Tofacitinib
Generic Name: tofacitinib
Brand Names:
Xeljanz, Xeljanz Xr
11 DESCRIPTION XELJANZ (tofacitinib) tablets, XELJANZ XR (tofacitinib) extended-release 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.
Overview
11 DESCRIPTION XELJANZ (tofacitinib) tablets, XELJANZ XR (tofacitinib) extended-release 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.
Uses
1 INDICATIONS AND USAGE XELJANZ (tablets and oral solution) and XELJANZ XR (extended-release tablets) are Janus kinase (JAK) inhibitors. XELJANZ tablets and XELJANZ XR 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.
Dosage
2 DOSAGE AND ADMINISTRATION Recommended Evaluations and Immunization Prior to Treatment Initiation • Prior to initiating XELJANZ/XELJANZ XR, consider performing an active and latent TB evaluation, viral hepatitis screening, a complete blood count, and updating immunizations. Avoid XELJANZ or XELJANZ XR initiation if absolute lymphocyte count 80 mL/min (normal renal function); >50 and ≤80 mL/min (mild renal impairment); ≥30 and ≤50 mL/min (moderate renal impairment); 50 and ≤80 mL/min) 5 mg twice daily 11 mg once daily Moderate RI (CLcr ≥30 and ≤50 mL/min) 5 mg once daily XELJANZ tablets 5 mg once daily Severe RI (CLcr 80 mL/min (normal renal function); CLcr >50 and ≤80 mL/min (mild renal impairment); ≥30 and ≤50 mL/min (moderate renal impairment); 50 and ≤80 mL/min) Same as patients with n...
Side Effects
6 ADVERSE REACTIONS 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) ] • Laboratory Abnormalities [see Warnings and Precautions (5.8) ] Most common adverse reactions are: • RA, PsA, and AS : Reported in ≥2% of adult patients treated with XELJANZ tablets monotherapy or in combina...
Interactions
7 DRUG INTERACTIONS Table 7 includes drugs with clinically significant drug interactions when concomitantly used with XELJANZ (tablets and oral solution) and XELJANZ XR (extended-release tablets) and instructions for preventing or managing them. Table 7: Clinically Significant Interactions Affecting XELJANZ/XELJANZ XR When Concomitantly Used with Other Drugs Strong CYP3A4 Inhibitors (e.g., ketoconazole) Clinical Impact Increased exposure to tofacitinib Intervention Dosage modification of XELJANZ/XELJANZ XR is recommended [see Dosage and Administration (2) , Clinical Pharmacology, Figure 3 (12.3) ] Moderate CYP3A4 Inhibitors Concomitantly Used with Strong CYP2C19 Inhibitors (e.g., fluconazole) Clinical Impact Increased exposure to tofacitinib Intervention Dosage modification of XELJANZ/XELJ...
Warnings
WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS, and THROMBOSIS WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS, and THROMBOSIS See full prescribing information for complete boxed warning. • Increased risk of serious bacterial, fungal, viral, and opportunistic infections, including tuberculosis (TB), leading to hospitalization or death. 5 WARNINGS AND PRECAUTIONS • Serious Infections : Avoid use of XELJANZ (tablets and oral solution) and XELJANZ XR (extended-release 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 ) • Laboratory Monitoring : Recommended due to potential changes in lymphocytes, neutrophils, hemoglobin, liver enzymes and lipids. ( 5.8 ) • Vaccinations : Avoid use of live vaccines concurrently with XELJANZ or XELJANZ XR. ( 5.9 ) 5.1 Serious Infections Serious and sometimes fatal infections may occur with XELJANZ (tablets and oral solution) and XELJANZ XR (extended-release tablets). 4 CONTRAINDICATIONS None. None. ( 4 )
Pregnancy
8.1 Pregnancy Risk Summary The available data with XELJANZ (tablets and oral solution) and XELJANZ XR (extended-release 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 are risks to the mother and the fetus associated with RA and UC in pregnancy (see Clinical Considerations ) .
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING How Supplied Information for XELJANZ Tablets and XELJANZ XR How supplied information for XELJANZ tablets and XELJANZ XR (extended-release tablets) is shown in Table 23.
Frequently Asked Questions
What is Tofacitinib used for?▼
1 INDICATIONS AND USAGE XELJANZ (tablets and oral solution) and XELJANZ XR (extended-release tablets) are Janus kinase (JAK) inhibitors. XELJANZ tablets and XELJANZ XR 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.
What are the side effects of Tofacitinib?▼
6 ADVERSE REACTIONS 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) ] • Laboratory Abnormalities [see Warnings and Precautions (5.8) ] Most common adverse reactions are: • RA, PsA, and AS : Reported in ≥2% of adult patients treated with XELJANZ tablets monotherapy or in combina...
Can I take Tofacitinib during pregnancy?▼
8.1 Pregnancy Risk Summary The available data with XELJANZ (tablets and oral solution) and XELJANZ XR (extended-release 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 are risks to the mother and the fetus associated with RA and UC in pregnancy (see Clinical Considerations ) .
What are the important warnings for Tofacitinib?▼
WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS, and THROMBOSIS WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS, and THROMBOSIS See full prescribing information for complete boxed warning. • Increased risk of serious bacterial, fungal, viral, and opportunistic infections, including tuberculosis (TB), leading to hospitalization or death. 5 WARNINGS AND PRECAUTIONS • Serious Infections : Avoid use of XELJANZ (tablets and oral solution) and XELJANZ XR (extended-release 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 ) • Laboratory Monitoring : Recommended due to potential changes in lymphocytes, neutrophils, hemoglobin, liver enzymes and lipids. ( 5.8 ) • Vaccinations : Avoid use of live vaccines concurrently with XELJANZ or XELJANZ XR. ( 5.9 ) 5.1 Serious Infections Serious and sometimes fatal infections may occur with XELJANZ (tablets and oral solution) and XELJANZ XR (extended-release tablets). 4 CONTRAINDICATIONS None. None. ( 4 )
Related Medications
Tolnaftate 1% Helps With Fungal Nail
tolnaftate 1% helps with fungal nail
Purpose Antifungal
Ketoconazole Micronized
ketoconazole micronized
Dosage form: POWDER. Active ingredients: KETOCONAZOLE (1 kg/kg). Category: BULK INGREDIENT.
Cucurbita Pepo Var. Ovifera
cucurbita pepo var. ovifera
Dosage form: SOLUTION. Route: INTRADERMAL, PERCUTANEOUS, SUBCUTANEOUS. Active ingredients: CUCURBITA PEPO SUBSP. OVIFERA WHOLE (.025 g/mL). Category: BLA.
Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.