METHODS FOR TREATING OR PREVENTING CHOLESTEROL RELATED DISORDERS

• Main Authors: SCOTT WASSERMAN, TIMOTHY DAVID OSSLUND, CLAPTON S DIAS, JOHN P GIBBS, CHAN JOYCE CHI YEE, EVAN A STEIN, ROBERT ANDREW DONALD SCOTT, CHRISTI L CLOGSTON
• Format: Patent
• Language: English; Japanese
• Published: 20.12.2018
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

To provide a stable formulation suitable for parenteral administration, the formulation comprising a monoclonal antibody or a fragment thereof that is specifically bound to proprotein convertase subtilisin/kexin type 9 (PCSK9) and is useful for treating or preventing a cholesterol-related disorder.SOLUTION: According to the present invention, there is provided a stable formulation comprising: (a) a monoclonal antibody or fragment thereof having a specific amino acid sequence and present in an amount of 70 to 200 mg/mL that specifically binds to PCSK9; (b) 10 to 20 mM of sodium acetate; (c) 0.5 to 10% w/v of a stabilizer, which is polyhydroxy hydrocarbon selected from sorbitol, mannitol, and glycerol, or a disaccharide selected from sucrose, maltose, lactose, fructose, and trehalose; and (d) 0.004 to 0.01% w/v of polysorbate 20 or polysorbate 80, the formulation having (e) a pH of 5.0 to 5.5.SELECTED DRAWING: None 【課題】前駆タンパク質転換酵素サブチリシン／ケキシン９型（ＰＣＳＫ９）に対して特異的に結合し、コレステロール関連障害を治療又は予防するために有用なモノクロナール抗体又はその断片を含み、非経口投与に適する安定な製剤の提供。【解決手段】（ａ）特定のアミノ酸配列を有し、ＰＣＳＫ９に対して特異的に結合する、７０〜２００ｍｇ／ｍＬの量で存在するモノクローナル抗体又はその断片、（ｂ）１０〜２０ｍＭの酢酸ナトリウム、（ｃ）０．５〜１０％ｗ／ｖの安定剤であって、ソルビトール、マンニトール及びグリセロールから選択されるポリヒドロキシ炭化水素、又は、スクロース、マルトース、ラクトース、フルクトース及びトレハロースから選択される二糖類である安定剤、及び（ｄ）０．００４〜０．０１％ｗ／ｖのポリソルベート２０又はポリソルベート８０、を含み、（ｅ）ｐＨ５．０〜５．５を有する、安定な製剤。【選択図】なし