Products

Navitas’ lead asset has introduced a new drug class that is thought to act via enhanced coupling of eNOS (endothelial nitric oxide synthase), and is abbreviated “eNOSC” for eNOS coupler. The mechanism allows for the direct treatment of endothelial dysfunction, which is know to be a principal actor in hypertension. The drug’s efficacy in hypertension is evidenced by European clinical trials data from over 10,000 patients, and a US Phase II trial. Its favorable safety profile is supported by favorable US Phase II results, a strong European dossier, and about 2 million patient-years of post-launch exposure. The drug was developed and launched in Europe by a European company. Navitas has obtained from the drug’s European originator an exclusive US license on the compound as a monotherapy and a global license on the use of the drug in combination formulations. Additionally, Navitas has extensive intellectual property on isomer preparations of the drug.

The lead drug has been on the market in European countries for about 20 years, but its mechanism of action became clear only recently, when four different laboratories (one in the US, one in Japan and two in Europe) independently reported the drug’s favorable effects upon nitric oxide (NO).

On the basis of favorable, unexpected, statistically-significant US Phase II findings (taught against explicitly in the prior art), Navitas has created new intellectual property for application to the US market. An End of Phase II meeting was held with the FDA on 16 June 2006. Navitas was encouraged by the outcome of the meeting, whose official minutes are available under confidentiality.

The drug has been demonstrated as yielding clinically-significant improvements in blood pressure when added to the therapy of patients poorly controlled on other agents, including ACE inhibitors, calcium-channel blockers and beta blockers. This efficacy in hypertension resistant to a broad variety of agents underscores the potential of the drug as first in a new mechanistic class.

Consistent with the drug’s ability to treat endothelial dysfunction (eNOS uncoupling), the drug already has favorable clinical data in several diseases associated with endothelial dysfunction, including (among others):

• Pulmonary hypertension: Three favorable proof of concept trials (two with placebo control) in Europe, and a recent compassionate-use case in the US. Ready for US Phase III, which will be initiated shortly after funding.
• Systemic hypertension: Extensive trials (>10,000 patients); launched in France, Germany and several other countries.
• Diabetes: Blood glucose reduced among diabetes patients in hypertension trials.
• High lipids: Cholesterol and triglycerides reduced among patients in hypertension trials.
• Claudication: small study demonstrating increased walking distance.