JP4588448B2 - PPARγアゴニストによる治療に伴う体重増加を治療するためのPPARαアゴニストの使用 - Google Patents
PPARγアゴニストによる治療に伴う体重増加を治療するためのPPARαアゴニストの使用 Download PDFInfo
- Publication number
- JP4588448B2 JP4588448B2 JP2004530101A JP2004530101A JP4588448B2 JP 4588448 B2 JP4588448 B2 JP 4588448B2 JP 2004530101 A JP2004530101 A JP 2004530101A JP 2004530101 A JP2004530101 A JP 2004530101A JP 4588448 B2 JP4588448 B2 JP 4588448B2
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- JP
- Japan
- Prior art keywords
- agonist
- pparγ
- pparα
- weight gain
- treatment
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Emergency Medicine (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Child & Adolescent Psychology (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
この研究は、PPARγアゴニストのロシグリタゾンとPPARαアゴニストのフェノフィブラートとの組み合わせを糖尿病の治療に使用した効果を評価するために、また、この併用療法がロシグリタゾンによる治療に伴う体重増加を防げるかどうかを調べるために設計した。
動物:
9〜11週齢の雄Zuckerラット(ホモ体)及び肥満していないコントロールを、Iffa−Credo社(フランス)から入手した。ラットはそれぞれケージの中に入れ、温度、湿度及び光を調節した部屋(21〜23℃、明暗サイクル12時間)に静置した。ラットには研究用標準試料を与え、水は自由に飲ませた。順応させた後、体重に応じてラットを10つの群に無作為に分けた。
1群=肥満していないラット、非投与;
2群=肥満ラット、担体を経口で1日2回投与(午前8時及び午後8時);
3群=肥満ラット、フェノフィブラート100mg/kgを経口で1日2回投与(午前8時及び午後8時);
4群=肥満ラット、ロシグリタゾン0.3mg/kgを経口で1日2回投与(午前8時及び午後8時);
5群=肥満ラット、ロシグリタゾン3.0mg/kgを経口で1日2回投与(午前8時及び午後8時);
6群=肥満ラット、フェノフィブラート100mg/kg及びロシグリタゾン0.3mg/kgを経口で1日2回投与(午前8時及び午後8時);
7群=肥満ラット、フェノフィブラート100mg/kg及びロシグリタゾン3.0mg/kgを経口で1日2回投与(午前8時及び午後8時);
体重増加については、投与量に依存して体重が増加したのはロシグリタゾンのみであった。フェノフィブラートとロシグリタゾンとを併用することによって体重増加が著しく減少し、ロシグリタゾンの投与量が0.3mg/kgと少ない場合に体重増加の抑制がより大きかった。
方法
肥満した雄ZDFラット及び肥満していないコントロール(GMI、インディアナポリス)にPurina5008を自由に摂取させた。6.5週齢以降、ラットにフェノフィブラート(100mg/kg、経口で1日2回)、ロシグリタゾン(0.3mg/kg、経口で1日2回)、これらの組み合わせ又は担体を13週間投与した。
Claims (5)
- PPARγアゴニストによる治療によって誘発される体重増加を低減させる薬剤を製造するための、PPARαアゴニスト及び医薬品に許容される担体の使用であって、
PPARαアゴニストは、フェノフィブラートであって、
PPARγアゴニストは、ロシグリタゾンである
ことを特徴とする使用。 - PPARγアゴニストによる治療によって誘発される体重増加を低減させる薬剤を製造するための、PPARαアゴニスト、PPARγアゴニスト及び医薬品に許容される担体の使用であって、
PPARαアゴニストは、フェノフィブラートであって、
PPARγアゴニストは、ロシグリタゾンである
ことを特徴とする使用。 - PPARαアゴニスト及びPPARγアゴニストを同時に又は順次投与する
ことを特徴とする請求項1または2に記載の使用。 - PPARαアゴニストの有効投与量は、1日当たり約10〜約3000mgの範囲内である
ことを特徴とする請求項1〜3のいずれか1項に記載の使用。 - PPARγアゴニストの有効投与量は、1日当たり約0.5〜約3mgの範囲内である
ことを特徴とする請求項1〜4のいずれか1項に記載の使用。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP02291994A EP1388351A1 (en) | 2002-08-08 | 2002-08-08 | Use of fibrate to treat weight gain associated with rosiglitazone treatment |
EP02292830A EP1388352A1 (en) | 2002-08-08 | 2002-11-14 | Use of a ppar-alpha agonist to treat patients suffering from weight gain associated with a ppar-gamma agonist treatment |
PCT/EP2003/008756 WO2004018041A1 (en) | 2002-08-08 | 2003-08-06 | Use of a ppar-alpha agonist to treat weight gain associated with a ppar-gamma agonist treatment |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2005539033A JP2005539033A (ja) | 2005-12-22 |
JP4588448B2 true JP4588448B2 (ja) | 2010-12-01 |
Family
ID=30445152
