Generic
Upadacitinib
8 brands available in the market
At a glance
Upadacitinib is a Janus kinase (JAK) inhibitor indicated for moderate to severe active rheumatoid arthritis, psoriatic arthritis, atopic dermatitis, ulcerative colitis, Crohn's disease, ankylosing spondylitis, non-radiographic axial spondyloarthritis, and polyarticular juvenile idiopathic arthritis.
Description
Upadacitinib is a Janus kinase-1 (JAK1)-selective inhibitor. JAK1 is essential for signaling for certain cytokines to elicit signals from various interleukins, cardiotrophin, neurotrophin, and interferons. These signals are essential in maintaining the inflammatory condition in rheumatoid arthritis (RA); inhibition of JAK reduces production of and modulates proinflammatory cytokines central to RA.
Indications
- Rheumatoid arthritis
- Psoriatic arthritis
- Atopic dermatitis
- Ulcerative colitis
- Crohn's disease
- Ankylosing spondylitis
- Non-radiographic axial spondyloarthritis
- Polyarticular juvenile idiopathic arthritis
Therapeutic class
Drugs used for Rheumatoid Arthritis
Pharmacological class
Janus Kinase (JAK) Inhibitor
Pharmacology
Upadacitinib is a Janus kinase (JAK) inhibitor. JAKs are intracellular enzymes that transmit signals arising from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoiesis and immune cell function. Within the signaling pathway, JAKs phosphorylate and activate STATs. Upadacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs.
Mechanism of action
Inhibits JAK1, preventing STAT phosphorylation and activation, reducing proinflammatory cytokine production.
Dosage
Adult Dose (Oral):
- Rheumatoid arthritis: 15 mg once daily
- Psoriatic arthritis: 15 mg once daily
- Atopic dermatitis (12 years and older, weighing at least 40 kg): 15 mg once daily; may increase to 30 mg once daily
- Ulcerative colitis: Induction 45 mg once daily for 8 weeks; maintenance 15 mg once daily
- Crohn's disease: Induction 45 mg once daily for 12 weeks; maintenance 15 mg once daily
- Ankylosing spondylitis: 15 mg once daily
- Non-radiographic axial spondyloarthritis: 15 mg once daily
- Polyarticular juvenile idiopathic arthritis (30 kg and greater): 15 mg once daily
Hepatic Impairment: Mild or moderate: no dose adjustment; Severe: not recommended
Administration
- May be taken with or without food
- Swallow tablets whole
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as you remember; if almost time for next dose, skip it; do not double the dose.
Side effects
Common Side Effects:
- Upper respiratory tract infection (13.5%)
- Nausea (3.5%)
- Neutropenia (1.1-2.4%)
- Lymphopenia (0.3-2.4%)
- Cough (2.2%)
- Elevated ALT (0.8-2.1%)
- Increased creatine phosphokinase (0.3-1.6%)
- Elevated AST (1-1.5%)
- Pyrexia (1.2%)
- Pneumonia, herpes zoster, herpes simplex, oral candidiasis, anemia (<0.1%)
Precautions & warnings
- Malignancies reported; consider risks and benefits before initiating in patients with known malignancy
- Thrombosis reported, including DVT, PE, and arterial thrombosis
- Gastrointestinal perforation reported
- May cause neutropenia, lymphopenia, anemia, elevated lipids, or elevated liver enzymes; monitor for abnormal laboratory values
- May cause fetal harm based on animal studies; do not use during pregnancy
Contraindications
- Active, serious infection
- Known malignancy (other than previously treated nonmelanoma skin cancer)
- Severe hepatic impairment
- Pregnancy and lactation
Drug interactions
- Strong CYP3A4 inhibitors (ketoconazole): increased upadacitinib exposure; use with caution
- Strong CYP3A4 inducers (rifampin): decreased upadacitinib exposure; not recommended
Food interactions
Food interactions are not significant.
Use in pregnancy
Use in Pregnancy: Limited human data; animal studies show potential fetal harm; do not use during pregnancy.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Unknown if excreted in human milk; do not breastfeed during treatment and for 6 days (~10 half-lives) after last dose.
Pediatric use
No data available for pediatric patients under 2 years
Geriatric use
Caution required in elderly patients
Renal / hepatic impairment
Renal Impairment: Mild, moderate, or severe: no dose adjustment; ESRD: not studied
Hepatic Impairment: Mild or moderate: no dose adjustment; severe: not recommended
Overdose effects
Symptoms: Up to 60 mg daily AUC showed adverse events comparable to lower doses; no specific toxicities identified.
Treatment: Monitor for signs and symptoms of adverse reactions; provide appropriate treatment.
Storage conditions
Do not store above 25°C. Protect from light. Keep out of reach of children.