WO2017110965A1 - バソプレシン様作用増強剤 - Google Patents
バソプレシン様作用増強剤 Download PDFInfo
- Publication number
- WO2017110965A1 WO2017110965A1 PCT/JP2016/088283 JP2016088283W WO2017110965A1 WO 2017110965 A1 WO2017110965 A1 WO 2017110965A1 JP 2016088283 W JP2016088283 W JP 2016088283W WO 2017110965 A1 WO2017110965 A1 WO 2017110965A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- vasopressin
- antidiuretic
- imidafenacin
- action
- receptor agonist
- Prior art date
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Classifications
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4174—Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/08—Peptides having 5 to 11 amino acids
- A61K38/095—Oxytocins; Vasopressins; Related peptides
-
- 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
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
Definitions
- the present invention relates to a composition for enhancing the antidiuretic action of vasopressin or a vasopressin V2 receptor agonist, which contains imidafenacin.
- the present invention also relates to an antidiuretic composition containing imidafenacin, which has an action of enhancing the antidiuretic action of a vasopressin or vasopressin V2 receptor agonist.
- Imidafenacin is an anticholinergic that selectively inhibits muscarinic M1 and M3 receptors and is currently widely used as a treatment for urgency, frequent urination and urge urinary incontinence in overactive bladder (OAB) Yes. Imidafenacin is considered to exert a pharmacological effect in the bladder by exhibiting an acetylcholine release inhibitory action by M1 antagonism and a bladder smooth muscle contraction inhibitory action by M3 antagonism (Non-patent Document 1).
- Overactive bladder which is the efficacy and effect of imidafenacin, is a symptom syndrome that requires urgency, and it is usually said to accompany frequent urination and nocturia (Non-patent Document 2).
- nocturia is a complaint that must occur at least once for urination at night, and it is said that it is in a troubled state (Non-Patent Document 3).
- Imidafenacin has a nocturnal urine volume reduction effect, and as one of the background, it is reported that the antidiuretic effect via the bladder sensory nerve is considered, but the mechanism is still not well understood (Non-Patent Document 4). ).
- vasopressin is known as a hormone that regulates urine output.
- Vasopressin is a peptide also called an antidiuretic hormone, and V1a, V1b and V2 receptors are known as its receptors.
- the V2 receptor is present in the renal collecting duct, and binding of vasopressin promotes water reabsorption and decreases urine output (antidiuretic effect). Therefore, when the action of vasopressin decreases, polyuria, nocturnal enuresis, diabetes insipidus and the like are caused.
- desmopressin is known as a V2 receptor agonist showing a vasopressin-like antidiuretic action.
- Desmopressin is also a peptide and is currently used as a therapeutic agent for nocturnal enuresis and central diabetes insipidus by selectively binding to the V2 receptor and exerting an antidiuretic action.
- compositions containing a compound that enhances the antidiuretic action of vasopressin or a vasopressin V2 receptor agonist is used for the prevention or treatment of frequent urination, nocturia, polyuria, nocturia, nocturia, diabetes insipidus, etc. It seems useful as a composition.
- composition that enhances the antidiuretic action of vasopressin or a vasopressin V2 receptor agonist, and a means for preventing or treating frequent urination and nocturia due to nocturia, especially nocturia due to nocturia using the composition It is a problem to be solved by the present invention.
- the present inventors have found that imidafenacin enhances the antidiuretic action of vasopressin and a vasopressin V2 receptor agonist, and completed the present invention. That is, the present invention includes the following inventions.
- An antidiuretic composition containing imidafenacin which has an action of enhancing the antidiuretic action of a vasopressin or vasopressin V2 receptor agonist.
- imidafenacin can enhance the antidiuretic action of vasopressin or a vasopressin V2 receptor agonist, and prevent or treat frequent urination and nocturia due to nocturia, especially nocturia at night. be able to.
