Protease Inhibitors a milestone in the treatment of AIDS

Main Category: HIV / AIDS
Article Date: 13 Jul 2004 - 15:00 PDT

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Following more than a decade of early AIDS research, introduction of the first protease inhibitors remains one of the significant milestones in the development of treatments for AIDS and HIV-infected patients. The role of this therapeutic class continues to evolve as more tolerable, convenient, and efficacious agents are developed.

T he HIV protease enzyme breaks up large proteins into the smaller particles which are reassembled to make new copies of the "working" virus. Protease inhibitors (PIs) slow the rate of HIV replication by blocking the protease enzyme. The new HIV particles produced when protease is disabled are immature and non-infectious.

Protease inhibitors are considered by many to be the first real breakthrough in AIDS research. The first products in this therapeutic class were approved between the end of 1995 and through the first quarter of 1996. When PIs are taken in combination with other agents, the number of people becoming ill from opportunistic infections or dying from AIDS dropped by about 70%, according to the AIDS Treatment Data Network.



Drug resistance may develop as HIV makes copies of itself that are slightly different from its predecessors, with new protease made by the virus that can be less susceptible to the PI's enzyme blocking mechanism. Drug resistance is best avoided by greatly reducing the rate of HIV replication - the less HIV being made in the body, the less chance a drug-resistant virus will be created. Highly active anti-retroviral therapy (HAART) has become the standard therapeutic stratagem for keeping HIV levels as low as possible. Typical three-drug HAART regimens include a PI or non-nucleoside reverse transcriptase inhibitor (NNRTI) with a combination of two nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs).

Writing for HIV and Hepatitis.com (see Readings and Resources), Charles Hicks, MD of Duke University Medical Center suggests the goal of long-term therapeutic success has recently trended prescribing patterns toward non-PI based HAART regimens, a trend that bears re-examination as PIs have become simpler and more efficacious. Continues.....Physician's Weekly

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