tofacitinib citrate
tofacitinib citrate · by somerset theraps llc
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Overview
Tofacitinib extended-release tablets 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 C 16 H 20 N 6 O•C 6 H 8 O 7 . The chemical structure of tofacitinib citrate is: Tofacitinib extended-release tablets are supplied for oral administration as a 11 mg pink, oval, extended-release film-coated tablets, debossed with “TF” on one side and plain on other side. Each 11 mg tablet of tofacitinib extended-release contains 11 mg tofacitinib (equivalent to 17.77 mg of tofacitinib citrate) and the following inactive ingredients: povidone, hypromellose 2208, magnesium stearate, hydrophobic colloidal silica, lactose monohydrate, polyethylene glycol, polyvinyl alcohol, titanium dioxide, talc, red iron oxide, and yellow iron oxide. structure
How to use
Administration Instructions Tofacitinib extended-release tablets are not interchangeable or substitutable with tofacitinib oral solution. ( 2.1 ) Changes between tofacitinib tablets and tofacitinib extended-release tablets should be made by the healthcare provider. ( 2.1 ) Do not initiate tofacitinib extended-release tablets if absolute lymphocyte count <500 cells/mm 3 , an absolute neutrophil count (ANC) < 1,000 cells/mm 3 or hemoglobin < 9 g/dL. ( 2.1 ) Recommended Dosage Rheumatoid Arthritis Tofacitinib extended-release tablets 11 mg once daily. ( 2.2 ) Psoriatic Arthritis (in combination with nonbiologic DMARDs) Tofacitinib extended-release tablets 11 mg once daily. ( 2.2 ) Ankylosing Spondylitis Tofacitinib extended-release tablets 11 mg once daily. ( 2.2 ) Dosage Adjustment See the full prescribing information for dosage adjustments by indication for patients receiving CYP2C19 and/or CYP3A4 inhibitors; in patients with moderate or severe renal impairment or moderate hepatic impairment; and patients with lymphopenia, neutropenia, or anemia. ( 2.2 , 8.7 , 8.8 ) Use of tofacitinib extended-release tablets in patients with severe hepatic impairment is not recommended in any patient population. ( 2.2 , 8.8 ) 2.1 Important Administration Instructions Tofacitinib extended-release tablets are not interchangeable or substitutable with tofacitinib oral solution. Changes between…
Side effects
The following clinically significant adverse reactions are described elsewhere in the labeling: Serious Infections [see Warnings and Precautions ( 5.1 )] Mortality [see Warnings and Precautions ( 5.2 )] Malignancy and Lymphoproliferative Disorders [see Warnings and Precautions ( 5.3 )] Major Adverse Cardiovascular Events [see Warnings and Precautions ( 5.4 )] Thrombosis [see Warnings and Precautions ( 5.5 )] Gastrointestinal Perforations [see Warnings and Precautions ( 5.6 )] Hypersensitivity [see Warnings and Precautions ( 5.7 )] Laboratory Abnormalities [see Warnings and Precautions ( 5.8 )] Most common adverse reactions are: Rheumatoid Arthritis, Psoriatic Arthritis, and Ankylosing Spondylitis : Reported during the first 3 months in rheumatoid arthritis placebo-controlled clinical trials and occurring in ≥2% of patients treated with tofacitinib monotherapy or in combination with DMARDs: upper respiratory tract infection, nasopharyngitis, diarrhea, and headache. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Ajanta Pharma USA Inc. at 855-664-7744 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not predict the rates…
Warnings
Important safety information
WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS, and THROMBOSIS SERIOUS INFECTIONS Patients treated with tofacitinib extended-release tablets are at increased risk for developing serious infections that may lead to hospitalization or death [see Warnings and Precautions ( 5.1 ), Adverse Reactions ( 6.1 )]. Most patients who developed these infections were taking concomitant immunosuppressants such as methotrexate or corticosteroids. If a serious infection develops, interrupt tofacitinib extended-release tablets 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 tofacitinib extended-release tablets use and during therapy. Treatment for latent infection should be initiated prior to tofacitinib extended-release tablets use. Invasive fungal infections, including cryptococcosis and pneumocystosis. Patients with invasive fungal infections may present with disseminated, rather than localized, disease. Bacterial, viral, including herpes zoster, and other infections due to opportunistic pathogens. The risks and benefits of treatment with tofacitinib extended-release tablets should be carefully considered prior to initiating therapy in patients with chronic or recurrent infection. Patients should be…
Interactions
Table 6 includes drugs with clinically important drug interactions when administered concomitantly with tofacitinib and instructions for preventing or managing them. Table 6: Clinically Relevant Interactions Affecting Tofacitinib When Coadministered with Other Drugs Strong CP3A4 Inhibitors (e.g., ketoconazole) Clinical Impact Increased exposure to tofacitinib Intervention Dosage adjustment of tofacitinib is recommended [see Dosage and Administration ( 2 ), Clinical Pharmacology, Figure 3 ( 12.3 )] Moderate CYP3A4 Inhibitors Coadministered with Strong CYP2C19 Inhibitors (e.g., fluconazole) Clinical Impact Increased exposure to tofacitinib Intervention Dosage adjustment of tofacitinib is recommended [see Dosage and Administration ( 2 ), Clinical Pharmacology, Figure 3 ( 12.3 )] Strong CYP3A4 Inducers (e.g., rifampin) Clinical Impact Decreased exposure to tofacitinib and may result in loss of or reduced clinical response Intervention Coadministration with tofacitinib is not recommended [see Clinical Pharmacology, Figure 3 ( 12.3 )] Immunosuppressive Drugs (e.g., azathioprine, tacrolimus, cyclosporine) Clinical Impact Risk of added immunosuppression; coadministration with biologic DMARDs or potent immunosuppressants has not been studied in patients with rheumatoid arthritis, psoriatic arthritis, or ankylosing spondylitis. Intervention Coadministration with tofacitinib is not…
Drug class
May treat
Dosage forms
TABLET
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Frequently asked questions
- What is Tofacitinib Citrate?
- Tofacitinib extended-release tablets 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 C 16 H 20 N 6 O•C 6 H 8 O 7 . The chemical structure of tofacitinib citrate is: Tofacitinib extended-release tablets are supplied for oral administration as a 11 mg pink, oval, extended-release film-coated tablets, debossed with “TF” on one side and plain on other side. Each 11 mg tablet of tofacitinib extended-release contains 11 mg tofacitinib (equivalent to 17.77 mg of tofacitinib citrate) and the following inactive ingredients: povidone, hypromellose 2208, magnesium stearate, hydrophobic colloidal silica, lactose monohydrate, polyethylene glycol, polyvinyl alcohol, titanium dioxide, talc, red iron oxide, and yellow iron oxide. structure
- What does Tofacitinib Citrate treat?
- Tofacitinib Citrate (Tofacitinib Citrate) is indicated for arthritis, rheumatoid, per its drug-label indications. This is general reference, not medical advice.
Clinical content sourced from the FDA label via openFDA (U.S. FDA). Provided for general reference only — not medical advice. Always consult a licensed professional and the current prescribing information.
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