SBIR and STTR Success Story for
Signum Biosciences

(Information Posted/Updated on 04/20/2012)

Signum Biosciences
7 Deer Park Dr. Suite H
Monmouth Junction, NJ  08852

Contact:    Eduardo Perez
Phone:      732-329-6344
E-mail:      eperez@signumbio.com
Web Site:  http://www.argyletherapeutics.com/

Project Title:  A Topical Non Steroidal Anti-inflammatory for Rosacea
Related Award(s):  5R44AI062034
Technology Developed:
Isoprenylcysteine (IPC) analogs represent a novel class of topical anti-inflammatory compounds being developed as therapeutic agents for skin disease. Through this SBIR grant (funded by NIAID) we have identified a lead IPC drug candidate for rosacea SIG990, which has the potential to reduce erythema and decrease the pastules and pustules associated with the disease.

Key Words:  rosacea, isoprenylcysteine, toll-like receptor, g-protein, anti-inflammatory, topical.
Uses of Technology/Products/Service:
Several challenges including UV light, sun exposure, heat and microbes are sensed directly or indirectly by toll-like receptors (TLRs) in skin cells. TLR signaling induces cathelicidin (LL-37) and pro-inflammatory cytokine expression. Once produced, LL-37 and several cytokines act as ligands for G-protein-coupled receptors (GPCRs) activating further inflammatory signaling. Together, these effector molecules elicit vascular changes, neutrophil recruitment, lymphocyte infiltration and reactive oxygen species (ROS) production which contribute to the pathogenesis of rosacea. In vitro and in vivo results demonstrate SIG990 blocks both GPCR, TLR inflammatory signaling, cytokine and ROS production and thus represents a new chemical entity for potentially treating rosacea.

Benefit to Company:
- Allowed us to screen and identify several drug candidates for the treatment of rosacea. - Facilitated safety and toxicology testing of leads compounds, which ultimately led to the selection of the safe and efficacious lead molecule SIG990. - Included with several other cosmetic and Rx candidate molecules, we were able to spin out and form Argyle Therapeutics from Signum Biosciences as a Dermatology focused company. - Allowed for additional hiring and training of staff, increasing our technical expertise in rosacea and other inflammatory skin disorders. - Successful development of SIG990's CMC, safety and demonstration of its activity in several models has led to the out-licensing of this molecule to Brickell Biotech, allowing the Company to receive upfront and potential milestone payments. - Moving forward funding will permit the Company to perform additional safety, formulation and chemical manufacturing of SIG990, while our partner moves the compound into the clinic for testing.