Peramivir

Biological Activity

Peramivir is a transition-state analogue and a potent, specific influenza viral neuraminidase inhibitor with an IC50 of median 0.09 nM. The IC50 for peramivir is markedly lower than that for either zanamivir or oseltamivir. Peramivir increases survival in preclinical influenza models, including mouse and ferret models of highly pathogenic avian influenza H5N1. One day of treatment with peramivir is active, and multiple days of treatment rescues most or all mice with H5N1. Similar data have been obtained in ongoing murine experiments with seasonal influenza A (H1N1)/H274Y. After parenteral administration, peramivir reaches very high plasma concentrations. Peramivir is not metabolized, and is cleared by the means of renal filtration. It has a long half-life, especially in comparison with other neuraminidase inhibitors. Due to the failure of the metabolism of the antivirus compound peramivir, as well as its wide distribution and the excretion in the unchanged form in urine, dosing regimens can be adapted easily for patients with renal impairment and for pediatric populations. Peramivir is originally developed by BioCryst Pharmaceuticals. And peramivir is designed to aim to an antiviral agent. Peramivir has been performed phase III clinical trials for the treatment of influenza.

Another CAS# 229614-55-5

Product Citations

• 

  EBioMedicine. 2017 Aug;22:133-142.

  C-Reactive Protein Mediating Immunopathological Lesions: A Potential Treatment Option for Severe Influenza A Diseases
  Peramivir purchased from AbMole

Customer Product Validations & Biological Datas

	Source	EBioMedicine (2017). Figure 6. Peramivir (Abmole Bioscience, USA)
	Method	Mouse infection
	Cell Lines	C57 bl/6 mice
	Concentrations	3 mg/kg
	Incubation Time	48 h
	Results	In comparison, peramivir or 1,6-bis PC(L) treatment slightly improved the pathological damages. The pathological lesions showed moderate improvement in lungs of peramivir plus 1,6-bis PC treated mice.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

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 K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information

References

[1] No authors listed. Peramivir

[2] No authors listed. Aust Prescr. Peramivir for influenza

[3] Lesley J Scott. Peramivir: A Review in Uncomplicated Influenza

[4] No authors listed. Peramivir

[5] Milena M McLaughlin, et al. Peramivir: an intravenous neuraminidase inhibitor