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eltanexor + abiraterone + corticosteroids
- Development stage
- Unknown
- Lead developer
- Karyopharm Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Eltanexor + abiraterone + corticosteroids is an investigational combination regimen studied primarily in metastatic castration-resistant prostate cancer (mCRPC). Eltanexor is a second-generation, orally bioavailable selective inhibitor of nuclear export (SINE) compound that blocks exportin-1 (XPO1)-mediated nuclear export, leading to restoration of tumor suppressor protein function. Abiraterone is a selective, irreversible inhibitor of CYP17 (17α-hydroxylase/C17,20-lyase), causing androgen depletion. Corticosteroids, typically prednisone or prednisolone, mitigate the side effects of abiraterone-induced mineralocorticoid excess and may reduce constitutional adverse events from eltanexor. This combination is given orally, and has been studied in heavily pre-treated mCRPC patient cohorts. Initial studies suggest that corticosteroids may improve the tolerability of the regimen, and the combination warrants further investigation. The drugs act through synergistic antineoplastic and hormonal mechanisms targeting prostate cancer with resistance to conventional therapies[1][2][3][4].
- Other names
- eltanexor + abiraterone + corticosteroids
02
Targets
GR (Glucocorticoid receptor)XPO1 (Exportin-1)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)AR (Adrenergic receptors)
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