Nobex Corp. has completed a Phase I clinical trial in the development and commercialization of its Apaza compound, a new drug for the treatment of inflammatory bowel disease (IBD).

The trial, the first in human subjects, explored the tolerance, safety, and pharmacokinetics of Apaza and its metabolites. Nobex is based in RTP.

Apaza actually combines two marketed drugs, an anti-inflammatory drug (5-ASA), the standard of care in IBD today, and an immune modulator (4-APAA), a component of an established drug in Japan for treating rheumatoid arthritis. For the Apaza compound, these two drugs are chemically joined together for delivery into the colon, the site of the disease, where they are separated by enzymes present in the colon and then act through their different biological mechanisms, according to Nobex.

Nobex said Apaza was evaluated in 16 healthy volunteers in a randomized, placebo-controlled study. Four dose levels were assessed, and in each dose group, three subjects were given the active drug and one subject was given a placebo.

The data revealed that Apaza is safe at the doses studied. Analysis of blood and urine samples provided evidence of little absorption into the body of the intact Apaza molecule, the chemical bond between the two drugs was broken in the colon to release each drug, and blood and urine levels of 5-ASA and 4-APAA and their metabolites were low.

The finding that low amounts of drug and metabolites were discovered in the bloodstream is desirable, Nobex said, since it implies that most of the drug is acting in the gastrointestinal tract as intended and that there is likely to be a lower risk of side effects that could arise from wide distribution in the body by the bloodstream.

“We are confident of the strong clinical and market potential of this compound as the next generation of 5-ASA based drugs for IBD,” said Christopher Price, president and chief executive officer of Nobex. “Because Apaza utilizes two complementary mechanisms of action, anti-inflammatory and immune modulation, we believe the severity of inflammation in IBD, a debilitating, chronic disease, can be greatly reduced.”

Price added that the safety demonstrated in this trial and the pharmacokinetic data observed permit the development of Apaza to continue on schedule. It is projected to enter a first Phase II clinical trial in IBD patients in 2004, and Nobex said it is actively seeking partners for commercialization.

In addition to reporting the Phase I results, Nobex said it selected UK-based Avecia for process optimization and scale-up of Apaza to prepare clinical and commercial supplies.

Nobex Corp.: