INDICATION1

RINVOQ is indicated for the treatment of adults with moderately to severely active ulcerative colitis who have had an inadequate response or intolerance to one or more TNF blockers.

Limitations of Use: RINVOQ is not recommended for use in combination with other JAK inhibitors, biological therapies for ulcerative colitis, or with other potent immunosuppressants such as azathioprine and cyclosporine. 

IMPORTANT SAFETY INFORMATION1

WARNING: Serious Infections, Mortality, Malignancies, Major Adverse Cardiovascular Events, and Thrombosis.

SERIOUS INFECTIONS

Patients treated with RINVOQ are at increased risk for developing serious infections that may lead to hospitalization or death. Most patients who developed these infections were taking concomitant immunosuppressants, such as azathioprine and cyclosporine. If a 

IMPORTANT SAFETY INFORMATION1

WARNING: Serious Infections, Mortality, Malignancies, Major Adverse Cardiovascular Events, and Thrombosis.

SERIOUS INFECTIONS

Patients treated with RINVOQ are at increased risk for developing serious infections that may lead to hospitalization or death. Most patients who developed these infections were taking concomitant immunosuppressants, such as 

INDICATION1

RINVOQ is indicated for the treatment of adults with moderately to severely active ulcerative colitis who have had an inadequate response or intolerance to one or more TNF blockers.

Limitations of Use: RINVOQ is not recommended for use in combination with other JAK inhibitors, biological therapies for ulcerative colitis, or with other potent immunosuppressants such as azathioprine and cyclosporine. 

IMPORTANT SAFETY INFORMATION1

WARNING: Serious Infections, Mortality, Malignancies, Major Adverse Cardiovascular Events, and Thrombosis.

SERIOUS INFECTIONS

Patients treated with RINVOQ are at increased risk for developing serious infections that may lead to hospitalization or death. Most patients who developed these infections were taking concomitant immunosuppressants, such as azathioprine and cyclosporine. If a 

IMPORTANT SAFETY INFORMATION1

WARNING: Serious Infections, Mortality, Malignancies, Major Adverse Cardiovascular Events, and Thrombosis.

SERIOUS INFECTIONS

Patients treated with RINVOQ are at increased risk for developing serious infections that may lead to hospitalization or death. Most patients who developed these infections were taking concomitant immunosuppressants, such as

IMPORTANT SAFETY
INFORMATION & INDICATION1

INDICATION1

RINVOQ is indicated for the treatment of adults with moderately to severely active ulcerative colitis who have had an inadequate response or intolerance to one or more TNF blockers.

Limitations of Use: RINVOQ is not recommended for use in combination with other JAK inhibitors, biological therapies for ulcerative colitis, or with other potent immunosuppressants such as azathioprine and cyclosporine.

SERIOUS INFECTIONS

  • Active tuberculosis (TB), which may present with pulmonary or extrapulmonary disease. Test patients for latent TB before RINVOQ use and during therapy. Consider treatment for latent TB infection prior to RINVOQ use.
  • Invasive fungal infections, including cryptococcosis and pneumocystosis.
  • Bacterial, viral, including herpes zoster, and other infections due to opportunistic pathogens.

MORTALITY

MALIGNANCIES

MAJOR ADVERSE CARDIOVASCULAR EVENTS

THROMBOSIS

HYPERSENSITIVITY

GASTROINTESTINAL PERFORATIONS

LABORATORY ABNORMALITIES

EMBRYO-FETAL TOXICITY

VACCINATION

LACTATION

HEPATIC IMPAIRMENT

ADVERSE REACTIONS

For moderate to severe ulcerative colitis (UC) in adult TNFi-IR patients.1

RINVOQ IS A

JAK Inhibitor

RINVOQ is an oral small molecule that inhibits the JAK-STAT signaling pathway, utilized by pro-inflammatory cytokines.1,2

The relevance of inhibition of specific JAK enzymes to therapeutic effectiveness is not currently known.

IR=intolerance or inadequate response;
TNFi=tumor necrosis factor inhibitor

15mg pills

RINVOQ

Mechanism
of Action (MOA)
RINVOQ
Mechanism of
Action (MOA)
Mechanism of disease
Ulcerative Colitis:
Mechanism
of Disease (MOD)
Ulcerative Colitis:
Mechanism of
Disease (MOD)
 
Ulcerative Colitis (UC):

A chronic
& complex
disease
of the colon

UC is an immune-mediated, inflammatory condition of the large intestine and is characterized by bleeding, urgency and tenesmus.3

UC is an immune-mediated, inflammatory condition of the large intestine and is characterized by bleeding, urgency and tenesmus.3

 
Ulcerative Colitis (UC):

Several key cytokines are thought to use signaling networks such as the JAK-STAT Pathway.

