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Hetrombopag

Cat. No. M13352
Hetrombopag  Structure
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Biological Activity

Hetrombopag is an effective thrombopoietin receptor agonist. Hetrombopag is effective, well tolerated and has a controllable safety profile. Hetrombopag has the potential to be studied in immune thrombocytopenia.

Chemical Information
Molecular Weight 458.47
Formula C25H22N4O5
CAS Number 2114365-78-3
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] Yahiya Y Syed. Drugs. Hetrombopag: First Approval

[2] Heng Mei, et al. J Hematol Oncol. A multicenter, randomized phase III trial of hetrombopag: a novel thrombopoietin receptor agonist for the treatment of immune thrombocytopenia

[3] Zhenlei Wang, et al. Clin Ther. Effect of Food on the Pharmacokinetic and Pharmacodynamic Profiles of Hetrombopag in Healthy Volunteers

[4] Zhenlei Wang, et al. J Thromb Haemost. First-in-patient study of hetrombopag in patients with chronic idiopathic thrombocytopenic purpura

[5] Guoping Yang, et al. Br J Clin Pharmacol. Effect of postdose fasting duration on hetrombopag olamine pharmacokinetics and pharmacodynamics in healthy volunteers

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Keywords: Hetrombopag supplier, Thrombopoietin/Thrombin, inhibitors, activators


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