CIBINQO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CIBINQO (CIBINQO).
CIBINQO (abrocitinib) is a Janus kinase (JAK) inhibitor. It selectively inhibits JAK1, which modulates cytokine signaling involved in inflammatory pathways, including interleukin (IL)-4, IL-13, IL-31, and interferon-gamma, reducing the inflammatory response in atopic dermatitis.
| Metabolism | Metabolized primarily by CYP2C9 and to a lesser extent by CYP3A4. Two major metabolites: M1 (active, 5-fold less potent) and M2 (inactive). |
| Excretion | Primarily excreted via feces (69%) and urine (20%) after oral administration. Renal elimination accounts for <1% of unchanged drug. Biliary excretion is the major route for metabolites. |
| Half-life | Terminal elimination half-life is approximately 4-6 hours in healthy subjects, supporting twice-daily dosing. No significant accumulation after multiple doses. |
| Protein binding | Approximately 85-90% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is approximately 200 L (2.9 L/kg), indicating extensive tissue distribution beyond plasma volume. |
| Bioavailability | Absolute oral bioavailability is approximately 10-20% due to first-pass metabolism. Bioavailability is dose-proportional over the therapeutic range. |
| Onset of Action | Oral administration: Clinical effect (improvement in pruritus) observed within 2 weeks; maximal effect achieved by 4-6 weeks. |
| Duration of Action | Duration of action per dose corresponds to half-life, requiring twice-daily dosing to maintain therapeutic levels. Continuous treatment is needed for sustained response. |
100 mg orally once daily, with or without food.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (eGFR ≥30 mL/min/1.73 m²). Not recommended for severe renal impairment (eGFR <30 mL/min/1.73 m²) or ESRD. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: 50 mg orally once daily. Child-Pugh C: Not recommended. |
| Pediatric use | Safety and efficacy in pediatric patients (<12 years) have not been established; no approved pediatric dosing. |
| Geriatric use | No specific dose adjustment recommended based on age alone; monitor renal function closely as elderly patients may have reduced renal clearance. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CIBINQO (CIBINQO).
| Breastfeeding | No data on human milk excretion. Abrocitinib is likely present in milk based on animal studies. M/P ratio unknown. Risk of serious adverse effects in nursing infants; breastfeeding is contraindicated during treatment and for 1 week after last dose. |
| Teratogenic Risk | Abrocitinib is contraindicated in pregnancy. Animal studies show teratogenicity at exposures below human exposure at the recommended dose. First trimester: high risk of major congenital malformations. Second and third trimesters: risk of fetal growth restriction and potential effects on immune development. |
■ FDA Black Box Warning
WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS, AND THROMBOSIS. Serious infections including tuberculosis, bacterial, invasive fungal, viral, and opportunistic infections have been reported; some fatal. Patients should be tested for latent TB before initiation; if positive, treated prior to use. Increased rate of all-cause mortality including sudden cardiovascular death. Lymphoma and other malignancies have been observed. Major adverse cardiovascular events (MACE) including myocardial infarction and stroke occurred in patients with risk factors. Thrombosis including deep vein thrombosis, pulmonary embolism, and arterial thrombosis reported.
| Serious Effects |
Absolute: Known hypersensitivity to abrocitinib or excipients. Relative: Active serious infections, including TB; severe hepatic impairment; pregnancy and lactation (limited data); use with strong CYP2C9 inhibitors (e.g., amiodarone, fluconazole) requires dose reduction.
| Precautions | Serious infections; viral reactivation (herpes zoster, hepatitis B); hypersensitivity reactions; thrombocytopenia; lipid elevations; liver enzyme elevations; vaccination with live vaccines not recommended; increased risk of malignancies; gastrointestinal perforation; avoid use in patients with severe hepatic impairment. |
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| Fetal Monitoring |
| Pregnancy test prior to initiation. Monthly pregnancy tests during therapy. Use effective contraception during treatment and for 1 week after last dose. No specific fetal monitoring required if pregnancy occurs; refer to teratology specialist. |
| Fertility Effects | Animal studies show reduced fertility in males and females at clinically relevant exposures. Reversible after discontinuation. Human data lacking. May impair spermatogenesis and ovulation. |