生物活性

Dolutegravir (DTG) is a second-generation integrase strand transfer inhibitor (INSTI) and INSTIs are the latest class of potent anti-HIV drugs.Compared to the first generation INSTIs, raltegravir, and elvitegravir, Dolutegravir shows a limited cross-resistance profile.More interestingly, clinical resistance mutations to Dolutegravir in treatment-naive patents have not been observed to this date.Dolutegravir is a dominant strategy in the management of TN and TE patients when compared to recommended comparators.Dolutegravir had no effect on NGM/EE PK or PD. NGM/EE can be administered with DTG without dose adjustment.Dolutegravir is the integrase inhibitor of choice for rescue therapy in multiresistant HIV infection, both in integrase inhibitor-naive patients and in those previously treated with raltegravir or elvitegravir.Treatment with DTG led to less HIV-1 genetic and amino-acid diversification over time, as compared to treatment with RAL or the absence of drug.

化学数据

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

储备液配制

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。