Medication Pearl of the Day: Abrocitinib (Cibinqo)
Indication: Abrocitinib(Cibinqo) is a Janus kinase (JAK) inhibitor indicated for the treatment of adults with refractory moderate-to-severe atopic dermatitis whose disease is not adequately controlled with other systemic drug products, including biologics, or when use of those therapies is inadvisable.
- Dosing: Recommended dosage is 100 mg orally once daily.
- Dosage forms: Tablets 50 mg, 100 mg, and 200 mg.
- Adverse events: Most common adverse reactions (≥1%) in those receiving 100 mg and 200 mg include nasopharyngitis, nausea, headache, herpes simplex, increased blood creatinine phosphokinase, dizziness, urinary tract infection, fatigue, acne, vomiting, oropharyngeal pain, influenza, and gastroenteritis.
- Mechanism of action: Abrocitinib reversibly inhibits JAK1 by blocking the adenosine triphosphate binding site. In a cell-free isolated enzyme assay, abrocitinib was selective for JAK1 over JAK2 (28-fold), JAK3 (>340-fold), and tyrosine kinase 2 (43-fold), as well as the broader kinome. The relevance of inhibition of specific JAK enzymes to therapeutic effectiveness is not currently known. Both the parent compound and the active metabolites inhibit JAK1 activity in vitro with similar levels of selectivity.
- Manufacturer: Pfizer