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Obicetrapib

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Obicetrapib
Clinical data
Other namesTA-8995; AMG-899
Legal status
Legal status
  • Investigational
Identifiers
  • 4-[2-[[3,5-bis(trifluoromethyl)phenyl]methyl-[(2R,4S)-1-ethoxycarbonyl-2-ethyl-6-(trifluoromethyl)-3,4-dihydro-2H-quinolin-4-yl]amino]pyrimidin-5-yl]oxybutanoic acid
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC32H31F9N4O5
Molar mass722.609 g·mol−1
3D model (JSmol)
  • CC[C@@H]1C[C@@H](C2=C(N1C(=O)OCC)C=CC(=C2)C(F)(F)F)N(CC3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)C4=NC=C(C=N4)OCCCC(=O)O
  • InChI=1S/C32H31F9N4O5/c1-3-22-14-26(24-13-19(30(33,34)35)7-8-25(24)45(22)29(48)49-4-2)44(28-42-15-23(16-43-28)50-9-5-6-27(46)47)17-18-10-20(31(36,37)38)12-21(11-18)32(39,40)41/h7-8,10-13,15-16,22,26H,3-6,9,14,17H2,1-2H3,(H,46,47)/t22-,26+/m1/s1
  • Key:NRWORBQAOQVYBJ-GJZUVCINSA-N

Obicetrapib is an experimentalCETP inhibitor that is intended to treatdyslipidemia. In a clinical trial, as an add-on to statins, compared with placebo, it decreased concentrations ofLDL-C (by up to 51%),apolipoprotein B (by up to 30%) and non-high-density lipoprotein cholesterol (non-HDL-C) (by up to 44%), and increasedHDL-C concentration (by up to 165%).[1][2] As of 2023, it is in a Phase III trial.[3]

History

[edit]

Obicetrapib was initially developed byAmgen as AMG-899 and was abandoned in 2017.[4] In 2020, Amgen licensed the drug to NewAmsterdam Pharma.[5]

References

[edit]
  1. ^Ballantyne, Christie M.; Ditmarsch, Marc; Kastelein, John JP; Nelson, Adam J.; Kling, Douglas; Hsieh, Andrew; Curcio, Danielle L.; Maki, Kevin C.; Davidson, Michael H.; Nicholls, Stephen J. (July 2023)."Obicetrapib plus ezetimibe as an adjunct to high-intensity statin therapy: A randomized phase 2 trial".Journal of Clinical Lipidology.17 (4):491–503.doi:10.1016/j.jacl.2023.05.098.
  2. ^Nicholls, Stephen J.; Ditmarsch, Marc; Kastelein, John J.; Rigby, Scott P.; Kling, Douglas; Curcio, Danielle L.; Alp, Nicholas John; Davidson, Michael H. (August 2022)."Lipid lowering effects of the CETP inhibitor obicetrapib in combination with high-intensity statins: a randomized phase 2 trial".Nature Medicine.28 (8):1672–1678.doi:10.1038/s41591-022-01936-7.ISSN 1546-170X.
  3. ^"NewAmsterdam Pharma concludes enrolment in LDL lowering therapy trial".Clinical Trials Arena. 26 July 2023.
  4. ^Amgen kills off CETP inhibitor after seeing Merck data
  5. ^NewAmsterdam bags $196M to resurrect Amgen's discarded CETP drug
GI tract
Cholesterol absorption inhibitors,NPC1L1
Bile acid sequestrants/resins (LDL)
Liver
Statins (HMG-CoA reductase,LDL)
Niacin and derivatives (HDL andLDL)
MTTP inhibitors (VLDL)
ATP citrate lyase inhibitors (LDL)
Thyromimetics (VLDL)
Blood vessels
PPAR agonists (LDL)
Fibrates
Others
CETP inhibitors (HDL)
PCSK9 inhibitors (LDL)
ANGPTL3 inhibitors (LDL/HDL)
Combinations
Other
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