R333 - discoid lupus

Topical JAK/SYK inhibitor for the skin:

• Discoid lupus erythematosus (DLE) is a chronic autoimmune disease of the skin.


• Approximately 300,000 Americans suffer from discoid lupus and, according to the Lupus Foundation of America, more than 16,000 new cases are diagnosed in the US each year.


• DLE is characterized by disc-shaped sores with inflammation, swelling, scaling, scarring, pigment discolorations and even hair loss. The lesions most commonly appear in sun exposed areas, predominantly on the face, chest and scalp.


• Cutaneous lupus incidence approximates systemic lupus.


• Approximately 10-20% of discoid lupus patients go on to develop systemic lupus.


• Current treatments have either poor efficacy or significant toxicities. Rigel's R333 is a potent, topical JAK and SYK inhibitor that is designed to interrupt pivotal inflammatory cascade signals with the potential to prevent or diminish both acute and chronic symptoms.


• A Phase 2 clinical study of R333 was initiated in Q3' 2012. Rigel expects results in mid 2013.

Latest News:

• Rigel Announces Fourth Quarter and Year End 2012 Financial Results


• Rigel Initiates Phase 2 Clinical Studies with R343 for Asthma and R333 for Discoid Lupus

Disease background
DLE is a chronic skin condition of sores with inflammation and scarring favoring the face, ears, and scalp and at times on other body areas. These lesions develop as a red, inflamed patch with a scaling and crusty appearance. The center areas may appear lighter in color with a rim darker than the normal skin. When lesions occur in hairy areas such as the beard or scalp, permanent scarring and hair loss can occur. A small percentage of patients with discoid lupus can develop disease of the internal organs.

It is thought to be an autoimmune disease with the body's immune system incorrectly attacking normal skin. This condition tends to run in families. Females outnumber males with this condition 3 to 1.