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Difference between normal and WHHL rabbits in susceptibility to the adrenal toxicity of an acyl-CoA: Cholesterol acyltransferase inhibitor, FR145237
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231207 Difference between normal and WHHL rabbits in susceptibility to the adrenal toxicity of an acyl-CoA: Cholesterol acyltransferase inhibitor, FR145237. Matsuo M, Hashimoto M, Suzuki J, Iwanami K, Tomoi M, Shimomura K Toxicol Appl Pharmacol 1996 140 2 387-392
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246571 Fabre sets up in UK to launch Navelbine. Scrip 1997 2231 13
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Drug development pipeline - Eptapirone, F-12511, F-11782, donitriptan, KpOMpA, F-50077, F-50008, F-50003, F-50000, F-50028, F-2692, F-12682
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399986; February 23
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399986 Drug development pipeline - Eptapirone, F-12511, F-11782, donitriptan, KpOMpA, F-50077, F-50008, F-50003, F-50000, F-50028, F-2692, F-12682. Pierre Fabre SA Company Communication 2001 February 23
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Pierre Fabre SA Company Communication
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Lack of toxic effects of F 12511, a novel potent inhibitor of acylcoenzyme A:cholesterol O-acyltransferase, on human adrenocortical cells in culture
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407413; note
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407413 Lack of toxic effects of F 12511, a novel potent inhibitor of acylcoenzyme A:cholesterol O-acyltransferase, on human adrenocortical cells in culture. Junquero D, Pilon A, Carilla-Durand E, Patoiseau J-F, Tarayre J-P, Torpier G, Staels B, Fruchart J-C, Colpaert FC, Clavey V, Delhon A Biochem Pharmacol 2001 61 4 387-398 Report of the preclinical safety evaluation of eflucimibe in the NCI-H295R cell line (which has functional comparable to those of normal human adrenal cells), showing lack of toxic effects.
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Biochem Pharmacol
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Overexpression of SR-BI in hamsters treated with a novel ACAT inhibitor (F12511)
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407414; note
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407414 Overexpression of SR-BI in hamsters treated with a novel ACAT inhibitor (F12511). Milliat F, Ferezou J, Delhon A, Lutton C C R Acad Sci Ser III 2001 324 3 229-234 Describes the decreased absorption coefficient of dietary cholesterol and the increased expression of hepatic SR-BI in eflucimibe-treated hamsters.
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Milliat, F.1
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F 12511, a novel ACAT inhibitor, and atorvastatin regulate endogenous hypercholesterolemia in a synergistic manner in New Zealand rabbits fed a casein-enriched diet
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407415; note
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407415 F 12511, a novel ACAT inhibitor, and atorvastatin regulate endogenous hypercholesterolemia in a synergistic manner in New Zealand rabbits fed a casein-enriched diet. Junquero D, Bruniquel F, N'Guyen X, Autin JM, Patoiseau JF, Degryse AD, Colpaert FC, Delhon A Atherosclerosis 2001 155 1 131-142 Eflucimibe is 3- to 4-fold more potent than atorvastatin in reducing total plasma cholesterol. When co-administered, the agents lowered plasma total cholesterol and apoB-100-containing lipoproteins to a greater extent and more rapidly than either agent alone.
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Atherosclerosis
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Pharmacological profile of F 12511, (S)-2′,3′,5′-trimethyl-4′-hydroxy-α-dodecylthioace tanilide a powerful and systemic acylcoenzyme A:cholesterol acyltransferase inhibitor
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407416; note
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407416 Pharmacological profile of F 12511, (S)-2′,3′,5′-trimethyl-4′-hydroxy-α-dodecylthioace tanilide a powerful and systemic acylcoenzyme A: Cholesterol acyltransferase inhibitor. Junquero D, Oms P, Carilla-Durand E, Autin J, Tarayre JP, Degryse AD, Patoiseau JE, Colpaert FC, Delhon A Biochem Pharmacol 2001 61 1 97-108 Describes the pharmacological profile of eflucimibe, lipid-lowering effects in small animal models and a preclinical safety evaluation of eflucimibe in guinea pigs, showing minimal adrenal toxicity.
