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BIT225

Names
IUPAC name N-Carbamimidoyl-5-(1-methyl-1H-pyrazol-4-yl)-2-naphthamide
Other names BIT-225
Identifiers
CAS Number	917909-71-8
3D model (JSmol)	Interactive image
ChemSpider	10176885
PubChem CID	12004418
UNII	M9C27TI12U
CompTox Dashboard (EPA)	DTXSID401031931
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
Except where otherwise noted, data are given for materials in their standard state (at 25 °C , 100 kPa). Infobox references

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. Because it targets replication in monocyte derived macrophages, it offers promise for treatment of viral reservoirs that are unaffected by standard treatments. The activity of BIT225 is post-virus integration, with no direct effects on the HIV enzymes reverse transcriptase and protease. 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.

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

• Antiretroviral drugs
• Pyrazoles
• Acylguanidines
• Experimental antiviral drugs