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Long‐Acting Octreotide and Prolonged‐Release Lanreotide Formulations Have Different Pharmacokinetic Profiles
Author(s) -
Astruc Beatrice,
Marbach Peter,
Bouterfa Hakim,
Denot Caroline,
Safari Mitra,
Vitaliti Alessandra,
Sheppard Michael
Publication year - 2005
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270005277936
Subject(s) - lanreotide , octreotide , pharmacokinetics , somatostatin , therapeutic index , medicine , pharmacology , chemistry , endocrinology , acromegaly , drug , hormone , growth hormone
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 day 1, lag from days 2 to 6, then prolonged plateau phase (days 11–41); 60‐mg PK was dose proportional. Lanreotide 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 mg/28 d suggested a C mean of 4455 ρg/mL (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, prolonged‐release lanreotide requires exposure constantly above the therapeutic target to enable monthly longterm therapy.