What to Know About Rinvoq (Upadacitinib)

If you have rheumatoid arthritis (RA), your healthcare provider might prescribe Rinvoq (upadacitinib). There is no generic form of the drug. It comes as a tablet you take daily. It is often prescribed to people who have not had an adequate response to methotrexate. 

Rinvoq is a Janus kinase (JAK) inhibitor available for treating adults with moderate to severe RA. JAK inhibitors are a fairly new class of drugs.

They inhibit the activity of one or more of the JAK family of enzymes, interfering with signaling pathways and cellular processes that contribute to RA, inflammation, and several inflammatory diseases.

Approved in 2019 by the Food and Drug Administration (FDA), Rinvoq joins Xeljanz (tofacitinib) and Olumiant (baricitinib) as JAK inhibitor options for treating RA. All three drugs are effective and reasonably safe for the treatment of moderate to severe RA. The FDA has also approved Xelijanz to treat psoriatic arthritis and ulcerative colitis.

Please keep reading to learn about Rinvoq, its uses, what to know before starting it, how to take it, side effects, and precautions. 

Uses

Rinvoq (upadacitinib) is primarily used to treat rheumatoid arthritis, a chronic inflammatory autoimmune disease that mainly affects joints, including the hands and feet.

It is prescribed to people with RA with moderate to severe disease who have not responded well to methotrexate or who cannot take methotrexate. Rinvoq can be taken alone, with methotrexate, or with non-biologic disease-modifying antirheumatic drugs (DMARDs), like Plaquenil and Arava.

In April 2022, the FDA approved Rinvoq to treat adults with active ankylosing spondylitis (AS) who have had an inadequate response or intolerance to TNF inhibitors, such as Remicade (infliximab). It is also approved for treating other inflammatory disorders, including psoriatic arthritis (PsA), atopic dermatitis, and ulcerative colitis.

There have been many studies looking at the effectiveness of Rinvoq. Most have compared the effectiveness of Rinvoq to a placebo or a DMARD. A placebo drug is an inactive drug that looks like the drug being tested.

Many studies have found that people who take Rinvoq alone or with methotrexate or another DMARD for RA have better results than those taking methotrexate alone.

Rinvoq studies have looked at how much relief the drug offers for managing symptoms, including inflammation, pain, and the number of swollen joints. They have also looked at improvements in physical function.

According to studies included on the U.S. National Library of Medicine drug information page for Rinvoq, the use of Rinvoq for 12 to 14 weeks compared to methotrexate or a placebo showed:

For the people who took Rinvoq:

• Up to a 76% improvement of symptoms and an up to 20% improvement in physical function
• Up to a 52% improvement of symptoms and an up to 50% improvement in physical function
• Up to a 32% improvement of symptoms and an up to 70% improvement in physical function

For methotrexate, the studies showed:

• Up to a 54% improvement of symptoms and an up to 20% improvement in physical function
• Up to a 28% improvement of symptoms and an up to 50% improvement in physical function
• Up to a 14% improvement of symptoms and an up to 70% improvement in physical function

For the participants taking the placebo, the percentages for symptom and function improvement were significantly much lower.

Research shows Rinvoq can increase the probability of remission. Clinical remission in inflammatory conditions like RA means symptoms have lessened to the point they are mostly absent or gone.

One phase 3 study found that more than 35% who took the drug reached remission within 12 weeks, compared to 14% who took methotrexate at the same time.

The maker of Rinvoq has revealed the drug might be more effective than Humira (adalimumab) for treating RA and increasing the incidence of remission. AbbVie manufactures both drugs. 

Other Inflammatory Conditions

Rinvoq is approved to treat other inflammatory disorders, including psoriatic arthritis (PsA), ankylosing spondylitis (AS), and ulcerative colitis.

One phase 2/3 study reported in August 2020 showed significant symptom improvement in people with active AS who took Rinvoq. Here, up to 52% of people receiving Rinvoq met the primary endpoint assessments. Additionally, the drug's safety profile was consistent with that of other studies of Rinvoq, with no new safety risks found.

In phase 3 studies for PsA, Rinvoq users who had inadequate responses to non-biologic DMARDs were meeting primary endpoint responses by the end of week 12 of treatment.

Researchers also determined that Rinvoq was much more effective for treating PsA than Humira by week 12. Additionally, people using Rinvoq were showing greater improvements in physical function and skin symptoms. They were also achieving minimal disease activity response by week 24.

Phase 3 studies of Rinvoq for treating moderate to severe ulcerative colitis found that the drug was effective in the achievement of clinical remission as early as eight weeks. In this study, 26% of study participants hit clinical remission, and up to 73% experienced clinical response (reduction in symptoms) by at least week eight.

Off-Label Uses

Rinvoq may also be used off-label to treat additional medical conditions. Off-label use means that a drug that has been approved for one purpose may be used for other purposes.

An off-label use purpose has to be submitted to the Food and Drug Administration for review with information that shows the drug is safe and effective for the intended use.

Rinvoq has not been FDA approved for treating atopic dermatitis, a chronic skin condition that can make skin swollen and itchy. However, Rinvoq has been used to treat atopic dermatitis.

A study reported in 2019 in the Journal of Allergy and Clinical Immunology showed that even a low dose of Rinvoq could improve atopic dermatitis, with a 30-milligram dose offering the greatest clinical benefit.

Before Taking

Before taking Rinvoq, you should let your healthcare provider know if you have signs of an infection—fever, chills, aches, tiredness, and cough. People with active infections shouldn’t take Rinvoq.

Your healthcare provider might perform tests to make sure you don’t have tuberculosis (TB) or another serious infection. Tell your practitioner if you have TB or have been in close contact with someone who has TB.

