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Etavopivat

Cat. No. M21076
Etavopivat Structure
Synonym:

FT-4202

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Biological Activity

Etavopivat, an oral erythrocyte pyruvate kinase (PKR) activator, is being developed for sickle cell disease and other hemoglobinopathies, previously reported in 2019.

Chemical Information
Molecular Weight 457.50
Formula C22H23N3O6S
CAS Number 2245053-57-8
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] Bruno Fattizzo, et al. Front Med (Lausanne). Rise of the planet of rare anemias: An update on emerging treatment strategies

[2] Patricia Schroeder, et al. J Pharmacol Exp Ther. Etavopivat, a Pyruvate Kinase Activator in Red Blood Cells, for the Treatment of Sickle Cell Disease

[3] Sanjeev Forsyth, et al. Clin Pharmacol Drug Dev. Safety, Pharmacokinetics, and Pharmacodynamics of Etavopivat (FT-4202), an Allosteric Activator of Pyruvate Kinase-R, in Healthy Adults: A Randomized, Placebo-Controlled, Double-Blind, First-in-Human Phase 1 Trial

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  Catalog
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Keywords: Etavopivat, FT-4202 supplier, Pyruvate Kinase, inhibitors, activators


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