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The newly disclosed small molecule
therapeutics include: IWY357 (Novartis, Emeryville, CA, presented by Tom Kirrane): A pyrazine-2-carboxamide that is a
prolonged suppressor of Plasmodium falciparum blood stage for the treatment of uncomplicated
malaria currently undergoing Ph. I evaluation. elunonavir (GS-1156) (Gilead, Foster City, CA, presented by Elbert Chin): An
HIV protease inhibitor with a high resistance barrier and exceptional metabolic
stability, designed to overcome rapid CYP-mediated metabolism, allowing for
significantly extended half-life and the potential for less frequent dosing
without the need for a pharmacokinetic enhancer. BAY 2925976 (Bayer AG, Wuppertal, DE, presented by Michael Hahn): A
highly selective ARα2C (alpha-2c adrenergic receptor) antagonist with improved
brain penetration and efficacy, aimed at treating OSA (obstructive sleep apnea)
by stabilizing upper airways and preventing collapse through increased
hypoglossal motoneuron activity. AZD
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