| Stereochemistry | ABSOLUTE |
| Molecular Formula | C11H15N5O3.ClH |
| Molecular Weight | 301.729 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.NC1=NC=NC2=C1NC=C2[C@@H]3N[C@H](CO)[C@@H](O)[C@H]3O
InChI
InChIKey=PCCHVYNGFMEGIG-QPAIBFMUSA-N
InChI=1S/C11H15N5O3.ClH/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);1H/t5-,7+,9-,10+;/m1./s1
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C11H15N5O3 |
| Molecular Weight | 265.2685 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
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
AUC
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
Sourcing
PubMed
Patents
Sample Use Guides
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
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.
