Active moiety
Active Moiety[edit | edit source]
An active moiety refers to the part of a drug or compound that is responsible for its biological or pharmacological effects. In pharmacology, understanding the active moiety is crucial for drug development, as it helps in identifying the component of a drug that interacts with biological targets to produce a therapeutic effect.
Definition[edit | edit source]
The term "active moiety" is defined by the U.S. Food and Drug Administration (FDA) as the molecule or ion, excluding those appended portions of the molecule that cause the drug to be an ester, salt (including a salt with hydrogen or coordination bonds), or other noncovalent derivative (such as a complex, chelate, or clathrate) of the molecule, responsible for the physiological or pharmacological action of the drug substance.
Importance in Drug Development[edit | edit source]
Understanding the active moiety is essential in the process of drug development and pharmacokinetics. It allows researchers to:
- Identify the specific part of the drug that interacts with the biological target, such as a receptor or enzyme.
- Optimize the drug's efficacy by modifying the active moiety to enhance its interaction with the target.
- Reduce side effects by minimizing interactions with non-target sites.
- Develop generic drugs by focusing on the active moiety rather than the entire drug compound.
Examples[edit | edit source]
- In the case of aspirin, the active moiety is the salicylate ion, which is responsible for its anti-inflammatory and analgesic effects.
- For prodrugs like enalapril, the active moiety is enalaprilat, which is formed after the prodrug is metabolized in the body.
Regulatory Considerations[edit | edit source]
Regulatory agencies, such as the FDA, often focus on the active moiety when considering the approval of new drugs or generic drug applications. The active moiety is a key factor in determining whether a new drug is considered a "new chemical entity" (NCE) or if it is similar enough to existing drugs to be considered a generic.
Also see[edit | edit source]
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