长效注射用艾滋病预防药物的前景与风险
The promise and pitfalls of long-acting injectable agents for HIV prevention.
作者信息
Landovitz Raphael J, Kofron Ryan, McCauley Marybeth
机构信息
aUCLA Center for Clinical AIDS Research & Education, Los Angeles, California bFHI 360, Connecticut Avenue, Washington, District of Columbia, USA.
出版信息
Curr Opin HIV AIDS. 2016 Jan;11(1):122-8. doi: 10.1097/COH.0000000000000219.
Abstract
PURPOSE OF REVIEW
Preexposure prophylaxis for HIV prevention is highly effective when taken as prescribed. Adherence to required dosing regimens for protection may pose challenges. Long-acting agents for HIV prevention may have the potential to improve adherence via favorable pharmacokinetics supportive of infrequent dosing. This review focuses on the potential benefits and considerations for the study and use of 2 long-acting injectable agents, cabotegravir (GSK1265744LA, CAB LA) and rilpivirine (TMC278LA, RPV LA), for use as chemoprophylaxis for HIV prevention.
RECENT FINDINGS
Oral RPV is United States Food and Drug Administration approved for HIV treatment (in combination with other antiretrovirals). Both CAB LA and RPV LA are currently in phase 2a safety/tolerability/pharmacokinetic studies in anticipation and support of future efficacy evaluation. Both agents have favorable pharmacokinetics, and use is complicated by injection site reactions.
SUMMARY
Long-acting injectable formulations, if safe and well tolerated, may improve pharmacokinetic coverage of exposures to HIV infection. Complexities around safety, tolerability, and starting/stopping protocols require careful consideration.
摘要
综述目的
暴露前预防用药在按规定服用时对预防HIV非常有效。坚持采用所需的给药方案以实现保护可能会带来挑战。用于预防HIV的长效药物可能有潜力通过支持不频繁给药的良好药代动力学来提高依从性。本综述重点关注两种长效注射用药物，卡博特韦（GSK1265744LA，CAB LA）和rilpivirine（TMC278LA，RPV LA），用作HIV预防化学预防的潜在益处及相关考量。
最新发现
口服RPV已获美国食品药品监督管理局批准用于HIV治疗（与其他抗逆转录病毒药物联合使用）。CAB LA和RPV LA目前均处于2a期安全性/耐受性/药代动力学研究阶段，以期并支持未来的疗效评估。两种药物均具有良好的药代动力学特性，且使用过程中会出现注射部位反应。
总结
长效注射用制剂如果安全且耐受性良好，可能会改善对HIV感染暴露的药代动力学覆盖。围绕安全性、耐受性以及起始/停药方案的复杂性需要仔细考虑。
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