Cubist Pharmaceuticals Inc announced the issuance by the United States Patent and Trademark Office of patent number 6,248,360, entitled "Complexes to Improve Oral Absorption of Poorly Absorbable Antibiotics." The patent, assigned to International Health Management Associates Inc (IHMA), covers oral formulations of multiple antibiotics, including ceftriaxone, to which Cubist licensed exclusive rights in late 2000. At that time, Cubist acquired rights from IHMA to negotiate for several other oral antibiotics as well.

In conjunction with the patent issuance, Cubist announced that it had achieved clinically relevant systemic levels of ceftriaxone delivered intraduodenally, or directly to the small intestine, in non-human primates. These data confirm earlier studies performed in rodents. Cubist also announced that it has now optimized formulations of oral ceftriaxone for use in proof-of-principle studies in man, expected to commence by the end of 2001.

Hoffmann-La Roche's Rocephin (intravenous ceftriaxone) had sales of over $1 billion in 2000. Intravenous ceftriaxone has been successfully and safely prescribed for over 15 years in both adults and children. The drug is a third-generation cephalosporin that has demonstrated a broad spectrum of bactericidal activity against Gram-positive and Gram-negative bacteria. These organisms are responsible for the majority of community-based infections, which include upper and lower respiratory tract infections (including otitis media, sinusitis, bronchitis and community-acquired pneumonia) and skin and soft tissue infections. These infections result in nearly 80 million treated patients annually in the United States.

Third generation cephalosporins, although effective against some of the more resistant bacteria, are normally poorly absorbed through the mucosal membrane of the intestines, and thus have difficulty reaching the bloodstream systemically. As a result, their use has been predominantly restricted to intravenous use. This newly issued patent protects technology that facilitates the systemic absorption of difficult-to-absorb antibiotics. Importantly, all of the components used to facilitate transport across the intestinal lining are considered safe by the U.S. Food and Drug Administration and appear on the agency's GRAS list (substances Generally Recognized As Safe).

To date, ceftriaxone has been primarily used to treat hospital in-patients due to the lack of an oral version. If successfully developed, Cubist believes that an oral formulation could greatly expand the utility and revenue potential of ceftriaxone through community-based prescribing. In addition, the Company believes oral ceftriaxone could also be used for the continuation of parenteral antibiotic therapy (step-down therapy). Step-down therapy provides multiple benefits: convenience and cost savings of an oral therapy versus parenteral therapy, potential earlier hospital discharge and associated healthcare cost savings, and increased physician confidence in an optimal therapeutic outcome given that a discharged patient is receiving the same therapy taken intravenously in the hospital setting.