Product Development Pipeline
The following table outlines the drug candidates we have generated using our KinAce platform:

KRX-131 - Chemotherapy-Induced Hair Loss
According to the American Cancer Society, over 1.2 million cases of cancer are diagnosed annually in the United States (excluding most skin cancers). It has been estimated that more than 80% of cancer patients receive chemotherapy, which results in hair loss for the duration of treatment in nearly all recipients and as such poses a significant quality of life problem for these patients. (Source: Seminars in Oncology 25:562, 1998).

Using our KinAce platform, we have designed a compound, KRX-131, that modulates the activity of the transforming growth factor beta (TGF- ß) receptor kinase which regulates hair growth. KRX-131 has already been shown to prevent chemotherapy-induced hair loss in in vivo testing.

KRX-211 - Septic Shock
There are an estimated 500,000 cases of septic shock, a life threatening reaction to a severe infection, for which there is currently no FDA-approved treatment in the United States. (Source: New England Journal of Medicine 340: 207, 1999). The mortality rate for those with septic shock is approximately 50%.

Using our KinAce platform, we have designed KRX-211 to modulate the activity of JAK3, a protein kinase implicated in septic shock. We have demonstrated the effectiveness of KRX-211 in an in vivo model of septic shock. Recently the NIH selected KRX-211 to undergo extensive in vivo testing in preparation for clinical trials.

KRX-167 - Bone Growth Stimulant
There is a growing need to accelerate bone healing following medical procedures that affect bone structure. According to a recent study conducted by the National Osteoporosis Foundation, the total economic cost of bone fractures caused by osteoporosis in the United States was an estimated $13 billion.

Using our KinAce platform,we have designed KRX-167 to promote bone growth by stimulating bone morphogenic proteins (BMP), receptor protein kinases that are involved in the regulation of the growth and differentiation of cartilage and bone. In in vivo trials, KRX-167 has consistently shown evidence of enhanced bone formation and increased relative bone density when compared to the control groups.

KRX-291 - Sunless Tanning
The American Cancer Society estimates that there will be approximately 1.3 million cases of skin cancer diagnosed in the U.S. this year. Exposure to the sun causes tanning by increasing the skin pigment known as melanin. However, exposure to the sun can also cause skin cancer.

Using our KinAce platform, we designed KRX-291 to stimulate synthesis of melanin in skin cells without exposing them to the risks associated with overexposure to the sun. In in vivo testing of KRX-291, we have been able to demonstrate sunless tanning.

KRX-613 - Diabetes
Diabetes is among the most prevalent chronic diseases in the world and represents the fourth most common reason for patient contact with a physician in the United States. According to the American Diabetes Association (ADA), there are an estimated 10.3 million diagnosed diabetics in the United States. Historically, the mainstay of treatment of Type I diabetic patients and many Type II diabetic patients has been insulin which is expensive to synthesize and must be administered by injection. As a result, many companies are searching for alternatives to insulin therapy for the treatment of diabetes. The market size for insulin worldwide is in excess of $2 billion.

Using our KinAce platform, we designed KRX-613 to stimulate glucose uptake by activating the Insulin Receptor Kinase (IRK) without requiring insulin. In vitro tests have shown that KRX-613's application leads to glucose uptake comparable to levels achieved with insulin.