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Upadacitinib

Also known as: Rinvoq

Janus Kinase InhibitorJanus Kinase Inhibitors

Route: Oral

5 interactions on record⛔ Black Box Warning

Upadacitinib has 5 known drug interactions based on U.S. FDA drug labeling data. Of these, 1 are contraindicated combinations that should be avoided entirely. Notable interactions include combinations with Rifampin, Clarithromycin, Grapefruit Products. Patients taking Upadacitinib should inform their healthcare provider of all current medications — including over-the-counter drugs and supplements — to avoid potentially harmful combinations. Data sourced from OpenFDA and the NIH National Library of Medicine.

Total: 5
Contraindicated: 1
Moderate: 3

Contraindicated (1)

Upadacitinib + Rifampin— Strong CYP3A4 inducer that decreases upadacitinib exposure and may lead to reduced therapeutic effect. Coadministration …

Moderate (3)

Upadacitinib + Clarithromycin— Strong CYP3A4 inhibitor that increases upadacitinib exposure, may increase risk of adverse reactions. Dosage modificatio…
Upadacitinib + Grapefruit Products— Strong CYP3A4 inhibitor that increases upadacitinib exposure. Food or drink containing grapefruit should be avoided duri…
Upadacitinib + Ketoconazole— Strong CYP3A4 inhibitor that increases upadacitinib exposure, may increase risk of adverse reactions. Dosage modificatio…

Upadacitinib + Rifampin⛔Contraindicated

Strong CYP3A4 inducer that decreases upadacitinib exposure and may lead to reduced therapeutic effect. Coadministration is not recommended.

Upadacitinib + Clarithromycin🟡Moderate

Strong CYP3A4 inhibitor that increases upadacitinib exposure, may increase risk of adverse reactions. Dosage modification required based on indication.

Upadacitinib + Grapefruit Products🟡Moderate

Strong CYP3A4 inhibitor that increases upadacitinib exposure. Food or drink containing grapefruit should be avoided during treatment.

Upadacitinib + Ketoconazole🟡Moderate

Strong CYP3A4 inhibitor that increases upadacitinib exposure, may increase risk of adverse reactions. Dosage modification required based on indication.

Upadacitinib + Nirmatrelvir And Ritonavirℹ️Unknown

upadacitinib ↑ upadacitinib Dosing recommendations for co-administration of upadacitinib with PAXLOVID depends on the upadacitinib indication. Refer to the upadacitinib prescribing information for more information.

⛔ FDA Black Box Warning

WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS, and THROMBOSIS SERIOUS INFECTIONS Patients treated with RINVOQ /RINVOQ LQ are at increased risk for developing serious infections that may lead to hospitalization or death [see Warnings and Precautions ( 5.1 ), Adverse Reactions ( 6.1 )]. Most patients who developed these infections were taking concomitant immunosuppressants such as methotrexate or corticosteroids. If a serious infection develops, interrupt RINVOQ /RINVOQ LQ until the infection is controlled. Reported infections include: Active tuberculosis, which may present with pulmonary or extrapulmonary disease. Patients should be tested for latent tuberculosis before RINVOQ /RINVOQ LQ use and during therapy. Treatment for latent infection should be considered prior to RINVOQ /RINVOQ LQ use. Invasive fungal infections, including cryptococcosis and pneumocystosis. Bacterial, viral, including herpes zoster, and other infections due to opportunistic pathogens. The risks and benefits of treatment with RINVOQ /RINVOQ LQ should be carefully considered prior to initiating therapy in patients with chronic or recurrent infection. Patients should be closely monitored for the development of signs and symptoms of infection during and after treatment with RINVOQ /RINVOQ LQ , including the possible development of tuberculosis in patients who tested negative for latent tuberculosis infection prior to initiating therapy [see Warnings and Precautions ( 5.1 )]. MORTALITY In a large, randomized, postmarketing safety study in rheumatoid arthritis (RA) patients 50 years of age and older with at least one cardiovascular risk factor comparing another Janus kinase (JAK) inhibitor to tumor necrosis factor (TNF) blockers, a higher rate of all-cause mortality, including sudden cardiovascular death, was observed with the JAK inhibitor [see Warnings and Precautions ( 5.2 )] . MALIGNANCIES Lymphoma and other malignancies have been observed in patients t

Contraindications

4 CONTRAINDICATIONS RINVOQ/RINVOQ LQ is contraindicated in patients with known hypersensitivity to upadacitinib or any of its excipients [see Warnings and Precautions ( 5.6 )] . Known hypersensitivity to upadacitinib or any of the excipients in RINVOQ/RINVOQ LQ. ( 4 , 5.6 )

Pregnancy & Breastfeeding

8.1 Pregnancy Pregnancy Surveillance Program There is a pregnancy surveillance program for RINVOQ/RINVOQ LQ that monitors pregnancy outcomes in women exposed to RINVOQ/RINVOQ LQ. If RINVOQ/RINVOQ LQ exposure occurs during pregnancy, healthcare providers or patients should report the pregnancy by calling 1-800-633-9110. Risk Summary Available data from the pharmacovigilance safety database and postmarketing case reports on use of RINVOQ in pregnant women are not sufficient to evaluate a drug-associated risk for major birth defects or miscarriage. Based on animal studies, RINVOQ/RINVOQ LQ has the potential to adversely affect a developing fetus. Advise patients of reproductive potential and pregnant patients of the potential risk to the fetus. In animal embryo-fetal development studies, oral upadacitinib administration to pregnant rats and rabbits at exposures equal to or greater than approximately 1.6 and 15 times the 15 mg tablet dose, 0.8 and 7.6 times the 30 mg tablet dose, and 0.6 and 5.6 times the maximum recommended human dose (MRHD) of 45 mg (on an AUC basis) resulted in dose-related increases in skeletal malformations (rats only), an increased incidence of cardiovascular malformations (rabbits only), increased post-implantation loss (rabbits only), and decreased fetal body weights in both rats and rabbits. No developmental toxicity was observed in pregnant rats and rabbits treated with oral upadacitinib during organogenesis at exposures approximately 0.29 and 2.2 times the 15 mg dose, 0.15 times and 1.1 times the 30 mg dose, and at 0.11 and 0.82 times the MRHD (on an AUC basis). In a pre- and post-natal development study in pregnant female rats, oral upadacitinib administration at exposures approximately 3 times the 15 mg dose, 1.4 times the 30 mg dose, and the same as the MRHD (on an AUC basis) resulted in no maternal or developmental toxicity ( see Data ) . The background risks of major birth defects and miscarriage for the indicated populations are unknown

Data sourced from U.S. FDA drug labeling via openFDA and the NIH National Library of Medicine. For informational purposes only. Always consult your pharmacist or physician.