RINVOQ LQ

Clinical safety rating: caution

Comprehensive clinical and safety monograph for RINVOQ LQ (RINVOQ LQ).

How it works

Janus kinase (JAK) inhibitor; selectively inhibits JAK1 and JAK3, modulating cytokine signaling involved in inflammation.

What the body does with it

Metabolism	Primarily metabolized by CYP3A4; minor contribution from CYP2D6.
Excretion	Renal (24% unchanged, 20% as metabolites), biliary/fecal (48% as metabolites), total radiolabeled dose recovery ~96% over 14 days.
Half-life	Terminal half-life 3.5-7.9 hours; at steady state, effective half-life ~4.5 hours, supports twice-daily dosing.
Protein binding	~52% bound to albumin and alpha-1-acid glycoprotein, independent of concentration.
Volume of Distribution	Gastrointestinal absorption is essentially complete; oral bioavailability is not determined due to lack of IV formulation. Based on population PK, apparent Vd/F is approximately 200 L, indicating extensive tissue distribution.
Bioavailability	Oral bioavailability ~76% following oral administration of the solution formulation.
Onset of Action	Improvement in rheumatoid arthritis symptoms as early as 2 weeks after oral administration.
Duration of Action	Clinically meaningful effect persists over 24 hours with twice-daily dosing; symptoms may return if doses are missed.

Classification & Brands

Dosing & administration

15 mg orally once daily; may increase to 30 mg once daily for inadequate response in certain conditions (e.g., rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, atopic dermatitis, ulcerative colitis, Crohn's disease).

Dosage form	SOLUTION
Renal impairment	No dose adjustment required for mild (eGFR ≥60 mL/min/1.73 m²) to moderate (eGFR 30-59 mL/min/1.73 m²) renal impairment. Not recommended in severe renal impairment (eGFR <30 mL/min/1.73 m²) or ESRD; use with caution if benefit outweighs risk.
Liver impairment	Child-Pugh Class A (mild): 15 mg once daily. Child-Pugh Class B (moderate): 15 mg once daily. Child-Pugh Class C (severe): not recommended; no data available.
Pediatric use	Atopic dermatitis: Age ≥12 years, weight ≥40 kg: 15 mg once daily. Age 2 to <12 years, weight ≥15 kg: 3 mg/mL oral solution (0.15 mg/kg) once daily for weight 15 to <30 kg; 0.2 mg/kg once daily for weight 30 to <45 kg; 0.25 mg/kg once daily for weight 45 to <60 kg; maximum 15 mg/day. Ulcerative colitis: Age ≥12 years: same as adult dosing. Crohn's disease: Age ≥16 years: same as adult dosing.
Geriatric use	No specific dose adjustment; use caution due to increased risk of infections and adverse events in patients ≥65 years. Monitor renal function, infections, and malignancies closely.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for RINVOQ LQ (RINVOQ LQ).

Breastfeeding	No data on presence in human milk, effects on breastfed infant, or milk production. In animal studies, upadacitinib was excreted in milk. M/P ratio is unknown. Risk to infant cannot be excluded; therefore, breastfeeding is not recommended during treatment and for 6 days after last dose.
Teratogenic Risk	Upadacitinib (RINVOQ LQ) is teratogenic in animal studies at exposures similar to human therapeutic doses. In pregnant women, there are no adequate and well-controlled studies; however, based on animal data, there is a risk of fetal malformations including cardiovascular and skeletal anomalies, particularly during the first trimester. Use is contraindicated during pregnancy.

Warnings & precautions

■ FDA Black Box Warning

Serious infections, malignancy, thrombosis, and mortality risk with tofacitinib (class warning); RINVOQ LQ carries FDA boxed warning for serious infections, lymphoma, and other malignancies.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to upadacitinib or excipients","Active severe infection (including tuberculosis)","Severe hepatic impairment (Child-Pugh Class C)"]

Clinical Precautions

Precautions

["Serious infections (bacterial, mycobacterial, fungal, viral)","Malignancies (lymphoma, lung cancer, other)","Thrombosis (DVT, PE, arterial thrombosis)","Gastrointestinal perforation","Laboratory abnormalities (neutropenia, lymphopenia, anemia, elevated liver enzymes, lipid elevations)","Vaccination avoidance with live vaccines","Hypersensitivity reactions"]

Clinical Tips & Counseling

Drug interactions

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RINVOQ LQ

Clinical safety rating: caution

Comprehensive clinical and safety monograph for RINVOQ LQ (RINVOQ LQ).

