2023-09-27 06:30:50
Lipoprotein A is now well associated with atherosclerotic disease and aortic stenosis. This phase I trial suggests that muvalaplin, an orally administered small molecule inhibiting lipoprotein A formation, is not associated with tolerability issues and did reduce lipoprotein A levels by up to 65%. following daily administration for 14 days, in healthy participants.
Good safety, good pharmacokinetics
Phase I trial looked at whether muvalapline might achieve safe and tolerable plasma concentrations, sufficient to reduce and stabilize lipoprotein A levels, without modulating the activity of plasminogen (the enzyme that destroys the clot). The study is involving 114 healthy participants – 105 of whom completed the trial – allocated to receive muvalapline orally in single increasing doses ranging from 1 mg to 800 mg and in multiple increasing doses ranging from 30 mg to 800 mg for 14 days. The analysis shows that:
the candidate induces a reduction in lipoprotein A levels but without disrupting plasminogen activity; muvalaplin induces a dose-dependent plasma concentration of lipoprotein A; no adverse effects in terms of safety or tolerability are observed the reduction in lipoprotein A levels occurs within 24 hours following administration of the first dose, with a further reduction in the event of repeated administration.
These positive initial data support further clinical evaluation in patients with elevated lipoprotein A levels, therefore conclude the researchers.
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#CORONARY #DISEASE #pill #formation #lipoproteins