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2004530101A Expired - Fee Related JP4588448B2 (ja) | 2002-08-08 | 2003-08-06 | PPARγアゴニストによる治療に伴う体重増加を治療するためのPPARαアゴニストの使用 |
Country Status (10)
Country | Link |
---|---|
US (2) | US20040110799A1 (ja) |
EP (2) | EP1388352A1 (ja) |
JP (1) | JP4588448B2 (ja) |
CN (1) | CN1674959A (ja) |
AT (1) | ATE536913T1 (ja) |
AU (1) | AU2003260380B2 (ja) |
CA (1) | CA2493747A1 (ja) |
ES (1) | ES2379165T3 (ja) |
NO (1) | NO20050526L (ja) |
WO (1) | WO2004018041A1 (ja) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GT200600046A (es) | 2005-02-09 | 2006-09-25 | Terapia de combinacion |
Family Cites Families (26)
Publication number | Priority date | Publication date | Assignee | Title |
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US5071773A (en) | 1986-10-24 | 1991-12-10 | The Salk Institute For Biological Studies | Hormone receptor-related bioassays |
EP0842925A1 (en) | 1987-09-04 | 1998-05-20 | Beecham Group Plc | Substituted thiazolidinedione derivatives |
US4981784A (en) | 1987-12-02 | 1991-01-01 | The Salk Institute For Biological Studies | Retinoic acid receptor method |
CA2067216A1 (en) | 1989-10-25 | 1991-04-26 | Cary Alan Weinberger | Receptor infection assay |
EP0441483A3 (en) | 1990-01-16 | 1992-11-19 | Baylor College Of Medicine | Expression vectors that produce steroid receptors, steroid receptor chimera, screening assays for steroid receptors and clinical assays using synthesized receptors and receptor vectors |
CA2090407A1 (en) | 1990-09-21 | 1992-03-22 | Ronald M. Evans | Functional antagonism between proto-oncoprotein c-jun and hormone receptors |
GB9027023D0 (en) | 1990-12-12 | 1991-01-30 | Wellcome Found | Anti-atherosclerotic aryl compounds |
JPH07503609A (ja) | 1991-12-06 | 1995-04-20 | ザ ソールク インスチチュート フォア バイオロジカル スタディズ | リセプターのステロイド/甲状腺スーパーファミリーのメンバーの多量体型 |
JPH07509694A (ja) | 1992-05-14 | 1995-10-26 | ベイラー・カレッジ・オブ・メディシン | 突然変異したステロイドホルモン受容体,その使用方法および遺伝子治療のための分子スイッチ |
WO1994023068A1 (en) | 1993-04-07 | 1994-10-13 | Ligand Pharmaceuticals, Incorporated | Method for screening for receptor agonists |
US5506102A (en) | 1993-10-28 | 1996-04-09 | Ligand Pharmaceuticals Incorporated | Methods of using the A form of the progesterone receptor to screen for antagonists of steroid intracellar receptor-mediated transcription |
WO1995018380A1 (en) | 1993-12-30 | 1995-07-06 | The Salk Institute For Biological Studies | Novel uses for gal4-receptor constructs |
WO1997028149A1 (en) | 1996-02-02 | 1997-08-07 | Merck & Co., Inc. | Method for raising hdl cholesterol levels |
ATE293963T1 (de) | 1996-02-02 | 2005-05-15 | Merck & Co Inc | Verfahren zur behandlung von diabetes und verwandter krankheitszustände. |
JP2002503202A (ja) | 1996-02-02 | 2002-01-29 | メルク エンド カンパニー インコーポレーテッド | 抗糖尿病薬 |
ATE262334T1 (de) | 1996-02-02 | 2004-04-15 | Merck & Co Inc | Antidiabetisches mittel |
