LY335979

LY335979 (also known as Zosuquidar) is a third-generation P-glycoprotein inhibitor. It is a synthetic compound that has been extensively studied for its potential use in the treatment of multidrug resistance in cancer patients.

Chemistry

LY335979 is a rhodamine derivative. It is a small molecule that is designed to bind to the P-glycoprotein, thereby inhibiting its function. The chemical structure of LY335979 is characterized by a central quinoline ring, flanked by two benzene rings.

Mechanism of Action

LY335979 works by inhibiting the P-glycoprotein, a protein that is often overexpressed in cancer cells and is responsible for the efflux of many chemotherapeutic drugs from the cells. By inhibiting the P-glycoprotein, LY335979 increases the intracellular concentration of these drugs, thereby enhancing their cytotoxic effect.

Clinical Trials

Several clinical trials have been conducted to evaluate the efficacy and safety of LY335979 in combination with various chemotherapeutic agents in the treatment of different types of cancer. However, the results have been mixed, with some studies showing a significant improvement in response rates and others showing no significant benefit.

Side Effects

The most common side effects of LY335979 include nausea, vomiting, and diarrhea. Less common side effects include fatigue, anemia, and neutropenia.

Future Directions

Despite the mixed results of clinical trials, research on LY335979 continues, with a focus on identifying the optimal dosing regimen and combination of drugs to maximize its efficacy while minimizing its side effects.