Luhan Pharmachem Co., Ltd.

What is Tofacitinib citrate?

Tofacitinib is a drug discovered and developed by Pfizer. It is currently approved for the treatment of rheumatoid arthritis (RA) in the United States and is being studied for treatment of psoriasis, diagnosis inflammatory bowel disease, and other immunological diseases, as well as for the prevention of organ transplant rejection.

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)-?-oxo-1-piperidinepropanenitrile, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) . It is freely soluble in water.

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.

Tofacitinib citrate Drug Interactions

Potent CYP3A4 Inhibitors

Tofacitinib exposure is increased when Tofacitinib is coadministered with potent inhibitors of cytochrome P450 (CYP) 3A4 (e.g., ketoconazole).

Moderate CYP3A4 and Potent CYP2C19 Inhibitors

Tofacitinib exposure is increased when Tofacitinib is coadministered with medications that result in both moderate inhibition of CYP3A4 and potent inhibition of CYP2C19 (e.g., fluconazole).

Potent CYP3A4 Inducers

Tofacitinib exposure is decreased when Tofacitinib is coadministered with potent CYP3A4 inducers (e.g., rifampin).

Immunosuppressive Drugs

There is a risk of added immunosuppression when Tofacitinib is coadministered with potent immunosuppressive drugs (e.g., azathioprine, tacrolimus, cyclosporine). Combined use of multiple-dose Tofacitinib with potent immunosuppressives has not been studied in rheumatoid arthritis.

Precautions before using Tofacitinib citrate

Serious Infections – Do not administer Tofacitinib during an active infection, including localized infections. If a serious infection develops, interrupt Tofacitinib until the infection is controlled.

Lymphomas and other malignancies have been reported in patients treated with Tofacitinib.

Gastrointestinal Perforations – Use with caution in patients that may be at increased risk.

Laboratory monitoring – Recommended due to potential changes in lymphocytes, neutrophils, hemoglobin, liver enzymes and lipids.

Immunizations – Live vaccines should not be given concurrently with Tofacitinib.

Severe hepatic impairment – Not recommended

Tofacitinib citrate Side effects

The most commonly reported adverse reactions during the first 3 months in controlled clinical trials (occurring in greater than or equal to 2% of patients treated with Tofacitinib monotherapy or in combination with DMARDs) were upper respiratory tract infections, headache, diarrhea and nasopharyngitis.

Tofacitinib citrate Storage

Store at 20°C to 25°C (68°F to 77°F). [See USP Controlled Room Temperature].Do not repackage.

Disclaimer:

Information on this page is provided for general information purposes. You should not make a clinical treatment decision based on information contained in this page without consulting other references including the package insert of the drug, textbooks and where relevant, expert opinion. We cannot be held responsible for any errors you make in administering drugs mentioned on this page, nor for use of any erroneous information contained on this page.