Drug nameMegestrol
Description17-Hydroxy-6-methylpregna-3,6-diene-3,20-dione. A progestational hormone used most commonly as the acetate ester. As the acetate, it is more potent than progesterone both as a progestagen and as an ovulation inhibitor. It has also been used in the palliative treatment of breast cancer. [PubChem]
DrugBankPrimary Accession Number: DB00351
DIN02223112
TypeApproved, Small Molecule
IndicationFor the treatment of anorexia, cachexia, or an unexplained, significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS). Also used to treat breast cancer, endometrial cancer, and prostate cancer in Canada and some other countries.
Mechanism of ActionSeveral investigators have reported on the appetite enhancing property of megestrol acetate and its possible use in cachexia. The precise mechanism by which megestrol acetate produces effects in anorexia and cachexia is unknown at the present time. The biochemical mechanism of progestin antitumour activity is not well but may involve interaction with progesterone and glucocorticoid receptors, androgenic properties. Megestrol also has direct cytotoxic effects on breast cancer cells in tissue culture and suppresses luteinising hormone release from the pituitary.
AbsorptionVariable, but well absorbed orally.
ToxicityNo serious unexpected side effects have resulted from studies involving megestrol acetate oral suspension administered in dosages as high as 1200 mg/day.
Protein BindingNot available
Interactions
RXListhttp://www.rxlist.com/cgi/generic4/megace_es.htm
KEGGdrug: Not available / compound: C07120
PubChemcompound: 19090 / substance: 9331
PharmGKBPA450351
Metabolizing Enzymes
NameGeneEntrezIDUniprotSNP
Target
NameGeneEntrezIDSwissprotSNP
Estrogen receptorESR12099ESR1_HUMANrs2228480 rs2077647 rs4986934 rs1801132 rs34840398 rs17847076 rs17847067 rs17847065 rs9341069 rs9341068 rs9340802 rs9340773 rs1141584 rs746432
Progesterone receptorPGR5241PRGR_HUMANrs1042839 rs500760 rs1042838 rs36055552 rs35747049 rs35131968 rs34852313 rs11571252 rs11571222 rs11571179 rs11571152 rs11571151 rs11571150 rs11571149 rs11571148 rs11571147 rs11571146 rs11571145 rs11571144 rs11571143 rs10160726 rs10160588 rs3740754 rs3740753 rs2020880 rs2020878 rs2020876 rs2020874 rs1379130
FilesDB00351.mol | DB00351_2005-07-01.pdf | DB00351_653.pdf | pdb_4963628424834-0.pdb | sdf_2764532414996-0.sdf |
Smilesisomeric:
CC(=O)[C@@]1(O)CC[C@H]2[C@@H]3C=C(C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C
canonical:
CC(=O)C1(O)CCC2C3C=C(C)C4=CC(=O)CCC4(C)C3CCC12C

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