BIT225 is in mid‑stage clinical development for treatment of HIV-1 and Hepatitis C virus (HCV) infections, with seven clinical trials completed. BIT225 has been dosed in 55 healthy human volunteers and 94 subjects infected with either HIV-1, HCV or co-infected with HIV-1/HCV.
Clinical trial results for BIT225 include:
HIV-1
- BIT225 is a novel first-in-class HIV-1 Vpu protein inhibitor with the aim of inhibiting virus replication in cellular reservoirs.
- In vitro studies have shown BIT225
- Significantly inhibits HIV-1 release in a dose dependent manner from CD14+ and CD16+ monocyte subsets at various stages of differentiation and monocyte-derived dendritic cells (MDDC)
- Significantly reduces cell-cell transmission of virus from HIV-1 infected myeloid lineage cells to CD4+ T cell targets
- Has broad spectrum activity against clinical isolates from different virus clades and selected drug resistant strains
- Has additive or synergistic inhibition of virus replication in combination with marketed HIV-1 anti-retroviral drugs from different classes
- Studies in the clinic have demonstrated
- BIT225 treated isolated cells from HIV-1 infected patients show reduced HIV-1 release from CD14+ monocytes
- Following 10 days of monotherapy in HIV-1 infected patients, BIT225 can reduce viral copy numbers and inhibit replication in myeloid lineage cells (including dendritic cells)
- BIT225 may impact on macrophage associated immune activation
- BIT225 is able to cross the blood-brain barrier, with potential to treat HIV-associated neurocognitive disorder (HAND)
HCV
- BIT225 is a novel first-in-class viral assembly inhibitor that targets HCV p7 protein
- In vitro studies have shown
- Pan genotypic activity in HCV infectious clone assay
- Synergy with marketed drugs for the treatment of HCV
- High barrier to antiviral resistance
- Studies in the clinic have demonstrated
- Clinical antiviral efficacy against HCV genotypes 1 and 3
- BIT225 treatment is associated with faster viral clearance in treated HCV patients
- Substantial safety, tolerability and pharmacokinetic data in both Phase 1 and 2 clinical trials of up to 3 months dosing duration
Completed Human Clinical Trials:
- BIT225-001 – Phase 1, single-dose, dose escalating study (n=48)
- BIT225-003 – Phase 1b, HCV-infected patients (n=18)
- BIT225-004 – Phase 1b/2a, HIV-1 infected patients (n=21) Trial registration on ANZCTR
- BIT225-005 – Phase 2a, HCV-infected patients (n=24) Trial registration on ANZCTR
- BIT225-006 – Phase 2, HIV/HCV co-infected (n=12) Trial registration on ANZCTR
- BIT225-007 – Phase 1 capsule formulation, cross-over study (n=14) Trial registration on ANZCTR
- BIT225-008 – Phase 2, repeat dose (n=60) Trial registration on ANZCTR
