new drug VX 702

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Company to begin clinical development of new drug for treating

inflammatory diseases

(Posted June 17, 2002)

Vertex Pharmaceuticals Inc. announced recently the initiation of a Phase

I clinical trial with VX-702, a novel, orally administered inhibitor of

p38 mitogen-activated protein (MAP) kinase, targeting the treatment of

inflammatory diseases.

According to a company release, the p38 MAP kinase enzyme regulates the

production of key proinflammatory cytokines such as tumor necrosis

factor-alpha (TNF-alpha), interleukin-1 beta (IL-1 beta) and

interleukin-6 (IL-6). Based on their mechanism of action, inhibitors of

p38 MAP kinase could play a future role in the treatment of acute and

chronic inflammatory diseases, including rheumatoid arthritis,

osteoarthritis, and Crohn's disease.

" The p38 MAP kinase enzyme represents a promising intervention point for

inhibiting TNF-alpha and IL-1 beta in a highly targeted manner, " stated

Dr. J. Alam, Senior Vice President of Drug Evaluation and Approval.

" Injectable agents that inhibit TNF-alpha and IL-1 beta have emerged as

clinically important strategies for controlling the onset and

progression of inflammation. As an oral drug candidate that inhibits p38

MAP kinase and has potential for once daily dosing, VX-702 represents a

potentially powerful and convenient treatment approach for a number of

inflammatory diseases. "

VX-702 shows potent effects on lowering cytokine production and in

decreasing the signs of arthritis in animal models of inflammation and

arthritis. The activity of VX-702 in vitro and in animal models provides

strong rationale for the clinical development of this compound.

The Phase I double-blind, placebo-controlled, randomized clinical trial

is designed to evaluate the safety, tolerability and pharmacokinetics of

VX-702 in approximately 50 healthy volunteers. As part of the study,

researchers will analyze blood samples to determine the ability of

different doses of VX-702 to inhibit experimentally induced cytokine

production using specific biochemical assays. Vertex is conducting the

study in Europe. Based on information from this study, Vertex expects to

initiate studies in one or more inflammatory disease indications,

including rheumatoid arthritis.