| Candidate ID: | R0127 |
| Source ID: | DB00351 |
| Source Type: | approved; investigational; vet_approved |
| Compound Type: |
small molecule
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| Compound Name: |
Megestrol acetate
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| Synonyms: |
17-Acetoxy-6-methylpregna-4,6-diene-3,20-dione; 17-Hydroxy-6-methylpregna-4,6-diene-3,20-dione 17-acetate; 17alpha-Acetoxy-6-dehydro-6-methylprogesterone; 17alpha-Hydroxy-6-methylpregna-4,6-diene-3,20-dione acetate; 17α-Acetoxy-6-dehydro-6-methylprogesterone; 17α-Hydroxy-6-methylpregna-4,6-diene-3,20-dione acetate; 6-Dehydro-6-methyl-17alpha-acetoxyprogesterone; 6-Dehydro-6-methyl-17α-acetoxyprogesterone; 6-Methyl-17alpha-acetoxypregna-4,6-diene-3,20-dione; 6-Methyl-17alpha-hydroxy-delta(sup 6)-progesterone acetate; 6-Methyl-17α-acetoxypregna-4,6-diene-3,20-dione; 6-Methyl-17α-hydroxy-delta(sup 6)-progesterone acetate; 6-Methyl-6-dehydro-17alpha-acetoxyprogesterone; 6-Methyl-6-dehydro-17α-acetoxyprogesterone; 6-Methyl-delta(sup 4,6)-pregnadien-17alpha-ol-3,20-dione acetate; 6-Methyl-delta(sup 4,6)-pregnadien-17α-ol-3,20-dione acetate; 6-Methyl-delta(sup 6)-dehydro-17alpha-acetoxyprogesterone; 6-Methyl-delta(sup 6)-dehydro-17α-acetoxyprogesterone; Megestrol acetate; MGA
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| Molecular Formula: |
C24H32O4
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| SMILES: |
[H][C@@]12CC[C@](OC(C)=O)(C(C)=O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])C=C(C)C2=CC(=O)CC[C@]12C
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| Structure: |
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| DrugBank Description: |
17-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.
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| CAS Number: |
595-33-5
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| Molecular Weight: |
384.516
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| DrugBank Indication: |
For the treatment of anorexia, cachexia, or an unexplained, significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS). Also used for the palliative management of recurrent, inoperable, or metastatic breast cancer, endometrial cancer, and prostate cancer in Canada and some other countries.
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| DrugBank Pharmacology: |
Megestrol is a synthetic progestin and has the same physiologic effects as natural progesterone. These effects include induction of secretory changes in the endometrium, increase in basal body temperature, pituitary inhibition, and production of withdrawal bleeding in the presence of estrogen. Mestrogel has slight glucocorticoid activity and very slight mineralocorticoid activity. This drug has no estrogenic, androgenic, or anabolic activity. The precise mechanism of megestrol’s antianorexic and anticachetic effects is unknown. Initially developed as a contraceptive, it was first evaluated in breast cancer treatment in 1967.
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| DrugBank MoA: |
The precise mechanism by which megestrol acetate produces effects in anorexia and cachexia is unknown at the present time, but its progestin antitumour activity may involve suppression of luteinizing hormone by inhibition of pituitary function. Studies also suggest that the megestrol's weight gain effect is related to its appetite-stimulant or metabolic effects rather than its glucocorticoid-like effects or the production of edema. It has also been suggested that megestrol may alter metabolic pathyways via interferences with the production or action of mediators such as cachectin, a hormone that inhibits adipocyte lipogenic enzymes.
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| Targets: |
Progesterone receptor agonist; Glucocorticoid receptor agonist
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| Inclusion Criteria: |
Therapeutic strategy associated
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