Overexpression of these key cytokines can lead to excess inflammation and may contribute to the signs and symptoms of UC.4,5

CYTOKINES

Pro-inflammatory Cytokines
Involved in UC Pathogenesis1,5
 
 
 
 

Inside the cell

The cytokines that activate JAK-STAT pathways contribute to the pathogenesis of UC through their role in inflammation. However, these same cytokines are also important for general cellular functions such as immune system modulation, cell growth, and hematopoiesis.1,5

The cytokines that activate JAK-STAT pathways contribute to the pathogenesis of UC through their role in inflammation. However, these same cytokines are also important for general cellular functions such as immune system modulation, cell growth, and hematopoiesis.1,5

 
Mechanism
of Action
RINVOQ
 

Cytokine

Jak

Rinvoq

How Rinvoq Works

RINVOQ targets JAK, affecting the JAK-STAT pathway inside the cell, which is linked to the signalling of pro-inflammatory cytokines.1,2

Based on enzymatic and cellular assays, RINVOQ demonstrated greater inhibitory potency for JAK1 and JAK2 relative to JAK3 and TYK2.1,2

The relevance of inhibition of specific JAK enzymes to therapeutic effectiveness is not known.

Cytokine

Jak

Rinvoq

STAT

How Rinvoq Works

By binding JAK, RINVOQ prevents the phosphorylation and activation of STATs, disrupting the pro-inflammatory signaling cascade.1,2

The relevance of inhibition of specific JAK enzymes to therapeutic effectiveness is not known.

The relevance of inhibition of specific JAK enzymes to therapeutic effectiveness is not known.

ONE PILL,

Once-Daily
30 mg and 15 mg QD bottles

In clinical trials, RINVOQ has been shown to provide significant clinical remission at Week 8 and Week 52 and powerful histo-endoscopic mucosal improvement* for moderate to severe UC in adult TNFi-IR patients.1

*The relationship between this endpoint
to disease progression and long-term outcomes
was not evaluated.
*The relationship between this endpoint to disease progression
and long-term outcomes was not evaluated.
The recommended dose of RINVOQ for maintenance treatment is 15 mg once daily. A maintenance dose of 30 mg once daily may be considered for patients with refractory, severe or extensive disease.
The recommended dose of RINVOQ for maintenance treatment is 15 mg once daily. A maintenance dose of 30 mg once daily may be considered for patients with refractory, severe or extensive disease.
 
Mechanism
of Disease
 
The Role of the

JAK-STAT PATHWAY4,5

Pro-inflammatory cytokines utilize signaling pathways — such as the JAK-STAT pathway — to communicate with the cell nucleus.

The cytokine binds to a specific receptor on the cell surface that modulates JAK-mediated signaling.

Inside the cell

Jak

Jak

 
The Role of the

JAK-STAT PATHWAY4,5

The receptor spans the cell's membrane and cytokine binding triggers JAK activation inside the cell.

 

STAT

STAT

The Role of the

JAK-STAT PATHWAY4,5

The activated JAK then mobilizes STATs,
which transmit the signal into the cell nucleus.

JAK Inhibitor

STAT

STAT

Inside the cell

The Role of the

JAK-STAT PATHWAY4,5

This signaling contributes to the inflammatory response in UC.

 

RINVOQ IS A

JAK Inhibitor

By targeting JAK, RINVOQ is thought to block the
recruitment, phosphorylation, and activation of
STATs and inhibit the pro-inflammatory processes
associated with the JAK-STAT pathway.1,4,5

By targeting JAK, RINVOQ is
thought to block the recruitment,
phosphorylation, and activation
of STATs and inhibit the
pro-inflammatory processes
associated with the JAK-STAT
pathway.1,5

The relevance of inhibition of specific JAK enzymes
to therapeutic effectiveness is not currently known.

The relevance of inhibition
of specific JAK enzymes to therapeutic effectiveness is not currently known.

 

IMPORTANT SAFETY
INFORMATION & INDICATION1

INDICATION1

RINVOQ is indicated for the treatment of adults with moderately to severely active ulcerative colitis who have had an inadequate response or intolerance to one or more TNF blockers.

Limitations of Use: RINVOQ is not recommended for use in combination with other JAK inhibitors, biological therapies for ulcerative colitis, or with other potent immunosuppressants such as azathioprine and cyclosporine.


SERIOUS INFECTIONS

  • Active tuberculosis (TB), which may present with pulmonary or extrapulmonary disease. Test patients for latent TB before RINVOQ use and during therapy. Consider treatment for latent TB infection prior to RINVOQ use.
  • Invasive fungal infections, including cryptococcosis and pneumocystosis.
  • Bacterial, viral, including herpes zoster, and other infections due to opportunistic pathogens.

MORTALITY

MALIGNANCIES

MAJOR ADVERSE CARDIOVASCULAR EVENTS

THROMBOSIS

HYPERSENSITIVITY

GASTROINTESTINAL PERFORATIONS

LABORATORY ABNORMALITIES

EMBRYO-FETAL TOXICITY

VACCINATION

LACTATION

HEPATIC IMPAIRMENT

ADVERSE REACTIONS

 


REFERENCES

  1. RINVOQ [package insert]. North Chicago, IL: AbbVie Inc.
  2. Parmentier JM, Voss J, Graff C, et al. In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494). BMC Rheumatol. 2018;2:23.
  3. Rubin DT, Ananthakrishnan AN, Siegel CA, et al. ACG Clinical Guideline: Ulcerative Colitis in Adults. Am J Gastroenterol. 2019;114:384-413.
  4. Neurath M. Cytokines in inflammatory bowel disease. Nat Rev Immunol. 2014;14:329–342.
  5. Salas A, Hernandez-Rocha C, Duijvestein M, et al. JAK-STAT pathway targeting for the treatment of inflammatory bowel disease. Nat Rev Gastroenterol Hepatol. 2020;17(6):323-337.