Xeljanz (tofacitinib)

Tofacitinib (Xeljanz; pronounced: ZEL-jans) is a Janus kinase (JAK) inhibitor manufactured by Pfizer Inc. It is indicated (approved for use) for the treatment of adult patients with moderately- to severely-active RA who have had an inadequate response or intolerance to methotrexate. It may be used as alone (as monotherapy) or in combination with methotrexate or other conventional disease-modifying anti-rheumatic drugs (DMARDs). Xeljanz should not be used in combination with biologic DMARDs or potent immunosuppressant drugs such as azathioprine and cyclosporine.

 

Tofacitinib (Xeljanz): overview and efficacy

Tofacitinib (Xeljanz; pronounced: ZEL-jans) is a Janus kinase (JAK) inhibitor manufactured by Pfizer Inc. It is indicated (approved for use) for the treatment of adult patients with moderately- to severely-active RA who have had an inadequate response or intolerance to methotrexate. It may be used alone (as monotherapy) or in combination with methotrexate or other conventional disease-modifying anti-rheumatic drugs (DMARDs). Xeljanz should not be used in combination with biologic DMARDs or potent immunosuppressant drugs such as azathioprine and cyclosporine.1

 

How is Xeljanz taken?

Xeljanz is currently the only approved biologic treatment for RA that is available for oral administration. It is available in 5 mg tablets and the recommended dose of Xeljanz is 5 mg twice daily.1

You can take Xeljanz with or without food. If you take too much Xeljanz, call your doctor immediately and go right away to the nearest emergency room.1

 

How does Xeljanz work?

Xeljanz is a JAK inhibitor. JAKs are enzymes that work within the immune system and other cells to transmit signals that influence basic cell functions. By inhibiting JAKs in immune cells, Xeljanz can interfere with the immune processes in RA.1

 

Are there people who should not take Xeljanz?

There is an increased risk for serious infections with Xeljanz. This is because Xeljanz can decrease the ability of the immune system to fight infections. If you have an active infection, you should not take Xeljanz. If you develop a serious infection while taking Xeljanz, contact your doctor immediately. You may need to interrupt or discontinue treatment with Xeljanz.1

Xeljanz is a pregnancy category C drug. In animal studies, Xeljanz did result in birth defects in the developing fetus. There have been no well-controlled studies in humans. Xeljanz should only be used in pregnant women if the potential benefits justify the risk to the fetus.1

It is unknown whether Xeljanz is excreted into human milk. Because of the potential for adverse effects to the nursing infant, a nursing woman should either stop taking the drug or discontinue nursing while taking Xeljanz.1

 

What is the evidence that Xeljanz works in RA?

The effectiveness of Xeljanz in patients with RA was evaluated in two randomized, controlled trials testing a range of doses of Xeljanz versus placebo, conducted in a total of 891 patients with active RA who had had an inadequate response to methotrexate and/or other DMARDs. Results from these studies established Xeljanz 5 mg and 10 mg as the most safe and effective doses for further study.

Five additional randomized, controlled trials were conducted in patients with moderately- to severely-active RA.

One study (Study 1) tested Xeljanz 5 mg or 10 mg twice daily as monotherapy (alone) versus placebo in 610 patients who had had an inadequate response to a conventional DMARD or biologic.

In another study (Study 2), 792 patients who had had an inadequate response to a conventional DMARD were randomized to Xeljanz 5 mg or 10 mg twice daily or placebo, each combined with background DMARD treatment (excluding immunosuppressive treatments such as azathioprine or cyclosporine).

Another study (Study 3) was conducted in 717 patients who had had an inadequate response to methotrexate. These patients were randomized to Xeljanz 5 mg or 10 mg twice daily, adalimumab (Humira) 40 mg, or placebo, each combined with background methotrexate treatment.

In one 2-year study (Study 4) (currently listed as ongoing) 797 patients who had had an inadequate response to methotrexate were randomized to Xeljanz 5 mg or 10 mg twice daily or placebo, each combined with background methotrexate.

In another study (Study 5), 399 patients who had had an inadequate response to at least one anti-TNF treatment were randomized to Xeljanz 5 mg or 10 mg twice daily or placebo, each added to background methotrexate.

 
Disease control and clinical response. In each of the five randomized, controlled studies, Xeljanz (at both doses) resulted in higher rates of ACR20, 50, and 70 response compared with placebo, with or without background DMARD treatment. These higher rates of response were evident as early as 2 weeks and remained consistent through 6 and 12 months of treatment.

 

Rates of ACR responses from two clinical trials of Xeljanz

Study 1: Monotherapy in DMARD and biologic failures Study 4: MTX failures Study 5: anti-TNF failures
Xeljanz 5 mg (N=243) Xeljanz 10 mg (N=245) Placebo + MTX (N=122) Xeljanz 5 mg + MTX (N=321) Xeljanz 10 mg + MTX (N=316) Placebo + MTX (N=160) Xeljanz 5 mg + MTX (N=321) Xeljanz 10 mg + MTX (N=316) Placebo + MTX (N=160)
ACR20
Mo 3 59% 65% 26% 55% 67% 27% 41% 48% 24%
Mo 6 69% 70% 50% 62% 25% 51% 54%
AC50
Mo 3 31% 36% 12% 29% 37% 8% 26% 28% 8%
Mo 6 42% 46% 32% 44% 9% 37% 30%
ACR70
Mo 3 15% 20% 6% 11% 17% 3% 14% 10% 2%
Mo 6 22% 29% 14% 23% 1% 16% 16%

 

Is there a generic form of Xeljanz?

There is no generic form of Xeljanz.

Written by: Jonathan Simmons | Last reviewed: September 2013.
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