Levalbuterol

Bronchial asthma is a chronic respiratory disease with a continuously rising prevalence globally. In racemic albuterol commonly used in clinical practice, the dextrorotatory component not only has no obvious anti-asthmatic effect, but also may cause adverse reactions such as hand tremor and palpitations. As a highly selective β₂ adrenoceptor agonist, levalbuterol is the single effective levo-enantiomer of racemic albuterol. It can rapidly relax airway smooth muscle and relieve bronchospasm by activating β₂ receptors on airway smooth muscle, and its incidence of adverse reactions is significantly lower than that of the racemic dosage form. It is mainly used for the treatment of adult and pediatric patients aged 6 years and older with bronchial asthma and chronic obstructive pulmonary disease (COPD) accompanied by bronchospasm, and is one of the first-choice relieving medications for clinically mild to moderate acute asthma attacks.

The global market size of levalbuterol exceeded USD 1.8 billion in 2023, with an annual compound growth rate maintained at approximately 7.2%. The growth momentum mainly comes from the rising prevalence of respiratory diseases and the increasing clinical demand for highly safe anti-asthmatic drugs. For the domestic market, levalbuterol has been included in the centralized procurement catalogs of multiple provinces since 2020, with the terminal price dropping by 68% during the procurement cycle, which has rapidly promoted the increase of its clinical penetration rate at the primary level. The domestic market size is expected to exceed RMB 1.2 billion in 2024. At present, the domestic preparation market is mainly dominated by the original research product and 3 local generic pharmaceutical enterprises, and the upstream API supply still has large space for domestic substitution, and there is no publicly verifiable data on the concentration of API production capacity.

The original research enterprise of levalbuterol is GlaxoSmithKline in the United Kingdom, with the original trade name "Xopenex". Its core compound patent for the US market expired in 2010, and the compound patent within the territory of China also expired in 2010. The main marketed dosage forms of the original drug include inhalation solution (0.31mg/3ml, 0.63mg/3ml, 1.25mg/3ml) and aerosol (each actuation contains 45μg of levalbuterol). Among them, the inhalation solution has been included in the *Catalogue of Reference Preparations for Chemical Drugs (29th Batch)* of China, and is also listed in the FDA Reference Preparation Catalogue. Up to now, 5 domestic enterprises have obtained Class A status for their levalbuterol APIs through CDE registration, and another 12 enterprises have obtained marketing approval for levalbuterol inhalation solution. (Data as of June 2025, please refer to the official CDE website for the latest information)

CATO provides a full set of levalbuterol impurity reference standards, covering all categories of enantiomeric impurities, process impurities and degradation impurities, which can meet the full-process research requirements of API synthesis process optimization, quality research and generic drug consistency evaluation. Most products are in stock, and in-stock products ordered before 16:00 will be shipped on the same day. All reference standards comply with the compliance requirements of multiple regulations including the Chinese Pharmacopoeia and FDA, and complete structure confirmation and content calibration reports can be provided.