2018年5月22日，阿斯利康宣布（AstraZeneca），美国FDA批准新药Lokelma（sodium zirconium cyclosilicate，环硅酸钠锆，曾用名ZS-9），用于治疗罹患高钾血症（hyperkalaemia）的成人患者。这是一种严重的疾病，表现为与心血管、肾脏和代谢相关的血钾水平升高。
  高血钾风险在慢性肾病（CKD）患者以及服用普通心力衰竭（HF）药物（如肾素-血管紧张素-醛固酮系统[RAAS]抑制剂）的患者中显著增加，因为这种药物会增加血钾水平。为了帮助预防高钾血症的复发，通常需要调整或停止RAAS抑制剂治疗，而这可能会危及心脏和肾脏健康，并增加死亡风险。这些患者急需新的治疗方法来降低高血钾风险，同时又避免发生其它的副作用。
  Lokelma是一种高度选择性的口服除钾剂，有望为这一患者群体带来全新治疗选择。该药物无味，且在室温下稳定，目前已经在三项双盲安慰剂对照试验和两项为期12个月的开放标签临床试验中进行了研究。该药物于今年3月底在欧盟获批上市。
  此次Lokelma获得FDA的批准是基于三项双盲、安慰剂对照试验和两项开放标签试验数据的支持。这些研究表明，Lokelma的起效时间是服药后1.0小时，达到正常血钾水平的中位时间是2.2小时，92％的患者在基线后48小时内达到正常血钾水平。该药物的治疗效果可维持长达12个月。
  阿斯利康全球药品开发执行副总裁兼首席医学官Sean Bohen博士表示：“我们很高兴FDA批准Lokelma，它使我们能够帮助解决一项长期的临床需求，为高钾血症患者提供快速和持久的治疗，高钾血症的后果可能非常严重。对于医生来说，这是令人欣慰的，因为Lokelma已经证实可以降低慢性肾病、心力衰竭、糖尿病患者和服用RAAS抑制剂患者的血钾水平。”
  霍夫斯特拉·诺斯维尔Donald and Barbara Zucker医学院教授Steven Fishbane博士表示：“FDA的这一批准是一个令人兴奋的里程碑，它为美国的高钾血症患者提供了一种快速、有效且通常具有良好耐受性的治疗方案。

 完整说明书资料附件：https://www.azpicentral.com/lokelma/lokelma_pi.pdf#page=1
LOKELMA(sodium zirconium cyclosilicate)
IMPORTANT SAFETY INFORMATION FOR LOKELMA™ (sodium zirconium cyclosilicate) 10g FOR ORAL SUSPENSION
WARNINGS AND PRECAUTIONS:
Gastrointestinal Adverse Events in Patients with Motility Disorders: Avoid LOKELMA in patients with severe constipation, bowel obstruction or impaction, including abnormal post-operative bowel motility disorders. LOKELMA has not been studied in patients with these conditions and it may be ineffective and may worsen gastrointestinal conditions
Edema: Each 5 g dose of LOKELMA contains approximately 400 mg of sodium. In clinical trials of LOKELMA, edema was generally mild to moderate in severity and was more commonly seen in patients treated with 15 g once daily. Monitor for signs of edema, particularly in patients who should restrict their sodium intake or are prone to fluid overload (eg., heart failure or renal disease). Advise patients to adjust dietary sodium, if appropriate. Increase the dose of diuretics as needed
ADVERSE REACTIONS: The most common adverse reaction with LOKELMA was mild to moderate edema. In placebo-controlled trials up to 28 days, edema was reported in 4.4%, 5.9%, 16.1% of patients treated with 5 g, 10 g and 15 g of LOKELMA once daily, respectively vs 2.4% of patients receiving placebo.
DRUG INTERACTIONS: LOKELMA can transiently increase gastric pH. In general, oral medications with pH-dependent solubility should be administered at least 2 hours before or 2 hours after LOKELMA. Spacing is not needed if it has been determined the concomitant medication does not exhibit pH-dependent solubility.
INDICATION AND LIMITATION OF USE
LOKELMA is indicated for the treatment of hyperkalemia in adults.
LOKELMA should not be used as an emergency treatment for life-threatening hyperkalemia because of its delayed onset of action.