Recent advances in antiemetics: new formulations of 5HT3 -receptor antagonists

Cancer Management and Research
James GilmoreLee Schwartzberg

Abstract

To discuss new therapeutic strategies for chemotherapy-induced nausea and vomiting (CINV) involving 5-hydroxytryptamine type 3 (5HT3)-receptor antagonists (RAs). CINV remains poorly controlled in patients receiving moderately emetogenic chemotherapy (MEC) or highly emetogenic chemotherapy (HEC); nausea and delayed-phase CINV (24-120 hours after chemotherapy) are the most difficult to control. National Comprehensive Cancer Network (NCCN) and American Society of Clinical Oncology (ASCO) antiemesis-guideline recommendations for HEC include a four-drug regimen (5HT3 RA, neurokinin 1 [NK1] RA, dexamethasone, and olanzapine). For some MEC regimens, a three-drug regimen (5HT3 RA, NK1 RA, and dexamethasone) is recommended. While 5HT3 RAs have dramatically improved CINV in the acute phase (0-24 hours after chemotherapy), their efficacy declines in the delayed phase. Newer formulations have been developed to extend 5HT3-RA efficacy into the delayed phase. Granisetron extended-release subcutaneous (GERSC), the most recently approved 5HT3 RA, provides slow, controlled release of therapeutic granisetron concentrations for ≥5 days. GERSC is included in the NCCN and ASCO guidelines for MEC and HEC, with NCCN-preferred status for MEC in the ab...Continue Reading

Citations

Nov 8, 2018·Neurogastroenterology and Motility : the Official Journal of the European Gastrointestinal Motility Society·Marta Martín-RuízRaquel Abalo
Sep 30, 2019·Gut·Madhusudan GroverVincenzo Stanghellini
Jul 22, 2019·Nature Communications·Sandip BasakSudha Chakrapani
Nov 18, 2020·Advanced Drug Delivery Reviews·Christian Isalomboto NkangaFarshad Ramazani
Sep 19, 2020·Biophysical Journal·Noelia Rodriguez AraujoJeremías Corradi
Jun 24, 2021·Asia-Pacific Journal of Oncology Nursing·Xinjuan HuangJing Cheng

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