BIT225

Last updated
BIT225
BIT225.svg
Names
IUPAC name
N-Carbamimidoyl-5-(1-methyl-1H-pyrazol-4-yl)-2-naphthamide
Other names
BIT-225
Identifiers
3D model (JSmol)
ChemSpider
PubChem CID
UNII
  • 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
  • CN1C=C(C=N1)C2=CC=CC3=C2C=CC(=C3)C(=O)NC(=N)N
Properties
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).

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]

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References