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    CONCOMITANT ADMINISTRATION OF GLUCOCORTICOID RECEPTOR MODULATOR RELACORILANT AND CYP2C8 SUBSTRATES
    64.
    发明申请
    CONCOMITANT ADMINISTRATION OF GLUCOCORTICOID RECEPTOR MODULATOR RELACORILANT AND CYP2C8 SUBSTRATES 有权

    公开(公告)号：US20210369690A1

    公开(公告)日：2021-12-02

    申请号：US17331032

    申请日：2021-05-26

    Applicant: Corcept Therapeutics Incorporated

    Inventor： Hazel Hunt ,  Joseph Custodio

    IPC: A61K31/444 ,  A61K31/4439 ,  A61K31/4166

    Abstract: Relacorilant is useful in the treatment of cancer and hypercortisolism. Many drugs useful in treating cancer or hypercortisolism are metabolized by CYP2C8 enzymes. The effects of concomitant administration of relacorilant and a CYP2C8 substrate are disclosed herein.
    Relacorilant potently inhibited CYP2C8 in an in vitro test, indicating that co-administration of relacorilant and a CYP2C8 substrate would be expected to increase the CYP2C8 substrate plasma exposure more than five-fold in vivo. Significant reductions in CYP2C8 substrate doses would be expected to be required when administered with relacorilant.
    Surprisingly, no such increase in plasma exposure was seen in human studies. Applicant discloses that relacorilant may be safely co-administered with unmodified doses of CYP2C8 substrates such as pioglitazone, rosiglitazone, and enzalutamide. Relacorilant and unmodified doses of enzalutamide may be co-administered to treat cancer, e.g., prostate cancer. Relacorilant and unmodified doses of pioglitazone or rosiglitazone may be co-administered to treat cancer or hypercortisolism.

    CONCOMITANT ADMINISTRATION OF GLUCOCORTICOID RECEPTOR MODULATOR RELACORILANT AND CYP2C9 SUBSTRATES
    65.
    发明申请
    CONCOMITANT ADMINISTRATION OF GLUCOCORTICOID RECEPTOR MODULATOR RELACORILANT AND CYP2C9 SUBSTRATES 有权

    公开(公告)号：US20210369689A1

    公开(公告)日：2021-12-02

    申请号：US17330987

    申请日：2021-05-26

    Applicant: Corcept Therapeutics Incorporated

    Inventor： Hazel Hunt ,  Joseph Custodio

    IPC: A61K31/444 ,  A61K31/64 ,  A61K31/337

    Abstract: Relacorilant is useful in the treatment of hypercortisolism and cancer. Many drugs useful in treating hypercortisolism or cancer are metabolized by CYP2C9 enzymes. The effects of concomitant administration of relacorilant and a CYP2C9 substrate are disclosed herein.
    Relacorilant potently inhibited CYP2C9 in an in vitro test, indicating that co-administration of relacorilant and a CYP2C9 substrate would be expected to increase the CYP2C9 substrate plasma exposure more than five-fold in vivo. Significant reductions in CYP2C9 substrate doses would be expected to be required when administered with relacorilant.
    Surprisingly, no such increase in plasma exposure was seen in human studies. Applicant discloses that relacorilant may be safely co-administered with unmodified doses of a CYP2C9 substrate such as, e.g., tolbutamide, glimepiride, and glipizide. Relacorilant and unmodified doses of CYP2C9 substrate such as tolbutamide, glimepiride, and glipizide may be co-administered to treat hypercortisolism, or may be co-administered to a cancer patient.

