Here we go again with a selection of five recent international patent applications that involve drug repurposing. We at H.M. Pharma Consultancy are as happy as ever to see the attention this service to the public is attracting. – Follow @hmpharmaconon Twitter to receive updates on our non-confidential activities, and on what we simply find interesting. Or check our Google+ corporate page (and include it in your circles!) — it collects all twits and blogposts along with whatever we do on Google+.
Transvaginal PDE Inhibitors For Infertility
It is known that pentoxifylline, a nonspecific inhibitor of phosphodiesterases (PDEs), can improve sperm motility in vitro, which is why it is used in assisted reproduction (Hum Reprod. 1996; 11(6):1236-9; PDF here); given orally it also has some effect in men suffering from asthenozoospermia. Selective PDE4 inhibitors increase sperm motility while selective PDE1 inhibitors stimulate the acrosome reaction (Hum Reprod.1998; 13(5):1248-54; PDF here). WO/2012/175775(Individuals [ES]; December 27, 2012) proposes vaginal gels or foams (preferably administered immediately before and after intercourse) containing pentoxifylline, rolipram, ibudilastor milrinoneto facilitate conception in couples who are infertile because of male sperm deficiency conditions. In a trial with 20 couples a fertilization efficiency of 20% was obtained, which – though certainly not a quantum leap – is higher than the 15% typically seen in conjugal artificial insemination.
Sorafenib For Age-Related Macular Degeneration
Claiming oncology drugs with anti-angiogenic modes of action for exudative AMD has become commonplace: the kinase-driven mechanisms of the underlying choroidal neovascularization (CNV) mirrors what occurs in the growth of solid tumors. Little wonder that, in WO/2013/000909(Bayer Healthcare [DE]; Jan. 3, 2013), the kinase inhibitor sorafenib( Nexavar®, Bayer/Onyx) is claimed for this pupose. Well, it works: in the rat model of laser-induced CNV the area of neovascularization and vascular leakage angiography scores were reduced by 30-40% by simple twice-daily application of 10 µl of a 20 mg/mg suspension of sorafenib in paraffin- or water-based matrices.
A Beta-Lactamase Inhibitor Calms Restless Legs
It was only in 1945 that restless leg syndrome (RLS) – the strong urge to move the legs so that paresthesias are alleviated, especially at night – was described as a distinct medical condition, and it was not before the 2000s that dopamine agonists (those already approved for Parkinson’s disease) got approval extensions for RLS. This class of drugs continues to dominate RLS therapy although direct dopaminergic stimulation has many drawbacks, including narcolepsy. It is quite fascinating to hear thatWO/2013/006808(Rexahn Pharmaceuticals [US]; Jan. 10, 2013)claimsclavulanic acid, a beta-lactam inhibitor of beta-lactamaseand therefore a resistance-breaking component of Augmentin and its generics, for this condition. Fascinating but not unexpected, considering that Rexahn had already published (Neurosci Lett. 2011; 504(2):170-5; here) that clavulanic acid enhances dopamine release in neuronal PC12 and SH-SY5Y cells – presumably through a mechanism involving Munc18-1and Rab4modulation – without affecting dopamine synthesis. It is also protects dopaminergic neurons against neurotoxin-induced loss of mitochondrial function (Brain Res. 2012; 1469:129-3, here). The company has conducted Phase II trials with its extended-release formulation, Serdaxin® (RX-10100) for major depression (NCT00839176, NCT01273376) and erectile dysfunction (NCT00693056).In a mouse RLS model of chronic dietary iron deficiency, “parameters are normalized to control levels upon treatment with clavulanic acid,” but no results are presented.
Ultra-Low-Dose AnticonvulsantsFor Adult Psychiatric Spectrum Disorders
“Unexpectedly and serendipitously,” improvements were noted in individuals with symptoms of attention-deficit/hyperactivity disorder on doses of phenytoin that were only 20% or even less than 2.5% of thosetherapeutically effectivein epilepsyor mood stabilization: This is one of the core findings in WO/2013/007698(Gosforth Center [AU]; Jan. 17, 2013). Not only were the higher doses ineffective, they were also associated with significant cognitive side effects. It was only on a dose reduction that the clinical improvements were sustained.Autism and cognitive or behavioral problems after traumatic brain injury are other conditions that reponded to ultra-low doses of phenytoin or valproate. In the case of phenytoin, a suitable sub-therapeutic dose is in the range of from 1 mg to less than 40 mg/day, The document goes on for 117 pages and claims many dozens of known compounds, and also claims cholinesterase inhibitors as components of combination treatment.
Botulinum Toxins Melt Fat Pads
Analysts who track of Allergan’s patent portfolio for Botox®, Dysport®and Myobloc®(that must be just short of a full-time job), here is something for you: WO/2013/013042(Allergan [US]; Jan. 24, 2013)claims Botulinum toxin type A – the most lethal natural biological agent known to man – for treating adipose deposits(lipomas, but also simple fat pads or cellulite) by local intradermal injection (10 – 400 units)or by applying a cream. Data are limited to two case reports, showing improvements within 4 weeks. – The question,“Botulinum toxin injections to reduce adiposity: possibility, or fat chance?”has been raised years ago by a team at the National University of Singapore (Med Hypotheses2006;67(5):1086-9; here), and a pilot study investigating the lipolytic effect of s.c. Botulinum toxin injection in rabbits (Anal Quant Cytol Histol.2010; 32(4):186-91; here) has been published by the Shiraz University of Medical Sciences in Iran a year before the priority date of the present application… which therefore, in our opinion, does not stand a fat chance to be granted.