Products
Revefenacin was approved in the United States in 2018 as a monodose inhalation solution (Yupelri). The active ingredient belongs to the LAMA group.
Structure and properties
Revefenacin (C35H43N5O4, Mr = 597.8 g/mol) exists as a white crystalline powder and is sparingly soluble in water. It has an active metabolite formed by hydrolysis.
Effects
Revefenacin has bronchodilator and parasympatholytic (anticholinergic) properties. The effects are due to the reversal of the effects of acetylcholine on airway smooth muscle cells, which induces bronchoconstriction. Revefenacin is a selective, competitive, and reversible antagonist at muscarinic acetylcholine receptors. Revefenacin belongs to the LAMAs and, accordingly, has a long duration of action of more than 24 hours.
Indications
For maintenance therapy of chronic obstructive pulmonary disease (COPD).
Dosage
According to the SmPC. The solution is inhaled once daily with a nebulizer (nebulizer). Clinical studies were performed with PARI models.
Contraindications
- Hypersensitivity
Revefenacin is not suitable for the treatment of acute symptoms (bronchospasm). Full precautions can be found in the drug label.
Interactions
Drug-drug interactions may occur with other anticholinergics. The active metabolite of revefenacin is a substrate of OATP1B1 and OATP1B3. Inhibitors such as rifampicin and ciclosporin may increase concentrations of the active metabolite.
Adverse effects
The most common potential adverse effects include cough, upper respiratory tract infection, headache, and back pain.
