dupilumab

History

Dupilumab was first approved by the FDA in 2017 for atopic dermatitis. In the United States, subsequent approvals extended to include moderate-to-severe asthma in 2018, based on Phase III trials that confirmed improvements in lung function and reductions in exacerbation frequency. Further, Dupixent was approved for chronic rhinosinusitis with nasal polyposis (CRSwNP), an indication where inflammatory mediators play a key role in symptomatology. More recently, the FDA approved Dupixent for eosinophilic esophagitis in patients 12 years and older, representing a significant advance in managing this debilitating gastrointestinal disorder. Additionally, the drug received approval for prurigo nodularis, thereby expanding its portfolio of applications in chronic dermatological diseases characterized by intense pruritus.

Uses

Dupilumab, also known as Dupixent, is a treatment for severe atopic eczema.

Mechanism of action

Biologics work by blocking ILs from binding to their cell receptors (protein molecules that receive chemical signals from outside a cell); this stops the immune system from overreacting. Dupilumab works on two specific ILs thought to contribute to atopic conditions: IL-4 and IL-13. By blocking IL-4 and IL-13 from binding to their cell receptors, dupilumab limits the overreaction of the immune system, dampening down the chronic inflammatory response and lessening the symptoms of atopic eczema.

Pharmacokinetics

Dupilumab shows a non-linear rate in regard to the target.Dupilumab is also reported to have a bioavailability of 64%, with the average concentration occurring one week after in one week after injection.

Side effects

The most common side effects reported by the US Food and Drug Administration (FDA) include injection site reactions, upper respiratory tract infections, joint pain, and herpes viral infections.The most common side effects reported by the European Medicines Agency (EMA) include injection-site reactions (such as redness, swelling including due to fluid build-up, itching and pain), conjunctivitis (redness and discomfort in the eye) including conjunctivitis due to allergy, joint pain, cold sores, and increased blood levels of a type of white blood cell called eosinophils.

IC 50

IL-2; IL-4; IL-13