Drug intelligence / Profile preview

conjugated estrogen + fluoxetine

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

Conjugated estrogen + fluoxetine is a combination of two pharmacologically active agents used off-label for the management of menopausal depression and climacteric symptoms. Conjugated estrogens are a mixture of naturally occurring estrogens, primarily estrone sulfate and equilin sulfate, used in hormone replacement therapy (HRT) to alleviate symptoms associated with menopause such as hot flashes, vaginal atrophy, and osteoporosis. Fluoxetine is a selective serotonin reuptake inhibitor (SSRI) antidepressant that increases synaptic serotonin levels by inhibiting its reuptake in the central nervous system. The combination leverages both hormonal modulation (via estrogen receptor agonism) and serotonergic neurotransmission enhancement to address mood disturbances and vasomotor symptoms in menopausal women. Clinical studies suggest that this combination may be more effective than HRT alone for treating depressive symptoms during menopause[2][7].

02

Targets

SERT (Sodium-dependent serotonin transporter)ESR2 (ERβ)ESR1 (ERα)

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