    METHODS FOR SHRINKING PITUITARY TUMORS
    66.
    发明申请
    METHODS FOR SHRINKING PITUITARY TUMORS 有权

    公开(公告)号：US20210177817A1

    公开(公告)日：2021-06-17

    申请号：US17185133

    申请日：2021-02-25

    Applicant: Corcept Therapeutics Incorporated

    Inventor： Andreas Moraitis

    IPC: A61K31/444 ,  A61P35/00

    Abstract: Pituitary tumors may be reduced in size by administration of relacorilant. Pituitary tumors include, without limitation, non-secreting tumors, hormone-secreting tumors, adenomas, and carcinomas. Relacorilant administration may be effective to reduce hormone secretion from a hormone-secreting pituitary tumor, e.g., to reduce adrenocorticotrophic hormone (ACTH) secretion. A pituitary tumor may be imaged before and/or after relacorilant administration. Relacorilant may be administered independent of surgery, and before, during, or after surgery to treat a pituitary tumor. Relacorilant may aid or improve surgical outcomes, and may reduce the size or growth of pituitary tumor tissue before surgery, and any tumor tissue remaining following surgical treatment.
    Relacorilant may be orally administered for the treatment of pituitary tumors. Relacorilant may be orally administered to a fasted patient, or to a fed patient. Relacorilant may be administered in conjunction with other pituitary tumor targeting treatments, including surgical treatments, radiation treatments, chemotherapy for carcinomas, and other pharmaceutical treatments.

    Therapeutic Uses of Relacorilant, a Heteroaryl-ketone Fused Azadecalin Glucocorticoid Receptor Modulator
    67.
    发明申请
    Therapeutic Uses of Relacorilant, a Heteroaryl-ketone Fused Azadecalin Glucocorticoid Receptor Modulator 审中-公开

    公开(公告)号：US20200268723A1

    公开(公告)日：2020-08-27

    申请号：US16797421

    申请日：2020-02-21

    Applicant: Corcept Therapeutics Incorporated

    Inventor： Andreas Moraitis

    IPC: A61K31/437 ,  A61P5/44

    Abstract: Methods and compositions are disclosed for diagnosing a patient suspected of suffering from, and for treating a patient suffering from, a disorder such as hypercortisolemia, metabolic syndrome, pre-diabetes, diabetes, Cushing's syndrome, Cushing's Disease, hyperglycemia secondary to hypercortisolemia, a liver disease, a cardiac disorder, high blood pressure, a blood clotting disorder, a cancer, a psychological disorder, weight gain, a disorder of glucose control, a bone disorder (e.g., osteoporosis), hypogonadism, pseudoacromegaly, pituitary tumors, functional hypercortisolism, ACTH secreting tumors, peripheral neuropathy, dyslipidemia and other disorders.The methods and compositions include administration of a heteroaryl-ketone fused azadecalin glucocorticoid receptor modulator (GRM). The preferred heteroaryl-ketone fused azadecalin GRM is relacorilant ((R)-(1-(4-fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone). In some cases, the GRM (e.g., relacorilant) is orally administered. In some cases, the GRM (e.g., relacorilant) is orally administered without food.

    Intermittent Dosing of Glucocorticoid Receptor Modulators for the Treatment of Ovarian and Other Cancers
    69.
    发明申请
    Intermittent Dosing of Glucocorticoid Receptor Modulators for the Treatment of Ovarian and Other Cancers 有权

    公开(公告)号：US20250041432A1

    公开(公告)日：2025-02-06

    申请号：US18797328

    申请日：2024-08-07

    Applicant: Corcept Therapeutics Incorporated

    Inventor： Stacie Shepherd ,  Joseph K. Belanoff

    IPC: A61K47/64 ,  A61K31/337 ,  A61K31/4745 ,  A61P15/00 ,  A61P35/00

    Abstract: Methods and compositions for treating cancer (e.g., ovarian, fallopian tube, uterine, cervical, vaginal, vulvar, or peritoneal cancer) are disclosed. The methods include intermittent administration of a glucocorticoid receptor modulator (GRM), such as a non-steroidal GRM (e.g., relacorilant), which may be orally administered, along with a cancer chemotherapy agent (such as, e.g., bevacizumab) to the patient. The GRM may be administered: at intervals separated by at least one day without GRM administration; by a schedule linked to the cancer chemotherapy schedule (e.g., a weekly chemotherapy regimen); the day of, or the day before, or the day after, chemotherapy administration; by combinations thereof; and/or on other days. Ovarian cancer patients receiving intermittent relacorilant administration along with nab-paclitaxel administration had improved overall survival, improved progression free survival, improved duration of response, and other benefits as compared to patients not receiving relacorilant while receiving nab-paclitaxel.

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