NEWS
Scilex Bio, a Controlling Interest of Joint Venture by Scilex Holding Company, Reports Phase 2 Trial for Obesity Currently Enrolling with U.S. Patient Cohort to be Added in 2025. Scilex Bio Reports Positive Results from the Recently Completed Phase 1 Trials Conducted by NeuroBiogen for KDS2010, a Novel Oral Tablet Recently Synthesized Potent, Selective, and Reversible Monoamine Oxidase B inhibitor
Wednesday, 11th December at 7:30 am
• The ongoing obesity Phase 2 trial is a randomized, double-blind, placebo-controlled, dose finding, clinical trial to evaluate the safety and efficacy of KDS2010 in approximately 75 overweight or obese patients currently enrolling in South Korea with a cohort in U.S. to be added in 2025.
• KDS2010 has shown promising preclinical results with a novel mechanism of blocking MAO-B-dependent aberrant GABA (gamma-aminobutyric acid) production in reactive astrocytes and eliminates neuronal inhibition in Lateral Hypothalamic Area, stimulating metabolism and energy expenditure without affecting appetite.
• MAO-B controls tonic levels of GABA, a chief inhibitory neurotransmitter in the central nervous system. Selective inhibition of astrocytic GABA is a new molecular target for treating obesity.
• KDS2010 pharmacokinetics, lack of food effect, safety and dose selection have been characterized in Single Ascending Dose and Multiple Ascending Dose Phase 1 clinical trials with 88 healthy young adults and elderly subjects, demonstrating favorable safety and tolerability and adequate pharmacokinetics for once-daily dosing.
• Several important pharmacological attributes distinguish KDS2010 from molecules of this class.
◦ Firstly, reversibility of the MAO-B inhibition is critical for long-lasting efficacy. Irreversible inhibitors such as selegiline covalently modify the MAO-B enzyme and destroy the enzyme itself to turn on the compensatory expression of enzyme diamine oxidase, which continues to produce GABA, whereas reversible inhibitor occupies the active site of MAO-B competitively, resulting in an intact MAO-B enzyme with no compensatory mechanism.
◦ Secondly, only the selective inhibition of MAO-B shown to have selective inhibition of astrocytic GABA, important for anti-obesity effect.
◦ Lastly, easy penetration of Blood-Brain Barrier by KDS2010 is very important for targeting astrocytes in Lateral Hypothalamic Area.
Wednesday, 11th December at 7:30 am
• The ongoing obesity Phase 2 trial is a randomized, double-blind, placebo-controlled, dose finding, clinical trial to evaluate the safety and efficacy of KDS2010 in approximately 75 overweight or obese patients currently enrolling in South Korea with a cohort in U.S. to be added in 2025.
• KDS2010 has shown promising preclinical results with a novel mechanism of blocking MAO-B-dependent aberrant GABA (gamma-aminobutyric acid) production in reactive astrocytes and eliminates neuronal inhibition in Lateral Hypothalamic Area, stimulating metabolism and energy expenditure without affecting appetite.
• MAO-B controls tonic levels of GABA, a chief inhibitory neurotransmitter in the central nervous system. Selective inhibition of astrocytic GABA is a new molecular target for treating obesity.
• KDS2010 pharmacokinetics, lack of food effect, safety and dose selection have been characterized in Single Ascending Dose and Multiple Ascending Dose Phase 1 clinical trials with 88 healthy young adults and elderly subjects, demonstrating favorable safety and tolerability and adequate pharmacokinetics for once-daily dosing.
• Several important pharmacological attributes distinguish KDS2010 from molecules of this class.
◦ Firstly, reversibility of the MAO-B inhibition is critical for long-lasting efficacy. Irreversible inhibitors such as selegiline covalently modify the MAO-B enzyme and destroy the enzyme itself to turn on the compensatory expression of enzyme diamine oxidase, which continues to produce GABA, whereas reversible inhibitor occupies the active site of MAO-B competitively, resulting in an intact MAO-B enzyme with no compensatory mechanism.
◦ Secondly, only the selective inhibition of MAO-B shown to have selective inhibition of astrocytic GABA, important for anti-obesity effect.
◦ Lastly, easy penetration of Blood-Brain Barrier by KDS2010 is very important for targeting astrocytes in Lateral Hypothalamic Area.
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