从专利视角谈药物二次创新与仿制药开发——以HIV蛋白酶抑制剂洛匹那韦为例

Suggestions for secondary innovations and generic development for drugs from the perspective of patent——taking HIV protease inhibitor lopinavir as an example

从HIV蛋白酶抑制剂洛匹那韦的国内外专利状况分析出发,基于该药物的上市产品Kaletra的配伍策略,对蛋白酶抑制剂的二次创新和仿制药开发思路进行了探讨,提出该类药物与具有CYP450酶抑制作用的抗菌、抗病毒药物的联用将对艾滋病及其相关的感染类并发症产生良好的疗效,以期从药物复方和适应证扩展技术方向寻求该类专利到期药物的二次创新突破点。

Protease inhibitors （PIs） are a class of antiviral drugs widely used for the treatment of HIV/ AIDS. The status of intellectual property of HIV protease inhibitors lopinavir is briefly reviewed in this paper. Based on the indication of Kaletra, the follow-up studies and generic development of PIs were discussed. It was concluded that the combination of PIs and anti-bacterial/anti-fungal drugs with CYP450 inhibitory effects would be of great use for AIDS and the infectious complications, in the hope of seeking the secondary innovation of other drugs with expired patents in the fields of drug combination and indication expansion.