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Megestrol

Cat. No. M20989
Megestrol Structure
Synonym:

Megace

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Quality Control & Documentation
Biological Activity

Megestrol, a synthetic progestin, is approved for the treatment of anorexia, cachexia, or an unexplained significant weight loss in patients with an acquired immunodeficiency syndrome diagnosis. Megestrol acetate (Megace) is one of the first progestational agents to be evaluated for use in the hormonal therapy of advanced breast cancer.

Chemical Information
Molecular Weight 342.47
Formula C22H30O3
CAS Number 3562-63-8
Solubility (25°C) DMSO 68 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] Nicole C Cheung, et al. Sr Care Pharm. Efficacy and Safety of Megestrol in the Hospitalized Older Person

[2] Emilio Garca Garca, et al. Med Clin (Barc). Megestrol-induced adrenal insufficiency in children and adolescents

[3] Jennifer A Pruskowski. Am J Geriatr Psychiatry. Another Strike Against Megestrol Acetate Therapy?

[4] R Canetta, et al. Cancer Treat Rev. Megestrol acetate

[5] L Schacter, et al. Cancer Treat Rev. Megestrol acetate: clinical experience

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Keywords: Megestrol, Megace supplier, Estrogen Receptor, inhibitors, activators


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