Safinamide is a selective and reversible monoamine oxidase-B (MAO-B) inhibitor used as an antiparkinsonian pharmaceutical active ingredient. The pharmaceutical substance is supplied as Safinamide Mesylate, also known as Safinamide Mesilate, and is identified by CAS No. 202825-46-5. FDA product information describes Safinamide Mesylate as the active pharmaceutical substance used in XADAGO, with a molecular formula of C17H19FN2O2·CH4O3S and molecular weight of 398.45 g/mol.
Safinamide belongs to the antiparkinsonian drug class and is used as an adjunctive treatment in patients with Parkinson's disease. Its primary pharmacological action is selective inhibition of monoamine oxidase-B, an enzyme involved in dopamine metabolism. By inhibiting MAO-B, safinamide helps increase and maintain dopamine availability in the brain.
The active pharmaceutical substance is generally manufactured and supplied as Safinamide Mesylate rather than the free-base form. The mesylate is a 1:1 salt of safinamide and methanesulfonic acid. FDA identifies the pharmaceutical substance as (S)-2-[[4-[(3-fluorophenyl)methoxy]phenyl]methyl]aminopropanamide methanesulfonate.
Safinamide Mesylate has the molecular formula C18H23FN2O5S when the salt is represented as a complete molecular formula and a molecular weight of approximately 398.45 g/mol. The parent free-base Safinamide has CAS 133865-89-1, molecular formula C17H19FN2O2 and molecular weight 302.34 g/mol.
Safinamide Mesylate is described as a white to off-white crystalline powder. Regulatory information identifies an anhydrous polymorphic Form A1 as the form used for the drug substance, with additional polymorphic forms including A2 and a hemi-hydrate form. Control of solid-state form is therefore an important quality attribute during pharmaceutical manufacturing.
Safinamide API is primarily used in the manufacture of pharmaceutical products for Parkinson's disease. As a selective MAO-B inhibitor, it contributes to dopaminergic treatment and is used as an adjunct to levodopa therapy, with or without other Parkinson's disease treatments.
In pharmaceutical manufacturing, consistent control of chemical purity, stereochemical identity, salt form, polymorphic form, residual solvents and related substances is important for producing a reliable Safinamide API.
Quality testing of Safinamide Mesylate can include identity testing, HPLC assay, related-substance analysis, water or moisture determination, residual-solvent testing, elemental impurities, stereochemical purity and solid-state characterization.
A current regulatory assessment from the Australian TGA notes that there was no BP or USP monograph for Safinamide Mesylate at the time of its assessment. Therefore, numerical values should not be presented as USP or BP limits unless supported by a specific current pharmacopoeial source.
Commercial analytical sources report Safinamide Mesylate at ≥98% HPLC purity, which can be used as a reference/commercial specification rather than represented as a universal pharmacopoeial assay.
Safinamide Mesylate manufacturing requires appropriate control of the active stereoisomer, chemical purity, related substances and solid-state form. Analytical procedures should be validated for the intended pharmaceutical application and should be capable of detecting relevant process-related and degradation impurities.
Pharmaceutical manufacturers may require batch-specific Certificates of Analysis, specifications, HPLC chromatograms, residual-solvent information, safety documentation and technical data supporting quality assessment.
Safinamide Mesylate should be protected from excessive moisture and unsuitable environmental conditions. Regulatory information identifies multiple solid-state forms, including a humidity-associated hemi-hydrate, making moisture and polymorphic-form control relevant to storage and manufacturing.
Commercial API packaging should therefore provide suitable protection from moisture, contamination and environmental exposure. Final storage conditions should follow validated stability data and the approved product specification.
Typical documentation for Safinamide API may include a Certificate of Analysis, product specification, batch analytical report, HPLC chromatogram, residual-solvent information, Safety Data Sheet, stability information and technical/regulatory documentation where applicable.
Safinamide Mesylate is a specialized pharmaceutical API used in Parkinson's disease treatment and has a well-defined chemical and stereochemical identity. Its quality profile requires control of assay, related substances, stereochemical purity, residual solvents, moisture and solid-state form.
For pharmaceutical manufacturing, appropriate analytical characterization and controlled production processes are essential to maintain consistent Safinamide API quality and support downstream formulation and regulatory requirements.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Melting Point | 216–217°C |