"(Reuters) - Sanofi SA and Regeneron Pharmaceuticals Inc on Friday said U.S. regulators had declined to approve their experimental treatment for rheumatoid arthritis because of manufacturing deficiencies.
The companies, in a release, s"...
SERIOUS INFECTIONS AND MALIGNANCY
Patients treated with XELJANZ/XELJANZ XR are at increased risk for developing serious infections that may lead to hospitalization or death [see WARNINGS AND PRECAUTIONS and ADVERSE REACTIONS]. Most patients who developed these infections were taking concomitant immunosuppressants such as methotrexate or corticosteroids.
If a serious infection develops, interrupt XELJANZ/XELJANZ XR until the infection is controlled.
Reported infections include:
- Active tuberculosis, which may present with pulmonary or extrapulmonary disease. Patients should be tested for latent tuberculosis before XELJANZ/XELJANZ XR use and during therapy. Treatment for latent infection should be initiated prior to XELJANZ/XELJANZ XR use.
- Invasive fungal infections, including cryptococcosis and pneumocystosis. Patients with invasive fungal infections may present with disseminated, rather than localized, disease.
- Bacterial, viral, and other infections due to opportunistic pathogens.
The risks and benefits of treatment with XELJANZ/XELJANZ XR should be carefully considered prior to initiating therapy in patients with chronic or recurrent infection.
Patients should be closely monitored for the development of signs and symptoms of infection during and after treatment with XELJANZ/XELJANZ XR, including the possible development of tuberculosis in patients who tested negative for latent tuberculosis infection prior to initiating therapy [see WARNINGS AND PRECAUTIONS].
Lymphoma and other malignancies have been observed in patients treated with XELJANZ. Epstein Barr Virus-associated post-transplant lymphoproliferative disorder has been observed at an increased rate in renal transplant patients treated with XELJANZ and concomitant immunosuppressive medications [see WARNINGS AND PRECAUTIONS].
XELJANZ/XELJANZ XR 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 5 mg tofacitinib (equivalent to 8 mg tofacitinib citrate) white round, immediate-release film-coated tablet. Each tablet of XELJANZ contains the appropriate amount of tofacitinib as a citrate salt and the following inactive ingredients: microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate, HPMC 2910/Hypromellose 6cP, titanium dioxide, macrogol/PEG3350, and triacetin.
XELJANZ XR is supplied for oral administration as 11 mg tofacitinib (equivalent to 17.77 mg tofacitinib citrate) pink, oval, extended release film-coated tablet with a drilled hole at one end of the tablet band. Each tablet of XELJANZ XR contains the appropriate amount of tofacitinib as a citrate salt and the following inactive ingredients: sorbitol, hydroxyethyl cellulose, copovidone, magnesium stearate, cellulose acetate, hydroxypropyl cellulose, HPMC 2910/Hypromellose, titanium dioxide, triacetin, and red iron oxide. Printing ink contains shellac glaze, ammonium hydroxide, propylene glycol, and ferrosoferric oxide/black iron oxide.
What are the possible side effects of tofacitinib (Xeljanz)?
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.
Serious and sometimes fatal infections may occur during treatment with tofacitinib. Stop using this medicine and call your doctor right away if you have signs of infection such as:
- fever, chills, tired feeling, night sweats;
- stomach pain, loss of appetite, diarrhea, weight loss, or a change in your bowel habits;
- pain or burning when you urinate;
- body aches, sore throat, flu...
Last reviewed on RxList: 3/7/2016
This monograph has been modified to include the generic and brand name in many instances.
Additional Xeljanz Information
Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.
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