Vortioxetine Hydrobromide is a synthetic small-molecule active pharmaceutical ingredient (API) belonging to the class of serotonin modulators and stimulators. It is the hydrobromide salt of vortioxetine and is used in pharmaceutical products for the treatment of major depressive disorder (MDD) in adults. The compound is also identified by the development code Lu AA21004. The FDA-approved TRINTELLIX product contains vortioxetine hydrobromide as its active ingredient.
Vortioxetine Hydrobromide has the molecular formula C18H22N2S·HBr, commonly represented as C18H23BrN2S, and a molecular weight of 379.36 g/mol. Its CAS Number is 960203-27-4. PubChem and FDA-linked chemical records identify the substance under this CAS number.
Vortioxetine Hydrobromide is chemically known as 1-[2-(2,4-Dimethyl-phenylsulfanyl)-phenyl]-piperazine hydrobromide. USP identifies it as Piperazine, 1-{2-[(2,4-dimethylphenyl)thio]phenyl}-, hydrobromide (1:1). The drug substance is a hydrobromide salt of the active moiety vortioxetine.
The molecule contains a piperazine ring connected to substituted aromatic groups through a sulfur linkage. Vortioxetine itself is an N-arylpiperazine and an aryl sulfide. The hydrobromide salt is the pharmaceutical form used in the marketed drug product.
The drug substance is described in regulatory documentation as a white to very slightly beige powder or white to off-white powder. USP reports that Vortioxetine Hydrobromide is soluble in ethanol and methanol and slightly soluble in water.
Vortioxetine has a multimodal serotonergic mechanism of action. FDA documentation states that its antidepressant effect is thought to be associated with enhancement of serotonergic activity through inhibition of serotonin reuptake.
Vortioxetine binds to the serotonin transporter and inhibits serotonin reuptake. It also interacts with several serotonin receptors, including 5-HT3, 5-HT1A, 5-HT7, 5-HT1D and 5-HT1B receptors. FDA characterizes vortioxetine as a 5-HT3, 5-HT1D and 5-HT7 receptor antagonist, a 5-HT1B receptor partial agonist and a 5-HT1A receptor agonist.
This combination of serotonin transporter inhibition and receptor modulation distinguishes vortioxetine from selective serotonin reuptake inhibitors that primarily act through serotonin transporter inhibition.
Vortioxetine Hydrobromide API is relevant to pharmaceutical manufacturers and formulation developers involved in antidepressant and central nervous system pharmaceutical products. As a Vortioxetine Hydrobromide API manufacturer and supplier in India, the material can be positioned for pharmaceutical development, formulation manufacturing and analytical applications requiring controlled-quality API.
Regulatory assessment documents indicate that the active substance specification includes testing for identification, assay, impurities, residual solvents, residue on ignition and heavy metals, with analytical methods appropriately validated for the drug substance.
Quality control of Vortioxetine Hydrobromide should therefore include appropriate chromatographic and spectroscopic procedures for identity, assay and purity, together with controls for process-related impurities, residual solvents and other applicable critical quality attributes.
Vortioxetine Hydrobromide is used as the active pharmaceutical ingredient in products indicated for the treatment of major depressive disorder in adults. FDA-approved TRINTELLIX is available as immediate-release oral tablets in 5 mg, 10 mg and 20 mg strengths.
The FDA label identifies vortioxetine hydrobromide as the active ingredient in TRINTELLIX. The amount of vortioxetine hydrobromide in the tablets is equivalent to 5 mg, 10 mg or 20 mg of vortioxetine, depending on tablet strength.
For pharmaceutical manufacturing purposes, Vortioxetine Hydrobromide can be categorized as an antidepressant API, serotonin modulator API, CNS API and pharmaceutical active ingredient.
Vortioxetine Hydrobromide has a molecular formula of C18H22N2S·HBr and molecular mass of 379.36 g/mol. PubChem reports the molecular formula in salt form as C18H23BrN2S and molecular weight of approximately 379.4 g/mol.
The drug substance is described as a white to very slightly beige powder. USP reports that it is soluble in ethanol and methanol and slightly soluble in water.
Canadian regulatory product information reports a melting point of approximately 231°C. The same regulatory source reports that Vortioxetine Hydrobromide is slightly soluble in water, with aqueous solubility of approximately 1.3 mg/mL at ambient temperature under the stated conditions.
A separate Canadian product monograph reports the pH of a 1% w/v aqueous suspension as approximately 5.05. This is a physicochemical reference value and should not automatically be treated as a universal API release limit.
