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Drugs. 2016 Dec;76(18):1779-1786. doi: 10.1007/s40265-016-0664-2.
An extended-release (ER) subcutaneously injectable formulation of the first-generation 5-HT receptor antagonist granisetron is now available in the USA (Sustol), where it is indicated for the prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV) following moderately emetogenic chemotherapy (MEC) or anthracycline and cyclophosphamide combination chemotherapy regimens in adults. Granisetron ER is administered as a single subcutaneous injection and uses an erosion-controlled drug-delivery system to allow prolonged granisetron release. Primary endpoint data from phase III studies after an initial cycle of chemotherapy indicate that, when used as part of an antiemetic regimen, granisetron ER injection is more effective than intravenous ondansetron in preventing delayed CINV following highly emetogenic chemotherapy (HEC); is noninferior to intravenous palonosetron in preventing both acute CINV following MEC or HEC and delayed CINV following MEC; and is similar, but not superior, to palonosetron in preventing delayed CINV following HEC. The benefits of granisetron ER were seen in various patient subgroups, including those receiving anthracycline plus cyclophosphamide-based HEC, and (in an extension of one of the studies) over multiple MEC or HEC cycles. Granisetron ER injection is generally well tolerated, with an adverse event profile similar to that of ondansetron or palonosetron. Thus, granisetron ER injection expands the options for preventing both acute and delayed CINV in adults with cancer receiving MEC or anthracycline plus cyclophosphamide-based HEC.
一种长效（ER）皮下注射剂型的第一代 5-HT 受体拮抗剂格拉司琼现已在美国上市（Sustol），用于预防成人中度致吐性化疗（MEC）或蒽环类和环磷酰胺联合化疗方案后急性和迟发性化疗引起的恶心和呕吐（CINV）。格拉司琼 ER 作为单次皮下注射给药，使用侵蚀控制药物递送系统来允许延长格拉司琼释放。化疗初始周期后 III 期研究的主要终点数据表明，当作为止吐方案的一部分使用时，格拉司琼 ER 注射在预防高度致吐性化疗（HEC）后迟发性 CINV 方面比静脉内昂丹司琼更有效；在预防 MEC 或 HEC 后急性 CINV 和 MEC 后迟发性 CINV 方面与静脉内帕洛诺司琼非劣效；在预防 HEC 后迟发性 CINV 方面与帕洛诺司琼相似，但不优于帕洛诺司琼。格拉司琼 ER 的益处见于各种患者亚组，包括接受蒽环类加环磷酰胺为基础的 HEC 以及（在一项研究的扩展中）多个 MEC 或 HEC 周期。格拉司琼 ER 注射通常具有良好的耐受性，不良事件谱与昂丹司琼或帕洛诺司琼相似。因此，格拉司琼 ER 注射扩大了在接受 MEC 或蒽环类加环磷酰胺为基础的 HEC 的癌症成人中预防急性和迟发性 CINV 的选择。
