Citation: | LIU Yuke, TAN Huiwen. Clinical Research Progress of the Non-Peptide Oral Somatostatin Receptor Ligand Paltusotine[J]. Journal of Rare Diseases, 2023, 2(3): 414-419. DOI: 10.12376/j.issn.2097-0501.2023.03.012 |
The research and development of somatostatin analogues is a hot area in endocrinology and metabolism. The first generation octreotide, lanreotide and the second generation pareotide have been approved to be effective for the treatment of neuroendocrine tumors such as acromegaly. However, paltusotine, a somatostatin receptor ligand, is a novel non-peptide small molecule drug which can be administered orally and inhibits excessive secretion of growth hormone and insulin-like growth factor 1. This review summarizes the research progress of the pharmacokinetics, pharmacodynamics, clinical efficacy, telerability, and safety of paltusotine.
[1] |
Zhao J, Fu H, Yu J, et al. Prospect of acromegaly therapy: molecular mechanism of clinical drugs octreotide and paltusotine[J]. Nat Commun, 2023, 14(1): 962. doi: 10.1038/s41467-023-36673-z
|
[2] |
Gadelha MR, Wildemberg LE, Kasuki L. The future of somatostatin receptor ligands in acromegaly[J]. J Clin Endocrinol Metab, 2022, 107(2): 297-308. doi: 10.1210/clinem/dgab726
|
[3] |
Stueven AK, Kayser A, Wetz C, et al. Somatostatin analogues in the treatment of neuroendocrine tumors: past, present and future[J]. Int J Mol Sci, 2019, 20(12): 3049. doi: 10.3390/ijms20123049
|
[4] |
Zhao J, Wang S, Markison S, et al. Discovery of paltusotine (CRN00808), a potent, selective, and orally bioavailable non-peptide SST2 agonist[J]. ACS Med Chem Lett, 2022, 14(1): 66-74.
|
[5] |
McLaren DS, Murray RD. Paltusotine, a novel oral somatostatin receptor ligand in the management of acromegaly[J]. J Clin Endocrinol Metab, 2023, 108(5): e193-e194. doi: 10.1210/clinem/dgac762
|
[6] |
Pawlikowski M, Mełeń-Mucha G. Somatostatin analogs-from new molecules to new applications[J]. Curr Opin Pharmacol, 2004, 4(6): 608-613. doi: 10.1016/j.coph.2004.06.010
|
[7] |
Patel M, Tena I, Jha A, et al. Somatostatin receptors and analogs in pheochromocytoma and paraganglioma: old players in a new precision medicine world[J]. Front Endocrinol (Lausanne), 2021, 12: 625312. doi: 10.3389/fendo.2021.625312
|
[8] |
Ishida A, Tajima Y, Okabe Y, et al. Discovery and SAR studies of orally active somatostatin receptor subtype-2 (SSTR2) agonists for the treatment of acromegaly[J]. ACS Chem Neurosci, 2020, 11(10): 1482-1494. doi: 10.1021/acschemneuro.0c00124
|
[9] |
Ionovici N, Carsote M, Terzea DC, et al. Somatostatin receptors in normal and acromegalic somatotroph cells: the U-turn of the clinician to immunohistochemistry report-a review[J]. Rom J Morphol Embryol, 2020, 61(2): 353-359. doi: 10.47162/RJME.61.2.05
|
[10] |
Ludlam WH, Anthony L. Safety review: dose optimization of somatostatin analogs in patients with acromegaly and neuroendocrine tumors[J]. Adv Ther, 2011, 28(10): 825-841. doi: 10.1007/s12325-011-0062-9
|
[11] |
Samson SL, Nachtigall LB, Fleseriu M, et al. Maintenance of acromegaly control in patients switching from injectable somatostatin receptor ligands to oral octreotide[J]. J Clin Endocrinol Metab, 2020, 105(10): e3785-e3797. doi: 10.1210/clinem/dgaa526
|
[12] |
Wolters TLC, Roerink SHPP, Sterenborg RBTM, et al. The effect of treatment on quality of life in patients with acromegaly: a prospective study[J]. Eur J Endocrinol, 2020, 182(3): 319-331. doi: 10.1530/EJE-19-0732
|
[13] |
Antunes X, Kasuki L, Gadelha MR. New and emerging pharmacological treatment options for acromegaly[J]. Expert Opin Pharmacother, 2021, 22(12): 1615-1623. doi: 10.1080/14656566.2021.1908998
|
[14] |
Fleseriu M, Biller BMK, Freda PU, et al. A pituitary society update to acromegaly management guidelines[J]. Pituitary, 2021, 24(1): 1-13. doi: 10.1007/s11102-020-01091-7
|
[15] |
李丹婷, 谭惠文. 生长抑素类似物帕瑞肽的药动学和药效学研究进展[J]. 现代医药卫生, 2021, 37(24): 4137-4141. doi: 10.3969/j.issn.1009-5519.2021.24.001
|
[16] |
谭惠文, 覃萌, 余叶蓉, 等. 肢端肥大症诊断和药物治疗进展——2021年《垂体协会肢端肥大症诊治指南更新》解读[J]. 中国全科医学, 2021, 24(27): 3397-3403. doi: 10.12114/j.issn.1007-9572.2021.02.016
|
[17] |
Theodoropoulou M, Stalla GK. Somatostatin receptors: from signaling to clinical practice[J]. Front Neuroendocrinol, 2013, 34(3): 228-252. doi: 10.1016/j.yfrne.2013.07.005
|
[18] |
Madan A, Markison S, Betz SF, et al. Paltusotine, a novel oral once-daily nonpeptide SST2 receptor agonist, suppresses GH and IGF-1 in healthy volunteers[J]. Pituitary, 2022, 25(2): 328-339. doi: 10.1007/s11102-021-01201-z
|
[19] |
Muhammad A, Coopmans EC, Gatto F, et al. Pasireotide responsiveness in acromegaly is mainly driven by somatostatin receptor subtype 2 expression[J]. J Clin Endocrinol Metab, 2019, 104(3): 915-924. doi: 10.1210/jc.2018-01524
|
[20] |
Gadelha MR, Gordon MB, Doknic M, et al. ACROBAT edge: safety and efficacy of switching injected SRLs to oral paltusotine in patients with acromegaly[J]. J Clin Endocrinol Metab, 2023, 108(5): e148-e159. doi: 10.1210/clinem/dgac643
|
[21] |
Coopmans EC, Muhammad A, van der Lely AJ, et al. How to position pasireotide lar treatment in acromegaly[J]. J Clin Endocrinol Metab, 2019, 104(6): 1978-1988. doi: 10.1210/jc.2018-01979
|
[22] |
US National Library of Medicine. ClinicalTrials. gov(2021). A study to evaluate the safety and efficacy of paltusotine for the treatment of acromegaly (ACROBAT Evolve). (2021-07-16)[2023-04-10]. https://clinicaltrials.gov/ct2/show/NCT03792555.
|
[23] |
US National Library of Medicine. ClinicalTrials. gov (2021). A study to evaluate the safety and efficacy of paltusotine for the treatment of acromegaly (ACROBAT edge)(2021-07-29)[2023-04-10]. https://clinicaltrials.gov/ct2/show/NCT03789656.
|
[24] |
Martin S, Bender RH, Krasner A, et al. Development and evaluation of the acromegaly symptom diary[J]. J Patient Rep Outcomes, 2023, 7(1): 15. doi: 10.1186/s41687-023-00541-7
|