Recent advances in antiemetics

New formulations of 5HT 3 -receptor antagonists

James Gilmore, Steven D’amato, Niesha Griffith, Lee Schwartzberg

Research output: Contribution to journalReview article

3 Citations (Scopus)

Abstract

Purpose: To discuss new therapeutic strategies for chemotherapy-induced nausea and vomiting (CINV) involving 5-hydroxytryptamine type 3 (5HT 3 )-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 (5HT 3 RA, neurokinin 1 [NK 1 ] RA, dexamethasone, and olanzapine). For some MEC regimens, a three-drug regimen (5HT 3 RA, NK 1 RA, and dexamethasone) is recommended. While 5HT 3 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 5HT 3 -RA efficacy into the delayed phase. Granisetron extended-release subcutaneous (GERSC), the most recently approved 5HT 3 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 NK 1 RA. Efficacy and safety of 5HT 3 RAs in the context of guideline-recommended antiemetic therapy are reviewed. Conclusion: Recent updates in antiemetic guidelines and the development of newer antiemetics should help mitigate CINV, this dreaded side effect of chemotherapy. GERSC, the most recently approved 5HT 3 -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.

Original languageEnglish (US)
Pages (from-to)1827-1857
Number of pages31
JournalCancer Management and Research
Volume10
DOIs
StatePublished - Jan 1 2018

Fingerprint

Antiemetics
Receptors, Serotonin, 5-HT3
Drug Therapy
Nausea
Granisetron
Vomiting
Neurokinin-1 Receptor Antagonists
Guidelines
olanzapine
Dexamethasone
Medical Oncology
Combination Drug Therapy
Pharmaceutical Preparations

All Science Journal Classification (ASJC) codes

  • Oncology

Cite this

Recent advances in antiemetics : New formulations of 5HT 3 -receptor antagonists. / Gilmore, James; D’amato, Steven; Griffith, Niesha; Schwartzberg, Lee.

In: Cancer Management and Research, Vol. 10, 01.01.2018, p. 1827-1857.

Research output: Contribution to journalReview article

Gilmore, James ; D’amato, Steven ; Griffith, Niesha ; Schwartzberg, Lee. / Recent advances in antiemetics : New formulations of 5HT 3 -receptor antagonists. In: Cancer Management and Research. 2018 ; Vol. 10. pp. 1827-1857.
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abstract = "Purpose: To discuss new therapeutic strategies for chemotherapy-induced nausea and vomiting (CINV) involving 5-hydroxytryptamine type 3 (5HT 3 )-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 (5HT 3 RA, neurokinin 1 [NK 1 ] RA, dexamethasone, and olanzapine). For some MEC regimens, a three-drug regimen (5HT 3 RA, NK 1 RA, and dexamethasone) is recommended. While 5HT 3 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 5HT 3 -RA efficacy into the delayed phase. Granisetron extended-release subcutaneous (GERSC), the most recently approved 5HT 3 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 NK 1 RA. Efficacy and safety of 5HT 3 RAs in the context of guideline-recommended antiemetic therapy are reviewed. Conclusion: Recent updates in antiemetic guidelines and the development of newer antiemetics should help mitigate CINV, this dreaded side effect of chemotherapy. GERSC, the most recently approved 5HT 3 -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.",
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