Quality control of Vortioxetine Hydrobromide API should include suitable analytical methods for identification, assay, organic impurities and residual solvents. USP's proposed drug-substance monograph describes a liquid chromatographic procedure for assay and organic impurities and a gas chromatographic procedure for additional organic impurities.
Regulatory assessment by EMA also confirms that the active-substance specification includes identification by HPLC, FTIR and NIR, assay by HPLC, impurities by HPLC and GC, residual solvents by GC, residue on ignition and heavy metals.
The API may exist in different crystalline and hydrated forms. Published patent literature describes several crystalline forms and demonstrates that water content and solid-state form can vary depending on the particular form and environmental conditions. Therefore, polymorphic form and water content may need to be controlled according to the applicable API specification.
Vortioxetine Hydrobromide is an established CNS pharmaceutical ingredient with extensive clinical and regulatory development. The compound was developed as Lu AA21004 and subsequently used in the development of vortioxetine pharmaceutical products.
During pharmaceutical development, control of chemical purity, related substances, residual solvents and solid-state characteristics is important. Regulatory documentation indicates that commercial and development batches of the active substance were evaluated and found consistent with the applicable specifications.
Vortioxetine Hydrobromide can therefore be categorized as a serotonin modulator API, antidepressant API, CNS API, psychiatric medicine API and pharmaceutical active ingredient.
Vortioxetine Hydrobromide is formulated as an immediate-release oral tablet. FDA-approved TRINTELLIX is available in 5 mg, 10 mg and 20 mg strengths.
The API must meet applicable identity, assay, purity and other quality requirements before incorporation into the finished dosage form. Appropriate controls should be maintained throughout raw-material qualification, API testing, dispensing, blending, compression, coating and finished-product testing.
The FDA label specifies that TRINTELLIX tablets contain vortioxetine hydrobromide equivalent to the labeled amount of vortioxetine. For example, 6.355 mg of vortioxetine hydrobromide corresponds to 5 mg of vortioxetine.
Vortioxetine Hydrobromide API should be stored and handled according to the applicable API specification, safety documentation and validated stability data.
Because Vortioxetine Hydrobromide can occur in different crystalline and hydrated forms, appropriate control of environmental conditions is important for maintaining the intended solid-state characteristics. Published research and patent documentation describe variations in hydration and water content among different crystalline forms.
Packaging and storage conditions should protect the API from conditions that may adversely affect chemical purity, moisture content or solid-state form. Pharmaceutical manufacturing facilities should maintain suitable procedures for sampling, handling and storage to minimize contamination and preserve API quality.
Vortioxetine Hydrobromide is an established pharmaceutical active ingredient used in antidepressant medicines. Its multimodal serotonergic pharmacology and established regulatory history make it a relevant API for pharmaceutical development and manufacturing.
For pharmaceutical manufacturers and developers, appropriate control of identity, assay, organic impurities, residual solvents, residue on ignition, heavy metals and solid-state characteristics is important for maintaining consistent drug-substance quality.
As a specialized pharmaceutical ingredient, Vortioxetine Hydrobromide can be positioned for applications involving antidepressant formulations, CNS medicines, serotonin-modulating medicines, pharmaceutical research and pharmaceutical manufacturing.
Vortioxetine Hydrobromide is a synthetic serotonin modulator and stimulator and the hydrobromide salt of vortioxetine. It has the molecular formula C18H22N2S·HBr, molecular weight 379.36 g/mol, and CAS Number 960203-27-4.
The drug substance is described as a white to very slightly beige powder, soluble in ethanol and methanol and slightly soluble in water. Regulatory information reports a melting point of approximately 231°C and a pH of approximately 5.05 for a 1% w/v aqueous suspension.
With its established application in major depressive disorder, Vortioxetine Hydrobromide is an important antidepressant API, CNS API, serotonin modulator API and pharmaceutical active ingredient for pharmaceutical development and manufacturing.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0–102.0% |
| Loss on Drying | NMT 2.0% |
| Residue on Ignition | NMT 0.10% |
| Heavy Metals | NMT 10 ppm |
| pH (1% Solution) | 5.05 — 1% |
| Individual Impurity | NMT 0.10% |
| Total Impurities | NMT 0.50% |
| Water Content | NMT 1.0% |
| Melting Point | 231°C |
| Solubility | Slightly soluble in water; soluble in ethanol and methanol |