De Clercq Erik
Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, KU Leuven, B-3000 Leuven, Belgium.
Viruses. 2025 Jul 8;17(7):959. doi: 10.3390/v17070959.
Rilpivirine (RPV, R278474) was highlighted in 2005, two years after the death of Dr. Paul Janssen, as the ideal non-nucleoside reverse transcriptase inhibitor (NNRTI) to treat HIV infections. For this purpose, it was subsequently combined with tenofovir disoproxil fumarate (TDF), tenofovir alafenamide (TAF), darunavir (boosted with ritonavir or cobicistat) or dolutegravir. Its wide-spread use is thanks to its combination with cabotegravir (CAB) in the form of a long-acting intramuscular injection once per month (QM), later twice per month (Q2M), for the treatment of adults, later extended to adolescents and pregnant women, with HIV infections. The long-acting CAB plus RPV should not be administered in patients treated with rifampicin or rifabutin, patients with virological failure or patients with resistance to CAB or RPV, or patients with hepatitis B virus (HBV) infection. Long-acting CAB+RPV may lead to pain at the site of injection which would diminish over time.
利匹韦林（RPV，R278474）在保罗·扬森博士去世两年后的2005年被视为治疗HIV感染的理想非核苷类逆转录酶抑制剂（NNRTI）。为此，它随后与富马酸替诺福韦二吡呋酯（TDF）、替诺福韦艾拉酚胺（TAF）、达芦那韦（与利托那韦或考比司他联用）或多替拉韦联合使用。其广泛应用得益于它与卡博特韦（CAB）以长效肌肉注射的形式联合，最初是每月一次（QM），后来是每月两次（Q2M），用于治疗成人HIV感染，后来扩展至青少年和孕妇。长效CAB加RPV不应给予接受利福平或利福布汀治疗的患者、病毒学治疗失败的患者、对CAB或RPV耐药的患者或乙型肝炎病毒（HBV）感染患者。长效CAB+RPV可能会导致注射部位疼痛，不过这种疼痛会随着时间减轻。
