Aplaviroc

Aplaviroc (also known by its developmental code name GW873140) is a pharmaceutical drug that was investigated for the treatment of HIV/AIDS. It belongs to a class of medications known as CCR5 receptor antagonists, which work by blocking the CCR5 receptor on CD4 cells. The CCR5 receptor is one of the pathways through which the Human Immunodeficiency Virus (HIV) enters cells. By inhibiting this receptor, aplaviroc aims to prevent HIV from entering and infecting CD4 cells, thereby slowing down the progression of the disease.

Mechanism of Action

Aplaviroc functions by selectively binding to the CCR5 receptor on the surface of CD4 cells. This receptor is a critical entry point used by the most common strains of HIV (R5-tropic HIV) to infect host cells. By blocking this receptor, aplaviroc prevents the virus from attaching to and entering the CD4 cells, thus inhibiting the replication cycle of HIV.

Clinical Trials and Development

The development of aplaviroc was initiated in the early 2000s, with several clinical trials conducted to assess its efficacy and safety in HIV-infected individuals. Initial phase I and II trials showed promise, indicating that aplaviroc could effectively reduce viral load in patients with R5-tropic HIV. However, during phase III clinical trials, concerns arose regarding the drug's safety profile, particularly liver toxicity. These safety concerns led to the discontinuation of aplaviroc's development for the treatment of HIV/AIDS.

Safety and Side Effects

The clinical trials of aplaviroc identified potential liver toxicity as a significant concern. Some participants in the trials experienced elevated liver enzymes, a sign of liver damage, which in some cases led to the cessation of the drug's administration. Due to these safety issues, the development of aplaviroc was halted, and it never received approval for clinical use.

Current Status

As of the last update, aplaviroc is not available for the treatment of HIV/AIDS. The drug's development was discontinued due to safety concerns, and it did not proceed to market approval. Research in the field of HIV treatment continues, with other CCR5 antagonists and various antiretroviral therapies being explored and developed to provide effective treatment options for individuals living with HIV/AIDS.

See Also

• Antiretroviral drug
• HIV/AIDS
• CCR5 receptor
• CD4 cell