How it works

Janus kinase (JAK) inhibitor; selectively inhibits JAK1 and JAK3, modulating cytokine signaling involved in inflammation.

What the body does with it

Metabolism	Primarily metabolized by CYP3A4; minor contribution from CYP2D6.
Excretion	Renal (24% unchanged, 20% as metabolites), biliary/fecal (48% as metabolites), total radiolabeled dose recovery ~96% over 14 days.
Half-life	Terminal half-life 3.5-7.9 hours; at steady state, effective half-life ~4.5 hours, supports twice-daily dosing.
Protein binding	~52% bound to albumin and alpha-1-acid glycoprotein, independent of concentration.
Volume of Distribution	Gastrointestinal absorption is essentially complete; oral bioavailability is not determined due to lack of IV formulation. Based on population PK, apparent Vd/F is approximately 200 L, indicating extensive tissue distribution.
Bioavailability	Oral bioavailability ~76% following oral administration of the solution formulation.
Onset of Action	Improvement in rheumatoid arthritis symptoms as early as 2 weeks after oral administration.
Duration of Action	Clinically meaningful effect persists over 24 hours with twice-daily dosing; symptoms may return if doses are missed.

Classification & Brands

Dosing & administration

Dosage form	SOLUTION
Renal impairment	No dose adjustment required for mild (eGFR ≥60 mL/min/1.73 m²) to moderate (eGFR 30-59 mL/min/1.73 m²) renal impairment. Not recommended in severe renal impairment (eGFR <30 mL/min/1.73 m²) or ESRD; use with caution if benefit outweighs risk.
Liver impairment	Child-Pugh Class A (mild): 15 mg once daily. Child-Pugh Class B (moderate): 15 mg once daily. Child-Pugh Class C (severe): not recommended; no data available.
Pediatric use	Atopic dermatitis: Age ≥12 years, weight ≥40 kg: 15 mg once daily. Age 2 to <12 years, weight ≥15 kg: 3 mg/mL oral solution (0.15 mg/kg) once daily for weight 15 to <30 kg; 0.2 mg/kg once daily for weight 30 to <45 kg; 0.25 mg/kg once daily for weight 45 to <60 kg; maximum 15 mg/day. Ulcerative colitis: Age ≥12 years: same as adult dosing. Crohn's disease: Age ≥16 years: same as adult dosing.
Geriatric use	No specific dose adjustment; use caution due to increased risk of infections and adverse events in patients ≥65 years. Monitor renal function, infections, and malignancies closely.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for RINVOQ LQ (RINVOQ LQ).

Breastfeeding	No data on presence in human milk, effects on breastfed infant, or milk production. In animal studies, upadacitinib was excreted in milk. M/P ratio is unknown. Risk to infant cannot be excluded; therefore, breastfeeding is not recommended during treatment and for 6 days after last dose.
Teratogenic Risk	Upadacitinib (RINVOQ LQ) is teratogenic in animal studies at exposures similar to human therapeutic doses. In pregnant women, there are no adequate and well-controlled studies; however, based on animal data, there is a risk of fetal malformations including cardiovascular and skeletal anomalies, particularly during the first trimester. Use is contraindicated during pregnancy.

Warnings & precautions

■ FDA Black Box Warning

Serious infections, malignancy, thrombosis, and mortality risk with tofacitinib (class warning); RINVOQ LQ carries FDA boxed warning for serious infections, lymphoma, and other malignancies.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to upadacitinib or excipients","Active severe infection (including tuberculosis)","Severe hepatic impairment (Child-Pugh Class C)"]