Long-acting octreotide and prolonged-release lanreotide formulations have different pharmacokinetic profiles

Single-dose pharmacokinetic (PK) profiles and multiple-dose PK modeling were compared for long-acting octreotide (20 or 60 mg) and prolonged-release lanreotide (90 or 120 mg) over 91 days; steady-state profiles were simulated. All treatments were well tolerated. Octreotide 20-mg profile showed increased concentration on clay 1, lag from days 2 to 6, then prolonged plateau phase (days 11-41); 60-mg PK was dose proportionol. Lonreotide 90-mg profile showed C-max on day 1 then elimination (apparent t(1/2) 25.5 days); 120-mg profile was underproportional. Steady-state PK of octreotide 20 mg/28 d suggested a C-mean of 1216 pg/mL (range, 1065-1585) with low fluctuation index (43%). Steady-state PK of lanreotide 90 mgl 28 d suggested a C-mean of 4455 pglmL (range, 2499-9279) with high fluctuation index (152%). Long-acting octreotide had more predictable PK than prolonged-release lanreotide. Simulated steady-state profiles suggest long-acting octreotide could be optimized to meet individual patient needs. In contrast, proloned-release lanreotide requires exposure canstantly above the therapeutic target to enable monthly long-term therapy.