MX2022014923A - Administracion concomitante del modulador del receptor de glucocorticoides relacorilant y sustratos cyp2c9. - Google Patents
Administracion concomitante del modulador del receptor de glucocorticoides relacorilant y sustratos cyp2c9.Info
- Publication number
- MX2022014923A MX2022014923A MX2022014923A MX2022014923A MX2022014923A MX 2022014923 A MX2022014923 A MX 2022014923A MX 2022014923 A MX2022014923 A MX 2022014923A MX 2022014923 A MX2022014923 A MX 2022014923A MX 2022014923 A MX2022014923 A MX 2022014923A
- Authority
- MX
- Mexico
- Prior art keywords
- relacorilant
- cyp2c9
- administered
- substrate
- doses
- Prior art date
Links
- 102000002269 Cytochrome P-450 CYP2C9 Human genes 0.000 title abstract 9
- 108010000543 Cytochrome P-450 CYP2C9 Proteins 0.000 title abstract 9
- WANIDIGFXJFFEL-SANMLTNESA-N [(4ar)-1-(4-fluorophenyl)-6-(1-methylpyrazol-4-yl)sulfonyl-4,5,7,8-tetrahydropyrazolo[3,4-g]isoquinolin-4a-yl]-[4-(trifluoromethyl)pyridin-2-yl]methanone Chemical compound C1=NN(C)C=C1S(=O)(=O)N1C[C@@]2(C(=O)C=3N=CC=C(C=3)C(F)(F)F)CC(C=NN3C=4C=CC(F)=CC=4)=C3C=C2CC1 WANIDIGFXJFFEL-SANMLTNESA-N 0.000 title abstract 8
- 229940070103 relacorilant Drugs 0.000 title abstract 8
- 239000000758 substrate Substances 0.000 title abstract 7
- 229940117965 Glucocorticoid receptor modulator Drugs 0.000 title 1
- 208000014311 Cushing syndrome Diseases 0.000 abstract 3
- 208000037171 Hypercorticoidism Diseases 0.000 abstract 3
- 206010028980 Neoplasm Diseases 0.000 abstract 3
- 201000005255 adrenal gland hyperfunction Diseases 0.000 abstract 3
- 201000011510 cancer Diseases 0.000 abstract 3
- JLRGJRBPOGGCBT-UHFFFAOYSA-N Tolbutamide Chemical compound CCCCNC(=O)NS(=O)(=O)C1=CC=C(C)C=C1 JLRGJRBPOGGCBT-UHFFFAOYSA-N 0.000 abstract 2
- WIGIZIANZCJQQY-RUCARUNLSA-N glimepiride Chemical compound O=C1C(CC)=C(C)CN1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)N[C@@H]2CC[C@@H](C)CC2)C=C1 WIGIZIANZCJQQY-RUCARUNLSA-N 0.000 abstract 2
- 229960004346 glimepiride Drugs 0.000 abstract 2
- ZJJXGWJIGJFDTL-UHFFFAOYSA-N glipizide Chemical compound C1=NC(C)=CN=C1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)NC2CCCCC2)C=C1 ZJJXGWJIGJFDTL-UHFFFAOYSA-N 0.000 abstract 2
- 229960001381 glipizide Drugs 0.000 abstract 2
- 229960005371 tolbutamide Drugs 0.000 abstract 2
- 238000011260 co-administration Methods 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 230000009467 reduction Effects 0.000 abstract 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
-
- 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
- A61K31/64—Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
- A61P5/08—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
El relacorilant es útil en el tratamiento contra el hipercortisolismo y cáncer. Diversos fármacos útiles para el tratamiento contra el hipercortisolismo o el cáncer son metabolizados por enzimas CYP2C9. En la presente se describen los efectos de la administración concomitante de relacorilant y un sustrato de CYP2C9. El relacorilant inhibió potentemente a CYP2C9 en una prueba in vitro, lo que indica que se espera que la administración conjunta de relacorilant y un sustrato de CYP2C9 aumente la exposición plasmática del sustrato de CYP2C9 más de cinco veces in vivo. Se espera que se requieran reducciones significativas en las dosis de sustrato de CYP2C9 cuando se administra con relacorilant. De manera inesperada, no se observó tal aumento en la exposición plasmática en estudios en humanos. El solicitante describe que relacorilant puede ser coadministrable de forma segura con dosis no modificadas de un sustrato de CYP2C9 tal como, por ejemplo, tolbutamida, glimepirida y glipizida. Pueden ser administrables conjuntamente el relacorilant y dosis no modificadas del sustrato de CYP2C9 tal como tolbutamida, glimepirida y glipizida para tratar el hipercortisolismo, o puede ser coadministrable a un paciente oncológico.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063030809P | 2020-05-27 | 2020-05-27 | |
