Vortioxetine is a synthetic pharmaceutical active ingredient belonging to the serotonin modulator and stimulator class. It is used as Vortioxetine Hydrobromide, the hydrobromide salt of vortioxetine. Vortioxetine has a multimodal pharmacological profile involving serotonin receptor modulation together with inhibition of serotonin reuptake.
Vortioxetine Hydrobromide is chemically known as 1-{2-[(2,4-dimethylphenyl)sulfanyl]phenyl}piperazine monohydrobromide. The drug substance has the molecular formula C18H22N2S·HBr and a molecular weight of 379.36 g/mol. The hydrobromide substance is identified by CAS Number 960203-27-4.
The drug substance is described as a white to very slightly beige powder. It is slightly soluble in water and soluble in ethanol and methanol. Its aqueous solubility is pH dependent, with reported solubility equivalent to approximately 1.3 mg/mL of vortioxetine base at pH 5.5 and approximately 50 µg/mL of vortioxetine base at pH 7.4.
Vortioxetine is an achiral molecule, with no defined stereocenters. The active moiety has a molecular weight of approximately 298.45 g/mol, while the hydrobromide salt has a relative molecular mass of 379.36 g/mol.
Vortioxetine contains an N-aryl piperazine structure connected to a substituted phenylthio group. Its chemical structure includes two aromatic rings, a sulfur linkage and a piperazine ring. These structural characteristics contribute to its physicochemical and pharmacological properties.
The drug substance has reported pKa values of approximately 9.1 ± 0.1 and 3.0 ± 0.2. Because of its ionization characteristics, the solubility of Vortioxetine Hydrobromide varies with the pH of the surrounding medium.
Vortioxetine has a multimodal mechanism involving several components of the serotonin system. It inhibits the serotonin transporter and also interacts with several serotonin receptors, including agonist, partial agonist and antagonist activity at different receptor subtypes.
The combined activity of vortioxetine distinguishes it from conventional selective serotonin reuptake inhibitors and forms the basis of its classification as a serotonin modulator and stimulator.
Vortioxetine Hydrobromide is the pharmaceutical salt form used in the marketed drug product. Current product information identifies the beta polymorph of Vortioxetine Hydrobromide in the immediate-release tablet formulation.
Control of the physical form is therefore an important consideration during API manufacturing and pharmaceutical development. Appropriate characterization can include chromatographic, spectroscopic and solid-state analytical procedures.
Vortioxetine Hydrobromide is a chemically synthesized small-molecule API. Manufacturing requires appropriate control of starting materials, intermediates, reaction conditions, purification and final crystallization.
Quality control of Vortioxetine Hydrobromide can include identity testing, assay determination, organic impurity testing, residual-solvent analysis, physical-form characterization and particle-size evaluation. The proposed USP drug-substance monograph includes validated chromatographic procedures for assay and organic impurities.
Analytical characterization can include IR spectroscopy, HPLC, gas chromatography and other validated analytical procedures. USP information identifies separate liquid- and gas-chromatographic procedures for the drug substance and lists Vortioxetine Related Compounds G, H and I as reference standards.
Vortioxetine Hydrobromide is primarily associated with pharmaceutical development and manufacturing of products used for major depressive disorder. The marketed immediate-release tablet contains Vortioxetine Hydrobromide as the active pharmaceutical ingredient.
Vortioxetine API is therefore relevant to pharmaceutical formulation development, analytical development, generic drug development and commercial API manufacturing.
Important quality attributes for Vortioxetine Hydrobromide include chemical identity, assay, organic impurities, residual solvents, physical form, particle-size characteristics and appropriate control of the salt form.
Because USP currently identifies the Vortioxetine Hydrobromide monograph as a proposed monograph, exact numerical acceptance criteria should be taken from the applicable validated API specification rather than presented as established USP limits.
Swapnroop Drugs & Pharmaceuticals provides pharmaceutical API solutions for pharmaceutical development and manufacturing requirements. Vortioxetine Hydrobromide is relevant to pharmaceutical applications involving serotonin-modulating antidepressant therapies.
Vortioxetine API can be evaluated according to the required pharmaceutical quality, analytical, regulatory and commercial specifications. Appropriate documentation and validated analytical testing are important for maintaining consistent API quality.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |