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Review
. 2018 Jul 3:10:1827-1857.
doi: 10.2147/CMAR.S166912. eCollection 2018.

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

James Gilmore  1 , Steven D'Amato  2 , Niesha Griffith  3 , Lee Schwartzberg  4   5
Affiliations
Review

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

James Gilmore et al. Cancer Manag Res. .

Abstract

Purpose: To discuss new therapeutic strategies for chemotherapy-induced nausea and vomiting (CINV) involving 5-hydroxytryptamine type 3 (5HT3)-receptor antagonists (RAs).

Summary: 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 absence of an NK1 RA. Efficacy and safety of 5HT3 RAs in the context of guideline-recommended antiemetic therapy are reviewed.

Conclusion: Recent updates in antiemetic guidelines and the development of newer antiemet-ics should help mitigate CINV, this dreaded side effect of chemotherapy. GERSC, the most recently approved 5HT3-RA formulation, is indicated for use with other antiemetics to prevent acute and delayed nausea and vomiting associated with initial and repeat courses of MEC and anthracycline-cyclophosphamide combination-chemotherapy regimens.

Keywords: chemotherapy-induced nausea and vomiting; granisetron; granisetron extended-release injection; granisetron extended-release subcutaneous; serotonin-receptor antagonist.

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Conflict of interest statement

Disclosure JG has served as a member of a speaker bureau or advisory committee for Heron Therapeutics. LS has acted in a consultant/advisory role for Eisai, Helsinn, Merck, and Tesaro, received research funding from Helsinn, and served as a member of a speaker bureau or advisory committee for Helsinn and Merck. NG has served as a member of a speaker bureau or advisory committee for Eisai, Heron, and Tesaro. The authors report no other conflicts of interest in this work.

Figures

Figure 1
Figure 1
Extended-release formulations of granisetron: plasma granisetron concentrations following administration. Notes: Data from these studies.–, Dashed line indicates minimum therapeutic concentration of granisetron 2 ng/mL (data from patent application 20120258164 for granisetron transdermal delivery system).
Figure 2
Figure 2
Biochronomer technology mechanism of action.
See this image and copyright information in PMC

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