Tofacitinib is an oral small molecule Janus kinase (JAK) inhibitor that regulates immune cell activity and inflammatory response by selectively inhibiting the JAK-STAT signaling pathway.

1、 Drug name

1. Product Name: XELJANZ ®

2. Common name: Tofacitinib

2、 Indications

Tofacitinib is suitable for the treatment of the following diseases, and patients have insufficient response or intolerance to one or more tumor necrosis factor (TNF) blockers:

1. Moderate to severe active rheumatoid arthritis (RA).

2. Active psoriatic arthritis (PsA).

3. Active ankylosing spondylitis (AS).

4. Moderate to severe active ulcerative colitis (UC).

5. Active psoriatic arthritis (PsA) or polyarticular juvenile idiopathic arthritis (pcJIA) in children aged 2 years and above.

3、 Specifications

5mg * 60 tablets/box.

4、 Main components

Active ingredient: Tofacitinib (present in the form of tofacitinib citrate).

5、 Usage and dosage

1. Adult RA, PsA or AS:

Tofacitinib tablets: 5mg twice daily, or Tofacitinib sustained-release tablets: 11mg once daily.

2. Adult UC:

Induction therapy: Tofacitinib tablets 10mg twice daily for 8 weeks; According to the therapeutic effect, it can be extended to 16 weeks.

Maintenance therapy: Tofacitinib Z tablets 5mg twice daily.

3. Children with PsA or pcJIA (2 years old and above):

Weight ≥ 40kg: XELJANZ tablets or oral solution 5mg twice daily.

Weight range of 10kg to<40kg: Adjust the dosage according to body weight, 5mg or equivalent dose twice a day based on body weight.

6、 Dose adjustment

1. Adjust the dosage based on the damage to kidney and liver function.

2. In specific circumstances (such as concomitant use of CYP3A4 and/or CYP2C19 inhibitors, or occurrence of lymphopenia, neutropenia, anemia), dose adjustment is necessary.

7、 Medication precautions

1. Before and after meals: Tofacitinib should be taken with food or on an empty stomach.

2. Missed dose: If a dose is missed, it should be replenished as soon as possible; If it is close to the next medication time, skip the missed dose and take the next dose at the regular time.

3. Vomiting: If vomiting occurs after taking medication, there is no need to take the next dose as usual.

8、 Medication for special populations

1. Pregnancy: Pregnant women should not use it unless it is explicitly necessary.

2. Breastfeeding period: It is recommended that lactating women do not breastfeed.

3. Children: Tofacitinib oral solution and tablets are suitable for the treatment of PsA and pcJIA in children aged 2 years and above.

4. Elderly individuals: Patients aged 65 and above may have an increased risk of infection and should use with caution.

5. Renal and liver function impairment: Adjust the dosage according to the degree of impairment.

9、 Adverse reactions

1. Common adverse reactions include upper respiratory tract infection, nasopharyngitis, diarrhea, headache, etc.

2. Serious adverse reactions include severe infections, increased mortality rates, malignant tumors, major cardiovascular adverse events, thrombosis, etc.

10、 Contraindications

Patients who are allergic to tofacitinib or any ingredients in the drug are prohibited from using it.

11、 Drug interactions

1. Avoid co administration with potent CYP3A4 inducers.

2. When combined with potent CYP3A4 inhibitors or moderate CYP3A4 inhibitors and potent CYP2C19 inhibitors, the dosage needs to be adjusted.

3. Avoid co administration with biological DMARDs or potent immunosuppressants such as azathioprine and cyclosporine.

12、 Storage method

Store at 20 ° C to 25 ° C (68 ° F to 77 ° F), controlled at room temperature.

Tofacitinibinformation