A somatostatin receptor agonist
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Lanreotide is a peptide analog of somatostatin that binds to somatostatin receptors (SSTRs) with a higher affinity for the somatostatin subgroup 2 receptors SST2, SST3, and SST5 (IC50s = 0.5-1.8, 43-107, and 5.6-32 nM, respectively) than for the subgroup 1 receptors, SST1 and SST4 (IC50s = 500-2,330 and 66-2,100 nM, respectively). Lanreotide (100 nM) inhibits the release of growth hormone from patient-derived pituitary adenoma cells in vitro. It also inhibits tumor growth in human small cell lung cancer (SCLC) mouse xenograft models when administered at a dose of 250 µg, twice daily. Formulations containing lanreotide have been used in the treatment of acromegaly and neuroendocrine tumors.
LX1606 Hippurate (Telotristat etiprate)
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