MX2022014922A - Administracion concomitante del modulador del receptor de glucocorticoides relacorilant y sustratos de cyp2c8. - Google Patents
Administracion concomitante del modulador del receptor de glucocorticoides relacorilant y sustratos de cyp2c8.Info
- Publication number
- MX2022014922A MX2022014922A MX2022014922A MX2022014922A MX2022014922A MX 2022014922 A MX2022014922 A MX 2022014922A MX 2022014922 A MX2022014922 A MX 2022014922A MX 2022014922 A MX2022014922 A MX 2022014922A MX 2022014922 A MX2022014922 A MX 2022014922A
- Authority
- MX
- Mexico
- Prior art keywords
- relacorilant
- cyp2c8
- administered
- doses
- cancer
- Prior art date
Links
- 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 17
- 229940070103 relacorilant Drugs 0.000 title abstract 17
- 102000002263 Cytochrome P-450 CYP2C8 Human genes 0.000 title abstract 15
- 108010000561 Cytochrome P-450 CYP2C8 Proteins 0.000 title abstract 15
- 239000000758 substrate Substances 0.000 title abstract 11
- 229940117965 Glucocorticoid receptor modulator Drugs 0.000 title 1
- 206010028980 Neoplasm Diseases 0.000 abstract 8
- YASAKCUCGLMORW-UHFFFAOYSA-N Rosiglitazone Chemical compound C=1C=CC=NC=1N(C)CCOC(C=C1)=CC=C1CC1SC(=O)NC1=O YASAKCUCGLMORW-UHFFFAOYSA-N 0.000 abstract 8
- 201000011510 cancer Diseases 0.000 abstract 8
- HYAFETHFCAUJAY-UHFFFAOYSA-N pioglitazone Chemical compound N1=CC(CC)=CC=C1CCOC(C=C1)=CC=C1CC1C(=O)NC(=O)S1 HYAFETHFCAUJAY-UHFFFAOYSA-N 0.000 abstract 8
- 208000014311 Cushing syndrome Diseases 0.000 abstract 6
- 208000037171 Hypercorticoidism Diseases 0.000 abstract 6
- 201000005255 adrenal gland hyperfunction Diseases 0.000 abstract 6
- WXCXUHSOUPDCQV-UHFFFAOYSA-N enzalutamide Chemical compound C1=C(F)C(C(=O)NC)=CC=C1N1C(C)(C)C(=O)N(C=2C=C(C(C#N)=CC=2)C(F)(F)F)C1=S WXCXUHSOUPDCQV-UHFFFAOYSA-N 0.000 abstract 4
- 229960004671 enzalutamide Drugs 0.000 abstract 4
- 229960005095 pioglitazone Drugs 0.000 abstract 4
- 229960004586 rosiglitazone Drugs 0.000 abstract 4
- 206010060862 Prostate cancer Diseases 0.000 abstract 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 abstract 2
- 238000011260 co-administration Methods 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 229940079593 drug Drugs 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 238000000338 in vitro Methods 0.000 abstract 2
- 238000001727 in vivo Methods 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 230000009467 reduction Effects 0.000 abstract 2
- 230000008826 genomic mutation 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
- A61K31/395—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
- A61K31/41—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
- A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
-
- 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
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/46—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
-
- 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)
- 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)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
El relacorilant es útil en el tratamiento contra el cáncer y el hipercortisolismo. Diversos fármacos útiles para el tratamiento contra el cáncer o el hipercortisolismo son metabolizados por enzimas CYP2C8. En la presente se describen los efectos de la administración concomitante de relacorilant y un sustrato de CYP2C8. El relacorilant inhibió potentemente a CYP2C8 en una prueba in vitro, lo que indica que se espera que la administración conjunta de relacorilant y un sustrato de CYP2C8 aumente la exposición plasmática del sustrato de CYP2C8 más de cinco veces in vivo. Se espera que se requieran reducciones significativas en las dosis de sustrato de CYP2C8 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 sustratos de CYP2C8 tales como pioglitazona, rosiglitazona y enzalutamida. Pueden ser coadministrados relacorilant y dosis no modificadas de enzalutamida para el tratamiento contra el cáncer, por ejemplo, cáncer de próstata. Pueden ser coadministrados relacorilant y dosis no modificadas de pioglitazona o rosiglitazona para el tratamiento contra el cáncer o el hipercortisolismo.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US202063030789P | 2020-05-27 | 2020-05-27 | |
PCT/US2021/034325 WO2021242905A1 (en) | 2020-05-27 | 2021-05-26 | Concomitant administration of glucocorticoid receptor modulator relacorilant and cyp2c8 substrates |