ES2194179T3 (es) | 1996-02-02 | 2003-11-16 | Merck & Co Inc | Derivados heterociclicos como agentes antidiabeticos y antiobesidad. |
AU4050797A (en) * | 1996-08-02 | 1998-02-25 | Ligand Pharmaceuticals Incorporated | Prevention or treatment of type 2 diabetes or cardiovascular disease with ppar modulators |
TW438784B (en) | 1997-08-29 | 2001-06-07 | Ssp Co Ltd | Triazole derivative or salt thereof and pharmaceutical composition for treating mycosis containing the same |
AU4713499A (en) * | 1998-06-27 | 2000-01-17 | Photogenesis, Inc. | Ophthalmic uses of ppargamma agonists and ppargamma antagonists |
CA2329004C (en) * | 1998-06-30 | 2009-04-14 | Takeda Chemical Industries, Ltd. | Combination of insulin sensitizer with anorectic for treating or preventing diabetes |
BR0110208A (pt) | 2000-04-19 | 2003-01-28 | Borody Thomas J | Composições e terapias para distúrbios associados com hiperlipidemia |
DE60128475T2 (de) * | 2000-07-25 | 2008-02-07 | Merck & Co., Inc. | N-substituierte indole mit anwendung in der behandlung von diabetes |
AU2001255515A1 (en) * | 2000-09-20 | 2002-04-02 | Skyepharma Canada Inc. | Stabilised fibrate microparticles |
AU2001291233A1 (en) * | 2000-10-05 | 2002-04-15 | Dr. Reddy's Research Foundation | Polymorphs of pioglitazone hydrochloride and their use as antidiabetics |
ATE423559T1 (de) * | 2001-04-04 | 2009-03-15 | Ortho Mcneil Janssen Pharm | Kombinationstherapie durch glukoseresorptionshemmer und ppar modulatoren |
-
2002
- 2002-11-14 EP EP02292830A patent/EP1388352A1/en not_active Withdrawn
-
2003
- 2003-08-06 CN CNA038191350A patent/CN1674959A/zh active Pending
- 2003-08-06 AT AT03792272T patent/ATE536913T1/de active
- 2003-08-06 ES ES03792272T patent/ES2379165T3/es not_active Expired - Lifetime
- 2003-08-06 JP JP2004530101A patent/JP4588448B2/ja not_active Expired - Fee Related
- 2003-08-06 EP EP03792272A patent/EP1526894B1/en not_active Expired - Lifetime
- 2003-08-06 WO PCT/EP2003/008756 patent/WO2004018041A1/en active Application Filing
- 2003-08-06 CA CA002493747A patent/CA2493747A1/en not_active Abandoned
- 2003-08-06 AU AU2003260380A patent/AU2003260380B2/en not_active Ceased
- 2003-08-08 US US10/636,670 patent/US20040110799A1/en not_active Abandoned
-
2005
- 2005-01-31 NO NO20050526A patent/NO20050526L/no not_active Application Discontinuation
-
2008
- 2008-10-10 US US12/249,027 patent/US20090099238A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
AU2003260380B2 (en) | 2008-11-06 |
JP2005539033A (ja) | 2005-12-22 |
NO20050526L (no) | 2005-03-02 |
WO2004018041A1 (en) | 2004-03-04 |
ES2379165T3 (es) | 2012-04-23 |
US20090099238A1 (en) | 2009-04-16 |
US20040110799A1 (en) | 2004-06-10 |
EP1526894B1 (en) | 2011-12-14 |
CA2493747A1 (en) | 2004-03-04 |
EP1526894A1 (en) | 2005-05-04 |
CN1674959A (zh) | 2005-09-28 |
EP1388352A1 (en) | 2004-02-11 |
ATE536913T1 (de) | 2011-12-15 |
AU2003260380A1 (en) | 2004-03-11 |
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