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Rilematovir (JNJ-53718678)

Cat. No. M21280
Rilematovir (JNJ-53718678) Structure
Synonym:

Rilematovir；JNJ-678

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Biological Activity

Rilematovir (JNJ-53718678) is a potent and orally available fusion inhibitor of the RSV virus, optimized from a prior oral inhibitor, BMS-433771.

Chemical Information
Molecular Weight 500.92
Formula C21H20ClF3N4O3S
CAS Number 1383450-81-4
Solubility (25°C) DMSO : 65 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Bart Remmerie, et al. Adv Ther. Integrating Duodenal Sampling in a Human Mass Balance Study to Quantify the Elimination Pathways of JNJ-53718678, a Respiratory Syncytial Virus Fusion Protein Inhibitor

[2] John H Beigel, et al. Antiviral Res. Advances in respiratory virus therapeutics - A meeting report from the 6th isirv Antiviral Group conference

[3] Marita Stevens, et al. J Infect Dis. Antiviral Activity of Oral JNJ-53718678 in Healthy Adult Volunteers Challenged With Respiratory Syncytial Virus: A Placebo-Controlled Study

[4] Dirk Roymans, et al. Nat Commun. Therapeutic efficacy of a respiratory syncytial virus fusion inhibitor

[5] Dymphy R H Huntjens, et al. Clin Pharmacokinet. Population Pharmacokinetic Modeling of JNJ-53718678, a Novel Fusion Inhibitor for the Treatment of Respiratory Syncytial Virus: Results from a Phase I, Double-Blind, Randomized, Placebo-Controlled First-in-Human Study in Healthy Adult Subjects

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Keywords: Rilematovir (JNJ-53718678), Rilematovir；JNJ-678 supplier, RSV, inhibitors, activators

 
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