Lenacapavir Exhibits Atropisomerism - Mechanistic Pharmacokinetics and Disposition Studies of Lenacapavir Reveal Intestinal Excretion as a Major Clearance Pathway.

bioavailability clearance excretion intestinal bioavailability pharmacokinetic

Journal

The Journal of pharmacology and experimental therapeutics
ISSN: 1521-0103
Titre abrégé: J Pharmacol Exp Ther
Pays: United States
ID NLM: 0376362

Informations de publication

Date de publication:
08 Aug 2024
Historique:
accepted: 31 07 2024
received: 13 05 2024
revised: 28 07 2024
medline: 9 8 2024
pubmed: 9 8 2024
entrez: 8 8 2024
Statut: aheadofprint

Résumé

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

Identifiants

pubmed: 39117460
pii: jpet.124.002302
doi: 10.1124/jpet.124.002302
pii:
doi:

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Informations de copyright

© 2024 The Authors. This is an open access article under the terms of the Creative Commons Attribution CC BY License, which permits use, distribution, and reproduction in any medium, provided that the original work is properly cited.

Auteurs

Jim Zheng (J)

Gilead Science Inc, United States.

Bing Lu (B)

Gilead Sciences, Inc, United States.

Gavin Carr (G)

Gilead Sciences, Inc., United States.

Judy Mwangi (J)

Drug Metabolism and Pharmacokinetics, Gilead Sciences, United States.

Kelly Wang (K)

Gilead Sciences Inc, United States.

Jia Hao (J)

Gilead Sciences Inc, United States.

Kelly MacLennan Staiger (KM)

Drug Metabolism and Pharmacokinetics, Gilead Sciences, United States.

Nathan Kozon (N)

Gilead Sciences, Inc., United States.

Bernard P Murray (BP)

Drug Metabolism, Gilead Sciences, United States.

Mohammad Bashir (M)

Labcorp Drug Development, United States.

Mark A Gohdes (MA)

Drug Metabolism, Covance Inc., United States.

Winston C Tse (WC)

Gilead Sciences, United States.

Scott Schroeder (S)

Gilead Sciences, Inc., United States.

Michael Graupe (M)

Gilead Sciences, Inc., United States.

John O Link (JO)

Gilead Sciences, Inc., United States.

Jungjoo Yoon (J)

Gilead Sciences, Inc., United States.

Anna Chiu (A)

Gilead Sciences, Inc., United States.

William Rowe (W)

Gilead Sciences, Inc., United States.

Bill J Smith (BJ)

Drug Metabolism and Pharmacokinetics, Gilead Sciences, United States.

Raju Subramanian (R)

Drug Metabolism and Pharmacokinetics, Gilead Sciences, United States raju.subramanian@gilead.com.

Classifications MeSH