Elacestrant dihydrochloride

China [CN]

I. Basic Information

Item | Details

English Name | (R)-6-(2-(Ethyl(4-(2-(ethylamino)ethyl)benzyl)amino)-4-methoxyphenyl)-5,6,7,8-tetrahydronaphthalen-2-ol dihydrochloride

Chinese Name | (R)-6-(2-(Ethyl(4-(2-(ethylamino)ethyl)benzyl)amino)-4-methoxyphenyl)-5,6,7,8-tetrahydronaphthalen-2-ol dihydrochloride (Elacestrant Hydrochloride)

CAS Number | 1349723-93-8

Molecular Formula | C₃₀H₄₀Cl₂N₂O₂ (C₃₀H₃₈N₂O₂·2HCl) FDA Access Data

Molecular Weight | 531.56 FDA Access Data

Target | ERα (IC₅₀=48 nM), ERβ (IC₅₀=870 nM), highly selective degradation of ERα

Development/Marketing | Developed by Radius Health, approved by FDA in 2023; globally commercialized by Menarini

Dosage Form and Strength | Film-coated tablets: 86 mg (containing 100 mg dihydrochloride), 345 mg (containing 400 mg dihydrochloride) FDA Access Data

II. Physicochemical Properties

Parameter | Data

Appearance | White to off-white to gray solid FDA Access Data

Solubility | pH-dependent: readily soluble in 0.01N HCl (approximately 52 mg/mL), only 0.01 mg/mL at pH 6.8

Chirality | Single R configuration, optical purity >99.5%

Partition Coefficient (logP) | Free base: 5.2 (predicted value); Dihydrochloride: 2.8 (pH 2.0, predicted value)

Stability | Stable for 36 months at 25℃/60% RH, store in a sealed, cool, and dry place, avoid strong light/high temperature FDA Access Data

BCS Classification | Class II (high permeability, pH-dependent low solubility)