Desvenlafaxine Succinate

Inquiry

Cat Number

API0232133

CAS Number

448904-47-0

If you have any other questions, please contact our experts.

Product Detail Description Scientific Support Customer Q&A

CAS Number

448904-47-0

EINECS

112-525-3

Storage

Store at room temperature

Synonyms

O-Desmethylvenlafaxine succinate; Desvenlafaxine succinate anhydrous; H9E1T0BI90; DTXSID701044359

Molecular Formula

C20H31NO6

Molecular Weight

381.5

Smiles

CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O.C(CC(=O)O)C(=O)O

Appearance

White to off-white powder

Melting Point

208-213°C

Boiling Point

403.8±25.0°C at 760 mmHg

Relative Density

1.1±0.1

General Description

Desvenlafaxine succinate is the succinate salt of the major active metabolite of venlafaxine. The parent compound, desvenlafaxine (O-desmethylvenlafaxine), is a serotonin-norepinephrine reuptake inhibitor (SNRI) with a phenylethylamine structure. The succinate salt improves solubility and stability. Unlike venlafaxine, desvenlafaxine does not require hepatic metabolism for activity, providing more predictable pharmacokinetics.

Mechanism of Action

Desvenlafaxine potently and selectively inhibits the reuptake of serotonin (5-HT) and norepinephrine (NE) by binding to their respective transporters (SERT and NET). This increases synaptic concentrations of both monoamines in brain regions regulating mood, anxiety, and pain perception. It has negligible affinity for muscarinic, histaminergic, or α1-adrenergic receptors, accounting for its improved tolerability compared to tricyclic antidepressants.

Application

Desvenlafaxine is indicated for the treatment of major depressive disorder (MDD) in adults. It has also demonstrated efficacy for vasomotor symptoms (hot flashes) associated with menopause and for fibromyalgia (off-label). The prolonged half-life (approximately 11 hours) allows once-daily dosing. As a primary active agent, its effects are less variable than those of venlafaxine, which depends on CYP2D6 activity for conversion.

Pooled analysis of eight randomized trials (3,384 patients with major depressive disorder) showed that desvenlafaxine 50 or 100 mg/day produced significantly greater categorical improvements in Sheehan Disability Scale subscales (functional impairment) at week 8 compared to placebo (all P≤0.02). Early improvement at week 2 or 4 strongly predicted functional outcome at week 8 (P<0.0001). Monitoring functional status early in treatment may help clinicians decide whether to adjust antidepressant therapy.

Fig. 1 Percentage change from baseline over time in SDS total and subscale scores. (Soares CN, et al., 2019)

References

Soares CN, et al. Categorical improvement in functional impairment in depressed patients treated with desvenlafaxine. CNS Spectr. 2019;24(3):322-332.

Does Desvenlafaxine Succinate require protection from light during storage?

Yes, it is moderately photosensitive. Prolonged light exposure can cause discoloration and degradation. Store in light-resistant containers.

What is the recommended storage temperature for Desvenlafaxine Succinate?

Store at controlled room temperature (15-25°C). Avoid temperatures above 30°C, which can accelerate hydrolysis of the succinate salt and formation of cyclic impurities.

Is Desvenlafaxine Succinate hygroscopic, and how is this managed?

It is slightly hygroscopic. Under high humidity (>70% RH), it may absorb moisture and clump. Storage in tightly sealed containers with desiccant is recommended.

How is the impurity desvenlafaxine lactam (cyclic degradation product) monitored?

This degradation product is specifically quantified using a stability-indicating HPLC method, ensuring it remains within ICH limits.