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Basic Characteristics of Mutations
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Mutation Site
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N74D |
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Mutation Site Sentence
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Treatment-emergent capsid resistance occurred in 19% (14/72) of participants, including capsid mutations M66I, Q67H/K/N, K70H/N/R/S, and/or N74D/H/K, which were all associated with functional lenacapavir monotherapy. |
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Mutation Level
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Amino acid level |
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Mutation Type
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Nonsynonymous substitution |
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Gene/Protein/Region
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CA |
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Standardized Encoding Gene
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Gag
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Genotype/Subtype
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HIV-1 |
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Viral Reference
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-
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Functional Impact and Mechanisms
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Disease
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HIV Infections
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Immune
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- |
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Target Gene
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-
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Clinical and Epidemiological Correlations
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Clinical Information
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- |
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Treatment
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lenacapavir |
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Location
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United States;Canada;Dominican Republic;France;Germany;Italy;Japan;South Africa;Spain;Taiwan;Thailand |
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Literature Information
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PMID
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39873394
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Title
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Resistance Analyses in Heavily Treatment-Experienced People With HIV Treated With the Novel HIV Capsid Inhibitor Lenacapavir After 2 Years
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Author
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Margot NA,Jogiraju V,Pennetzdorfer N,Naik V,VanderVeen LA,Ling J,Singh R,Dvory-Sobol H,Ogbuagu O,Segal-Maurer S,Molina JM,Rhee MS,Callebaut C
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Journal
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The Journal of infectious diseases
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Journal Info
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2025 Jun 2;231(5):1239-1245
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Abstract
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BACKGROUND: Lenacapavir is a highly potent first-in-class inhibitor of HIV-1 capsid that was approved for the treatment of heavily treatment-experienced people with HIV-1 harboring multidrug-resistant virus, and it is used in combination with an optimized background regimen (OBR). Resistance analyses conducted after 2 years of lenacapavir treatment in the phase 2/3 CAPELLA study are described. METHODS: CAPELLA enrollment consisted of viremic cases of heavily treatment-experienced people with HIV-1 and resistance to >/=2 drugs per class in at least 3 of the 4 main drug classes. Postbaseline resistance in participants experiencing virologic failure was evaluated by resistance assays (HIV-1 capsid, protease, reverse transcriptase, and integrase genotypic/phenotypic tests). Adherence to OBR was assessed by plasma drug measurement via liquid chromatography-tandem mass spectrometry. RESULTS: After 2 years, lenacapavir + OBR treatment led to HIV-1 RNA suppression in 82% of participants (missing = excluded). Treatment-emergent capsid resistance occurred in 19% (14/72) of participants, including capsid mutations M66I, Q67H/K/N, K70H/N/R/S, and/or N74D/H/K, which were all associated with functional lenacapavir monotherapy. Seven participants with lenacapavir resistance reattained HIV-1 RNA <50 copies/mL upon OBR resumption or change while maintaining lenacapavir treatment. CONCLUSIONS: Emergence of lenacapavir resistance after 2 years in CAPELLA was a consequence of functional lenacapavir monotherapy. In half of participants with lenacapavir resistance, continued treatment with lenacapavir + active OBR led to HIV-1 RNA resuppression.
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Sequence Data
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-
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