Bimekizumab

Monoclonal antibody approved in the EU as the first selective inhibitor of the interleukins (IL) IL-17A and IL-17F. Bimzelx® (bimekizumab) entered the German market on September 15, 2021 for the treatment of plaque psoriasis. Two anti-IL-17A antibodies, ixekizumab and secukinumab, are already approved as of September 2021 for the treatment of patients with psoriasis, psoriatic arthritis and ankylosing spondylitis. These have been shown in clinical trials to have superior clinical efficacy compared to the established treatments ustekinumab (anti-IL-12/IL-23) and etanercept (soluble TNF receptor inhibitor), respectively, in psoriasis.

Bimekizumab is a humanized IgG1/κ monoclonal antibody that selectively binds with high affinity to the cytokines IL-17A as well as IL-17F, blocking their interaction with the IL-17RA/IL-17RC receptor complex. Misregulated expression of IL-17A and IL-17F is associated with chronic inflammatory diseases such as psoriasis, psoriatic arthritis, rheumatoid arthritis, ankylosing spondylitis(ankylosing spondylitis) and certain forms of bronchial asthma.

Bimekizumab is a monoclonal antibody. The drug can be expected to be degraded into small peptides and amino acids via catabolic pathways, analogous to endogenous immunoglobulins. The mean terminal half-life is 23 days.

Pregnancy: To date, there is very limited experience with the use of bimekizumab in pregnant women. Animal studies did not reveal any evidence of direct or indirect adverse health effects related to pregnancy, embryonic/fetal development, parturition, or postnatal development. However, for precautionary reasons, use of bimekizumab during pregnancy should be avoided.

Lactation: It is not known whether bimekizumab passes into breast milk. Since a risk to the newborn/infant cannot be excluded, a decision must be made as to whether breastfeeding should be interrupted or whether treatment with bimekizumab should be discontinued. Both the benefit of breastfeeding for the child and the benefit of the therapy for the woman have to be taken into account

Dosing: 320 mg in two subcutaneous injections at 0-4-8-12 and 16 weeks apart, then every 8 weeks - Rapid response: At 4 weeks and PASI 90 in 87% of patients at week 48.

Most commonly reported were upper respiratory tract infections (14.5%) (most commonly nasopharyngitis) and oral candidiasis (7.3%).

Since the formation of some cytochrome 450 enzymes are suppressed by increased cytokine levels in chronic inflammation, treatment with Bimzelx, may result in normalization of CYP450 levels. This may result in lower exposure of CYP450-metabolized drugs.

Therefore, when using CYP450 substrates with a narrow therapeutic range (e.g., warfarin), the dose should be individually adjusted and therapeutic monitoring should be considered at the start of bimekizumab therapy.

Furthermore, live vaccines should not be administered during treatment with bimekizumab.

Bimekizumab must not be used in case of:

• Hypersensitivity to the active substance or any of the other ingredients mentioned.
• Clinically relevant active infections such as active tuberculosis.
• concomitant use of live vaccines
• Trafficability: Bimekizumab has no or negligible effect on trafficability and the ability to operate machinery.

^Bimzelx®

1. Adams R et al (2021) Bimekizumab, a Novel Humanized IgG1 Antibody That Neutralizes Both IL-17A and IL-17F. Front Immunol. 11:1894
2. Blauvelt A et al (2020) Bimekizumab for patients with moderate to severe plaque psoriasis: 60-week results from BE ABLE 2, a randomized, double-blinded, placebo-controlled, phase 2b extension study. J Am Acad Dermatol. 83: 1367-1374.

3. Malakouti M et al (2015) The role of IL-17 in psoriasis. J Dermatolog Treat 26:41-44.