Vilanterol

Products

Vilanterol is commercially available as a fixed combination with fluticasone furoate in powder inhaler form (Relvar Ellipta / Breo Ellipta). It was approved in the US and EU in 2013 and in many countries in 2014. The fixed combination with umeclidinium bromide (Anoro Ellipta) was also registered in many countries in 2014. In 2017, a combination of umeclidinium bromide, fluticasone furoate, and vilanterol was released (Trelegy Ellipta), and in many countries in 2018.

Structure and properties

Vilanterol (C₂₄H₃₃Cl₂NO₅, M_r = 486.4 g/mol) is structurally related to epinephrine and other beta2-sympathomimetics such as salbutamol (Ventolin, generics) and is a saligenin derivative. It is an analog of salmeterol (Serevent, Seretide, all GlaxoSmithKline) and was developed as an antedrug. In the drug product, it is present as vilanterol trifenate, a white powder that is virtually insoluble in water.

Effects

Vilanterol (ATC R03AK10, ATC R03AL03) has bronchodilator (bronchospasmolytic) properties. It is a long-acting, beta2-specific sympathomimetic with relaxing effects on bronchial smooth muscle. The effects occur rapidly, within 5-15 minutes, and last for a long time, approximately 24 hours (LABA).

Indications

• Chronic obstructive pulmonary disease (COPD).
• Bronchial asthma (only fixed combination with fluticasone furoate).

Dosage

According to the professional information. The drug, unlike other agents in the same group, only needs to be inhaled once daily, which may be an advantage for treatment adherence.