Aplaviroc
Overview[edit | edit source]
Aplaviroc is a pharmaceutical compound that was investigated as a potential treatment for HIV/AIDS. It belongs to a class of drugs known as CCR5 receptor antagonists, which are designed to block the entry of the HIV virus into human cells. Aplaviroc was developed to target the CCR5 co-receptor on the surface of CD4+ T cells, which is one of the primary entry points for the virus.
Mechanism of Action[edit | edit source]
Aplaviroc functions by binding to the CCR5 receptor, thereby preventing the HIV virus from attaching to and entering the CD4+ T cells. This mechanism is crucial because the CCR5 receptor is one of the two main co-receptors, along with CXCR4, that HIV uses to gain entry into host cells. By blocking this pathway, aplaviroc aims to reduce the viral load in patients and slow the progression of HIV/AIDS.
Development and Clinical Trials[edit | edit source]
Aplaviroc was developed by GlaxoSmithKline and underwent several phases of clinical trials. During these trials, the drug was evaluated for its efficacy in reducing HIV viral load and its safety profile in patients. However, the development of aplaviroc was eventually discontinued due to concerns about liver toxicity observed in some patients during the trials.
Pharmacokinetics[edit | edit source]
The pharmacokinetics of aplaviroc involve its absorption, distribution, metabolism, and excretion in the human body. Aplaviroc is administered orally and is absorbed into the bloodstream, where it exerts its effects on the CCR5 receptors. The drug is metabolized primarily in the liver and excreted through the kidneys.
Side Effects[edit | edit source]
During clinical trials, aplaviroc was associated with several side effects. The most significant concern was hepatotoxicity, which led to the discontinuation of its development. Other side effects included gastrointestinal disturbances, headache, and fatigue. The risk of liver damage was deemed too high to continue its development as a safe therapeutic option for HIV/AIDS patients.
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