This is a first-in-human (FIH), double-blind, placebo-controlled, randomized trial in healthy adult male subjects, to evaluate the safety, tolerability and pharmacokinetics (PK) of single ascending oral doses of BDM-2. The effect of food on the PK of a single dose of BDM-2 will also be evaluated.

Start Date17 May 2018

Sponsor / Collaborator

Hivih

[+1]

100 Clinical Results associated with BDM-2

100 Translational Medicine associated with BDM-2

100 Patents (Medical) associated with BDM-2

Literatures (Medical) associated with BDM-2

18 Jul 2023·Antimicrobial agents and chemotherapy

Biological and Structural Analyses of New Potent Allosteric Inhibitors of HIV-1 Integrase.

Article

Author: Emiliani, Stéphane ; Bonnard, Damien ; Amadori, Céline ; Singer, Matthew R ; Moreau, François ; Le Strat, Frédéric ; Chasset, Sophie ; Batisse, Claire ; Benarous, Richard ; Le Rouzic, Erwann ; Batisse, Julien ; Yu, Zhe ; Ledoussal, Benoit ; Cherepanov, Peter ; Ruff, Marc ; Pye, Valerie E

HIV-1 integrase-LEDGF allosteric inhibitors (INLAIs) share the binding site on the viral protein with the host factor LEDGF/p75. These small molecules act as molecular glues promoting hyper-multimerization of HIV-1 IN protein to severely perturb maturation of viral particles. Herein, we describe a new series of INLAIs based on a benzene scaffold that display antiviral activity in the single digit nanomolar range. Akin to other compounds of this class, the INLAIs predominantly inhibit the late stages of HIV-1 replication. A series of high-resolution crystal structures revealed how these small molecules engage the catalytic core and the C-terminal domains of HIV-1 IN. No antagonism was observed between our lead INLAI compound BDM-2 and a panel of 16 clinical antiretrovirals. Moreover, we show that compounds retained high antiviral activity against HIV-1 variants resistant to IN strand transfer inhibitors and other classes of antiretroviral drugs. The virologic profile of BDM-2 and the recently completed single ascending dose phase I trial (ClinicalTrials.gov identifier: NCT03634085) warrant further clinical investigation for use in combination with other antiretroviral drugs. Moreover, our results suggest routes for further improvement of this emerging drug class.

100 Deals associated with BDM-2

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