Tofacitinib 5 mg, 60 tablets: profile, composition and research

Reference page for Tofacitinib 5 mg, 60 tablets. Active substance: Тофацитиниб / Tofacitinib.

Key facts

What tofacitinib is

Tofacitinib is a synthetic substance from the Janus kinase (JAK) inhibitor group. It belongs to a relatively young class of medicines that act not on a symptom but on the intracellular transmission of inflammatory signals.

The tablets contain 5 mg of the active substance, 60 to a pack. Oral use suits long-term treatment of chronic inflammatory disease, where therapy continues for months and years.

The substance is classed as a targeted synthetic disease-modifying antirheumatic drug. That means it is brought in once standard agents no longer provide adequate control of the disease.

How tofacitinib works

The signalling pathway

Janus kinases (JAK1, JAK2, JAK3 and TYK2) are enzymes inside the cell that are bound to interleukin and interferon receptors. When a cytokine engages its receptor, the kinases pass the signal to STAT proteins, which move into the nucleus and switch on the reading of inflammatory genes.

The point of intervention

Tofacitinib inhibits mainly JAK1 and JAK3. As a result the signal is cut off from many cytokines at once, including interleukins IL-2, IL-4, IL-6, IL-7, IL-9, IL-15 and IL-21, as well as type I and type II interferons.

What this achieves

Blocking one node affects a wide range of immune reactions, which is why the medicine is used in several different diseases rather than one. The other side of that breadth is an effect on immune defence as a whole, hence the close attention to infection risk.

Approved uses

The prescribing information lists several immune-mediated inflammatory diseases in adults: rheumatoid arthritis of moderate or high activity when disease-modifying drugs, methotrexate included, have proved insufficient; psoriatic arthritis; ankylosing spondylitis; and moderate-to-severe chronic plaque psoriasis.

Ulcerative colitis is listed separately. There the medicine is used both to achieve remission and to maintain it in patients who have not responded to other agents or cannot tolerate them.

There is also a paediatric indication: polyarticular juvenile idiopathic arthritis in children weighing 40 kg or more. Choosing the medicine, weighing benefit against risk and the follow-up all belong to a physician.

Safety and monitoring

Tofacitinib affects immunity, so before treatment starts a physician assesses infection risk, reviews laboratory results and rules out contraindications. These include severe liver disease, active infections, carriage of hepatitis B or C virus, recent vaccination with live vaccines, and concurrent use of biologic agents or potent immunosuppressants.

In a large study of patients with rheumatoid arthritis who had cardiovascular risk factors, serious cardiovascular events and certain tumours were reported more often on tofacitinib than on tumour necrosis factor inhibitors. For that reason a physician weighs benefit and risk for each patient individually and may choose a different dose or a different agent.

During treatment, blood counts, liver and kidney function are monitored and signs of infection are watched for. Fever, cough or chills call for immediate contact with a doctor.

Published research

Primary sources, verified against PubMed:

• Efficacy and safety of tofacitinib monotherapy, tofacitinib with methotrexate, and adalimumab with methotrexate in patients with rheumatoid arthritis (ORAL Strategy): a phase 3b/4, double-blind, head-to-head, randomised controlled trial., PubMed 28629665 (Lancet, 2017).
• Tofacitinib as Induction and Maintenance Therapy for Ulcerative Colitis., PubMed 28467869 (N Engl J Med, 2017).
• Cardiovascular and Cancer Risk with Tofacitinib in Rheumatoid Arthritis., PubMed 35081280 (N Engl J Med, 2022).

Listed for reference. Publication of a study is not a claim about this particular product.

Precautions

• This is a prescription medicine. Prescribing, dosing and monitoring belong to a physician.
• Tofacitinib affects immune defence and raises the risk of infection. Fever, cough or chills call for immediate contact with a doctor.
• Before treatment starts a physician screens for infections, tuberculosis and viral hepatitis included, and reviews blood tests.
• Concurrent use with biologic agents and potent immunosuppressants is not allowed.
• Use during pregnancy or breastfeeding is discussed with a doctor individually.
• Do not stop or change the treatment on your own. Withdrawal and adjustment are handled only by a physician.

Frequently asked