Abstract
Octreotide acetate (octreotide) is the most prescribed and most studied somatostatin congener, or analog, for gastroenteropancreatic neuroendocrine tumors (GEP-NETs) and carcinoid syndrome, the latter of which may be characterized by debilitating diarrhea and flushing. Approved in the U.S. more than 30 years ago, octreotide is widely used to control the symptoms of carcinoid syndrome and has been shown to demonstrate antiproliferative activity. The two formulations available in the U.S. include a subcutaneous immediate-release (IR) injection introduced in 1989 and a long-acting repeatable (LAR) intramuscular injection approved in 1999. Lanreotide depot (lanreotide), a more recent somatostatin congener, has been available in the U.S. since 2014. Despite widespread use of octreotide LAR, several key challenges exist with the current depot-based treatment paradigm. Studies indicate that LAR formulations are associated with continued unmet patient needs, owing in part to a loss of bioactivity over time that may necessitate progressive supplemental treatment with IR octreotide to adequately control symptoms. Clinicians should understand the key differences in the pharmacokinetic profiles of the LAR and IR formulations that may contribute to bioactivity loss and somatostatin receptor desensitization. In addition, there is a need to re-evaluate the role of IR octreotide in combination with depot therapy to provide consistent bioavailability and better control of carcinoid syndrome symptoms. The purpose of this review is to explore all these issues and to re-establish a rationale for the IR formulation, particularly with respect to novel use cases and its use during the COVID-19 pandemic. Implications for Practice: There is a need to re-evaluate the role of immediate-release octreotide in combination with depot therapy to provide consistent bioavailability and better control of carcinoid syndrome symptoms.
| Original language | English |
|---|---|
| Pages (from-to) | e1171-e1178 |
| Journal | Oncologist |
| Volume | 26 |
| Issue number | 7 |
| DOIs | |
| State | Published - Jul 2021 |
Bibliographical note
Funding Information:We would like to thank Hospicom, Inc., for editorial support. L.B.A. and T.M.O.'s efforts are partially funded by Sun Pharmaceuticals Inc., an NCI Cancer Center Support Grant (P30 CA177558, L.B.A.), and the University of Iowa Specialized Program of Research Excellence (P50 CA174521, T.M.O.). We also wish to thank Donna Gilbreath of the U.K. Markey Cancer Center's Research Communications Office for assistance with the preparation of this manuscript.
Funding Information:
We would like to thank Hospicom, Inc., for editorial support. L.B.A. and T.M.O.'s efforts are partially funded by Sun Pharmaceuticals Inc., an NCI Cancer Center Support Grant (P30 CA177558, L.B.A.), and the University of Iowa Specialized Program of Research Excellence (P50 CA174521, T.M.O.). We also wish to thank Donna Gilbreath of the U.K. Markey Cancer Center's Research Communications Office for assistance with the preparation of this manuscript.
Publisher Copyright:
© 2021 The Authors. The Oncologist published by Wiley Periodicals LLC on behalf of AlphaMed Press.
Keywords
- Carcinoid syndrome
- Lanreotide
- Neuroendocrine tumors
- Octreotide
ASJC Scopus subject areas
- Oncology
- Cancer Research
