relugolix - Medications

MYFEMBREE tablets for oral administration contain a fixed-dose combination of relugolix 40 mg, estradiol 1 mg, and norethindrone acetate 0.5 mg as active ingredients. Relugolix is a non-peptide small molecule, GnRH receptor antagonist. It is a white to off white to slightly yellow solid and is sparingly soluble in water. The chemical name is N-(4-{1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl}phenyl)-N-methoxyurea with the empirical formula of C 29 H 27 F 2 N 7 O 5 S and a molecular weight of 623.63. The structural formula is: Estradiol (E2), an estrogen, is present as the hemihydrate (C 18 H 24 O 2 •½H 2 O) which is a white or almost white crystalline powder. Its chemical name is estra-1, 3, 5 ( 10 )-triene-3, 17β-diol with the empirical formula of C 18 H 24 O 2 and a molecular weight of 272.4. The structural formula is: Norethindrone acetate (NETA), a progestin, is a white or yellowish-white crystalline powder. Its chemical name is 17-Hydroxy-19-nor-17α-pregn-4-en-20-yn-3-one acetate with the empirical formula of C 22 H 28 O 3 and a molecular weight of 340.5. The structural formula is: Each MYFEMBREE (relugolix, estradiol, and norethindrone acetate) film-coated tablet contains the following inactive ingredients: hydroxypropyl cellulose, hypromellose, iron oxide yellow, lactose monohydrate, mannitol, magnesium stearate, sodium starch glycolate, titanium dioxide, and triacetin. Relugolix Structural Formula Estradiol Structural Formula Norethindrone Acetate Structural Formula

Relugolix is a nonpeptide small molecule, GnRH receptor antagonist. The chemical name is N-(4-{1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl}phenyl)-N'-methoxyurea. The molecular weight is 623.63 daltons and the molecular formula is C 29 H 27 F 2 N 7 O 5 S. The structural formula is: Relugolix is a white to off-white to slightly yellow solid with a solubility of 0.04 mg per mL in water at 25°C. ORGOVYX is provided as film-coated tablets for oral administration. Each tablet contains 120 mg of relugolix. The inactive ingredients are mannitol, sodium starch glycolate, hydroxypropyl cellulose, magnesium stearate, hypromellose, titanium dioxide, ferric oxide red, and carnauba wax. Structural Formula