You should also let your healthcare provider know if you:

• Are a current or former smoker or have had a heart attack, other heart problems, or a stroke 
• Have had any type of cancer, hepatitis B, shingles, a blood clot of the legs or lungs, diverticulitis (inflammation of the large intestine), or stomach ulcers or ulcers of the intestines
• Have diabetes, a liver problem, or a weak immune system
• Have lived or traveled to parts of the United States that increase your risk for certain fungal infections
• Have recently received or are scheduled for a live vaccine: People who take Rinvoq shouldn’t receive live vaccines, such as the shingles vaccine or the nasal flu vaccine.
• Are pregnant or plan to become pregnant
• Are breastfeeding

You should also let your healthcare provider know about all the medications you take, including prescription, over-the-counter (OTC) treatments, vitamins, and herbal supplements.

Your healthcare provider especially needs to know if you take medicines to treat fungal or bacterial infections, medicines that affect the immune system, rifampicin (an antibiotic commonly used to treat TB), or phenytoin (an anti-seizure drug).

Dosage

Your healthcare provider will give you instructions on how to take Rinvoq. They will also tell you how much to take and how often you should take it. Make sure you are following all of your practitioner’s instructions.

You will probably be taking Rinvoq for the long term. Your healthcare provider can answer questions about your treatment plan and what might work best for you. You will need to take Rinvoq for several weeks before you notice symptom improvement.

Rinvoq comes as a 15-milligram oral tablet you swallow. The manufacturer recommends taking the drug once per day. Take each dose with a full glass of water. Swallow the tablet whole and don’t crush, chew, or split it. If you have trouble swallowing pills, let your healthcare provider know.

If you miss a dose, take the missed dose as soon as you remember. But if it is already time for your next dose, don’t double up doses—just take the next dose. If you have any questions about a missed dose, get in touch with your healthcare provider.

You should store Rinvoq in its original container at room temperature but away from heat or moisture.

Side Effects

Like most medicines, Rinvoq may cause mild and serious side effects. Your healthcare provider or pharmacist can give you more information on side effects and how to reduce these effects.

Some mild side effects of Rinvoq include:

• Cough
• Fever
• Nausea
• Upper respiratory infections, including tonsilitis and the common cold 

Most side effects resolve within a few days or a couple of weeks of starting treatment. Talk to your healthcare provider if side effects become serious or bothersome.

Serious side effects from Rinvoq are rare, but they can occur. If you experience serious side effects, you should let your healthcare provider know right away. If you think you might be having a medical emergency, you should call 911 or head to your local emergency room.

Serious side effects of Rinvoq might include:

• Serious infections
• Increased cancer risk
• Blood clots
• Serious heart-related events
• Changes in levels of red blood cells or white blood cells, liver enzymes, or cholesterol
• Tears (perforation) of the stomach, small intestine, or large intestine
• Allergic reaction: Signs might include a rash or hives, shortness of breath, wheezing, rapid heartbeat, nausea or vomiting, swelling of the lips, face, tongue or throat, confusion, dizziness, or fainting.

Rinvoq comes with a black box warning for serious infections that could lead to hospitalization or death. Serious infections associated with Rinvoq might include TB and bacterial, fungal, and viral infections. If you develop a serious infection while on Rinvoq, the medication should be stopped until the infection has cleared. JAK inhibitors, including Rinvoq, have been shown to raise the risk of heart attack, stroke, blood clots, and death. If you any questions about Rinvoq, talk with your doctor, pharmacist, or other health care provider.

Warnings and Interactions

Some people shouldn’t take Rinvoq. This includes people who take medications that might interact with Rinvoq. When a drug interacts with another drug, this means that there might a change to the way the drug works.

Drugs that can interact with Rinvoq might include:

• Antibiotics: Medicines that fight infections caused by bacteria
• Anticonvulsants: Medications used to treat seizure disorders and some mental health conditions, including bipolar disorder and borderline personality disorder
• Antifungals: Drugs that treat fungal infections
• Antivirals: Medicines that fight viruses
• Calcium channel blockers: Medicines that lower blood pressure and other conditions that might cause an irregular heartbeat or heart problems. These drugs work by preventing calcium from entering the heart or arteries.
• Corticosteroids: A class of drugs that lowers inflammation in the body

It is unknown if there are any clinical interactions between Rinvoq and alcohol. Consuming alcohol can increase your risk for side effects, including liver problems. Talk to your healthcare provider about whether it is safe for you to consume alcohol while using Rinvoq.

Animal studies have found that Rinvoq can cause harm to an unborn fetus. And while animal studies are not true predictors of the effect a drug will have on people, taking Rinvoq while pregnant isn’t recommended.

People who are trying to become pregnant shouldn't take Rinvoq, and people who are capable of becoming pregnant should use birth control while on Rinvoq. People who are breastfeeding should also avoid taking the drug.

It is recommended that you avoid live vaccines while on Rinvoq. Live vaccines contain a small amount of the virus. In healthy people, the immune system would fight the virus.

However, because Rinvoq can weaken the immune system, this lowers the probability of your immune system responding appropriately to the vaccine. This might include raising your risk for the virus rather than protecting you from it.

You should avoid grapefruit while taking Rinvoq. Both grapefruit and grapefruit juice can affect how Rinvoq works for you.

Don’t take more Rinvoq than your healthcare provider has prescribed to you. Using more can lead to serious side effects, including overdose.

Reach out to your healthcare provider if you think you have taken too much Rinvoq. You can also reach out to the U.S. Poison Control Center at 1-800-222-1222. If you experience severe symptoms, call 911 or go to your local emergency room.