Varenicline is a critical pharmaceutical intermediate and API used in smoking cessation therapy. As a partial agonist of α4β2 nicotinic acetylcholine receptors, Varenicline provides relief from nicotine withdrawal symptoms while reducing the rewarding effects of smoking. The clinical success of Varenicline has established it as a first-line pharmacotherapy for smoking cessation, marketed under the trade names Chantix® and Champix®. In quality control contexts, Varenicline and its related substances—including various impurities and degradation products—are critical reference standards for analytical method development, method validation, and quality control applications. As a key smoking cessation therapeutic, Varenicline represents a significant advancement in addiction medicine, offering patients a pharmacologically targeted approach to achieving sustained tobacco abstinence.
Product Parameters
|
Parameter |
Specification |
|
Product Name |
Varenicline |
|
CAS Number |
249296-44-4 |
|
Molecular Formula |
C₁₃H₁₃N₃ |
|
Molecular Weight |
211.26 g/mol |
|
Physical Form |
Solid powder |
|
Melting Point |
138.5 °C |
|
Boiling Point |
400.6 ± 40.0 °C (Predicted) |
|
Density |
1.247 ± 0.06 g/cm³ (Predicted) |
|
pKa |
9.60 ± 0.20 (Predicted) |
|
Storage Condition |
–20 °C |
Mechanism Of Action
Product Advantages
Varenicline is a partial agonist of the α4β2 nicotinic acetylcholine receptor. It stimulates nicotine receptors more weakly than nicotine itself, providing relief from withdrawal symptoms, while simultaneously blocking nicotine from binding to these receptors, reducing the rewarding effects of smoking.
Clinically Validated Smoking Cessation Agent
Varenicline is a first-line pharmacotherapy for smoking cessation, marketed as Chantix® and Champix®. Clinical trials have demonstrated superior efficacy compared to placebo and other smoking cessation agents, making Varenicline the standard of care for tobacco dependence treatment.
Unique Pyrazino-Benzazepine Scaffold
The tetracyclic pyrazino-benzazepine scaffold of Varenicline is structurally related to the natural alkaloid cytisine. This unique scaffold provides high-affinity binding to α4β2 nAChRs with optimal partial agonist activity.
Dual-Use: API and Impurity Reference Standard
Varenicline serves as both the active pharmaceutical ingredient for smoking cessation and a reference standard for analytical method development. Related impurities—including nitrosamine impurities and regioisomeric impurities—are critical reference standards for spiking studies, method validation, and impurity profiling.
Well-Established Clinical and Regulatory Profile
Varenicline has been approved for smoking cessation in multiple countries, with extensive clinical data supporting its efficacy, safety, and tolerability. Generic manufacturers rely on Varenicline reference standards for ANDA filings and commercial production.
FAQ
A: Varenicline is a partial agonist of the α4β2 nicotinic acetylcholine receptor. It stimulates nicotine receptors more weakly than nicotine itself (providing relief from withdrawal symptoms) while blocking nicotine from binding to these receptors (reducing the rewarding effects of smoking).
Q2: What is the difference between Varenicline and varenicline tartrate?
A: Varenicline is the free base form of the drug, while varenicline tartrate (CAS 375815-87-5) is the tartrate salt used in pharmaceutical formulations. Varenicline serves as the key synthetic intermediate for manufacturing varenicline tartrate.
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