Torcetrapib

Torcetrapib (CP-529414) is a selective, potent cholesteryl ester transfer protein (CETP) inhibitor. A typical inhibition curve for whole human plasma, having a CETP concentration of 37 nM^[1]. In Vitro: The IC₅₀ for Torcetrapib determined from the linear portion of the curves (25 to 80 nM) is 52 and 65 nM for the ³H-HDL and ¹⁴C-LDL cholesteryl ester transfer assays, respectively, using the specific activity-adjusted calculation, and 47 and 61 nM using a single exponential decay function^[1].
Torcetrapib (0, 0.5, 1, 5, and 10 μM) significantly reduced MCF-7 cells growth^[2].
Torcetrapib (0, 1, 5, 10, and 20 μM) does not inducing MCF-7 cells apoptosis^[2].
Torcetrapib (10 μM) binds to CETP with high affinity and down-regulates CETP expression^[2]. In Vivo: Torcetrapib (3, 10, or 30 mg/kg every day [qd]; oral gavage for 14 days) significantly increases high-density lipoprotein (HDL) cholesterol and reduceslow-density lipoprotein (LDL) cholesterol, and there is a tendency for Torcetrapib to reduce very-low-density lipoprotein (VLDL) cholesterol and triglycerides. Maximal increase in HDL cholesterol is 53% with Torcetrapib^[3].