11 DESCRIPTION
XELJANZ/XELJANZ XR (tofacitinib) tablets and XELJANZ (tofacitinib) Oral Solution are formulated with the citrate salt of tofacitinib, a JAK inhibitor.
Tofacitinib citrate is a white to off-white powder with the following chemical name: (3R,4R)-4-methyl-3-(methyl-7H-pyrrolo [2,3-d]pyrimidin-4-ylamino)-ß-oxo-1-piperidinepropanenitrile, 2-hydroxy-1,2,3-propanetricarboxylate (1:1).
The solubility of tofacitinib citrate in water is 2.9 mg/mL.
Tofacitinib citrate has a molecular weight of 504.5 Daltons (or 312.4 Daltons as the tofacitinib free base) and a molecular formula of C16H20N6O∙C6H8O7. The chemical structure of tofacitinib citrate is:
XELJANZ is supplied for oral administration as a 5 mg white round, immediate-release film-coated tablet. Each tablet of XELJANZ contains 5 mg tofacitinib (equivalent to 8.08 mg tofacitinib citrate) and the following inactive ingredients: croscarmellose sodium, HPMC 2910/Hypromellose 6cP, lactose monohydrate, macrogol/PEG3350, magnesium stearate, microcrystalline cellulose, titanium dioxide, and triacetin.
XELJANZ is supplied for oral administration as a 10 mg blue round, immediate-release film-coated tablet. Each 10 mg tablet of XELJANZ contains 10 mg tofacitinib (equivalent to 16.16 mg of tofacitinib citrate) and the following inactive ingredients: croscarmellose sodium, FD&C Blue #1/Brilliant Blue FCF Aluminum Lake, FD&C Blue #2/Indigo Carmine Aluminum Lake, HPMC 2910/Hypromellose 6cP, lactose monohydrate, macrogol/PEG3350, magnesium stearate, microcrystalline cellulose, titanium dioxide, and triacetin.
XELJANZ XR is supplied for oral administration as a 11 mg pink, oval, extended-release film-coated tablet with a drilled hole at one end of the tablet band. Each 11 mg tablet of XELJANZ XR contains 11 mg tofacitinib (equivalent to 17.77 mg tofacitinib citrate) and the following inactive ingredients: cellulose acetate, copovidone, hydroxyethyl cellulose, hydroxypropyl cellulose, HPMC 2910/Hypromellose, magnesium stearate, red iron oxide, sorbitol, titanium dioxide and triacetin. Printing ink contains, ammonium hydroxide, ferrosoferric oxide/black iron oxide, propylene glycol, and shellac glaze.
XELJANZ XR is supplied for oral administration as a 22 mg beige, oval, extended-release film-coated tablet with a drilled hole at one end of the tablet band. Each 22 mg tablet of XELJANZ XR contains 22 mg tofacitinib (equivalent to 35.54 mg tofacitinib citrate) and the following inactive ingredients: cellulose acetate, copovidone, FD&C Blue #2 Aluminum Lake, hydroxyethyl cellulose, hydroxypropyl cellulose, HPMC 2910/Hypromellose, magnesium stearate, red iron oxide, sorbitol, titanium dioxide, triacetin, and yellow iron oxide. Printing ink contains ammonium hydroxide, ferrosoferric oxide/black iron oxide, propylene glycol, and shellac glaze.
XELJANZ Oral Solution is supplied for oral administration as a 1 mg/mL clear, colorless solution. Each 1 mL of XELJANZ Oral Solution contains 1 mg of tofacitinib (equivalent to 1.62 mg tofacitinib citrate) and the following inactive ingredients: grape flavor (natural), hydrochloric acid, lactic acid, purified water, sodium benzoate, sucralose, and xylitol.