BIT225
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IUPAC name N-Carbamimidoyl-5-(1-methyl-1H-pyrazol-4-yl)-2-naphthamide | |
Other names BIT-225 | |
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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 |
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]
References
- ^ BIT225 therapy reduces HIV-1 burden in monocyte cells and decreases immune activation
- ^ BIT225, a Novel Assembly Inhibitor, Cuts HIV Load in Monocyte Reservoir
- ^ Antiviral Efficacy of the Novel Compound BIT225 against HIV-1 Release from Human Macrophages
- ^ BIT225 Trial Results Show Effective Cure of Hepatitis C
- v
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(Discovery and development)
(Integrase strand transfer inhibitors (INSTI))
(Discovery and development)
1st generation | |
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2nd generation |
inhibitors (RTIs)
Nucleoside and nucleotide (NRTI) | |||||
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Non-nucleoside (NNRTI) (Discovery and development) |
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- Abacavir/lamivudine#
- Abacavir/dolutegravir/lamivudine°
- Abacavir/lamivudine/zidovudine
- Atazanavir/cobicistat
- Bictegravir/emtricitabine/tenofovir alafenamide°
- Cabotegravir/rilpivirine
- Darunavir/cobicistat
- Darunavir/cobicistat/emtricitabine/tenofovir alafenamide°
- Dolutegravir/emtricitabine/tenofovir alafenamide
- Dolutegravir/lamivudine°
- Dolutegravir/lamivudine/tenofovir alafenamide°
- Dolutegravir/lamivudine/tenofovir disoproxil°#
- Dolutegravir/rilpivirine
- Doravirine/lamivudine/tenofovir disoproxil
- Efavirenz/emtricitabine/tenofovir disoproxil#
- Efavirenz/lamivudine/tenofovir disoproxil#
- Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide
- Elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil
- Emtricitabine/tenofovir alafenamide
- Emtricitabine/rilpivirine/tenofovir alafenamide
- Emtricitabine/rilpivirine/tenofovir disoproxil
- Emtricitabine/tenofovir disoproxil#
- Lamivudine/nevirapine/stavudine
- Lamivudine/nevirapine/zidovudine
- Lamivudine/raltegravir
- Lamivudine/tenofovir disoproxil#
- Lamivudine/zidovudine#
- Lopinavir/ritonavir#
Uncoating inhibitors |
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Transcription inhibitors |
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Translation inhibitors | |
BNAbs | |
Other | |
Failed agents |
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III