BIT225

BIT225 is an experimental drug candidate under development by Biotron Limited for use in the treatment of both HIV and hepatitis C infection. By blocking Vpu ion channel activity, it disrupts HIV assembly within host monocyte cells; its method of action is a first for HIV drugs.[1] Because it targets replication in monocyte derived macrophages, it offers promise for treatment of viral reservoirs that are unaffected by standard treatments.[2] The activity of BIT225 is post-virus integration, with no direct effects on the HIV enzymes reverse transcriptase and protease.[3] Since Vpu ion channel activity is highly conserved, the virus is unlikely to become resistant via generation of Vpu ion-independent virus. In addition, the drug also has been credited with curing hepatitis C after 12 weeks of treatment.[4]

BIT225
Names
IUPAC name
N-Carbamimidoyl-5-(1-methyl-1H-pyrazol-4-yl)-2-naphthamide
Other names
BIT-225
Identifiers
CAS Number
3D model (JSmol)
ChemSpider
PubChem CID
UNII
InChI
  • InChI=1S/C16H15N5O/c1-21-9-12(8-19-21)13-4-2-3-10-7-11(5-6-14(10)13)15(22)20-16(17)18/h2-9H,1H3,(H4,17,18,20,22)
    Key: WVROWPPEIMRGAB-UHFFFAOYSA-N
  • InChI=1/C16H15N5O/c1-21-9-12(8-19-21)13-4-2-3-10-7-11(5-6-14(10)13)15(22)20-16(17)18/h2-9H,1H3,(H4,17,18,20,22)
    Key: WVROWPPEIMRGAB-UHFFFAOYAP
SMILES
  • CN1C=C(C=N1)C2=CC=CC3=C2C=CC(=C3)C(=O)NC(=N)N
Properties
Chemical formula
 C16H15N5O
Molar mass 293.330 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references

References
  1. BIT225 therapy reduces HIV-1 burden in monocyte cells and decreases immune activation
  2. BIT225, a Novel Assembly Inhibitor, Cuts HIV Load in Monocyte Reservoir
  3. Antiviral Efficacy of the Novel Compound BIT225 against HIV-1 Release from Human Macrophages
  4. BIT225 Trial Results Show Effective Cure of Hepatitis C
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