Publications (1)
Publication Number | Publication Date |
---|---|
MX2022014922A true MX2022014922A (es) | 2023-01-04 |
Family
ID=78707252
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2022014922A MX2022014922A (es) | 2020-05-27 | 2021-05-26 | Administracion concomitante del modulador del receptor de glucocorticoides relacorilant y sustratos de cyp2c8. |
Country Status (10)
Country | Link |
---|---|
US (1) | US20210369690A1 (es) |
EP (1) | EP4157275A4 (es) |
JP (1) | JP7536118B2 (es) |
KR (1) | KR20230017821A (es) |
CN (1) | CN115666573A (es) |
AU (1) | AU2021282256A1 (es) |
CA (1) | CA3178767A1 (es) |
IL (1) | IL298151A (es) |
MX (1) | MX2022014922A (es) |
WO (1) | WO2021242905A1 (es) |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6673823B2 (en) * | 2002-06-04 | 2004-01-06 | Cedars-Sinai Medical Center | Use of peroxisome proliferator activated receptor (PPAR)-γ ligands as a treatment for pituitary tumors and associated conditions, such as Cushing's syndrome |
JP4880671B2 (ja) * | 2005-04-05 | 2012-02-22 | エフ.ホフマン−ラ ロシュ アーゲー | 1H−ピラゾール4−カルボキシルアミドその製造方法および11β−ヒドロキシステロイドデヒドロゲナーゼとしてのその使用 |
US8859774B2 (en) * | 2012-05-25 | 2014-10-14 | Corcept Therapeutics, Inc. | Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators |
CA2984623C (en) | 2015-05-18 | 2023-05-02 | Corcept Therapeutics, Inc. | Methods for diagnosing and assessing treatment for cushing's syndrome |
WO2017120218A1 (en) * | 2016-01-04 | 2017-07-13 | The Regents Of The University Of Colorado, A Body Corporate | Treatment of prostate cancer cells with fat oxidation inhibitors and enzalutamide |
WO2017151613A1 (en) | 2016-03-01 | 2017-09-08 | Corcept Therapeutics, Inc. | The use of glucocorticoid receptor modulators to potentiate checkpoint inhibitors |
US20190134004A1 (en) * | 2016-06-16 | 2019-05-09 | The University Of Chicago | Methods and compositions for treating breast and prostate cancer |
US9943505B2 (en) | 2016-09-09 | 2018-04-17 | Corcept Therapeutics, Inc. | Glucocorticoid receptor modulators to treat pancreatic cancer |
RU2019129299A (ru) | 2017-03-31 | 2021-04-30 | Корсепт Терапьютикс, Инк. | Модуляторы глюкокортикоидного рецептора для лечения рака шейки матки |
EP3609872A1 (en) * | 2017-04-11 | 2020-02-19 | Oric Pharmaceuticals, Inc. | Glucocorticoid receptor modulators |
MX2020003845A (es) * | 2017-10-16 | 2020-11-06 | Aragon Pharmaceuticals Inc | Antiandrógenos para el tratamiento de cáncer de próstata no metastásico resistente a la castración. |
WO2020081329A1 (en) * | 2018-10-18 | 2020-04-23 | Camp4 Therapeutics Corporation | Methods and compositions for modulating pcsk9 and angptl3 expression |
UA125365C2 (uk) * | 2018-11-09 | 2022-02-23 | Корсепт Терапьютікс Інкорпорейтед | Спосіб зменшення розміру видимої пухлини гіпофіза |
US11389432B2 (en) * | 2018-12-19 | 2022-07-19 | Corcept Therapeutics Incorporated | Methods of treating cancer comprising administration of a glucocorticoid receptor modulator and a cancer chemotherapy agent |
IL298149A (en) * | 2020-05-27 | 2023-01-01 | Corcept Therapeutics Inc | Concomitant administration of glucocorticoid receptor modulator relacorilant and paclitaxel, a dual substrate of cyp2c8 and cyp3a4 |
-
2021
- 2021-05-26 WO PCT/US2021/034325 patent/WO2021242905A1/en unknown
- 2021-05-26 JP JP2022573331A patent/JP7536118B2/ja active Active
- 2021-05-26 KR KR1020227045370A patent/KR20230017821A/ko unknown
- 2021-05-26 AU AU2021282256A patent/AU2021282256A1/en active Pending
- 2021-05-26 MX MX2022014922A patent/MX2022014922A/es unknown
- 2021-05-26 IL IL298151A patent/IL298151A/en unknown
- 2021-05-26 EP EP21813099.5A patent/EP4157275A4/en active Pending
- 2021-05-26 US US17/331,032 patent/US20210369690A1/en active Pending
- 2021-05-26 CA CA3178767A patent/CA3178767A1/en active Pending
- 2021-05-26 CN CN202180038805.3A patent/CN115666573A/zh active Pending
Also Published As
Publication number | Publication date |
---|---|
KR20230017821A (ko) | 2023-02-06 |
CA3178767A1 (en) | 2021-12-02 |
JP2023533142A (ja) | 2023-08-02 |
WO2021242905A1 (en) | 2021-12-02 |
CN115666573A (zh) | 2023-01-31 |
IL298151A (en) | 2023-01-01 |
US20210369690A1 (en) | 2021-12-02 |
EP4157275A4 (en) | 2024-06-05 |
EP4157275A1 (en) | 2023-04-05 |
AU2021282256A1 (en) | 2022-12-15 |
JP7536118B2 (ja) | 2024-08-19 |
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