Protease Inhibitor

Protease inhibitor is a class of antiviral drugs widely used in treated of HIV/AIDS and hepatitis which is caused by hepatitis C virus. Protease inhibitor prevents viral replication by selectively binding to viral proteases (for instance HIV-1 protease) and blocking proteolytic cleave of  protein precursors that are important for infectious viral particles production.

Protease inhibitor has been developed or is currently undergoing testing for treatment of various viruses such as the ones listed below:

• Hepatitis C: telaprevir, boceprevir
• HIV/AIDS-antiretroviral protease inhibitors

This inhibitor prevents HIV from multiplying and also reduces the level of virus in the body. Whenever the level of virus in the blood is kept low, the immune system has a better chance of growing stronger and recovering. Protease inhibitor was the second class of antiretroviral drugs to be developed. The first were saquinavir (Hoffman-La Roche) and Ritonovir (Abbott) which were approved in the late 1955 to 1996.

Researchers are carrying out investigations into use of protease inhibitor that is developed for treatment of HIV as anti-protozoals for use against gastrointestinal and malaria protozoal infections:

• Lopinavir and ritonavir combination was found to be effective against infections such as Giardia
• Cysteine protease inhibitor drug has the property to cure Chagas disease common in mice
• Lopinavir, Saquinavir and ritonavir have anti-malarial properties

When protease inhibitor is used as a combination therapy, it helps in the following ways:

• Reduced viral loads that can lead to increase or stable CD4+ cell counts. This is also a sign that the immune system has the ability to fight off any opportunistic infections.
• Helps to decrease the severity and number of opportunistic infections
• Prevents or reduced occurrence of resistance to medication
• Goes a long way to help in prolonging life.

Researchers are also investigating to determine whether protease inhibitor can possible be used for the treatment of cancer. For instance, atazanavir and nelfinavir have the ability to kill tumor cells in culture.

The effect has not been tested or examined in humans yet through studies in a laboratory with mice has shown nelfinavir can suppress tumor growth in these animals thus representing the promise that the same tests can be carried out in humans.

Inhibitors of proteasome like Bortezomb and Velcade are in the front line of drugs that are been used to treat different types of cancer most notably, Multiple Myeloma. Protease inhibitor also has some side effects which include kidney stones, lipodystrophy, diabetes mellitus type 2 and hyperlipidaemia.

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