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cyproterone acetate + medroxyprogesterone acetate + venlafaxine

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intramuscular, Subcutaneous
01

Overview

A three-drug combination of the steroidal antiandrogen/progestin cyproterone acetate, the progestin medroxyprogesterone acetate, and the serotonin-norepinephrine reuptake inhibitor venlafaxine. It has been investigated as pharmacologic management of androgen-deprivation therapy–associated vasomotor hot flushes in men with prostate cancer, with randomized trial evidence comparing each component separately showing that cyproterone acetate and medroxyprogesterone acetate reduce hot-flush scores more than venlafaxine over 1 month, though all three are effective. Mechanistically, cyproterone acetate suppresses androgen activity via androgen receptor antagonism and antigonadotropic effects; medroxyprogesterone acetate exerts progestogenic negative feedback to reduce hot flushes; venlafaxine reduces hot flushes via central monoamine reuptake inhibition affecting thermoregulatory control.[3][5][2][4][7]

Other names
CPA + MPA + venlafaxinecyproterone + medroxyprogesterone + venlafaxine
02

Targets

NET (Norepinephrine Transporter)PR (Progesterone receptor)SERT (Sodium-dependent serotonin transporter)AR (Adrenergic receptors)

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