- an antidiuretic composition containing imidafensin based on the action of imidafenacin can be provided.
- the oral dose of imidafenacin is preferably 0.05 to 1.0 mg / day, more preferably 0.1 to 0.4 mg / day, and particularly preferably 0.2 mg / day.
- the above dose may be orally administered twice a day after breakfast and dinner, or may be orally administered once a day after dinner.
- vasopressin V2 receptor agonist refers to a compound that binds to the V2 receptor, which is a vasopressin receptor, and causes a vasopressin-like action (antidiuretic action).
- a particularly preferred vasopressin V2 receptor agonist in the present invention is desmopressin or a pharmaceutically acceptable salt thereof.
- vasopressin V2 receptor agonist and V2 receptor agonist are synonymous.
- “enhancement of the antidiuretic action of a vasopressin or vasopressin V2 receptor agonist” represents a state showing an antidiuretic action exceeding the antidiuretic action of a vasopressin or vasopressin V2 receptor agonist alone.
- composition of the present invention can contain any pharmaceutically acceptable carrier.
- composition of the present invention can also contain any pharmaceutically acceptable additive.
- the additive include an excipient, a disintegrant, a binder, a lubricant, a coating agent, a coloring agent, and a brightening agent.
- excipient examples include sugars such as lactose and glucose, sugar alcohols such as D-sorbitol and mannitol, celluloses such as crystalline cellulose, starches such as partially pregelatinized starch and corn starch.
- disintegrant examples include carboxymethylcellulose calcium, low-substituted hydroxypropylcellulose, croscarmellose sodium, celluloses such as methylcellulose, crospovidone, and the like.
- binder examples include celluloses such as crystalline cellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, ethylcellulose, and methylcellulose, gelatin, polyvinyl alcohol, polyvinyl alcohol partial saponified product, and polyvinylpyrrolidone.
- lubricant examples include stearic acid and its metal salts, talc, hydrogenated oil, light anhydrous silicic acid, hydrous silicon dioxide, and sucrose fatty acid ester.
- Coating agents include celluloses such as hydroxypropylcellulose, hydroxypropylmethylcellulose, ethylcellulose, methylcellulose, hydroxypropylmethylcellulose phthalate, methacrylic acid copolymer, povidone, stearyl alcohol, ammonio methacrylate copolymer, aminoalkyl methacrylate copolymer E, polyvinyl acetal Examples include diethylaminoacetate and methacrylic acid copolymer (L, S).
- colorant examples include titanium oxide and iron sesquioxide.
- brighteners examples include carnauba wax.
- composition of the present invention is administered, for example, in an oral dosage form such as a tablet, capsule, granule, powder, inhalant, syrup or jelly, or a parenteral dosage form such as an injection, suppository or patch. can do.
- an oral dosage form such as a tablet, capsule, granule, powder, inhalant, syrup or jelly
- a parenteral dosage form such as an injection, suppository or patch. can do.
- composition of the present invention can be produced by a method commonly used in the art.
- the composition of the present invention when the composition of the present invention is a film-coated tablet, it can be produced by the method described in International Publication WO2001 / 034147.
- the composition of this invention when the composition of this invention is an orally disintegrating tablet, it can manufacture by the method as described in international publication WO2009 / 0965559.
- imidafenacin had a dose-dependent antidiuretic effect.
- the urine volume reduction effect was about 50% at the maximum.
- FIG. 2 shows the antidiuretic action of desmopressin. As shown in FIG. 2, a dose-dependent antidiuretic effect was observed for desmopressin. In addition, the urine volume reduction effect was about 100% at maximum.
- FIG. 3 shows the antidiuretic effect when imidafenacin and desmopressin are administered in combination.
- the antidiuretic effect was enhanced when both were used in combination, compared to when imidafenacin or desmopressin was administered alone.
- the combination of imidafenacin and desmopressin was found for the first time by the present invention to enhance the antidiuretic action, and since these drugs have different mechanisms of action, the potentiating effect is an unexpected result. is there.
