ERA-45 is a synthetic estrogen and a selective agonist of the ERα. ^{[1] [2] [3] [4]} It shows 286-fold selectivity for transactivation of the ERα over the ERβ, with EC₅₀ values of 0.37 nM for the ERα (7-fold weaker than estradiol) and 13 nM for the ERβ (20,000-fold weaker than estradiol). ^[1] However, another found only about 35-fold potency for transactivation of the ERα over the ERβ. ^[2] The drug has no antagonistic activity at either receptor. ^[1] ERA-45 induced prostate cancer development in preclinical models when it was given in combination with testosterone, whereas testosterone alone did not do so. ^{[1] [5]} In contrast, the selective ERβ agonist ERB-26 was protective against the development of prostate cancer produced by these two drugs. ^{[1] [5]} These findings suggest opposing roles of the ERα and ERβ in the prostate gland. ^[1] The chemical structure of ERa-45 does not appear to have been disclosed.

See also

• 16α-LE2
• ERA-63
• GTx-758
• Methylpiperidinopyrazole
• Propylpyrazoletriol

References

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