We are developing QRX-401 as a potential new therapy for the treatment of patients with elevated levels of LDL cholesterol and Lp(a). QRX-401 appears to be unique in its mechanism for lowering LDL cholesterol and Lp(a). The liver synthesizes cholesterol into either bile acids or particles such as LDL cholesterol. The farnesyl X receptor, or FXR, indirectly regulates this conversion of cholesterol into bile acids by the liver. QRX-401 has been shown in preclinical studies to be an FXR antagonist, which means that it blocks the consequent decrease in the amount of cholesterol available for LDL cholesterol formation by the liver. Other mechanisms may also contribute to the observed effects of QRX-401 on LDL and Lp(a) in animal models.

Development Program

We have conducted a total of four single and multiple dose tolerance studies of QRX-401 in normal volunteers at doses of up to 250 mg/day for 14 days. In all of these studies, QRX-401 has been well-tolerated with no safety issues identified to date. We have also completed a single-center, randomized, balanced, single-dose, crossover study of the pharmacokinetics of 150 mg QRX-401 in fed and fasted healthy male subjects. This trial demonstrated that QRX-401 was rapidly absorbed and metabolized and that safety and tolerability parameters were similar between the fasted and fed states.

Current Clinical Studies

We are currently conducting a multiple-dose pharmacokinetic drug interaction study between QRX-401 and simvastatin, a commonly used statin marketed as Zocor by Merck & Co., in healthy male volunteers to evaluate the potential for a pharmacokinetic drug interaction of QRX-401 on simvastatin as well as to assess the safety, tolerance and pharmacodynamic effects of the co-administration of QRX-401 and simvastatin when administered once daily for two weeks. A secondary objective is to evaluate the potential for a pharmacokinetic drug interaction of simvastatin on QRX-401 as compared to historical single dose 250 mg QRX-401 pharmacokinetic data.

Related Topics

Clinical Portfolio / QRX-401 / About Dyslipidemia