MTC896 – MC5R Antagonist for the Treatment of Excessive Sebum Production

Acne is a skin condition characterised by the over production of sebum, clogged pores and their resulting pimples.  Hair grows out of tiny pores in the skin, held in place by follicles.  Small glands known as sebaceous glands located in the dermis on either side of the follicle empty an oily mixture of dead cells called sebum into the follicles.  This sometimes clogs the follicles and sebum builds up in the pores.  This fluid-filled pore is conducive to the growth of bacteria called Propionibacterium acnes.  Our body tries to fight off these bacteria, giving us pimples in the process. Nearly 85 percent of people between the ages of 12 and 24 will develop acne.

There are treatments available to kill the bacteria, prevent cells in the follicles from clumping and clogging, shrinking the sebaceous glands, and heal the affected skin. There is a high unmet clinical need for new and better treatments, given the increase in antibiotic-resistant strains of P. acnes and the regulatory restrictions placed on the use of isotretinoin.

Mimetica has developed MTC896 as a topical gel for the treatment of excessive sebum production in subjects with acne and other skin conditions.  There are currently no other approved topical products available on the market for the treatment of excessive sebum production.

MTC896 is a highly selective and potent antagonist (<10 nM) of the Melanocortin-5 Receptor (MC5R).  MC5R plays a pivotal role in regulating sebum secretion from the sebaceous glands. ¹    Studies ²    of MC5R antagonists on lipogenesis in primary cultures of human sebocytes and on human skin explants have confirmed MC5R is a highly prospective target for reducing sebum production and potential treatment for acne.

MTC896 was selected from a lead series of molecules for enhanced physical and chemical stability.  MTC896 displays a favorable human skin permeability profile and shows no clinical signs of skin irritation (minipigs, rabbits, rats and mice, following single or multiple daily applications).  MTC896 is stable in skin homogenates persisting unchanged in the skin for periods greater than 48 hours following a single application.  Systemic exposure after topical application is negligible due to very limited uptake from the skin and high metabolism in the liver.

Clinical development

MTC896 is currently in Phase I clinical trials under an Investigational New Drug (IND) application with the United States (US) Food and Drug Administration (FDA).  Mimetica will complete a battery of safety studies evaluating the effects of MTC896 Gel in healthy volunteers prior to embarking on a Human Proof of Concept study in subjects with excessive sebum production.  The Human Proof of Concept Study is planned for Q2 2010.

Commercialisation Partners

Mimetica is currently seeking interest from potential commercial partners, licensees or strategic investors to facilitate further development of MTC896.

For more information, please contact:

Michael Thurn, Ph.D.
Chief Executive Officer
Tel: +617 3020 3406
Fax: +617 3020 3550
Email: m.thurn@mimetica.com.au

Zhang L, Li, W-H, Anthonavage, M, Eisinger, M. (2006) Melanocortin-5 receptor: a marker of human sebocyte differentiation.  Peptides 27:  413-420