Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C11H15N5O3 |
Molecular Weight | 265.2685 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=C2NC=C([C@@H]3N[C@H](CO)[C@@H](O)[C@H]3O)C2=NC=N1
InChI
InChIKey=AMFDITJFBUXZQN-KUBHLMPHSA-N
InChI=1S/C11H15N5O3/c12-11-8-6(14-3-15-11)4(1-13-8)7-10(19)9(18)5(2-17)16-7/h1,3,5,7,9-10,13,16-19H,2H2,(H2,12,14,15)/t5-,7+,9-,10+/m1/s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/24590073Curator's Comment: Description was created using several sources including:
https://www.ncbi.nlm.nih.gov/pubmed/27838352
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24590073
Curator's Comment: Description was created using several sources including:
https://www.ncbi.nlm.nih.gov/pubmed/27838352
BCX-4430 hydrochloride is a salt of an antiviral adenosine analog BCX4430 (Immucillin-A) that acts as a viral RNA-dependent RNA polymerase (RdRp) inhibitor. It was developed as a potential treatment for deadly filovirus infections such as Ebola virus disease and Marburg virus disease but also demonstrated broad-spectrum antiviral effectiveness against a range of other RNA virus families, including, bunyaviruses, arenaviruses, paramyxoviruses, and coronaviruses. Biochemical, reporter-based and primer-extension assays indicate that BCX4430 inhibits viral RNA polymerase function, acting as a non-obligate RNA chain terminator. BCX4430 inhibits infection of distinct filoviruses in human cells. Post-exposure administration of BCX4430 protects rodents against Ebola and Marburg virus disease and cynomolgus macaques from Marburg virus when administered as late as 48 hours after infection. BCX4430 is highly active in a Syrian golden hamster model of yellow fever, even when treatment is initiated at the peak of viral replication. BCX4430 also showed efficacy against Zika virus in a mouse model.
Originator
Approval Year
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5540 ng/mL |
5 mg/kg single, intravenous dose: 5 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
GALIDESIVIR plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
10300 ng/mL |
10 mg/kg single, intravenous dose: 10 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
GALIDESIVIR plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
17730 ng/mL |
15 mg/kg single, intravenous dose: 15 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
GALIDESIVIR plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
20490 ng/mL |
20 mg/kg single, intravenous dose: 20 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
GALIDESIVIR plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
21160 ng × h/mL |
5 mg/kg single, intravenous dose: 5 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
GALIDESIVIR plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
37080 ng × h/mL |
10 mg/kg single, intravenous dose: 10 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
GALIDESIVIR plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
65860 ng × h/mL |
15 mg/kg single, intravenous dose: 15 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
GALIDESIVIR plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
81230 ng × h/mL |
20 mg/kg single, intravenous dose: 20 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
GALIDESIVIR plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27095300
BCX-4430 dose of 2.5 mg/kg QD for 7 days in healthy subjects to evaluate the safety, tolerability, and pharmacokinetics of BCX4430. Up to 4 ascending dose (up to 10.0 mg/kg) cohorts treated in a sequential manner.
Route of Administration:
Intramuscular
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27095300
Variation in and low efficiency of conversion of BCX4430 to BCX4430-TP were studied in cell lines commonly used for in vitro evaluation of antiviral activity of test agents. VERO, VERO-76, HeLa, HuH7b and MDCK cell lines were incubated with 10 uM BCX4430 for 1, 4 and 24 hours, and the levels of BCX4430-TP were quantitated by HPLC.
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300000017472
Created by
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DB11676
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C172613
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Galidesivir
Created by
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10445549
Created by
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249503-25-1
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OLF97F86A7
Created by
admin on Fri Dec 15 20:36:45 GMT 2023 , Edited by admin on Fri Dec 15 20:36:45 GMT 2023
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10284
Created by
admin on Fri Dec 15 20:36:45 GMT 2023 , Edited by admin on Fri Dec 15 20:36:45 GMT 2023
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
SALT/SOLVATE (PARENT)