CA2865845C - An iloperidone metabolite for use in the treatment of psychiatric disorders - Google Patents
An iloperidone metabolite for use in the treatment of psychiatric disorders Download PDFInfo
- Publication number
- CA2865845C CA2865845C CA2865845A CA2865845A CA2865845C CA 2865845 C CA2865845 C CA 2865845C CA 2865845 A CA2865845 A CA 2865845A CA 2865845 A CA2865845 A CA 2865845A CA 2865845 C CA2865845 C CA 2865845C
- Authority
- CA
- Canada
- Prior art keywords
- day
- iloperidone
- once daily
- disorder
- 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.)
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Links
- XMXHEBAFVSFQEX-UHFFFAOYSA-N iloperidone Chemical class COC1=CC(C(C)=O)=CC=C1OCCCN1CCC(C=2C3=CC=C(F)C=C3ON=2)CC1 XMXHEBAFVSFQEX-UHFFFAOYSA-N 0.000 title abstract description 45
- 208000020016 psychiatric disease Diseases 0.000 title abstract description 11
- 150000003839 salts Chemical class 0.000 claims abstract description 33
- 150000002148 esters Chemical class 0.000 claims abstract description 26
- 239000008194 pharmaceutical composition Substances 0.000 claims description 11
- 239000003937 drug carrier Substances 0.000 claims description 5
- 239000004480 active ingredient Substances 0.000 claims description 4
- 229960003162 iloperidone Drugs 0.000 abstract description 41
- 208000028017 Psychotic disease Diseases 0.000 abstract description 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract description 10
- 208000035475 disorder Diseases 0.000 abstract description 10
- 201000000980 schizophrenia Diseases 0.000 abstract description 10
- 206010003805 Autism Diseases 0.000 abstract description 9
- 208000020706 Autistic disease Diseases 0.000 abstract description 9
- 208000020925 Bipolar disease Diseases 0.000 abstract description 9
- 208000001914 Fragile X syndrome Diseases 0.000 abstract description 8
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- 208000029560 autism spectrum disease Diseases 0.000 abstract description 8
- 208000024714 major depressive disease Diseases 0.000 abstract description 8
- 208000022610 schizoaffective disease Diseases 0.000 abstract description 8
- 239000003693 atypical antipsychotic agent Substances 0.000 abstract description 6
- 229940127236 atypical antipsychotics Drugs 0.000 abstract description 6
- 238000000034 method Methods 0.000 description 9
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- AUVALWUPUHHNQV-UHFFFAOYSA-N 2-hydroxy-3-propylbenzoic acid Chemical class CCCC1=CC=CC(C(O)=O)=C1O AUVALWUPUHHNQV-UHFFFAOYSA-N 0.000 description 1
- 244000215068 Acacia senegal Species 0.000 description 1
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- 108010010803 Gelatin Proteins 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 229920000084 Gum arabic Polymers 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
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- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
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- 230000008841 allosteric interaction Effects 0.000 description 1
- 230000000561 anti-psychotic effect Effects 0.000 description 1
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- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
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- UORVGPXVDQYIDP-BJUDXGSMSA-N borane Chemical class [10BH3] UORVGPXVDQYIDP-BJUDXGSMSA-N 0.000 description 1
- 229910000085 borane Inorganic materials 0.000 description 1
- 239000001506 calcium phosphate Substances 0.000 description 1
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- 235000012241 calcium silicate Nutrition 0.000 description 1
- OYACROKNLOSFPA-UHFFFAOYSA-N calcium;dioxido(oxo)silane Chemical compound [Ca+2].[O-][Si]([O-])=O OYACROKNLOSFPA-UHFFFAOYSA-N 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
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- 235000014113 dietary fatty acids Nutrition 0.000 description 1
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- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000006194 liquid suspension Substances 0.000 description 1
- 239000007937 lozenge Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000037353 metabolic pathway Effects 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
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- 235000010446 mineral oil Nutrition 0.000 description 1
- 239000002480 mineral oil Substances 0.000 description 1
- 239000002687 nonaqueous vehicle Substances 0.000 description 1
- 239000008188 pellet Substances 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000003449 preventive effect Effects 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
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- GOLXNESZZPUPJE-UHFFFAOYSA-N spiromesifen Chemical compound CC1=CC(C)=CC(C)=C1C(C(O1)=O)=C(OC(=O)CC(C)(C)C)C11CCCC1 GOLXNESZZPUPJE-UHFFFAOYSA-N 0.000 description 1
