| S2748 |
Anacetrapib (MK-0859)
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Anacetrapib (MK-0859) is a potent, selective, reversible rhCETP and mutant CETP(C13S) inhibitor with IC50 of 7.9 nM and 11.8 nM. It increases HDL-C and decreases LDL-C, and does not increase aldosterone or blood pressure. This compound is in Phase 3.
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Circulation, 2021, 143(9):921-934
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J Phys Chem B, 2016, 120(33):8254-63
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Atherosclerosis, 2014, 235(2):449-62
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| S2792 |
Torcetrapib
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Torcetrapib (CP-529414) is a CETP inhibitor with IC50 of 37 nM, elevates HDL-C and reduces nonHDL-C in plasma. Phase 3.
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J Immunother Cancer, 2024, 12(11)e009805
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| S2772 |
Dalcetrapib (JTT-705)
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Dalcetrapib (JTT-705) is a rhCETP inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol. This compound is in Phase 3.
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Atherosclerosis, 2014, 235(2):449-62
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| S2925 |
Evacetrapib (LY2484595)
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Evacetrapib (LY2484595) is a potent and selective inhibitor of CETP with IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure. Phase 3.
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| E1561 |
Obicetrapib
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Obicetrapib (TA-8995, AMG-899, DEZ-001) is an inhibitor of Cholesteryl Ester Transfer Protein (CETP) that significantly reduces non-HDL cholesterol (non-HDL-C) and lipoprotein(a) levels while increasing high-density lipoprotein cholesterol (HDL-C). It also has the potential to reduce major adverse cardiovascular events.
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