Objective. To systematically review the literature about the pharmacology, pharmacokinetics, efficacy, dosing, and adverse effects of dolasetron, and to define its role in the management of chemotherapy-and radiation-induced nausea and vomiting.

Data Synthesis. A MedLine search was conducted using 5-HT3-receptor antagonists, antiemetics, chemotherapy toxicity, dolasetron, emesis, nausea, and vomiting as search terms. Reference lists and bibliographies of pertinent articles were also identified and reviewed. Both preclinical and clinical literature were reviewed and analyzed.

Data Synthesis. Dolasetron is a serotonin type 3 (5-HT3)-receptor antagonist with potent antiemetic effects in the management of nausea and vomiting. Following administration, dolasetron is rapidly converted to hydrodolasetron, which is believed to be responsible for the drug's antiemetic activity. Results of multiple studies have demonstrated the efficacy of this agent in the prevention of chemotherapy-induced emesis, including that induced by cisplatin. As a single agent, dolasetron produces a complete response rate (RR) in 44% to 57% of patients treated with cisplatin (≥70 mg/m2) and in 59% to 80% of patients treated with moderately emetogenic chemotherapy, such as cyclophosphamide, methotrexate, and fluorouracil (CMF) therapy. When combined with dexamethasone, the RRs are increased. Dolasetron is well tolerated, with headache (24%) and diarrhea (12%) the most commonly reported adverse effects. The efficacy and safety of dolasetron are comparable to those observed with other 5-HT3-receptor antagonists. According to four recently published clinical practice guidelines for use of antiemetics, dolasetron is an appropriate first-line option for the prevention of nausea and vomiting due to moderately to highly emetogenic chemotherapy. Further clinical trials will determine the optimal dose and the role of this highly effective antiemetic agent for other purposes, such as treatment of delayed emesis and emesis resulting from radiation therapy and high-dose chemotherapy followed by bone marrow transplantation.