P-gp inhibitor

P-glycoprotein inhibitor (also known as P-gp inhibitor) is a type of drug or compound that inhibits the action of P-glycoprotein (P-gp), a protein that pumps foreign substances out of cells. P-gp inhibitors are used in the treatment of various diseases, including cancer, HIV/AIDS, and epilepsy.

Overview

P-glycoprotein is a type of ATP-binding cassette transporter that is found in the cell membrane of many different types of cells. It functions as a pump, using energy from ATP to transport various substances out of the cell. This can include drugs, toxins, and other foreign substances.

P-gp inhibitors work by blocking the action of P-gp, thereby increasing the concentration of certain drugs within cells. This can enhance the effectiveness of these drugs, particularly in the treatment of diseases such as cancer, where drug resistance is a common problem.

Types of P-gp inhibitors

There are several different types of P-gp inhibitors, including:

• First-generation P-gp inhibitors: These are typically non-specific inhibitors that also affect other transporters. Examples include verapamil and cyclosporine.
• Second-generation P-gp inhibitors: These are more specific for P-gp and have fewer side effects. Examples include valspodar and biricodar.
• Third-generation P-gp inhibitors: These are highly specific for P-gp and have minimal side effects. Examples include tariquidar and elacridar.

Clinical use

P-gp inhibitors are used in the treatment of various diseases. In cancer, they are used to overcome multidrug resistance, a common problem where cancer cells become resistant to multiple types of chemotherapy drugs. By inhibiting P-gp, these drugs can increase the concentration of chemotherapy drugs within cancer cells, enhancing their effectiveness.

In HIV/AIDS, P-gp inhibitors are used to increase the concentration of antiretroviral drugs within cells, enhancing their effectiveness. In epilepsy, they are used to increase the concentration of antiepileptic drugs within brain cells, reducing the frequency and severity of seizures.

See also

• P-glycoprotein
• Drug resistance
• Chemotherapy
• Antiretroviral therapy
• Antiepileptic drug

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