OSI Pharmaceuticals Inc provided an update on the progress of two early clinical programmes from its diabetes and obesity R&D operations. Phase-I clinical trial data on both PSN821 and PSN602 showed positive evidence of clinical activity, and both candidates are now progressing to the next stage of clinical development. PSN821 completed a single dose phase-I trial in healthy volunteers and diabetes patients, where evidence of glucose lowering was seen in response to a standard nutrient challenge. PSN602 completed a phase-I trial, where indications of activity in the form of significant reductions in food intake in standardized meal intake assessments were seen after 14 days of dosing in overweight/obese subjects. PSN821, an oral GPR119 agonist being developed for the treatment of type-2 diabetes and PSN602, an oral dual monoamine reuptake inhibitor and 5-HT1A agonist being developed for the treatment of obesity, were discovered by OSI's diabetes and obesity R&D team and are wholly owned by OSI. Full data from the PSN602 phase-I trial will be presented at a scientific meeting in the second half of 2009.

"We are pleased with the progress we have made in the first-in-human studies of PSN821 and PSN602," stated Anker Lundemose, president of (OSI) Prosidion. "In keeping with our view that we should focus on establishing differentiation early in development programs, the follow-on studies for both PSN821 and PSN602 will include active comparator arms."

PSN821 has progressed to a 14-day phase-I trial which may allow a preliminary assessment of impacts on gastric emptying and glucose data in addition to safety. Presuming continued success in this programme, OSI will initiate a follow-on 28-day dosing phase-IIa study or a three-month dosing phase-IIb study in 2010. The phase-II study will include sitagliptin as a comparator. PSN602 is now progressing with a 28-day dosing phase-IIa study, which includes sibutramine as a comparator.

In the double-blind, placebo-controlled, ascending single dose first-in-human study, PSN821 was generally well tolerated at doses up to 3000mg in healthy volunteers and 1000mg (the top dose tested) in patients with type 2 diabetes, with no clinically important adverse effects on laboratory tests, 12-lead ECGs or vital signs.

In the double-blind, placebo-controlled, ascending single and multiple dose first-in-human study, PSN602 was generally well tolerated at doses up to 20mg daily for 14 days. At 30mg daily for 14 days, the incidence of adverse events increased and one subject experienced syncope.

OSI Pharma is committed to 'shaping medicine and changing lives' by discovering, developing and commercializing high-quality, novel and differentiated personalized medicines designed to extend life and improve the quality of life for patients with cancer and diabetes/obesity.