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

• Published in: Journal of antimicrobial chemotherapy Vol. 71; no. 3; pp. 731 - 738
• Main Authors: Wilkinson, John, Ewart, Gary, Luscombe, Carolyn, McBride, Kristin, Ratanasuwan, Winai, Miller, Michelle, Murphy, Robert L
• Format: Journal Article
• Language: English
• Published: England Oxford Publishing Limited (England) 01.03.2016
• Subjects: Adolescent; Adult; Aged; Anti-HIV Agents - adverse effects; Anti-HIV Agents - pharmacokinetics; Anti-HIV Agents - pharmacology; Antiviral drugs; Chemotherapy; Female; Guanidines - adverse effects; Guanidines - pharmacokinetics; Guanidines - pharmacology; HIV; HIV Core Protein p24 - analysis; HIV Infections - drug therapy; HIV Infections - virology; HIV-1 - isolation & purification; Human immunodeficiency virus; Human immunodeficiency virus 1; Humans; Kinetics; Male; Middle Aged; Monocytes - virology; Pharmacology; Placebos - administration & dosage; Pyrazoles - adverse effects; Pyrazoles - pharmacokinetics; Pyrazoles - pharmacology; Treatment Outcome; Viral Load; Young Adult

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 circulati...