- desmopressin is an analog of vasopressin, it is considered that the antidiuretic action of vasopressin is enhanced by concomitant use with imidafenacin as well as desmopressin.
- Mozabaptane is a so-called V2 antagonist that antagonizes vasopressin and desmopressin and inhibits their antidiuretic action.
- the inhibitory action of imidafenacin or desmopressin on the antidiuretic action of mozabaptan is shown in FIG.
- the antidiuretic effect of imidafenacin was completely suppressed by mozabaptan even at the maximum response dose of 300 ⁇ g / kg.
- the antidiuretic effect of desmopressin was also suppressed by mozabaptan, but the antidiuretic effect was restored at 0.1 ⁇ g / kg, which is the maximum response dose of desmopressin.
- vasopressin system is involved in the antidiuretic action of imidafenacin, and that imidafenacin exerts an antidiuretic action by enhancing the activity of vasopressin. It was first discovered by the present invention that the vasopressin system is involved in the antidiuretic action of imidafenacin. In addition, since imidafenacin does not affect the release of vasopressin in rats, it has been reported that vasopressin is not involved in the antidiuretic action of imidafenacin (Watanabe et al. fiber affiliates in the bladedder. BJU Int 112 (1) 131-6), the effect of the present invention is an unexpected and unexpected result.
- prevention or treatment of frequent urination or nocturia due to nocturia, particularly nocturia can be expected by enhancing the antidiuretic action of vasopressin or a vasopressin V2 receptor agonist with imidafenacin.
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Immunology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Gastroenterology & Hepatology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
[1]バソプレシン又はバソプレシンV2受容体アゴニストの抗利尿作用を増強するために使用される、イミダフェナシンを含有する医薬組成物。
[2]イミダフェナシンを含有する、バソプレシン又はバソプレシンV2受容体アゴニストの抗利尿作用の増強用組成物。
[3]バソプレシン又はバソプレシンV2受容体アゴニストの抗利尿作用の増強作用を有する、イミダフェナシンを含有する抗利尿用組成物。
[4]バソプレシン又はバソプレシンV2受容体アゴニストと共に使用される、イミダフェナシンを含有する抗利尿用組成物。
[5]イミダフェナシン、及びバソプレシン又はバソプレシンV2受容体アゴニストを含有する抗利尿用組成物。
[6]バソプレシンV2受容体アゴニストがデスモプレシン又はその薬学的に許容される塩である、[1]~[5]のいずれか1つに記載の組成物。
Claims (6)
- バソプレシン又はバソプレシンV2受容体アゴニストの抗利尿作用を増強するために使用される、イミダフェナシンを含有する医薬組成物。
- イミダフェナシンを含有する、バソプレシン又はバソプレシンV2受容体アゴニストの抗利尿作用の増強用組成物。
- バソプレシン又はバソプレシンV2受容体アゴニストの抗利尿作用の増強作用を有する、イミダフェナシンを含有する抗利尿用組成物。
- バソプレシン又はバソプレシンV2受容体アゴニストと共に使用される、イミダフェナシンを含有する抗利尿用組成物。
- イミダフェナシン、及びバソプレシン又はバソプレシンV2受容体アゴニストを含有する抗利尿用組成物。
- バソプレシンV2受容体アゴニストがデスモプレシン又はその薬学的に許容される塩である、請求項1~5のいずれか一項に記載の組成物。
Priority Applications (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP16878852.9A EP3395343A4 (en) | 2015-12-25 | 2016-12-22 | AMPLIFIER FOR THE ACTION OF VASOPRESSINE COMPOUNDS |
RU2018122072A RU2722344C2 (ru) | 2015-12-25 | 2016-12-22 | Усиливающий агент с вазопрессинподобным действием |
JP2017558242A JP6663933B2 (ja) | 2015-12-25 | 2016-12-22 | バソプレシン様作用増強剤 |
