Mechanism of Oleogel‐S10: A triterpene preparation for the treatment of epidermolysis bullosa

Abstract

Epidermolysis bullosa (EB) is a group of rare heterogeneous, genetic disorders. Currently, there is no effective pharmacological or genetic therapy for all EB subtypes. Dry extract from birch bark and betulin upregulate some pro‐inflammatory mediators and downregulate others. The increase in pro‐inflammatory cytokines is temporary and attenuated over long‐term treatment. This inflammatory stimulus is thought to be prerequisite for a secondary anti‐inflammatory response. Dry extract from birch bark and its active marker substances have also been shown to increase the migration of primary human keratinocytes, accelerate wound closure, and promote differentiation of keratinocytes in vitro and in vivo—processes that are essential for reepithelialization and maintenance of the skin barrier. Comprehensive clinical data are available to support the use of Oleogel‐S10 in the treatment of partial thickness wounds of different etiologies, and a proof‐of‐concept Phase 2 study in patients with dystrophic EB has suggested the potential for faster reepithelialization of wounds treated with Oleogel‐S10.

Botanical Drugs in Traditional Chinese Medicine With Wound Healing Properties

“…Results suggested that Oleogel-S10 significantly facilitated the healing of superficial partial thickness burn wounds and it was superior to Octenilin ® in terms of efficacy and tolerability. Oleogel-S10 was also clinically proven to be effective for epidermolysis bullosa by phase II and III trials, and the mechanism was to promote the re-epithelialization of wounds ( Schwieger-Briel et al, 2017 ; Kern et al, 2019 ; Schwieger-Briel et al, 2019 ).…”

Integrated Management Strategies for Epidermolysis Bullosa: Current Insights

“…It acts irrespective of the underlying molecular pathology in EB. 61 Currently, preliminary results from a Phase III double-blind, randomized, placebo-controlled “EASE” trial (NCT03068780) are showing sustained wound closure benefits in recessive DEB patients.…”

Investigational Treatments for Epidermolysis Bullosa

“…One aspiration in developing EB therapeutics is to identify a topical product that promotes wound healing in all types of EB, irrespective of the underlying molecular pathology. To that end, a triterpene extract in sunflower oil, oleogel-S10 (Amryt Pharma, Cambridge, USA), has been shown to promote wound healing through inflammation modulation, stimulation of keratinocyte migration and altered epidermal differentiation [144,145]. A prospective, placebo-controlled phase II trial in EB showed clinical improvements, in which five out of twelve treated wounds had faster reepithelialization as judged by two independent reviewers, while significance was not attained due to limited participant numbers [146].…”