第二代整合酶链转移抑制剂dolutegravir

摘要

Dolutegravir is the second-generation integrase strand transfer inhibitor, and it has higher barrier for resistance compared with raltegravir and elvitegravir and can be used once daily. Dolutegravir can be still administered to the patients who have HIV resistance to raltegravir and elvitegravir, however, its dosing frequency has to be changed to twice a day. This drug shares the mechanism of action with raltegravir and elvitegravir and dosage adjustments are not necessary for the patients with renal and hepatic impairment. The most common adverse reactions seen with dolutegravir in clinical trials are insomnia and headache, occurring in only 2%to 3%of patients. In conclusion, dolutegravir has characteristics of signiifcant efifcacy and good tolerance.%dolutegravir是第二代整合酶链转移抑制剂。与第一代整合酶链转移抑制剂相比，dolutegravir具有更高的耐药发展屏障，可一天1次给药。对已产生对拉替拉韦和elvitegravir耐药的人免疫缺陷病毒感染患者，仍可使用dolutegravir，但用药频率调整为一天2次。dolutegravir用于肝、肾功能损害患者时不需剂量调整。在临床试验中，dolutegravir治疗的最常见不良反应是失眠和头痛，发生率均为2%~3%。作为一种新的整合酶链转移抑制剂， dolutegravir具有疗效显著、耐受性好的特点。