMG-CoA reductase and competes with HMG-CoA, whose Ki value is about 1 nM^[3]. in vitro, at 0.01 pg/mL (26 nM), it reduced cholesterol synthesis by 50% compared with the control group^[2]. In addition, mevastatin can completely inhibit L cell growth at 1.3 μM. Mevastatin can also influence cell cycle and change cell morphology in cultured fibroblasts^[3]. In vivo, Mevastatin reduced serum cholesterol levels three hours after oral administration at doses of 5 mg/kg and 20 mg/kg. At a dose of 20 mg/kg, it reduces serum cholesterol levels by about 30 percent^[2]. Mevastatin reduces cholesterol production in the liver by competitively inhibiting HMG-CoA reductase. Cholesterol levels were reduced only after 28 days of treatment and were not associated with a reduction in infarcts. After 14 days of high-dose treatment, baseline absolute cerebral blood flow was 30% higher^[1]. In patients with familial hypercholesterolemia, mevastatin is effective in lowering plasma cholesterol. Treatment at 50 mg/day for 2 months reduced total cholesterol in FH heterozygous patients by 25%^[3].

• 动物研究
  剂量	Rabbit: 0.02 mg/kg[3] (intra-articular injections) Rat: 5 mg/kg, 20 mg/kg[2] (p.o.) Mice: 2 mg/kg, 20 mg/kg[1] (s.c.)
  给药途径	Intra-articular injections, p.o., s.c.

• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02441400	-	-	Recruiting	May 2019	Argentina ... more >> Fundacion Favaloro Recruiting Buenos Aires, Argentina Contact: Alejandro Nieponice, MD          Principal Investigator: Alejandro Nieponice, MD          Austria University Hospital Vienna Recruiting Vienna, Austria Contact: Sebastian Schoppmann, MD          Principal Investigator: Sebastian Schoppmann, MD          Denmark Aarhus University Hospital Recruiting Aarhus, Denmark Contact: Jan B Pedersen, MD          Principal Investigator: Jan B Pedersen, MD          Germany SANA Klinikum Lichtenberg Recruiting Berlin, Germany Contact: Dirk Federlein          Principal Investigator: Dirk Hartmann, MD          Evangelisches Krankenhaus Castrop-Rauxel Recruiting Castrop Rauxel, Germany Contact: Pravin Thattamparambil, MD          Principal Investigator: Pravin Thattamparambil, MD          St. Marienstift Krankenhaus Friesoythe Recruiting Friesoythe, Germany Contact: Ralf Weise, MD          Principal Investigator: Ralf Weise, MD          Hospital zum Heiligen Geist Fritzlar Recruiting Fritzlar, Germany Contact: Carsten Bismarck          Principal Investigator: Carsten Bismarck, MD          Klinikum Garmisch-Partenkirchen Recruiting Garmisch-Partenkirchen, Germany Contact: Holger Vogelsang          Principal Investigator: Holger Vogelsang, MD          Asklepios Klinik Altona Recruiting Hamburg, Germany Contact: Gero Puhl          Principal Investigator: Gero Puhl          KRH Klinikum Siloah Hannover Oststadt Recruiting Hannover, Germany Contact: Ahmed Madisch          Principal Investigator: Ahmed Madisch, MD          Evangelisches Krankenhaus Herne Recruiting Herne, Germany Contact: Matthias Kemen, MD          Principal Investigator: Matthias Kemen, MD          Klinikum Konstanz Recruiting Konstanz, Germany Contact: Ulrike Petzsche          Principal Investigator: Marcus Schuchmann, MD          Heilig Geist-Krankenhaus Köln Recruiting Köln, Germany Contact: Ernst Eypasch, MD          Principal Investigator: Ernst Eypasch, MD          Universitätsklinikum Magdeburg Recruiting Magdeburg, Germany Contact: Frank Benedix          Principal Investigator: Ulrike von Arnim          Universitätsmedizin Mannheim Recruiting Mannheim, Germany Contact: Mirko Otto          Principal Investigator: Kai Nowak, MD          Klinikum Memmingen Recruiting Memmingen, Germany Contact: Heinz Schlosser          Principal Investigator: Carsten Gutt, MD          Friedrich-Ebert-Krankenhaus Neumünster Recruiting Neumünster, Germany Contact: Andrea Pace          Principal Investigator: Andrea Pace, MD          Asklepios Schwalm-Eder Kliniken GmbH Recruiting Schwalmstadt, Germany Contact: Norbert Hesselbarth          Principal Investigator: Felix Meuschke, MD          Jung Stilling - Siegen Recruiting Siegen, Germany Contact: Daniela-Patricia Borkenstein          Principal Investigator: Joachim Labenz, MD          St. Marien-Krankenhaus Siegen Recruiting Siegen, Germany Contact: Dietmar Stephan, MD          Principal Investigator: Dietmar Stephan, MD          Ev. Krankenhaus Wesel GmbH Recruiting Wesel, Germany Contact: Vivianda Menke          Principal Investigator: Vivianda Menke, MD          Mexico Hospital San José Recruiting Monterrey, Mexico Contact: David Aguirre Mar, MD          Principal Investigator: David Aguirre Mar, MD          Netherlands Maastricht University Medical Center Recruiting Maastricht, Netherlands Contact: Nicole Bouvy, MD          Principal Investigator: Nicole Bouvy, MD          United Kingdom Spire Leicester Hospital Recruiting Leicester, United Kingdom Contact: Chris Sutton          Principal Investigator: Chris Sutton, MD          University Hospital Southampton Recruiting Southampton, United Kingdom Contact: Abrie Botha          Principal Investigator: Abrie Botha, MD Collapse <<
  NCT01382511	Pachyonychia Congenita	Not Applicable	Unknown	-	-

• 参考文献

• [3] The discovery and development of HMG-CoA reductase inhibitors