Tofacitinib

Tofacitinib tablets are Janus kinase (JAK) inhibitors. Tofacitinib tablets are indicated for the treatment of adult patients with: Moderately to severely active rheumatoid arthritis (RA), who have had an inadequate response or intolerance to one or more TNF blockers. Active psoriatic arthritis (PsA), who have had an inadequate response or intolerance to one or more TNF blockers. Active ankylosing spondylitis (AS), who have had an inadequate response or intolerance to one or more TNF blockers. Moderately to severely active ulcerative colitis (UC), who have had an inadequate response or intolerance to one or more TNF blockers. …

• Recommended Evaluations and Immunization Prior to Treatment Initiation Prior to initiating tofacitinib tablets, consider performing an active and latent TB evaluation, viral hepatitis screening, a complete blood count, and updating immunizations
• Avoid tofacitinib tablets initiation if absolute lymphocyte count

Tofacitinib tablets: 5 mg tofacitinib: White to off white colored, round shaped, biconvex, film-coated tablets, debossed with “T1” on one side and “M” on other side. 10 mg tofacitinib: Blue colored, round shaped, biconvex, film-coated tablets, debossed with “T2” on one side and “M” on other side. Tofacitinib tablets: 5 mg, 10 mg ( 3 )

• The safety and effectiveness of tofacitinib tablets
• In pediatric patients for indications, other than in patients with active pcJIA and PsA, have not been established
• The safety and effectiveness of tofacitinib tablets have not been established
• In pediatric patients less than 2 years of age
• Polyarticular Course Juvenile Idiopathic Arthritis (pcJIA) The safety and effectiveness of tofacitinib tablets
• For the treatment of active pcJIA have been established
• In pediatric patients 2 years of age and older who have had an inadequate response or intolerance to one or more TNF blockers. …

Of the 3315 adults who were enrolled in clinical trials with RA (Studies RA- I to V), a total of 505 patients were 65 years of age and older, including 71 patients 75 years and older. The frequency of serious infection among tofacitinib tablets-treated patients 65 years of age and older was higher than among those adults under the age of 65. …

• Advise patients to read the FDA-approved patient labeling (Medication Guide)
• Serious Infections Inform patients that tofacitinib tablets may lower the ability of their immune system to fight infections
• Advise patients not to start taking tofacitinib tablets if they have an active infection
• Instruct patients to contact their healthcare provider immediately during treatment if symptoms suggesting infection appear to ensure rapid evaluation and appropriate treatment [see Warnings and Precautions ]
• Advise patients that the risk of herpes zoster, some cases of which can be serious, is increased in patients treated with tofacitinib tablets [see Warnings and Precautions ]. …

• None
• None

Table 7 includes drugs with clinically significant drug interactions when concomitantly used with tofacitinib tablets and instructions for preventing or managing them. Table 7: Clinically Significant Interactions Affecting Tofacitinib Tablets When Concomitantly Used with Other Drugs Strong CYP3A4 Inhibitors (e.g., ketoconazole) Clinical Impact Increased exposure to tofacitinib I ntervention Dosage modification of tofacitinib tablets is recommended [see Dosage and Administration (2 ), Clinical Pharmacology, Figure 3 (12.3 )] Mo derate CYP3A4 Inhibitors Concomitantly Used with Strong CYP2C19 Inhibitors (e.g., fluconazole) Clinical Impact Increased exposure to tofacitinib I ntervention Dosage m …

Serious Infections: Avoid use of tofacitinib tablets during an active serious infection, including localized infections. ( 5.1 ) Gastrointestinal Perforations: Promptly evaluate patients at increased risk for gastrointestinal perforation who present with new onset abdominal symptoms. ( 5.6 ) Hypoglycemia in Patients with Diabetes: Consider increased monitoring of blood glucose; advise patients with diabetes to notify their healthcare provider if they develop signs or symptoms of hypoglycemia. ( 5.8 ) Laboratory Monitoring: Recommended due to potential changes in lymphocytes, neutrophils, hemoglobin, liver enzymes and lipids. …

The following clinically significant adverse reactions are described elsewhere in the labeling: Serious Infections [see Warnings and Precautions (5.1) ] Increased Risk of 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 Reactions [see Warnings and Precautions (5.7) ] Hypoglycemia in Patients with Diabetes [ see Warnings and Precautions (5.8) ] Laboratory Abnormalities [ see Warnings and Precautions (5.9) ] …

8.1 Pregnancy Risk Summary The available data with tofacitinib tablets from a pregnancy exposure registry that enrolled 11 exposed pregnant females, pharmacovigilance, and published literature are insufficient to draw conclusions about a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. …

There is no specific antidote for overdose with tofacitinib tablets. In case of an overdose, it is recommended that the patient be monitored for signs and symptoms of adverse reactions. In a study in patients with end-stage renal disease (ESRD) undergoing hemodialysis, plasma tofacitinib concentrations declined more rapidly during the period of hemodialysis and dialyzer efficiency, calculated as dialyzer clearance/blood flow entering the dialyzer, was high [mean (SD) = 0.73 (0.15)]. …

Take it when you remember, unless it is nearly time for the next dose. Then skip the missed one. Never take two doses at once to make up for it. Check your leaflet, as some medicines are different.