Olodaterol API Manufacturers & Suppliers
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Olodaterol | CAS No: 868049-49-4 | GMP-certified suppliers
A medication that provides long-lasting bronchodilation to manage chronic obstructive pulmonary disease, including chronic bronchitis and emphysema, improving airflow and respiratory function.
Therapeutic categories
Primary indications
- Olodaterol is indicated for use in chronic obstructive pulmonary disease (COPD), including chronic bronchitis and/or emphysema
- It is not indicated for the treatment of acute exacerbations of COPD or for the treatment of asthma
Product Snapshot
- Olodaterol is available primarily as a respiratory inhalation solution and aerosol metered sprays
- It is indicated for maintenance treatment in chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema
- The product is approved for use in major regulatory markets including the United States and Canada
Clinical Overview
Pharmacologically, olodaterol exhibits high selectivity and potency for human beta2-adrenergic receptors, which are predominantly expressed in pulmonary smooth muscle. Unlike beta1-adrenergic receptors found in cardiac tissue or beta3 receptors in adipose tissue, olodaterol’s activity at these receptors is minimal, reducing off-target cardiac and metabolic effects. Upon receptor binding, olodaterol activates a G protein-coupled receptor pathway that stimulates adenylate cyclase, increasing intracellular cyclic adenosine monophosphate (cAMP) levels. Elevated cAMP activates protein kinase A (PKA), leading to relaxation of airway smooth muscle and sustained bronchodilation. This mechanism facilitates improved airflow as reflected by increased forced expiratory volume (FEV1) observed up to 24 hours post-dosing, supporting once-daily administration.
Regarding pharmacokinetics, olodaterol is administered via inhalation, enabling targeted action in the lungs and minimizing systemic exposure. It is metabolized predominantly by cytochrome P450 enzymes CYP2C8 and CYP2C9, necessitating consideration of potential drug interactions involving these pathways. Although detailed absorption, distribution, metabolism, and excretion (ADME) parameters are compound-specific, olodaterol’s inhaled route generally confers a favorable safety profile.
Safety considerations include the potential for beta2-agonist class effects such as tachycardia, hypertension, and QT interval prolongation; however, olodaterol’s high receptor selectivity reduces these risks relative to non-selective agonists. It is contraindicated in acute bronchospasm and should be used with caution in patients with cardiovascular disorders.
Notable marketed formulations include combinations with muscarinic antagonists to optimize COPD management. In API procurement, ensuring the chemical purity and stereochemical integrity of olodaterol is critical given its boron-containing benzoxazinone structure. Suppliers should provide comprehensive validation data for identity, impurity profiles, and stability under storage conditions to support regulatory compliance and pharmaceutical quality standards.
Identification & chemistry
| Generic name | Olodaterol |
|---|---|
| Molecule type | Small molecule |
| CAS | 868049-49-4 |
| UNII | VD2YSN1AFD |
| DrugBank ID | DB09080 |
Pharmacology
| Summary | Olodaterol is a long-acting beta2-adrenergic receptor agonist that targets beta2 receptors in airway smooth muscle, leading to bronchodilation through cAMP-mediated relaxation. It demonstrates high selectivity for beta2 receptors over beta1 and beta3 subtypes, minimizing off-target cardiac and metabolic effects. Its therapeutic intent is to provide sustained bronchodilation in chronic obstructive pulmonary disease (COPD). |
|---|---|
| Mechanism of action | Olodaterol is a long-acting beta2-adrenergic agonist (LABA) that exerts its pharmacological effect by binding and activating beta2-adrenergic receptors located primarily in the lungs. Beta2-adrenergic receptors are membrane-bound receptors that are normally activated by endogenous epinephrine whose signalling, via a downstream L-type calcium channel interaction, mediates smooth muscle relaxation and bronchodilation. Activation of the receptor stimulates an associated G protein which then activates adenylate cyclase, catalyzing the formation of cyclic adenosine monophosphate (cAMP) and protein kinase A (PKA). Elevation of these two molecules induces bronchodilation by relaxation of airway smooth muscles. |
| Pharmacodynamics | Olodaterol is a potent agonist of the human beta2-adrenergic receptor in vitro, and is highly selective for this receptor, with much lower levels of activity at the b1- and b3-adrenergic receptors that are commonly expressed on cardiac smooth muscle and adipose tissue, respectively. Binding to the receptor causes smooth muscle relaxation in the lungs and bronchodilation. It has also been shown to potently reverse active bronchoconstriction. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Beta-2 adrenergic receptor | Humans | agonist |
ADME / PK
| Absorption | Olodaterol reaches maximum plasma concentrations generally within 10 to 20 minutes following drug inhalation. In healthy volunteers, the absolute bioavailability of olodaterol following inhalation was estimated to be approximately 30%, whereas the absolute bioavailability was below 1% when given as an oral solution. Thus, the systemic availability of olodaterol after inhalation is mainly determined by lung absorption, while any swallowed portion of the dose only negligibly contributes to systemic exposure. |
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| Half-life | The terminal half-life following intravenous administration is 22 hours. The terminal half-life following inhalation in contrast is about 45 hours, indicating that the latter is determined by absorption rather than by elimination processes. |
| Protein binding | In vitro binding of olodaterol to human plasma proteins is independent of concentration and is approximately 60%. |
| Metabolism | Olodaterol is substantially metabolized by direct glucuronidation and by O-demethylation at the methoxy moiety followed by conjugation. Of the six metabolites identified, only the unconjugated demethylation product binds to beta2-receptors. This metabolite, however, is not detectable in plasma after chronic inhalation of the recommended therapeutic dose. Cytochrome P450 isozymes CYP2C9 and CYP2C8, with negligible contribution of CYP3A4, are involved in the O-demethylation of olodaterol, while uridine diphosphate glycosyl transferase isoforms UGT2B7, UGT1A1, 1A7, and 1A9 were shown to be involved in the formation of olodaterol glucuronides. |
| Route of elimination | Following intravenous administration of [14C]-labeled olodaterol, 38% of the radioactive dose was recovered in the urine and 53% was recovered in feces. The amount of unchanged olodaterol recovered in the urine after intravenous administration was 19%. Following oral administration, only 9% of olodaterol and/or its metabolites was recovered in urine, while the major portion was recovered in feces (84%). |
| Volume of distribution | The volume of distribution is high (1110 L), suggesting extensive distribution into tissue. |
| Clearance | Total clearance of olodaterol in healthy volunteers is 872 mL/min, and renal clearance is 173 mL/min. |
Formulation & handling
- Olodaterol is a small molecule suitable for oral, buccal, and respiratory (inhalation) administration routes, with multiple metered aerosol and solution formulations.
