Fenfluramine is a synthetic serotonergic compound and pharmaceutical active ingredient belonging to the amphetamine-related class of compounds. It acts primarily through the serotonergic system and its pharmacological activity involves serotonin release and modulation of serotonin receptor signaling.
Fenfluramine has CAS Number 458-24-2, molecular formula C₁₂H₁₆F₃N, and molecular weight 231.26 g/mol.
Fenfluramine is a small-molecule pharmaceutical active ingredient. It is the active moiety of fenfluramine hydrochloride, the salt form used in pharmaceutical products.
Fenfluramine and its active metabolite norfenfluramine have activity at serotonin receptors, including 5-HT₂ receptors. The current FDA labeling states that the precise mechanism responsible for fenfluramine's therapeutic effects in seizures associated with Dravet syndrome and Lennox-Gastaut syndrome is not completely established.
| Parameter | Details |
|---|---|
| Product Name | Fenfluramine |
| CAS Number | 458-24-2 |
| Molecular Formula | C₁₂H₁₆F₃N |
| Molecular Weight | 231.26 g/mol |
| IUPAC Name | N-ethyl-1-[3-(trifluoromethyl)phenyl]propan-2-amine |
| Chemical Type | Synthetic small molecule |
| Pharmacological Class | Serotonergic agent |
| Therapeutic Area | Neurology |
| Related Salt | Fenfluramine Hydrochloride |
Fenfluramine and its metabolite norfenfluramine affect serotonergic neurotransmission. The FDA states that both compounds exhibit agonist activity at 5-HT₂ receptors. The precise mechanism underlying the therapeutic effect in seizure disorders remains unknown.
Because fenfluramine and norfenfluramine have activity at 5-HT₂B receptors, serotonergic pharmacology is clinically important; the FDA labeling notes an association between serotonergic drugs with 5-HT₂B agonist activity and risks of valvular heart disease and pulmonary arterial hypertension.
Fenfluramine hydrochloride is currently used in pharmaceutical formulations for the treatment of seizures associated with Dravet syndrome and Lennox-Gastaut syndrome in appropriate patients.
The approved indication depends on the specific pharmaceutical formulation and applicable regulatory labeling.
Fenfluramine is a synthetic small-molecule API. For pharmaceutical manufacturing, appropriate quality testing may include:
The exact numerical release criteria should be taken from the current manufacturer's approved specification and Certificate of Analysis (CoA).
Pharmaceutical-grade Fenfluramine should be manufactured and tested according to applicable GMP and regulatory requirements. Technical documentation may include:
Store Fenfluramine API in a tightly closed container under the manufacturer's validated storage conditions and protect it from unsuitable temperature, moisture and light exposure.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |