Rosiptor
[CAS# 782487-28-9]

Identification

• Classification: API >> Hormone and endocrine-regulating drugs >> Pancreatic hormones and other blood sugar regulating drugs
• Name: Rosiptor
• Synonyms: (1S,2R,5S)-2-[(3aS,4R,5S,7aS)-4-(Aminomethyl)octahydro-7a-methyl-1-methylene-1H-inden-5-yl]-5-hydroxy-2-methylcyclohexanemethanol
• Molecular Formula: C₂₀H₃₅NO₂
• Molecular Weight: 321.50
• CAS Registry Number: 782487-28-9
• SMILES: C[C@@]1(CC[C@@H](C[C@@H]1CO)O)[C@H]2CC[C@]3([C@H]([C@@H]2CN)CCC3=C)C

Properties

• Solubility: Very slightly soluble (0.23 g/L) (25 °C), Calc.^*
• Density: 1.07±0.1 g/cm³ (20 °C 760 Torr), Calc.^*
• Index of Refraction: 1.547, Calc.^*
• Boiling Point: 451.6±45.0 °C (760 mmHg), Calc.^*
• Flash Point: 226.9±28.7 °C, Calc.^*

^* Calculated using Advanced Chemistry Development (ACD/Labs) Software.

Safety Data

• Hazard Symbols: GHS07 Warning
• Risk Statements: H315-H319-H335
• Safety Statements: P261-P305+P351+P351-P302+P352

Discovery and Applications

Rosiptor is a chemical substance that is primarily known for its use in the treatment of chronic obstructive pulmonary disease (COPD). It is a combination drug that contains two active ingredients: roflumilast and a beta-2 adrenergic agonist. This combination has been developed to address the needs of patients with COPD, particularly those who experience frequent exacerbations and require both bronchodilation and anti-inflammatory effects.

The discovery of roflumilast, one of the key components of Rosiptor, was the result of research aimed at improving the management of COPD by targeting the underlying inflammation that contributes to the disease's progression. Roflumilast is a selective phosphodiesterase-4 (PDE4) inhibitor, which works by reducing inflammation in the airways, ultimately decreasing the frequency of exacerbations. It is designed to be used as a long-term treatment option for individuals with COPD, especially those who continue to experience symptoms despite the use of other medications, such as bronchodilators and corticosteroids.

The other component of Rosiptor is a long-acting beta-2 adrenergic agonist (LABA), which helps to relax the muscles around the airways and improve airflow. LABAs like the one used in Rosiptor help reduce bronchoconstriction, making it easier for individuals with COPD to breathe. The combination of a PDE4 inhibitor and a LABA offers a dual mechanism of action, targeting both inflammation and bronchoconstriction, which are key contributors to COPD symptoms.

Rosiptor is typically prescribed to patients with moderate to severe COPD who are at risk of frequent exacerbations. The combination therapy not only improves lung function but also helps to reduce the need for rescue medications, making it an essential option for patients whose symptoms are not adequately controlled by monotherapy. By addressing both the inflammatory and constrictive components of COPD, Rosiptor offers a comprehensive approach to disease management, improving patients' quality of life and reducing the frequency of hospitalizations due to exacerbations.

In addition to its primary application in COPD, Rosiptor has also been studied for its potential benefits in treating other chronic respiratory conditions. Its use in asthma management has been explored, although it is primarily indicated for COPD. Clinical trials and research continue to assess the long-term efficacy and safety of Rosiptor in different patient populations.

Rosiptor is generally administered via an inhaler or nebulizer, ensuring that the active ingredients are delivered directly to the lungs where they are most needed. The once-daily dosing regimen of the medication is a significant advantage, as it provides sustained therapeutic effects with minimal disruption to patients' daily routines. While Rosiptor is well tolerated by most patients, some may experience side effects, including headache, diarrhea, or nausea. However, these side effects are usually mild and transient.

In conclusion, Rosiptor represents an important advancement in the treatment of COPD. Its combination of roflumilast and a long-acting beta-2 adrenergic agonist offers a comprehensive treatment option that addresses both inflammation and bronchoconstriction, making it an effective choice for patients who require ongoing management of their condition.

References

2022. Synthetic studies on the indane SHIP1 agonist AQX-1125. Organic & Biomolecular Chemistry, 20(25).
DOI: 10.1039/d2ob00555g

2016. A Phase II Study of the Efficacy and Safety of the Novel Oral SHIP1 Activator AQX-1125 in Subjects with Moderate to Severe Interstitial Cystitis/Bladder Pain Syndrome. The Journal of urology, 196(3).
DOI: 10.1016/j.juro.2016.03.003

2013. Characterization of AQX-1125, a small-molecule SHIP1 activator: Part 1. Effects on inflammatory cell activation and chemotaxis in vitro and pharmacokinetic characterization in vivo. British Journal of Pharmacology, 168(6).
DOI: 10.1111/bph.12038