- The compound exhibits low aqueous solubility (7.03e-02 g/l) and moderate lipophilicity (LogP 1.19), which should be considered in formulation strategies for optimal bioavailability.
- Stability and handling requirements align with typical small molecules; no specific sensitivities to food or peptide/biologic-related concerns are noted.
Regulatory status
| Lifecycle | The API is marketed in the United States and Canada with initial patents expiring between 2017 and 2018, while later patents extend exclusivity in the US until 2027 and 2031, indicating a phased market maturity across regions. |
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| Markets | Canada, US |
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Supply Chain
| Supply chain summary | Olodaterol is marketed primarily through multiple branded products in the US and Canadian markets, indicating the presence of several originator companies involved in its manufacturing and supply. The patent portfolio includes protections extending in the US until at least 2027, with some patents expiring earlier, suggesting a phased potential entry of generic competition. The focus on North American markets highlights a regional supply chain footprint without significant expansion into European or other global markets. |
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Safety
| Toxicity | Adverse drug reactions that occurred at a frequency greater than 2% include nasopharyngitis (11.3%), upper respiratory tract infection (8.2%), bronchitis (4.7%), urinary tract infection (2.5%), cough (4.2%), dizziness (2.3%), rash (2.2%), diarrhea (2.9%), back pain (3.5%), and arthralgia (2.1%). |
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- Handle olodaterol with caution to minimize exposure due to potential respiratory and dermatologic adverse effects, including nasopharyngitis, bronchitis, cough, and rash
- Use appropriate respiratory protection and skin contact prevention measures during manufacturing and handling to reduce inhalation and dermal exposure risks
- Monitor for signs of irritation or sensitization in personnel routinely exposed to the substance
Olodaterol is a type of Adrenergic agents
Adrenergic agents are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that target the adrenergic system in the body. This system is responsible for regulating various physiological responses, including heart rate, blood pressure, and smooth muscle contraction.
Adrenergic agents can be further divided into two main groups: adrenergic agonists and adrenergic antagonists. Adrenergic agonists stimulate the adrenergic receptors, leading to an increase in sympathetic nervous system activity. This can result in effects such as vasoconstriction, bronchodilation, and increased heart rate. Adrenergic agonists are commonly used in the treatment of conditions such as asthma, hypotension, and cardiac arrest.
On the other hand, adrenergic antagonists block the adrenergic receptors, thereby inhibiting the effects of sympathetic nervous system activation. These agents are often employed to lower blood pressure, treat certain heart conditions, and manage symptoms associated with conditions like benign prostatic hyperplasia. Adrenergic antagonists can be further classified into alpha-adrenergic antagonists and beta-adrenergic antagonists, based on their selectivity for different adrenergic receptor subtypes.
Pharmaceutical companies extensively utilize adrenergic agents as key components in the development of various medications. Adrenergic APIs offer targeted effects on the adrenergic system, allowing for precise modulation of physiological responses. The understanding of adrenergic agents and their mechanisms of action is vital for the design and optimization of drugs used in the treatment of numerous medical conditions. Researchers and scientists continue to explore and innovate within this subcategory to develop new adrenergic agents with enhanced efficacy and fewer side effects, ultimately improving patient outcomes.
Olodaterol (Adrenergic agents), classified under Central Nervous System Agents
Central Nervous System (CNS) Agents are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that specifically target the central nervous system. The CNS encompasses the brain and spinal cord, playing a vital role in regulating and controlling various bodily functions, including cognition, movement, emotions, and sensory perception. These agents are designed to interact with specific receptors, enzymes, or ion channels within the CNS to modulate neural activity and restore normal functioning.
CNS agents comprise a diverse range of pharmaceutical APIs, including analgesics, anesthetics, antipsychotics, sedatives, hypnotics, anti-epileptics, and antidepressants. Each subcategory addresses distinct neurological disorders and conditions. For instance, analgesics alleviate pain by targeting receptors in the brain and spinal cord, while antipsychotics are employed to manage psychosis symptoms in mental illnesses such as schizophrenia.
The development of CNS agents involves rigorous research, molecular modeling, and extensive clinical trials to ensure safety, efficacy, and specific target engagement. Pharmaceutical companies invest significant resources in identifying novel drug targets, synthesizing new compounds, and optimizing their pharmacological properties. These agents undergo rigorous regulatory evaluations and must adhere to stringent quality standards and guidelines.
Given the prevalence of CNS disorders globally, the market demand for effective CNS agents is substantial. The development of innovative CNS APIs not only improves patient outcomes but also provides valuable commercial opportunities for pharmaceutical companies. Continued advancements in CNS agent research and development hold the promise of groundbreaking therapies that can improve the quality of life for individuals affected by neurological conditions.
