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Overview of Aplaviroc, an investigational drug

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Aplaviroc is an investigational drug that was developed 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 CCR5 receptor on the surface of T cells, preventing the HIV virus from entering these cells and replicating.

Mechanism of Action

Aplaviroc functions by selectively binding to the CCR5 receptor, a co-receptor that HIV uses to enter CD4+ T cells. By blocking this receptor, aplaviroc prevents the virus from attaching to and entering the host cells, thereby inhibiting its replication cycle. This mechanism is similar to other CCR5 antagonists, such as maraviroc, which are used in the treatment of HIV.

Development and Clinical Trials

Aplaviroc was developed by GlaxoSmithKline and underwent several phases of clinical trials. During these trials, the drug was evaluated for its efficacy in reducing viral load in patients with HIV, as well as its safety and tolerability. However, the development of aplaviroc was halted due to concerns about liver toxicity observed in some patients during the trials.

Pharmacokinetics

The pharmacokinetic profile of aplaviroc includes its absorption, distribution, metabolism, and excretion. Aplaviroc is administered orally and is absorbed into the bloodstream, where it exerts its effects on the CCR5 receptor. The drug is metabolized primarily in the liver and excreted through the kidneys.

Potential Side Effects

While aplaviroc showed promise in early trials, its development was discontinued due to adverse effects, particularly hepatotoxicity. Other potential side effects observed in clinical trials included gastrointestinal disturbances, headache, and dizziness. The risk of liver damage was a significant concern, leading to the cessation of further development.

Current Status

As of now, aplaviroc is not approved for use in any country, and its development has been discontinued. Research into CCR5 antagonists continues, with other drugs in this class being used in clinical practice.

Related Pages

• HIV/AIDS
• CCR5 receptor antagonist
• Maraviroc
• GlaxoSmithKline

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