Aildenafil citrate: A new potent and highly selective phosphodiesterase type5 inhibitor for the treatment of erectile dysfunction

Department of Urology, First Hospital of Peking University, Institute of Urology, Peking University, Beijing 100034, China.
Zhonghua nan ke xue = National journal of andrology 01/2007; 12(12):1080-3.
Source: PubMed


To evaluate the efficacy and safety of aildenafil citrate, an oral phosphodiesterase type 5 inhibitor, in the treatment of erectile dysfunction.
Integrated analyses were made of 8-week, randomized, double-blind, placebo-controlled phase 2 clinical trials involving 250 men with mild-to-severe erectile dysfunction of various etiologies who received aildenafil citrate 30 or 60 mg (n = 167) or placebo (n = 83).
The statistic results of International Index of Erectile Function, Patient Sexual Encounter Profile (SEP) diaries and Global Assessment Question (GAQ) were significantly higher in the aildenafil citrate patients than in the placebo controls. The main drug-related adverse events were flushing, headache, dizziness and naupathia, which were mild and could be self-relieved. Conclusion: The aildenafil citrate therapy significantly ameliorated erectile function and was well tolerated by a wide range of patients with erectile dysfunction.

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    • "Aildenafil was found to be present in two herbal supplements (VII and VIII) at levels of 49 and 46 mg per dose unit, respectively. Patent and scientific literature showed that the pharmacological effects and potency of aildenafil were similar to those of sildenafil (Liu 2005; He et al. 2006; Guo et al. 2007; Wang et al. 2007). Because the dose levels found for aildenafil with these herbal supplements exceeded the lowest commercially available sildenafil dose of a registered drug (Table 3), these supplements were considered to produce significant pharmacological effects. "
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    ABSTRACT: Aildenafil, 1-{[3-(6, 7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo [4, 3-d] primidin-5-yl)-4-ethoxyphenyl] sulfonyl}-cis-3, 5-dimethylpiperazine, a phosphodiesterase type V enzyme inhibitor (PDE5I), is under development for treatment of erectile dysfunction (ED). The purpose of this study was to elucidate metabolism of aildenafil in vivo in rats and in vitro in mouse, rat, dog, and human liver microsomes. Thirty-one phase I metabolites have been found by LTQ/Orbitrap hybrid mass spectrometry in rat urine, faeces, and bile after oral administration. Major biotransformation pathways of aildenafil included N-dealkylation of the piperazine ring, hydroxylation and dehydrogenation, aliphatic hydroxylation and loss of alkyl group of piperazine ring. Minor pathways involved hydroxylation on the phenyl ring, pyrazole N-demethylation, O-deethylation, loss of piperazine ring (cleavage of N-S bond) and dehydrogenation on the piperazine ring. Similar metabolic pathways of aildenafil were observed in the incubations of liver microsomes from mouse, rat, and dog as well as from human. The depletion rate of parent drug in mouse and rat liver microsomes was significantly different from that in human liver microsomes. The cytochrome P450 reaction phenotyping analysis was conducted using isozyme-specific inhibitors. The results indicated that CYP3A was the main isoenzyme involved in oxidative metabolism of aildenafil. Overall, these in vitro and in vivo findings should provide valuable information on possible metabolic behaviours of aildenafil in humans. Copyright © 2013 John Wiley & Sons, Ltd.
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