Drug intelligence / Profile preview

dexamethasone + everolimus + exemestane

Development stage
Unknown
Lead developer
Novartis
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral, Topical
01

Overview

This is a combination regimen consisting of dexamethasone, everolimus, and exemestane. Everolimus is an oral mTOR (mechanistic target of rapamycin) inhibitor used in hormone receptor-positive, HER2-negative advanced or metastatic breast cancer. Exemestane is a steroidal aromatase inhibitor that suppresses estrogen production and is used as endocrine therapy in postmenopausal women with breast cancer. Dexamethasone, a synthetic glucocorticoid corticosteroid with anti-inflammatory and immunosuppressive properties, is administered as an oral solution (mouthwash) to prevent or reduce the incidence and severity of stomatitis—a common adverse effect associated with everolimus therapy. This triple regimen has been studied primarily for the management of hormone receptor-positive advanced breast cancer in postmenopausal women who have progressed on prior non-steroidal aromatase inhibitors[1][2][4]. The addition of prophylactic dexamethasone mouthwash to everolimus plus exemestane significantly reduces the rate and severity of stomatitis without compromising efficacy[1][2][4].

02

Targets

GR (Glucocorticoid receptor)Mechanistic target of rapamycin complex 1CYP19A1 (Aromatase)

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