Dalcetrapib (JTT-705, RO4607381)
Molecular Weight(MW): 389.59
Dalcetrapib (JTT-705) is a rhCETP inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol. Phase 3.
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|Description||Dalcetrapib (JTT-705) is a rhCETP inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol. Phase 3.|
Dalcetrapib modulates CETP activity. Dalcetrapib induces a conformational change in CETP, when added to human plasma. CETP-induced pre-β-HDL formation in human plasma is unchanged by Dalcetrapib ≤3 µM and increased at 10 µM. Dalcetrapib statistically and significantly increases pre-β-HDL formation.  Dalcetrapib achieves 50% inhibition of CETP activity in human plasma at a concentration of 9 μM.  Dalcetrapib inhibits the CETP activity of media in HepG2 in a dose-dependent manner. 
|In vivo||Treatment with Dalcetrapib leads to significant increases in HDL-C levels. In hamsters injected with [3H]cholesterol-labeled autologous macrophages Dalcetrapib significantly increases fecal elimination of both [3H]neutral sterols and [3H]bile acids. Dalcetrapib increases plasma HDL-[3H]cholesterol.  Dalcetrapib has 95% inhibition of CETP activity in male Japanese white rabbits at an oral dose of 30 mg/kg. Dalcetrapib increases the plasma HDL cholesterol level by 27% and 54%, respectively, when given at oral doses of 30 mg/kg or 100 mg/kg once a day for 3 days to male Japanese white rabbits.  Treatment with Dalcetrapib markedly increases serum levels of HDL-C. The ratio of HDL2-C to HDL3-C is significantly higher in Dalcetrapib–treated rabbits than in control rabbits at 5 and 7 months, indicating that the inhibition of CETP activity by Dalcetrapib changes the distribution of HDL subfractions and preferentially increases HDL2-C levels. Dalcetrapib treatment increases serum paraoxonase activity and HDL-associated platelet-activating factor acetylhydrolase activity, but decreases the plasma lysophosphatidylcholine concentration. |
Inhibition of rhCETP and C13S CETP-mediated transfer of CE from HDL to LDL:The inhibitory potency (IC50) of Dalcetrapib to decrease CE transfer from HDL to LDL by rhCETP and C13S CETP is measured using a scintillation proximity assay kit. Briefly, [3H]CE-labeled HDL donor particles are incubated in the presence of purified CETP proteins (final concentration 0.5 µg/mL) and biotinylated LDL acceptor particles for 3 hours at 37 °C. Subsequently, streptavidin-coupled polyvinyltoluene beads containing liquid scintillation cocktail binding selectively to biotinylated LDL are added, and the amount of [3H]CE molecules transferred to LDL is measured by β counting.
-  Niesor EJ, et al. J Lipid Res. 2010, 51(12), 3443-3454.
-  Shinkai H, et al. J Med Chem. 2000, 43(19), 3566-3572.
-  Huang Z, et al. Am J Physiol Endocrinol Metab. 2003, 284(6), E1210-E1219.
|In vitro||DMSO||78 mg/mL (200.21 mM)|
|Ethanol||78 mg/mL (200.21 mM)|
|In vivo||0.5% methylcellulose||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02525939||Recruiting||Acute Coronary Syndrome||DalCor Pharmaceuticals|The Montreal Health Innovations Coordinating Center (MHICC)|Medpace, Inc.|Roche Molecular Systems, Inc||April 2016||Phase 3|
|NCT01516541||Completed||Cardiovascular Disease, Coronary Heart Disease, Dyslipidemia, Peripheral Arterial Disease (PAD)||Hoffmann-La Roche||January 2012||Phase 3|
|NCT01476267||Completed||Healthy Volunteer||Hoffmann-La Roche||October 2011||Phase 1|
|NCT01363999||Completed||Healthy Volunteer||Hoffmann-La Roche||June 2011||Phase 1|
|NCT01323153||Completed||Coronary Heart Disease||Hoffmann-La Roche||March 2011||Phase 3|
|NCT01059682||Terminated||Cardiovascular Disease||Hoffmann-La Roche||January 2010||Phase 3|
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