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- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
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
- A61K31/435—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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/42—Oxazoles
-
- 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
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/20—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- 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)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Psychiatry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261610664P | 2012-03-14 | 2012-03-14 | |
| US61/610,664 | 2012-03-14 | ||
| PCT/US2013/031413 WO2013138602A1 (en) | 2012-03-14 | 2013-03-14 | An iloperidone metabolite for use in the treatment of psychiatric disorders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2865845A1 CA2865845A1 (en) | 2013-09-19 |
| CA2865845C true CA2865845C (en) | 2020-02-18 |
Family
ID=48407766
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2865845A Active CA2865845C (en) | 2012-03-14 | 2013-03-14 | An iloperidone metabolite for use in the treatment of psychiatric disorders |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US10874659B2 (enExample) |
| EP (2) | EP3345603B1 (enExample) |
| JP (5) | JP2015510893A (enExample) |
| KR (2) | KR20140121487A (enExample) |
| CN (2) | CN108938632A (enExample) |
| AU (2) | AU2013232014B2 (enExample) |
| BR (1) | BR112014022687A8 (enExample) |
| CA (1) | CA2865845C (enExample) |
| CL (1) | CL2014002430A1 (enExample) |
| CO (1) | CO7091183A2 (enExample) |
| ES (2) | ES2677474T3 (enExample) |
| IL (1) | IL234412B (enExample) |
| IN (1) | IN2014DN08495A (enExample) |
| MX (1) | MX374067B (enExample) |
| RU (1) | RU2651710C2 (enExample) |
| WO (1) | WO2013138602A1 (enExample) |
| ZA (1) | ZA201406369B (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102870956B1 (ko) | 2015-02-17 | 2025-10-16 | 반다 파마슈티칼즈, 인코퍼레이티드. | 조현병의 치료를 위한 일로페리돈 |
| US11214827B2 (en) | 2018-08-30 | 2022-01-04 | Vanda Pharmaceuticals Inc. | Genetic markers for enhancing efficacy of antipsychotic treatment with iloperidone |
| EP4637768A1 (en) * | 2022-12-19 | 2025-10-29 | Vanda Pharmaceuticals Inc. | Dosage regime of iloperidone for treating bipolar i disorder and schizophrenia |
| CN121218989A (zh) * | 2023-06-02 | 2025-12-26 | 万达制药公司 | 使用伊潘立酮的治疗方法 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5364866A (en) | 1989-05-19 | 1994-11-15 | Hoechst-Roussel Pharmaceuticals, Inc. | Heteroarylpiperidines, pyrrolidines and piperazines and their use as antipsychotics and analetics |
| US7029694B2 (en) | 2000-04-26 | 2006-04-18 | Watson Laboratories, Inc. | Compositions and methods for transdermal oxybutynin therapy |
| WO2003020707A1 (en) | 2001-08-31 | 2003-03-13 | Novartis Ag | Optical isomers of an iloperidone metabolite |
| US20050059006A1 (en) | 2001-12-10 | 2005-03-17 | Sridhar Kudaravalli | Methods of treating psychosis and schizophrenia based on polymorphisms in the cntf gene |
| TW200410955A (en) | 2002-07-29 | 2004-07-01 | Altana Pharma Ag | Novel salt of (S)-PANTOPRAZOLE |
| GB0322994D0 (en) * | 2003-10-01 | 2003-11-05 | Novartis Ag | Organic compounds |
| WO2006039663A2 (en) | 2004-09-30 | 2006-04-13 | Vanda Pharmaceuticals, Inc | Methods for the administration of iloperidone |
| US20100063093A1 (en) * | 2007-03-28 | 2010-03-11 | Curt Wolfgang | Methods for the administration of iloperidone |
| AU2007253684A1 (en) * | 2006-05-22 | 2007-11-29 | Vanda Pharmaceuticals, Inc. | Treatment for depressive disorders |
| WO2008121899A2 (en) | 2007-03-29 | 2008-10-09 | Vanda Pharmaceuticals Inc. | Method of predicting a predisposition to qt prolongation |
| WO2009036100A2 (en) | 2007-09-10 | 2009-03-19 | Vanda Pharmaceuticals, Inc. | Prediction of qt prolongation based on snp genotype |
| US9328387B2 (en) | 2007-09-10 | 2016-05-03 | Vanda Pharmaceuticals, Inc. | Antipsychotic treatment based on SNP genotype |
| EP2416779B1 (en) | 2009-04-06 | 2016-03-09 | Vanda Pharmaceuticals Inc. | Method of predicting a predisposition to qt prolongation based on bai3 gene sequence or product thereof |
| CA2757717C (en) | 2009-04-06 | 2018-09-04 | Vanda Pharmaceuticals, Inc. | Method of predicting a predisposition to qt prolongation |
| EP2416778B1 (en) | 2009-04-06 | 2016-03-02 | Vanda Pharmaceuticals Inc. | Method of predicting a predisposition to qt prolongation based on abcc2 gene sequence or product thereof |
| HUE037724T2 (hu) | 2009-04-06 | 2018-09-28 | Vanda Pharmaceuticals Inc | Eljárás a KCNQ1 gén polimorfizmusán alapuló kezelésre |
| EP2430183B1 (en) | 2009-05-15 | 2014-12-17 | Vanda Pharmaceuticals Inc. | Antipsychotic treatment based on drd2 or ankk1 snp genotype |
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