Emisphere Technologies Inc announced the results of its PROTECT Phase III trial evaluating a liquid oral heparin. The PROTECT study demonstrated for the first time in patients that heparin, a macromolecule, could be delivered safely and effectively into the bloodstream in an oral form. While a liquid formulation of oral heparin in a 30-day treatment regimen was deemed to have poor tolerability due to its taste contributing to poor patient compliance in this study, its safety and therapeutic effect were noteworthy. The data presented today suggest that the oral liquid heparin candidate in a 30-day regimen was statistically comparable to its benchmark comparator, Lovenox (enoxaparin) in a 10-day treatment regimen, in reducing the incidences of deep vein thrombosis (DVT) following hip replacement surgery.

The following were highlights discussed by Dr. Hull after a complete review of the data from the PROTECT study:

· Using the Emisphere delivery agent, SNAC (Sodium N-[8-(2 hydroxybenzoyl)amino] caprylate), the liquid oral heparin formulation showed a therapeutic effect (i.e., DVT reduction) in total hip replacement patients that was comparable to injectable Lovenox and superior to historical placebo rates for this patient population.

· A therapeutic dose response of the liquid oral heparin was demonstrated, as evidenced by the statistically significant improvement in DVT reduction (p=0.001) of the high-dose over the low dose.

· There was no evidence of liver toxicity (i.e., no elevated liver enzymes) in patients receiving only the liquid oral heparin formulation.

· There was no evidence of heparin-induced thrombocytopenia (HIT) (i.e., no decreased platelet count) in patients receiving only the liquid oral heparin formulation.

· Bleeding rates were low, suggesting that a fixed dose and no monitoring would be feasible for this entirely oral dosing regimen.

· The high variability in DVT rates among centers, ranging from rates comparable to historical placebo in the total hip replacement patient population to rates consistent with what is considered to be the most effective prolonged outpatient prophylaxis regimen, suggests that certain patients may have over reported compliance rates.

· The liquid oral heparin formulation provided the anticipated anti-thrombotic protection in patients who complied with the protocol.

· The study provides a large patient safety database for support of Emisphere's eligen technology platform, and, more specifically for the Emisphere delivery agent, SNAC, the delivery agent being used in the development of solid oral formulations of heparin in tablet and capsule forms.

· The conclusion, based on the data presented, is that if compliance could be improved through better formulation of the oral SNAC/heparin product candidate, the potential exists to create a significantly efficacious drug in a patient-friendly dosing regimen that would meet or possibly exceed current safety standards, in a fixed dose, with no monitoring required.

· The complete analysis provides a foundation for accelerating the development plan for a solid form of heparin for oral administration in a tablet or capsule form, which could significantly improve upon compliance. Emisphere's first human data from the oral heparin tablet and capsule forms were presented in conjunction with Dr. Hull's presentation, and will be highlighted in a separate announcement to be issued by Emisphere.

Dr. Hull commented, "Our findings document that for the first time in patients, the macromolecule, heparin, in conjunction with the EMISPHERE(R) delivery agent, SNAC, can be delivered orally, and that as an entirely oral regimen, can significantly reduce the frequency of postoperative thromboembolic complications. The encouraging results of the liquid oral heparin regimen, including a promising safety profile, mandates that a solid formulation of unfractionated heparin with improved patient acceptability should be developed."