A Phase 1b/2a study of the safety, pharmacokinetics and antiviral activity of BIT225 in patients with HIV-1 infection | Zendy

John Wilkinson | Zendy; Gary Ewart | Zendy; Carolyn A. Luscombe | Zendy; Kristin McBride | Zendy; Winai Ratanasuwan | Zendy; Michelle Miller | Zendy; Robert L. Murphy | Zendy

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A Phase 1b/2a study of the safety, pharmacokinetics and antiviral activity of BIT225 in patients with HIV-1 infection

Author(s) -

John Wilkinson,

Gary Ewart,

Carolyn A. Luscombe,

Kristin McBride,

Winai Ratanasuwan,

Michelle Miller,

Robert L. Murphy

Publication year - 2015

Publication title -

journal of antimicrobial chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.124

H-Index - 194

eISSN - 1460-2091

pISSN - 0305-7453

DOI - 10.1093/jac/dkv389

Subject(s) - cd14 , monocyte , pharmacokinetics , in vivo , population , ex vivo , pharmacology , placebo , virus , virology , medicine , immunology , viral replication , in vitro , biology , immune system , pathology , biochemistry , alternative medicine , microbiology and biotechnology , environmental health

BIT225 (N-carbamimidoyl-5-(1-methyl-1H-pyrazol-4-yl)-2-naphthamide), a novel acyl-guanidine, is a novel antiviral drug that blocks Vpu ion channel activity and has anti-HIV-1 activity in vitro. The antiviral effect of BIT225 is most pronounced in cells of the myeloid lineage. With infected circulating monocytes and tissue-resident macrophages representing a key cellular reservoir of HIV-1, BIT225 has a potential role in the eradication of the virus from the host.

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