lexicon pharmaceuticals, inc. - Medication Listings

INPEFA tablets for oral administration contain sotagliflozin, a sodium-glucose cotransporter 2 (SGLT2) inhibitor. The chemical name of sotagliflozin is (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-(methylthio)tetrahydro-2H-pyran-3,4,5-triol. Its molecular formula is C 21 H 25 ClO 5 S and the molecular weight is 424.94. The structural formula is: Sotagliflozin is a white to off-white solid. It is practically insoluble in water. Each film-coated tablet of INPEFA contains 200 mg or 400 mg of sotagliflozin and the following inactive ingredients. The core of the tablet contains colloidal silicon dioxide, croscarmellose sodium, magnesium stearate, microcrystalline cellulose, and talc. The film coating for the 200 mg tablet contains: indigo carmine aluminum lake, polyethylene glycol, polyvinyl alcohol (partly hydrolyzed), talc, and titanium dioxide. The film coating for the 400 mg tablet contains: hypromellose, lactose monohydrate, titanium dioxide, triacetin, and yellow iron oxide. The 200 mg printed tablet also includes black ink which contains: ammonium hydroxide, black iron oxide, isopropyl alcohol, N-butyl alcohol, propylene glycol, and shellac. Structural Formula

Xermelo (telotristat ethyl) tablets contain telotristat ethyl as telotristat etiprate, a tryptophan hydroxylase inhibitor. Telotristat etiprate is the hippurate salt of telotristat ethyl [(S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate], which undergoes hydrolysis to the active metabolite, (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid. The molecular formula of telotristat etiprate is C 27 H 26 ClF 3 N 6 O 3 • C 9 H 9 NO 3 and its molecular weight is 754.2. The molecular weight of the free base (telotristat ethyl) is 575.0. Chemical Structure: Telotristat etiprate is a white to off-white solid. The solubility is a function of pH at 25°C; at pH 1 (0.1N HCl), the solubility is greater than 71 mg/mL., at pH 3 phosphate buffer, the solubility is 0.30 mg/mL, at a pH of 5 to 9, the solubility is negligible. In organic solvents, telotristat etiprate is freely soluble in methanol, soluble in acetone, and sparingly soluble in ethanol. Each Xermelo tablet contains 250 mg of telotristat ethyl (free base) which is equivalent to 328 mg telotristat etiprate. The inactive ingredients of Xermelo tablets include: colloidal silicon dioxide, croscarmellose sodium, hydroxypropyl cellulose, lactose anhydrous, macrogol/PEG, magnesium stearate, polyvinyl alcohol [part hydrolyzed], talc and titanium dioxide. Chemical Structure

Xermelo (telotristat ethyl) tablets contain telotristat ethyl as telotristat etiprate, a tryptophan hydroxylase inhibitor. Telotristat etiprate is the hippurate salt of telotristat ethyl [(S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate], which undergoes hydrolysis to the active metabolite, (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid. The molecular formula of telotristat etiprate is C 27 H 26 ClF 3 N 6 O 3 • C 9 H 9 NO 3 and its molecular weight is 754.2. The molecular weight of the free base (telotristat ethyl) is 575.0. Chemical Structure: Telotristat etiprate is a white to off-white solid. The solubility is a function of pH at 25°C; at pH 1 (0.1N HCl), the solubility is greater than 71 mg/mL, at pH 3 phosphate buffer, the solubility is 0.30 mg/mL, at a pH of 5 to 9, the solubility is negligible. In organic solvents, telotristat etiprate is freely soluble in methanol, soluble in acetone, and sparingly soluble in ethanol. Each Xermelo tablet contains 250 mg of telotristat ethyl (free base) which is equivalent to 328 mg telotristat etiprate. The inactive ingredients of Xermelo tablets include: colloidal silicon dioxide, croscarmellose sodium, hydroxypropyl cellulose, lactose anhydrous, macrogol/PEG, magnesium stearate, polyvinyl alcohol [part hydrolyzed], talc and titanium dioxide. Chemical Structure