RXi Pharmaceuticals Corporation (NASDAQ: RXII), a biotechnology company focused on discovering and developing innovative therapies primarily in the areas of dermatology and ophthalmology, presented new data, on Saturday, May 9, 2015, on the Company’s proprietary self-delivering RNAi ) compounds developed to target Tyrosinase (TYR) and Collagenase (MMP1) at the 74th Annual Meeting of the Society for Investigative Dermatology.
Poster 642 presented new data from one of the Company’s discovery stage programs, showing that sd‑rxRNA compounds developed to target TYR, lead to a visible reduction in pigmentation in cultured melanocytes. In vitro experiments have been carried out using a 3‑dimensional tissue culture model of human epidermis that contains melanocytes. The results of these experiments show that sd-rxRNA compounds targeting tyrosinase, in this model, are at least one hundred times more potent than kojic acid, a well-characterized skin lightening agent in reducing the melanin production in melanocytes.
Poster 487 presented results on sd-rxRNA compounds targeting MMP1. In this discovery program, multiple potent sd-rxRNAs that target MMP1 have been identified and evaluated. Data from this poster show a reduction in MMP1 mRNA levels that corresponds to a similar reduction in MMP1 enzyme activity in HT-1080 cells, a cell line useful for research related to cancer of connective tissues. In addition, silencing of MMP1 expression in an in vitro scratch assay resulted in reduced migration of A549 cells, a clinically relevant non-small cell lung cancer cell line. Reduced migration in a scratch assay may indicate a reduction in the invasive nature of the cancer cell due to MMP1 reduction as a result of sd-rxRNA treatment.
“We are excited to move these discovery programs forward,” said Dr. Karen Bulock, Vice President of Research at RXi Pharmaceuticals. She further added, “Not only do these TYR inhibitors have the potential to treat pigmentation disorders, both the TYR and MMP1 compounds may also be useful as adjuvant therapy for diseases such as melanoma and possibly cancer metastasis, respectively.”
Both posters are available on the Company’s website at www.rxipharma.com.
Tyrosinase is a key enzyme involved in the synthesis of melanin, which is produced by melanocytes. This is the pigment that gives human skin, hair and eyes their color. TYR-targeting compounds may be therapeutically useful in a number of areas including cutaneous hyperpigmentation disorders such as age spots, liver spots, freckles, and potentially melanoma.
Collagenases are enzymes that break the peptide bonds in collagen. Matrix metalloproteinase (MMP1) is a collagenase involved in the breakdown of extracellular matrix that specifically cleaves collagen I, II and III. MMP1-targeting compounds may be therapeutically beneficial in the treatment of skin aging disorders including photo aging, arthritis, acne scarring, blistering skin disorders, corneal erosions, endometriosis and possibly cancer metastasis.
About Self-delivering RNAi (sd-rxRNA®)
RXi’s novel, self-delivering RNAi (sd‑rxRNA) compounds are designed for therapeutic use and have drug-like properties, such as high potency, target specificity, serum stability, reduced immune response activation, and efficient cellular uptake. They are hybrid oligonucleotide molecules that combine the beneficial properties of both conventional RNAi and antisense technologies. The sd‑rxRNAs have a single-stranded phosphorothioate region, a short duplex region, and contain a variety of nuclease-stabilizing and lipophilic chemical modifications. The combination of these features has been shown in vitro and in animal tissues, to allow sd‑rxRNAs to achieve efficient spontaneous cellular uptake and potent, long-lasting intracellular activity.
RXI-109, an sd-rxRNA compound, is the Company’s first product candidate. RXI-109 silences Connective Tissue Growth Factor (CTGF), which plays a key role in tissue regeneration and repair and is initially being developed to reduce or inhibit scar formation in the skin and retina and is currently being evaluated in Phase 2a clinical trials. The Company’s sd-rxRNA technology platform is broadly protected by multiple issued patents and numerous patent applications.
About RXi Pharmaceuticals Corporation
RXi Pharmaceuticals Corporation (NASDAQ: RXII) is a biotechnology company focused on discovering and developing innovative therapeutics primarily in the area of dermatology and ophthalmology addressing high-unmet medical needs,. Our discovery and clinical development programs are based on siRNA technology as well as immunotherapy agents. These compounds include, but are not limited to, our proprietary, self-delivering RNAi (sd-rxRNA®) compounds for the treatment of dermal and retinal scarring. It also includes an immunomodulator, Samcyprone™, a proprietary topical formulation of diphenylcyclopropenone (DPCP), for the treatment of such disorders as alopecia areata, warts, and cutaneous metastases of melanoma.
RXi’s robust pipeline, coupled with an extensive patent portfolio, provides for product and business development opportunities across a broad spectrum. We are committed to being a partner of choice for academia, small companies, and large multinationals. We welcome ideas and proposals for strategic alliances, including in- and out-licensing opportunities, to advance and further develop strategic areas of interest.