Drug intelligence / Profile preview

PPL-100

Development stage
Discontinued
Lead developer
Ambrilia Biopharma
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

PPL-100 is a phosphorylated prodrug of the HIV-1 protease inhibitor PL-100. It was developed as an antiretroviral agent targeting HIV infection, specifically designed to inhibit the HIV-1 protease enzyme. This mechanism blocks viral replication by preventing the cleavage of viral polyproteins, which is essential for producing mature infectious virus particles. PPL-100 demonstrated potent activity against multiple strains of HIV-1, including those resistant to currently marketed protease inhibitors, due to its high genetic barrier and favorable cross-resistance profile. The drug was initially developed by Procyon Biopharma and Ambrilia Biopharma and later licensed to Merck for further development. Despite promising preclinical results and early clinical trials (Phase 1), development was ultimately discontinued[1][2][6][9].

02

Targets

PR (Progesterone receptor)

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