Olodaterol is a long-acting, selective β₂-adrenergic receptor agonist (LABA) used as a bronchodilator. The pharmaceutical active substance is olodaterol hydrochloride, developed under the code BI 1744 / BI-1744 CL. It is used for long-term maintenance treatment of airflow obstruction associated with chronic obstructive pulmonary disease (COPD).
Olodaterol hydrochloride is a synthetic small-molecule compound belonging to the benzoxazinone-derived β₂-adrenoceptor agonist class. The free-base olodaterol has a molecular weight of 386.44 g/mol, while the hydrochloride salt has a molecular weight of 422.90 g/mol.
Olodaterol selectively activates β₂-adrenergic receptors in airway smooth muscle. Activation of these receptors increases intracellular cyclic AMP and promotes relaxation of bronchial smooth muscle, producing prolonged bronchodilation.
The drug substance is specifically the R-enantiomer; the S-enantiomer is controlled as a related stereochemical impurity.
Olodaterol hydrochloride is used as a long-acting bronchodilator for maintenance treatment of airflow obstruction in patients with COPD, including chronic bronchitis and emphysema. It is the active drug substance in STRIVERDI RESPIMAT and is also used in combination with tiotropium in STIOLTO RESPIMAT.
The regulatory assessment describes olodaterol hydrochloride as a white to off-white crystalline non-hygroscopic powder. It is reported as sparingly to slightly soluble (>20–1.1 mg/mL) over the entire pH range, soluble in ethanol and freely soluble in methanol. The drug substance is specifically identified as the anhydrous form, with no polymorphs observed in the assessed material.
Olodaterol hydrochloride can be characterized using:
The regulatory quality assessment confirms that the drug-substance control strategy includes related substances including the S-enantiomer, solvents, metal catalyst residues, sulphated ash, heavy metals, water content and assay.
Unlike products where several commercially relevant polymorphs must be controlled, the regulatory assessment for olodaterol hydrochloride states that the drug substance is anhydrous and that polymorphs have not been observed in the characterized material.
The regulatory assessment reports stability studies at 25°C/60% RH, 30°C/75% RH and 40°C/75% RH, with a 48-month approved retest period and no special storage conditions for the solid drug substance. The material is sensitive to light when dissolved in water.
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder or crystals |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 0.5% |
| Residue on Ignition | NMT 0.2% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 1.0% |
| Melting Point | 153–155°C |