AbstractOver the last half of the 20th century, there have been a series of psychopharmacologic strategies for treatment of depression. As we approach the next century, new therapies in varying stages of American release are being developed. This review will focus on information available for the following proposed antidepressants: 1) reboxetine, a norepinephrine selective reuptake inhibitor; 2) milnacipran, a combined serotonin/norepinephrine reuptake inhibitor; 3) a new enantiomer of fluoxetine, a selective serotonin reuptake inhibitor; 4) duloxetine, another combined serotonin/norepinephrine reuptake inhibitor; 5) sunepitron, a combined 5-HT1A agonist and α2 antagonist; and, 6) MK-869, a substance P inhibitor. Finally, other possible developing directions will be reviewed, including corticotropin-releasing factor.

01 Nov 1998·Journal of Pharmaceutical and Biomedical AnalysisQ3 · MEDICINE

Assay and purity evaluation of sunepitron hydrochloride by reversed-phase liquid chromatography using a reference standard composite

Q3 · MEDICINE

Article

Author: Stephen T Colgan ; Monica L Dumont ; Sally G Ruggeri

A reference standard composite was prepared that contained the active pharmaceutical ingredient sunepitron and three potential impurities. This standard was characterized and used for concomitant quantitation of sunepitron and its potential impurities in samples of drug substance and drug product. This approach minimizes the number and quantity of reference standards which often are expensive to synthesize, characterize, and maintain. In addition, running assays becomes simpler because the number of reference standard solutions required for each assay is reduced. Reference standard composites can also be used for qualitative applications such as demonstrating system suitability or for retention times markers for process related impurities or degradants.

01 May 1998·Drug metabolism and disposition: the biological fate of chemicals

Metabolism and excretion of a new anxiolytic drug candidate, CP-93, 393, in healthy male volunteers.

Article

Author: Cui, D ; Bright, G M ; Wilner, K ; Baxter, J G ; Prakash, C ; Miceli, J

CP-93,393 [(7S,9aS)-1-(2-pyrimidin-2-yloctahydropyrido[1,2-a] pyrazin-7-ylmethyl)pyrrolidine-2,5-dione] is a new anxiolytic drug with highly selective serotonin 5-hydroxytryptamine 1A autoreceptor agonist, alpha2-adrenergic antagonist, and dopamine D2 agonist properties. The excretion, biotransformation, and pharmacokinetics of CP-93,393 were investigated in six healthy male volunteers after oral administration of a 5-mg dose of [14C]CP-93,393. The administered radioactivity was excreted predominantly in the urine. One week after administration of the dose, cumulative excretion amounted to 67.8 +/- 2.5% in the urine and 22.0 +/- 5.6% in the feces. In total, 89.8 +/- 5.7% of the radioactive dose was recovered in urine and feces. Mean maximum plasma concentration values for unchanged CP-93,393 were 10.92 and 1.02 ng/ml for poor metabolizers (PMs) and extensive metabolizers (EMs) of dextromethorphan, respectively. AUC0-infinity values for unchanged CP-93,393 were also greater for PMs than for EMs, whereas the mean maximum plasma concentration and AUC0-infinity values for total radioactivity were similar for the two phenotypes. Less than 0.5% of the dose was excreted in urine as unchanged drug for both EMs and PMs, suggesting extensive metabolism of CP-93,393 in both phenotypes. Hydroxylation at the 5-position of the pyrimidine ring was identified as the main metabolic pathway. 5-Hydroxy-CP-93,393 (M-15) and its glucuronide and sulfate conjugates (M-7 and M-13, respectively) accounted for approximately 51% of the administered dose in excreta of both PMs and EMs. Hydrolysis of the succinimide ring, in combination with 5-hydroxylation and/or conjugation or not, accounted for approximately 9% of the dose. A novel metabolite, apparently resulting from oxidative degradation of the pyrimidine ring, was characterized as the amidine analog M-18. M-15 (47-62%), its sulfate conjugate (M-13, approximately 9%), and the pyrimidine ring-cleaved product (M-18, 7-13%) were identified as the major circulating metabolites for both EMs and PMs. Therefore, CP-93,393 undergoes metabolism by three primary pathways, i.e. 1) aromatic hydroxylation followed by conjugation with glucuronic acid and sulfuric acid, 2) oxidative degradation of the pyrimidine ring, and 3) hydrolysis of the succinimide ring. The identified metabolites accounted for approximately 90, 91, and 92% of the total radioactivity present in urine, plasma, and feces, respectively. The major in vivo oxidative metabolites were also observed after in vitro incubations with human liver microsomes.

100 Deals associated with Sunepitron Hydrochloride

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KEGG	Wiki	ATC	Drug Bank
D02569	Sunepitron Hydrochloride	-	-

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Indication	Highest Phase	Country/Location	Organization	Date
Anxiety Disorders	Phase 3	-	Pfizer Inc.	-
Depressive Disorder	Phase 3	-	Pfizer Inc.	-

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