Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C16H10ClF3N2O |
| Molecular Weight | 338.712 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
FC(F)(F)OC1=CC=C(NC2=NC3=C(Cl)C=CC=C3C=C2)C=C1
InChI
InChIKey=OZOGDCZJYVSUBR-UHFFFAOYSA-N
InChI=1S/C16H10ClF3N2O/c17-13-3-1-2-10-4-9-14(22-15(10)13)21-11-5-7-12(8-6-11)23-16(18,19)20/h1-9H,(H,21,22)
| Molecular Formula | C16H10ClF3N2O |
| Molecular Weight | 338.712 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 12:05:13 UTC 2023
by
admin
on
Sat Dec 16 12:05:13 UTC 2023
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| Record UNII |
26RU378B9V
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| Record Status |
Validated (UNII)
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| Record Version |
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-
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26RU378B9V
Created by
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49846599
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12112
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C158506
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KL-38
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DB14828
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300000025974
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1258453-75-6
Created by
admin on Sat Dec 16 12:05:13 UTC 2023 , Edited by admin on Sat Dec 16 12:05:13 UTC 2023
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TARGET ORGANISM->INHIBITOR |
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| Related Record | Type | Details | ||
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ACTIVE MOIETY |
Drug: ABX 464(Primary); Indication: HIV infections; Focus: Therapeutic Use; Most Recent Events: 04 Feb 2015 New trial record, 02 Feb 2015 According to an Abivax media release, this study is planned to start in the second half of 2015.
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ACTIVE MOIETY |
RESULTS: ABX464 efficiently compromised viral proliferation in two humanized mouse models infected with HIV that require a combination of 3TC, Raltegravir and Tenofovir (HAART) to achieve viral inhibition in current protocols. Crucially, while viral load increased dramatically just one week after stopping HAART treatment, only slight rebound was observed following treatment cessation with ABX464 and the magnitude of the rebound was maintained below to that of HAART for two months after stopping the treatment. Using a system to visualize single HIV RNA molecules in living cells, we show that ABX464 inhibits viral replication by preventing Rev-mediated export of unspliced HIV-1 transcripts to the cytoplasm and by interacting with the Cap Binding Complex (CBC). Deep sequencing of viral RNA from treated cells established that retained viral RNA is massively spliced but importantly, normal cellular splicing is unaffected by the drug. Consistently ABX464 is non-toxic in humans and therefore represents a promising complement to current HIV therapies.
CONCLUSIONS: ABX464 represents a novel class of anti-HIV molecules with unique properties. ABX464 has a long lasting effect in humanized mice and neutralizes the expression of HIV-1 proviral genome of infected immune cells including reservoirs and it is therefore a promising drug toward a functional cure of HIV.
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