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- Desmethylsertraline
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Desmethylsertraline | CAS No: 87857-41-8 | GMP-certified suppliers
A medication that serves as the major active metabolite of sertraline, involved in central nervous system activity and influencing drug transport via P-glycoprotein inhibition.
Therapeutic categories
Product Snapshot
- Desmethylsertraline is a small molecule compound primarily formulated for oral administration
- It is under investigation for potential applications in central nervous system disorders
- The compound currently holds an experimental approval status and is not yet authorized by major regulatory agencies such as the FDA or EMA
Clinical Overview
No specific clinical indications have been established for desmethylsertraline independent of sertraline. Its pharmacodynamic profile and precise mechanism of action remain incompletely characterized, though its formation reflects hepatic metabolism primarily via cytochrome P450 enzymes. Desmethylsertraline retains structural features common to agents categorized as amines and naphthalenes and is identified as a P-glycoprotein inhibitor, which may influence drug transport and central nervous system penetration.
The compound is classified among agents that reduce seizure threshold, suggesting the potential for proconvulsant effects under certain conditions; however, detailed safety and toxicity data for desmethylsertraline specifically are limited. This aspect warrants caution in populations predisposed to seizures or when combined with other proconvulsant medications.
Key absorption, distribution, metabolism, and excretion (ADME) parameters for desmethylsertraline have been largely inferred from sertraline’s metabolic pathways. The metabolite is generated predominantly in the liver and exhibits a longer half-life than the parent compound, contributing to sertraline’s overall pharmacological activity.
There are no marketed formulations of desmethylsertraline as a distinct API, and its experimental status limits direct clinical application. For pharmaceutical sourcing, high purity and impurity profiling are critical, particularly regarding residual parent sertraline and other related metabolic products. Reliable analytical characterization and adherence to regulatory standards for metabolite impurities are essential when desmethylsertraline is encountered during sertraline API manufacturing or quality control processes.
Identification & chemistry
| Generic name | Desmethylsertraline |
|---|---|
| Molecule type | Small molecule |
| CAS | 87857-41-8 |
| UNII | CJJ71O9BE8 |
| DrugBank ID | DB14071 |
Pharmacology
Targets
| Target | Organism | Actions |
|---|---|---|
| P-glycoprotein 1 | Humans | inhibitor |
Formulation & handling
- Desmethylsertraline is a small molecule with low water solubility, suggesting formulation strategies may require solubilization techniques for oral administration. The compound's high LogP value indicates lipophilicity, potentially affecting absorption and distribution. Stability handling should consider standard solid API protocols due to its solid state and limited aqueous solubility.
Regulatory status
Desmethylsertraline is a type of Antimetabolites
Antimetabolites are a prominent category of pharmaceutical active pharmaceutical ingredients (APIs) utilized in the treatment of various diseases, particularly cancer. These compounds are structurally similar to naturally occurring metabolites essential for cellular processes such as DNA and RNA synthesis. By mimicking these metabolites, antimetabolites interfere with the normal functioning of cellular pathways, leading to inhibition of cancer cell growth and proliferation.
One of the widely used antimetabolites is methotrexate, a folic acid antagonist that inhibits the enzyme dihydrofolate reductase, disrupting the production of DNA and RNA. This disruption impedes the growth of rapidly dividing cancer cells. Another common antimetabolite is 5-fluorouracil (5-FU), which inhibits the enzyme thymidylate synthase, thereby interfering with DNA synthesis and inhibiting cancer cell proliferation.
Antimetabolites can be classified into several subcategories based on their mechanism of action and chemical structure. These include purine and pyrimidine analogs, folic acid antagonists, and pyrimidine synthesis inhibitors. Examples of antimetabolites in these subcategories include azathioprine, cytarabine, and gemcitabine.
Despite their effectiveness, antimetabolites can exhibit certain side effects due to their interference with normal cellular processes. These side effects may include gastrointestinal disturbances, myelosuppression (reduced production of blood cells), and hepatotoxicity.
In conclusion, antimetabolites are a vital category of pharmaceutical APIs used in the treatment of various diseases, especially cancer. By mimicking natural metabolites and disrupting crucial cellular processes, these compounds effectively inhibit cancer cell growth and proliferation. However, their usage should be carefully monitored due to potential side effects.
