Melasma is our current focus
EP0003 – A new treatment for dermatological disorders.
The compound EP0003 was acquired from AstraZeneca in 2014. The IP protection is strong with granted patents in several territories, including USA.
EP0003 is a low molecular compound. It is chemically very stable both in solid form and in solution. It is formulated in a cream for topical application.
EP0003 is a high affinity plasminogen binding inhibitor (PBI) and details of its binding mode are well established. The compound is pre-clinically well documented and a first time in human Phase I study with topical administration has been performed.
Rosacea - An opportunity for faster onset and improved efficiacy.
Rosacea is a common disease affecting 40 million people world-wide (16 million in the US). It is a chronic inflammation with great psycho-social impact. The cause of the disease is unknown. (see also www.rosacea.org)
Plasminogen binding inhibitors (tranexamic acid and ε-aminocaproic acid) have been tested for topical treatment of rosacea in small clinical studies. Positive effects were seen on both clinical and biochemical parameters. Based on this, and since rosacea patient are known to have a sensitive skin, rosacea patients were included in the Phase I study with EP0003.
The study included single ascending dose (SAD, n=18), multiple ascending dose (MAD, n=18) and a safety cohort (n=20), the latter treated for 2 weeks. More than half of the subjects had rosacea. Main endpoints were tolerability, safety and pharmacokinetics.
EP0003 was very well tolerated and pharmacokinetics showed that the compound was absorbed through the skin as predicted. No clinical improvements were seen, this is often the case in short Phase I studies.
Melasma is an acquired bilateral, facial hyperpigmentation disorder that worsens in combination with sun exposure. Like rosacea it has a psycho-social impact. It mainly affects women and is common in Asia, South America and USA and rare in northern Europe. Main treatments are hydroquinone-based products. Effects are modest and slow in onset, and the safety of hydroquinone is questioned.
Clinical experience with tranexamic acid show that plasminogen binding inhibitors (PBI´s) are effective. Tranexamic acid given orally is more effective than when given topically, indicating that this compound has poor skin penetrating properties.
EP0003, being >10 times more potent and much more lipophilic than tranexamic acid, should thus offer opportunities for improved topical treatment of the disorder.
Treatment of pigmentation disorders is a fast growing segment and Emeriti Pharma is currently looking for a partner to perform clinical studies in melasma.
(For info about melasma see e.g. www.aocd.org and www.aad.org )
Plasminogen/plasmin levels are increased in psoriatic lesions and a potent plasminogen binding compound (PBI) is expected to have a beneficial effect on the disease.
More than half of the large psoriasis population have mild disease, often manifested as plaque psoriasis. The current treatment of plaque psoriasis utilises topical vitamin D + corticosteroid. However, vitamin D is painful on normal skin and long-term treatment with potent corticosteroids is undesirable.
(For info about psoriasis see e.g. www.psoriasis.org)
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