Lux Biosciences, Inc.

Luveniq™

Luveniq is the oral form of a next-generation calcineurin inhibitor, voclosporin. Like other molecules of this class, the compound reversibly inhibits immunocompetent lymphocytes, particularly T-lymphocytes, and also inhibits lymphokine production and release. Although other calcineurin inhibitors like cyclosporine A (CsA) or tacrolimus are widely used and effective immunosuppressants, there are numerous adverse effects associated with these drugs, such as nephrotoxicity, hypertension, hepatotoxicity, hyperlipidemia, diabetogenesis, thrombotic microangiopathy, hirsutism, parathesia, neurotoxicity, and gingival hyperplasia. Of these, nephrotoxicity and hypertension (CsA) or diabetogenesis and tremor (tacrolimus) are the most problematic, dose-related adverse effects.

Luveniq (oral voclosporin) was discovered by Isotechnika Inc. based on unique insights into the in vivo metabolism of calcineurin inhibitors. Luveniq/oral voclosporin is highly potent in various animal models of autoimmune diseases, including experimental uveitis. The product exhibits features that may permit convenient and predictable dosing. Most importantly, based on early clinical studies, including one in more than 300 psoriasis patients, the therapeutic window of Luveniq/oral voclosporin appears to be wide, allowing for a 15-fold range in exposure between a clinically effective dose and the threshold for side effects. This profile would render the drug a highly valuable treatment option for a variety of autoimmune diseases and for solid organ transplantation, if confirmed further in large clinical trials.

Lux Biosciences has exclusively licensed the worldwide rights to this compound for ophthalmic use and is developing Luveniq for sight threatening, non-infectious uveitis. In June 2008, Lux Biosciences completed enrollment in the Phase 3 LUMINATE (Luveniq Uveitis Multicenter Investigation of a New Approach to TrEatment) clinical trials, encompassing more than 557 patients worldwide. If approved by FDA, this product would represent the first steroid-sparing product for the treatment of uveitis available in the United States. Details of the LUMINATE clinical trials can be found at www.clinicaltrials.gov.