Drug intelligence / Profile preview

prasterone sulfate

Development stage
Approved
Lead developer
Cosette Pharmaceuticals
Modality
Small Molecules
Administration
Intravenous
01

Overview

Prasterone sulfate, also known as dehydroepiandrosterone sulfate (DHEA-S), is a naturally occurring androstane steroid and the C3β-sulfate ester of prasterone (dehydroepiandrosterone; DHEA). It is marketed in Japan, Italy, Portugal, Argentina, and China under various brand names for use primarily as a labor inducer to treat insufficient cervical ripening and dilation during childbirth. Prasterone sulfate acts as a prohormone for DHEA and subsequently for both androgenic and estrogenic steroids. It also has intrinsic activity as a neurosteroid. Medically, it is administered via injection in the form of its sodium salt. Mechanistically, it serves as a precursor to more potent sex steroids through tissue-specific metabolism; it can be converted into androstenedione by 3β-hydroxysteroid dehydrogenase or into androstenediol by 17β-hydroxysteroid dehydrogenase—these metabolites are further transformed into testosterone or estrogens such as estradiol via aromatase. Prasterone/DHEA-S may also exert direct effects on plasma membrane receptors (including G-protein-coupled receptors), neuroreceptors (such as GABA-A, NMDA, sigma receptors), nuclear steroid hormone receptors (androgen receptor/estrogen receptor), peroxisome proliferator–activated receptor alpha (PPARα), constitutive androstane receptor (CAR), voltage-gated T-type calcium channels inhibition, and G-protein-coupled estrogen receptor 1 activation[1][4][5][6].

Brand names
AstenileDastonilDi Luo AnDinistenileLevospaMylisSinsurreneTeloin
Other names
dehydroepiandrosterone sulfate
02

Targets

GABRR (GABA-A receptor subunit rho)Glycine receptorNMDAR (Glutamate receptor ionotropic, NMDA)P2RX1 (Purinergic receptor P2X 1)SIGMAR1 (Sigma non-opioid intracellular receptor 1)TRPC5 (Transient receptor potential Canonical-5)TRPV1 (Transient receptor potential cation channel subfamily V member 1)NTRK1 (Tropomyosin-related receptor kinase A)AR (Adrenergic receptors)CXADR (Coxsackievirus and adenovirus receptor)ER (Estrogen receptor)GPER1 (G protein-coupled estrogen receptor 1)PPARA (Peroxisome proliferator-activated receptor alpha)CaV3 (Caveolin-3)

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