JNJ-10280205 and JNJ-10287069: novel PDE5 inhibitors as clinical candidates for erectile dysfunction

Qiu, Yuhong; Bhattacharjee, Sheela; Kraft, Patricia; John, T. M.; Haynes-Johnson, Donna; Jiang, Weiqin; Sui, Zhihua; Lundeen, Scott G.

doi:10.1038/sj.ijir.3901462

Cited by 6 publications

(3 citation statements)

References 30 publications

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“…UK369003, a second-generation PDE5 inhibitor, is now in Phase II trials for ED. JNJ-10280205 and JNJ-10287069 are other suitable agents for clinical trials in men with ED [62] .…”

Section: New-generation Pde5 Inhibitorsmentioning

confidence: 98%

Novel phosphodiesterase-5 (PDE5) inhibitors in the alleviation of erectile dysfunction due to diabetes and ageing-induced oxidative stress

Gür

Sikka

2008

Expert Opinion on Investigational Drugs

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Background : Diabetes and ageing are associated with erectile dysfunction (ED). Under these conditions, increased oxidative stress produces superoxide ions, which in turn suppresses the nitric oxide-cyclic guanosine monophosphate pathway. The phophodiesterase-5 (PDE5) inhibitors still remain ineffective in 15 -57% of impotent men. Objective : To identify the efficacy of conventional and novel PDE5 inhibitors on oxidative stress involved in diabetes and ageing. Methods : An electronic search of the literature was conducted to review published information relating diabetes and ageing to ED and to cover latestage developments of novel PDE5 inhibitors. Results/conclusion : Safe and more efficacious alternatives that can modulate PDE5 levels in ED regarding oxidative stress conditions are needed. Included in this review are updates on the new PDE5 inhibitors avanafil, udenafil, SLx-2101, and mirodenafil.

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“…UK369003, a second-generation PDE5 inhibitor, is now in Phase II trials for ED. JNJ-10280205 and JNJ-10287069 are other suitable agents for clinical trials in men with ED [62] .…”

Section: New-generation Pde5 Inhibitorsmentioning

confidence: 98%

Novel phosphodiesterase-5 (PDE5) inhibitors in the alleviation of erectile dysfunction due to diabetes and ageing-induced oxidative stress

Gür

Sikka

2008

Expert Opinion on Investigational Drugs

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“…In view of the significant number of patients who remain dissatisfied with the available therapies due to a lack of efficacy or discomfort arising from adverse events, the development of new PDE5 inhibitors with an enhanced selectivity for PDE5, a faster onset of action, improved oral bioavailability and an extended duration of drug action persists as an important topic and is being pursued vigorously. Currently, avanafil (originally developed by Mitsubishi Tanabe Pharma Corp., Yokohama, Japan, under the substance code TA-1790), JNJ-10280205, JNJ-10287069, lodenafil, mirodenafil, SLX-2101 and udenafil are under development for future use in the treatment of ED [Qiu et al 2006;Hatzimouratidis and Hatzichristou, 2008;Eardley et al 2010]. Some of these drugs have already entered into the clinical stage of testing (avanafil, lodenafil and mirodenafil) or have already been approved in some countries by the drug authorities in charge and are now being offered to patients (udenafil).…”

Section: Introductionmentioning

confidence: 99%

Avanafil for the treatment of erectile dysfunction: initial data and clinical key properties

Kedia

Ückert

Assadi-Pour

et al. 2012

Therapeutic Advances in Urology

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Orally active, selective inhibitors of phosphodiesterase type 5 (PDE 5, cyclic GMP PDE), such as sildenafil, tadalafil and vardenafil, are currently the first-choice treatment options for the clinical management of erectile dysfunction (ED) of various etiologies and severities. However, a significant number of patients remain dissatisfied with the available therapies due a lack of efficacy or discomfort arising from adverse events. Several new PDE5 inhibitors, among which are avanafil (TA-1790), lodenafil, mirodenafil, udenafil, SLX-2101, JNJ-10280205 and JNJ-10287069, have recently been approved and introduced into the market or are in the final stages of their clinical development. Avanafil (marketed in the US under the brand name STENDRA TM ) has been developed by VIVUS Inc. (Mountain View, CA, USA) and has recently received approval from the US Food and Drug Administration (FDA) for use in the treatment of male ED. The drug has demonstrated improved selectivity for PDE5, is rapidly absorbed after oral administration with a fast onset of action and a plasma half-life that is comparable to sildenfil and vardenafil. In phase II and phase III clinical trials that included a large number of patients, avanafil has been shown to be effective and well tolerated. Owing to its favorable pharmacodynamic and pharmacokinetic profile, avanafil is considered as a promising new option in the treatment of ED. The present article summarizes the initial data and clinical key properties of avanafil.

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“…In anesthetized dogs, they both exhibit similar efficacy as sildenafil in enhancing erectile function, with no significant effect on cardiovascular parameters. Both compounds are suitable candidates for clinical trials in men with ED 40. NCX 911 has a similar efficacy to sildenafil in causing corporal smooth muscle relaxation; however, since it generates NO it might have a promising role in the future in ED conditions with low NO 41…”

Section: Future Treatment Of Edmentioning

confidence: 99%

Future prospects in the treatment of erectile dysfunction: focus on avanafil

Alwaal¹,

Almannie²,

Carrier³

2011

DDDT

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The treatment of erectile dysfunction (ED) has been revolutionized in the last 15 years with the introduction of type 5 phosphodiesterase (PDE5) inhibitors. Their efficacy, safety, and ease of administration have made them first-line treatment for ED. This article reviews the current therapies available for ED, and the new PDE5 inhibitors that are being investigated. Furthermore, it examines all the current ED treatment options that are in different phases of development (including oral and topical pharmacotherapy, gene therapy, and tissue engineering). A special emphasis is on avanafil, a new PDE5 inhibitor that has been studied extensively in Phase I and II clinical trials and has undergone several Phase III trials. Avanafil is a promising medication for ED due to its favorable pharmacokinetics, safety, and efficacy.

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JNJ-10280205 and JNJ-10287069: novel PDE5 inhibitors as clinical candidates for erectile dysfunction

Cited by 6 publications

References 30 publications

Novel phosphodiesterase-5 (PDE5) inhibitors in the alleviation of erectile dysfunction due to diabetes and ageing-induced oxidative stress

Novel phosphodiesterase-5 (PDE5) inhibitors in the alleviation of erectile dysfunction due to diabetes and ageing-induced oxidative stress

Avanafil for the treatment of erectile dysfunction: initial data and clinical key properties

Future prospects in the treatment of erectile dysfunction: focus on avanafil

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