Pharmacokinetics and efficacy of the long-acting somatostatin analogue somatuline in acromegaly

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Abstract
Johnson MR, Chowdrey HS, Thomas F, Grint C, Lightman SL. Pharmacokinetics and efficacy of the long-acting somatostatin analogue somatuline in acromegaly. Eur J Endocrinol 1994;130:229–34. ISSN 0804–4643 The aim of this work was to assess the use of a sustained-release formulation of somatuline, a long-acting analogue of somatostatin, in the treatment of acromegaly. Fifteen patients with active acromegaly, as defined by random growth hormone (GH) levels greater than 10 mU/l, which fail to be suppressed to less than 5 mU/l following an oral glucose load, were studied. Somatuline was administered as an intramuscular injection in two regimens: eight patients were given a single injection of the sustained-release formulation and blood samples taken over the next month for the measurement of both basal levels of GH and the GH response to thyrotrophin-releasing hormone; and eight patients were given injections of the sustained-release formulation at 2-week intervals over a 6-month period and basal plasma GH levels and the GH response to both an oral glucose load and to thyrotrophin-releasing hormone was assessed. Following a single intramulscular dose of the sustained-release preparation, random GH levels were reduced to below 10 mU/l in five patients and by greater than 50% of basal levels in the remainder. The insulin-like growth factor I (IGF-I) levels fell to within the normal range in three patients. In the long-term efficacy study, GH levels were reduced to < 10 mU/l in 7/8 patients. The IGF-I levels were normalized in four patients. Five of the eight patients experienced diarrhoea, two of mild and three of moderate severity; none of the patients withdrew from the study. Somatuline has been shown to be effective in the treatment of acromegaly. In its sustained-release formulation it clearly represents a useful therapeutic advance, although at the dosage and frequency of injection used in the current protocols it did not provide optimum GH suppression in all patients. MR Johnson, Department of Medicine, Bristol Royal Infirmary, Upper Maudlin Road, Bristol BS2 8HW, UK

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