Title:Preparation of Long-Acting Somatostatin and GnRH Analogues and
Their Applications in Tumor Therapy
Volume: 19
Issue: 1
Author(s): Fang Yu*, Tingting Zhang, Fenghua Fu, Aiping Wang and Xinyong Liu
Affiliation:
- Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Shandong University), Ministry of Education,
School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, Ji'nan, People’s Republic
of China
- State Key Laboratory of Long-acting and Targeting Drug Delivery Technologies, Yantai, People’s
Republic of China
Keywords:
Hormonal drugs, long-acting analogues, somatostatin analogues, GnRH analogues, tumor therapy, hormone-sensitive tumors.
Abstract: Hormonal drugs are essential treatment options for some hormone-dependent or hormone-
sensitive tumors. The common dosage forms of hormonal drugs have a short half-life.
Hence, frequent administration is needed, which results in poor patient compliance. Nevertheless,
using drug delivery technology, somatostatin analogues (SSAs) and gonadotropin-releasing hormone
(GnRH) analogues are prepared into long-acting formulations that can significantly prolong
the action time of these drugs, reducing medication frequency and increasing patient compliance.
Such drugs are advantageous when treating acromegaly, gastroenteropancreatic neuroendocrine tumors
(GEP-NETs), breast cancer, prostate cancer, and other diseases having a relatively long
course. SSAs and GnRH analogues are two typical hormonal drugs, the long-acting formulations
of which are essential in clinical practice. This review summarized the preparation methods and
clinical application of long-acting formulations in cancer. Further, the action mechanism and new
research of SSAs and GnRH analogues were discussed, and suggestions related to the development
of long-acting SSAs and GnRH analogues were provided.