Zosuquidar trihydrochloride

Zosuquidar trihydrochloride is a third-generation P-glycoprotein inhibitor. It is an experimental drug that was developed by Eli Lilly and Company to overcome multidrug resistance in cancer treatment.

Chemistry

Zosuquidar trihydrochloride is a synthetic, lipophilic, and highly selective inhibitor of P-glycoprotein. Its chemical name is (R)-6,7-dimethoxy-4-(3-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)propoxy)-3-quinazolinamine trihydrochloride.

Mechanism of Action

Zosuquidar inhibits the drug efflux pump P-glycoprotein, which is often overexpressed in cancer cells and is associated with multidrug resistance. By inhibiting P-glycoprotein, zosuquidar allows for increased intracellular concentrations of other anticancer drugs, potentially enhancing their efficacy.

Clinical Trials

Zosuquidar has been tested in several clinical trials, including a Phase III trial in combination with daunorubicin and cytarabine for the treatment of acute myeloid leukemia (AML). However, the trial did not meet its primary endpoint of improved overall survival.

Side Effects

The most common side effects of zosuquidar include nausea, vomiting, and diarrhea. Other side effects may include fatigue, fever, and anemia.

See Also

• P-glycoprotein
• Multidrug resistance
• Eli Lilly and Company
• Clinical trial
• Daunorubicin
• Cytarabine
• Acute myeloid leukemia

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