Oct 112013



Lu AE58054


Valby, Denmark and Tokyo, Japan, 10 October 2013, 2013-10-10 09:15 CEST (GLOBE NEWSWIRE) —


•The clinical program in Alzheimer’s disease is planned to include approximately 3,000 patients from several countries worldwide
•Lu AE58054 is a selective 5-HT6 receptor antagonist under investigation for the treatment of Alzheimer’s disease[i]

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Lu AE58054 is a potent and selective 5-HT6 receptor antagonist under development by Lundbeck as an augmentation therapy for the treatment of cognitive deficits associated with Alzheimer’s disease and schizophrenia.[1][2] As of February 2010 it is in phase II clinical trials.[2]

Lu AE58054 Hydrochloride M.Wt: 434.83
Lu AE58054 Hydrochloride Formula: C20H20ClF5N2O
Lu AE58054 Hydrochloride Storage: at -20℃ 2 years
Lu AE58054 Hydrochloride CAS No.: 467458-02-2

Description: IC50 Value: 0.83 nm[1] Lu AE58054 is an in-vitro potency and selectivity, in-vivo binding affinity and effect of the 5-HT(6)R antagonist. in vitro: Lu AE58054 displayed high affinity to the human 5-HT(6) receptor (5-HT(6)R) with a Ki of 0.83 nm. In a 5-HT(6) GTPgammaS efficacy assay Lu AE58054 showed no agonist activity, but demonstrated potent inhibition of 5-HT-mediated activation. Besides medium affinity to adrenergic alpha(1A)- and alpha(1B)-adrenoreceptors, Lu AE58054 demonstrated >50-fold selectivity for more than 70 targets examined[1]. in vivo: Orally administered Lu AE58054 potently inhibited striatal in-vivo binding of the 5-HT(6) antagonist radioligand [(3)H]Lu AE60157, with an ED(50) of 2.7 mg/kg. Steady-state modelling of an acute pharmacokinetic/5-HT(6)R occupancy time-course experiment indicated a plasma EC(50) value of 20 ng/ml. Administration of Lu AE58054 in a dose range (5-20 mg/kg p.o.) leading to above 65% striatal 5-HT(6)R binding occupancy in vivo, reversed cognitive impairment in a rat novel object recognition task induced after subchronic treatment for 7 d with phencyclidine (PCP 2 mg/kg b.i.d., i.p. for 7 d, followed by 7 d drug free). The results indicate that Lu AE58054 is a selective antagonist of 5-HT(6)Rs with good oral bioavailability and robust efficacy in a rat model of cognitive impairment in schizophrenia[1]. Clinical trial: Lu-AE58054 Added to Donepezil for the Treatment for Moderate Alzheimer’s Disease. Phase2

References on Lu AE58054 Hydrochloride:

[1]. Arnt J, Bang-Andersen B, Grayson B, Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats. Int J Neuropsychopharmacol. 2010 Sep;13(8):1021-33.

[2]. Witten L, Bang-Andersen B, Nielsen SM, Characterization of [?H]Lu AE60157 ([?H]8-(4-methylpiperazin-1-yl)-3-phenylsulfonylquinoline) binding to 5-hydroxytryptamine? (5-HT?) receptors in vivo.Eur J Pharmacol. 2012 Feb 15;676(1-3):6-11.



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