"BI 224436"

Preclinical Profile of BI 224436, a Novel HIV-1 Non-Catalytic Site Integrase Inhibitor. BI 224436 is an HIV-1 integrase inhibitor with effective antiviral activity that acts through a mechanism that is distinct from that of integrase strand transfer inhibitors (INSTIs). This 3-quinolineacetic acid derivative series was identified using an enzymatic integrase long terminal repeat (LTR) DNA 3 '-processing assay. A combination of medicinal chemistry, parallel synthesis, and structure-guided drug design led to the identification of BI 224436 as a candidate for preclinical profiling. It has antiviral 50% effective concentrations (EC50s) of <15 nM against different HIV-1 laboratory strains and cellular cytotoxicity of >90 μM. BI 224436 also has a low, ∼2.1-fold decrease in antiviral potency

contribution of biliary excretion to in vivo clearance compared to BI 224436, the lead compound from the quinoline series of NCINIs.

)° * Raltegravir (RAL)° * BI 224436† * Cabotegravir

)° * Raltegravir (RAL)° * BI 224436† * Cabotegravir

)° * Raltegravir (RAL)° * BI 224436† * Cabotegravir

Safety and Pharmacokinetics of Single Rising Oral Doses of BI 224436 ZW in Healthy Male Volunteers. Safety and Pharmacokinetics of Single Rising Oral Doses of BI 224436 ZW in Healthy Male Volunteers. - Full Text View - ClinicalTrials.gov Try the modernized ClinicalTrials.gov beta website. Learn more about the modernization effort. Hide glossary GlossaryStudy record managers: refer to the Data WarningYou have reached the maximum number of saved studies (100).Please remove one or more studies before adding more. Safety and Pharmacokinetics of Single Rising Oral Doses of BI 224436 ZW in Healthy Male Volunteers. The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal

Safety and Pharmacokinetics of Multiple Rising Oral Doses of BI 224436 in Healthy Male Volunteers. Safety and Pharmacokinetics of Multiple Rising Oral Doses of BI 224436 in Healthy Male Volunteers. - Full Text View - ClinicalTrials.gov Try the modernized ClinicalTrials.gov beta website. Learn more about the modernization effort. Hide glossary GlossaryStudy record managers: refer to the Data WarningYou have reached the maximum number of saved studies (100).Please remove one or more studies before adding more. Safety and Pharmacokinetics of Multiple Rising Oral Doses of BI 224436 in Healthy Male Volunteers. The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal