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KMID : 1143420180110331082
Public Health Weekly Report
2018 Volume.11 No. 33 p.1082 ~ p.1092
An overview regarding development of therapeutic drugs against HIV/AIDS
Yoon Cheol-Hee

Lee So-Rim
Kim Ki-Soon
Abstract
Background: Current anti-human immunodeficiency virus (anti-HIV) drugs can reduce HIV-associated morbidity, prolong
survival, and prevent HIV transmission. However, the drug resistance is an emerging problem worldwide, because of chronic therapy without interruption during patient¡¯s life span. To overcome the drug-resistance, development of anti-HIV drugs is continued with finding new therapeutic targets that are essential for HIV replication.

Current status: The discovery of HIV as the causative agent of acquired immune deficiency syndrome (AIDS) and an
increasing understanding of the viral replication cycle have been instrumental in research of anti-HIV drug. Anti-HIV drug
discovery has been focused on targeted inhibition of HIV using specific pharmacological agents. Since the approval of
Zidovudine (AZT) in 1987, over 30 anti-HIV drugs belonging to six distinct classes based on their biological function and
resistance profiles are being used: (1) nucleoside-analog reverse transcriptase inhibitors (NRTIs), (2) non-nucleoside reverse transcriptase inhibitors (NNRTIs), (3) integrase inhibitors (INSTIs), (4) protease inhibitors (PIs), (5) fusion inhibitors, and (6) co-receptor antagonists. Additionally, several anti-HIV drugs are being developed, such as long active drugs, humanized antibody, and prodrug metabolized to active form in patients. In this review, we will outline the developmental history of anti-HIV drugs with their basic principles and limitations due to drug resistance.

Future perspective: Anti-HIV drugs are being developed to overcome the drug resistance, adverse effects, and limited
adherence shown in earlier drugs. Currently, reverse transcriptase, protease, and integrase inhibitors are available for
patient care. Although several anti-HIV drugs are effective for patient treatment, researchers have to continue discovering
new therapeutic targets before resistance to current drugs emerges. Furthermore, research and development focused on
agents that target persistent HIV reservoirs should be strengthened, which may lead to prolonged drug-free remission and
HIV cure.
KEYWORD
Human immunodeficiency virus (HIV), anti-HIV drug, Therapeutic target, Drug resistance
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