KR1020187017122A KR20180097551A (ko) | 2015-12-25 | 2016-12-22 | 바소프레신 유사 작용 증강제 |
US15/775,147 US10517851B2 (en) | 2015-12-25 | 2016-12-22 | Vasopressin-like action enhancer |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2015-253018 | 2015-12-25 | ||
JP2015253018 | 2015-12-25 |
Publications (1)
Publication Number | Publication Date |
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WO2017110965A1 true WO2017110965A1 (ja) | 2017-06-29 |
Family
ID=59089514
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/JP2016/088283 WO2017110965A1 (ja) | 2015-12-25 | 2016-12-22 | バソプレシン様作用増強剤 |
Country Status (7)
Country | Link |
---|---|
US (1) | US10517851B2 (ja) |
EP (1) | EP3395343A4 (ja) |
JP (1) | JP6663933B2 (ja) |
KR (1) | KR20180097551A (ja) |
RU (1) | RU2722344C2 (ja) |
TW (1) | TWI724084B (ja) |
WO (1) | WO2017110965A1 (ja) |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2001034147A1 (fr) | 1999-11-11 | 2001-05-17 | Kyorin Pharmaceutical Co., Ltd. | Preparation solide orale |
WO2009096559A1 (ja) | 2008-01-31 | 2009-08-06 | Kyorin Pharmaceutical Co., Ltd. | イミダフェナシンを有効成分とする口腔内速崩錠の製造方法 |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102341099A (zh) | 2009-03-03 | 2012-02-01 | 什诺波特有限公司 | R-巴氯芬前药的持续释放口服剂型 |
US8377956B2 (en) * | 2010-03-01 | 2013-02-19 | Xenoport, Inc. | Use of (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl) butanoic acid for treating urinary incontinence |
CN104274422B (zh) * | 2014-02-12 | 2018-01-19 | 天津市汉康医药生物技术有限公司 | 一种含咪达那新的药物组合物 |
-
2016
- 2016-12-22 KR KR1020187017122A patent/KR20180097551A/ko not_active Application Discontinuation
- 2016-12-22 WO PCT/JP2016/088283 patent/WO2017110965A1/ja active Application Filing
- 2016-12-22 RU RU2018122072A patent/RU2722344C2/ru active
- 2016-12-22 US US15/775,147 patent/US10517851B2/en not_active Expired - Fee Related
- 2016-12-22 EP EP16878852.9A patent/EP3395343A4/en not_active Withdrawn
- 2016-12-22 JP JP2017558242A patent/JP6663933B2/ja not_active Expired - Fee Related
- 2016-12-23 TW TW105143047A patent/TWI724084B/zh active
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2001034147A1 (fr) | 1999-11-11 | 2001-05-17 | Kyorin Pharmaceutical Co., Ltd. | Preparation solide orale |
WO2009096559A1 (ja) | 2008-01-31 | 2009-08-06 | Kyorin Pharmaceutical Co., Ltd. | イミダフェナシンを有効成分とする口腔内速崩錠の製造方法 |
Non-Patent Citations (8)
Also Published As
Publication number | Publication date |
---|---|
US20180344700A1 (en) | 2018-12-06 |
RU2018122072A (ru) | 2020-01-27 |
RU2018122072A3 (ja) | 2020-01-27 |
TWI724084B (zh) | 2021-04-11 |
JP6663933B2 (ja) | 2020-03-13 |
EP3395343A1 (en) | 2018-10-31 |
EP3395343A4 (en) | 2019-08-21 |
RU2722344C2 (ru) | 2020-05-29 |
TW201735920A (zh) | 2017-10-16 |
KR20180097551A (ko) | 2018-08-31 |
US10517851B2 (en) | 2019-12-31 |
JPWO2017110965A1 (ja) | 2018-10-18 |
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