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Biochem Pharmacol
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Lilly and bioMerieux-Pierre fabre to collaborate on ACAT inhibitor for atherosclerosis
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408118; May 03
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408118 Lilly and bioMerieux-Pierre fabre to collaborate on ACAT inhibitor for atherosclerosis. Eli Lilly & Co Press Release 2001 May 03
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Eli Lilly & Co Press Release
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Anti-atherosclerotic properties of the acyl-coenzyme A:cholesterol acyltransferase inhibitor F-12511 in casein-fed New Zealand rabbits
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440367; note
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440367 Anti-atherosclerotic properties of the acyl-coenzyme A: Cholesterol acyltransferase inhibitor F-12511 in casein-fed New Zealand rabbits. Rival Y, Junquero D, Bruniquel F, N'Guyen X, Faure P, Promies JP, Degryse AD, Delhon A J Cardiovasc Pharmacol 2002 39 2 181-191 Lipid lowering by eflucimibe reduces the incidence of vascular lesions and macrophage infiltration and may reinforce the fibrous skeleton of the atheroma.
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Crystalline polymorphism of eflucimibe
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477157 Crystalline polymorphism of eflucimibe. Ribet JP, Pena R, Chauvet A, Patoiseau JF, Autin JM, Segonds R, Basquin M, Autret JM Ann Pharm Fr 2002 60 3 177-186 Identifies and describes two crystalline polymorphic forms of eflucimibe using differential scanning calorimetry, X-ray powder diffraction from synchrotron radiation, infrared spectrometry, and solid-state nuclear magnetic resonance spectrometry.
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480708 Immunodepletion experiments suggest that acyl-coenzyme A:cholesterol acyltransferase-1 (ACAT1) protein plays a major catalytic role in adult human liver, adrenal gland, macrophages, and kidney, but not in intestines. Lee O, Chang CCY, Lee W, Chang TY J Lipid Res 1998 39 8 1722-1727
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480709 Identification of a form of acyl-CoA:cholesterol acyltransferase specific to liver and intestine in nonhuman primates. Anderson RA, Joyce C, Davis M, Reagan JW, Clark M, Shelness G, Rudel LL 1998 273 41 26747-26754
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Morphogenesis of a zone-specific adrenocortical cytotoxicity in guinea pigs administered PD132301-2, an inhibitor of acyl-coA:cholesterol acyltransferase
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480711 Morphogenesis of a zone-specific adrenocortical cytotoxicity in guinea pigs administered PD132301-2, an inhibitor of acyl-coA:cholesterol acyltransferase. Dominick MA, Bobrowski WA, MacDonald JR, Gough AW Toxicol Pathol 1993 21 1 54-62
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Hamsters predisposed to sucrose-induced cholesterol gallstones (LPN strain) are more resistant to excess dietary cholesterol than hamsters that are not sensitive to cholelithiasis induction
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480718 Hamsters predisposed to sucrose-induced cholesterol gallstones (LPN strain) are more resistant to excess dietary cholesterol than hamsters that are not sensitive to cholelithiasis induction. Souidi M, Combettes-Souverain M, Milliat F, Eckhardt ER, Audas O, Dubrac S, Parquet M, Ferezou J, Lutton C J Nutr 2001 131 6 1803-1811
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Research and development: Presentation and figures
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481165 Research and development: Presentation and figures. Pierre Fabre SA Company World Wide Web Site 2003 March 10
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Drug development pipeline - Eflucimibe
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481426; March 11
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481426 Drug development pipeline - Eflucimibe. Pierre Fabre SA Company Communication 2003 March 11
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(2003)
Pierre Fabre SA Company Communication
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