How Do 5-Lipoxygenase Inhibitors Work?

Reviewed on 11/16/2021

How Do 5-lipoxygenase Inhibitors Work?

Inhibitors of 5-lipoxygenase (5-LO) are medications prescribed for the treatment of asthma, an inflammatory bronchial condition that causes difficulty in breathing. Inhibitors of 5-LO relieve the symptoms of asthma by preventing the formation of leukotrienes, a group of fatty substances released during an asthma attack.

Asthma attacks are often triggered by allergens and the body’s immune system responds by releasing inflammatory substances to attack what it perceives as foreign to the body. Leukotrienes are one of the types of inflammatory molecules released by mast cells, which is part of the body’s frontline immune defense.

Inhibitors of 5-LO work by blocking the activity of 5-LO, an enzyme essential for the biosynthesis of leukotrienes. Inhibiting 5-LO prevents the formation of four types of leukotrienes, LTB4, LTC4, LTD4 and LTE4 which play a major role in promoting inflammation.

Leukotrienes promote inflammation in the following ways:

  • Increase the migration of immune cells such as eosinophils and neutrophils to the airways which further promote inflammation.
  • Induce the aggregation of neutrophils and monocytes, another type of immune cells.
  • Increase the permeability of small blood vessels (capillaries) so that inflammatory proteins and immune cells are able to leak out into the bronchial tissue.
  • Induce the contraction of airway smooth muscles.

Preventing the biosynthesis of leukotriene helps reduce inflammation, swelling of airways, excess mucus secretion and airway constriction, and eases breathing.

How Are 5-lipoxygenase Inhibitors Used?

Inhibitors of 5-lipoxygenase are oral tablets for prophylaxis and treatment of chronic asthma in patients above 12 years of age. Asthma is a condition in which the airways get inflamed, produce excess mucus, and become swollen and narrow, making it difficult to breathe. Inhaled corticosteroids are usually combined with 5-LO inhibitors.

What Are Side Effects of 5-lipoxygenase Inhibitors?

Side effects of 5-lipoxygenase inhibitors may include the following:

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

What Are Names of 5-lipoxygenase Inhibitor Drugs?

The generic and brand names of the FDA-approved 5-lipoxygenase inhibitor drug is:


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