| PCT/US2021/034338 WO2021242916A1 (en) | 2020-05-27 | 2021-05-26 | Concomitant administration of glucocorticoid receptor modulator relacorilant and cyp2c9 substrates |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2022014923A true MX2022014923A (es) | 2023-01-04 |
Family
ID=78707285
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2022014923A MX2022014923A (es) | 2020-05-27 | 2021-05-26 | Administracion concomitante del modulador del receptor de glucocorticoides relacorilant y sustratos cyp2c9. |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20210369689A1 (es) |
| EP (1) | EP4157274A4 (es) |
| JP (1) | JP7536119B2 (es) |
| KR (1) | KR20230016661A (es) |
| CN (1) | CN115916202A (es) |
| AU (1) | AU2021279006A1 (es) |
| CA (1) | CA3178771A1 (es) |
| IL (1) | IL298150A (es) |
| MX (1) | MX2022014923A (es) |
| WO (1) | WO2021242916A1 (es) |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1408966E (pt) * | 2001-07-17 | 2008-05-02 | N Gene Res Lab Inc | Combinações farmacêuticas sinergísticas para a prevenção ou tratamento da diabetes |
| IL309712A (en) | 2015-05-18 | 2024-02-01 | Corcept Therapeutics Inc | Methods for diagnosing and determining treatment for Cushing's syndrome |
| KR20180116372A (ko) * | 2016-03-01 | 2018-10-24 | 코어셉트 쎄라퓨틱스, 잉크. | 체크포인트 억제제를 강화시키기 위한 글루코코르티코이드 수용체 조정제의 용도 |
| US9943505B2 (en) | 2016-09-09 | 2018-04-17 | Corcept Therapeutics, Inc. | Glucocorticoid receptor modulators to treat pancreatic cancer |
| US10195214B2 (en) * | 2017-03-01 | 2019-02-05 | Corcept Therapeutics, Inc. | Concomitant administration of glucocorticoid receptor modulators and CYP3A inhibitors |
| JP7563882B2 (ja) | 2017-03-31 | 2024-10-08 | コーセプト セラピューティクス， インコーポレイテッド | 子宮頸がんを処置するためのグルココルチコイドレセプターモジュレーター |
| WO2019078920A1 (en) * | 2017-10-16 | 2019-04-25 | Aragon Pharmaceuticals, Inc. | ANTI-ANDROGENS FOR THE TREATMENT OF NON-METASTATIC RESISTANT PROSTATE CANCER |
| SG11202104732UA (en) * | 2018-11-09 | 2021-06-29 | Corcept Therapeutics Inc | Methods for shrinking pituitary tumors |
| MX2021007322A (es) * | 2018-12-19 | 2021-07-07 | Corcept Therapeutics Inc | Formulaciones farmaceuticas que contienen relacorilant, un compuesto de azadecalina fusionado con heteroaril-cetona. |
| US11058670B2 (en) * | 2019-02-22 | 2021-07-13 | Corcept Therapeutics Incorporated | Therapeutic uses of relacorilant, a heteroaryl-ketone fused azadecalin glucocorticoid receptor modulator |
-
2021
- 2021-05-26 MX MX2022014923A patent/MX2022014923A/es unknown
- 2021-05-26 CN CN202180038804.9A patent/CN115916202A/zh active Pending
- 2021-05-26 EP EP21812189.5A patent/EP4157274A4/en active Pending
- 2021-05-26 KR KR1020227045414A patent/KR20230016661A/ko active Search and Examination
- 2021-05-26 AU AU2021279006A patent/AU2021279006A1/en active Pending
- 2021-05-26 US US17/330,987 patent/US20210369689A1/en active Pending
- 2021-05-26 WO PCT/US2021/034338 patent/WO2021242916A1/en unknown
- 2021-05-26 IL IL298150A patent/IL298150A/en unknown
- 2021-05-26 CA CA3178771A patent/CA3178771A1/en active Pending
- 2021-05-26 JP JP2022573335A patent/JP7536119B2/ja active Active
Also Published As
| Publication number | Publication date |
|---|---|
| JP7536119B2 (ja) | 2024-08-19 |
| CA3178771A1 (en) | 2021-12-02 |
| EP4157274A1 (en) | 2023-04-05 |
| IL298150A (en) | 2023-01-01 |
| CN115916202A (zh) | 2023-04-04 |
| WO2021242916A1 (en) | 2021-12-02 |
| AU2021279006A1 (en) | 2022-12-15 |
| EP4157274A4 (en) | 2024-06-12 |
| US20210369689A1 (en) | 2021-12-02 |
| KR20230016661A (ko) | 2023-02-02 |
| JP2023532840A (ja) | 2023-08-01 |
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