Lenacapavir Exhibits Atropisomerism - Mechanistic Pharmacokinetics and Disposition Studies of Lenacapavir Reveal Intestinal Excretion as a Major Clearance Pathway [Metabolism, Transport, and Pharmacogenetics]
ASPET
AUGUST 8, 2024
Lenacapavir (LEN), a long-acting injectable, is the first approved human immunodeficiency virus type 1 capsid inhibitor and one of a few FDA-approved drugs that exhibit atropisomerism. LEN exists as a mixture of two class 2 atropisomers that interconvert at a fast rate (t 1/2 <2 hours) with a ratio that is stable over time and unaffected by enzymes or binding to proteins in plasma.
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