新型非肽类口服生长抑素受体配体paltusotine的临床研究进展

刘宇珂; 谭惠文

doi:10.12376/j.issn.2097-0501.2023.03.012

新型非肽类口服生长抑素受体配体paltusotine的临床研究进展

doi: 10.12376/j.issn.2097-0501.2023.03.012

刘宇珂¹,
谭惠文^{1, 2, ,}

1.
四川大学华西医院内分泌代谢科，成都 610041
2.
四川大学华西医院垂体瘤及相关疾病诊疗中心，成都 610041

基金项目:

四川省科技计划项目 2023YFS0259

详细信息

通信作者:
谭惠文，E-mail：tanhuiwen2016@scu.edu.cn

中图分类号: R584.1+1;R736.4;R977
计量
- 文章访问数: 20
- HTML全文浏览量: 1
- PDF下载量: 5
- 被引次数: 0
出版历程
- 收稿日期: 2023-04-10
- 录用日期: 2023-04-21
- 网络出版日期: 2023-09-09

Clinical Research Progress of the Non-Peptide Oral Somatostatin Receptor Ligand Paltusotine

LIU Yuke¹,
TAN Huiwen^{1, 2
, ,}

1.
Department of Endocrinology and Metabolism, West China Hospital, Sichuan University, Chengdu 610041, China
2.
Center for Pituitary Adnomas and Related Diseases, West China Hospital, Sichuan University, Chengdu 610041, China

Funding:

Key Project of Science and Technology Department of Sichuan Province 2023YFS0259

More Information

Corresponding author: TAN Huiwen, E-mail: tanhuiwen2016@scu.edu.cn

摘要

摘要: 生长抑素类似物相关制剂的研发是内分泌代谢领域的热点。第一代奥曲肽、兰瑞肽，第二代帕瑞肽已批准用于肢端肥大症等神经内分泌肿瘤的治疗。而生长抑素受体配体paltusotine作为一种可口服给药的新型非肽类小分子药物，可抑制生长激素和胰岛素样生长因子1的过度分泌。本文分析总结非肽类口服小分子生长抑素配体paltusotine的药物代谢动力学、药效动力学、临床疗效、耐受性和安全性等研究进展。
- 神经内分泌肿瘤 /
- 肢端肥大症 /
- 生长抑素受体配体 /
- 药物代谢动力学 /
- 药效动力学
Abstract: 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.
- neuro-endocrine malignancies /
- acromegaly /
- somatostatin receptor ligands /
- pharmacokinetics /
- pharmacodynamics
注释:

作者贡献：刘宇珂、谭惠文共同参与综述选题、文献检索、分析及论文撰写与修改。

利益冲突：所有作者均声明不存在利益冲突。

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图 1 高选择性生长抑素受体2(SSTR2)激动剂paltusotine的分子结构与作用机制

Figure 1. Molecular structure and mechanism of action of paltusotine, the highly selective somatostatin receptor 2(SSTR2) agonist

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图 2 口服非肽类高选择性生长抑素受体配体paltusotine的生物利用度^[18]

Figure 2. Bioavailability of the oral non-peptide somatostatin receptor ligands(SRLs) paltusotine^[18]

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图 3 Paltusotine对健康志愿者的生长激素和IGF-1分泌抑制效能^[18]

Figure 3. Effect of paltusotine on growth hormone and IGF-1 secretion in healthy volunteers^[18]

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图 4 Paltusotine与传统注射制剂SRLs的疗效比较生长抑素类似物^[20]

Figure 4. Comparison of the efficacy of paltusotine with traditional injectable formulations SRLs^[20]

下载: 全尺寸图片幻灯片

参考文献(24)

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