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Megestrol Acetate is the acetate salt form of megestrol, a synthetic derivative of the naturally occurring female sex hormone progesterone with potential anti-estrogenic and antineoplastic activity.
Megestrol acetate, a progestational agent, is frequently used in the treatment of patients with metastatic breast cancer.
Megestrol acetate is a synthetic progesterone.
Items | Specifications | Results |
Characteristics | White to creamy white,tasteless and essentially odorless,crystalline powder | Conform |
Identification | IR | Conform |
Solubility | Insoluble in water,soluble in acetone,sparingly soluble in alcohol. | Conform |
Residual solvents | Methanol ≤300ppm Ethanol ≤5000ppm Methylene chloride ≤600ppm | 16ppm Not detected 122ppm |
Specific rotation | +8.8~+12° | +10.6° |
Melting point | 213-220℃ | 214.1-217.0℃ |
Water | ≤0.5% | 0.11% |
Residue on Ignition | ≤0.2% | 0.08% |
Assay | 97.0~103.0% | 98.84% |
Micron | 100%≤20μm | 100%≤20μm |
Conclusion | The product conform to USP42 Standard. | |
| Product parameters | |
| Cas number: | 595-33-5 |
| Appearance: | White to creamy powder |
| Purity: | 97~103% |
| Package details: | 1kg/foil bag; 25kg/drum |
| Brand: | Fortunachem |
Megestrol Acetate is a synthetic progestin, which is a man-made version of the natural female hormone progesterone. Its chemical name reflects its structure, and it is significantly more potent than natural progesterone.
It is primarily used in medicine for two very different purposes: treating certain cancers and stimulating appetite.
Chemical Class: It is a synthetic steroid hormone, specifically a 17α-hydroxyprogesterone derivative.
Molecular Formula: C₂₄H₃₂O₄
Key Feature: Its structure is a modified version of the progesterone molecule. The key modifications (an additional double bond and an acetyl group at the 17th position) make it more potent and effective when taken orally, as it resists breakdown by the liver.
A simplified 2D diagram of its structure would look like this (focusing on the steroid backbone):
It is based on the pregnane skeleton (a four-ring steroid structure). Key modifications: 1. A double bond between carbons 6 and 7. 2. A methyl group at carbon 6. 3. An acetyl group (OCOCH3) at carbon 17.
Megestrol Acetate works through several pathways, depending on its use:
As an Anticancer Agent (for Breast/Endometrial Cancer):
Competitive Inhibition: It binds to the progesterone receptor in hormone-sensitive cancer cells.
Gene Expression Alteration: Once bound, it enters the cell nucleus and alters gene expression, ultimately inhibiting the growth-stimulating effects of estrogen.
Suppressing Estrogen Production: It can suppress the production of estrogen from the adrenal glands by inhibiting the release of gonadotropins (LH and FSH) from the pituitary gland. This "starves" estrogen-dependent tumors of the fuel they need to grow.
As an Appetite Stimulant (for Cachexia):
The exact mechanism for appetite stimulation is not fully understood but is believed to involve:
Activation of Neuropeptide-Y (NPY): It is thought to stimulate the synthesis and release of NPY in the hypothalamus, a part of the brain that is a powerful stimulator of appetite.
Inhibition of Cytokines: It may help by inhibiting the production of inflammatory cytokines (like TNF-α and IL-6) that contribute to the wasting process in cachexia.
Enhancing Fat Storage: Through its progestational activity, it can also promote lipid synthesis and storage, leading to weight gain, primarily as fat.
Palliative Treatment of Cancer:
Breast Cancer: Used as a second-line therapy for advanced, hormone-sensitive breast cancer in postmenopausal women.
Endometrial Cancer: Used for the treatment of advanced endometrial cancer.
Treatment of Cachexia (Wasting Syndrome):
AIDS
Cancer (Cancer Cachexia)
This is its most common use today. It is prescribed to treat anorexia (loss of appetite) or significant, unintentional weight loss in patients with:
Other Uses:
Hormone Therapy for Transgender Women: Sometimes used in feminizing hormone therapy as a progestin.
Managing Benign Prostatic Hyperplasia (BPH): Rarely used for this purpose today.
Formulation: It is available as an oral tablet and an oral suspension (liquid). The suspension is often preferred for appetite stimulation as it's easier to swallow for debilitated patients.
Common Side Effects:
Weight Gain: This is an intended effect for cachexia but can be an undesirable side effect in other contexts.
Adrenal Suppression: Long-term use can suppress the body's natural production of cortisol, a critical stress hormone. Abruptly stopping the drug can be dangerous and may require a gradual dose reduction.
Thromboembolism: Increased risk of blood clots.
Breakthrough Uterine Bleeding
Nausea, diarrhea, flatulence.
Black Box Warning (US FDA): The label carries a black box warning for several serious risks:
Increased risk of deep vein thrombosis (DVT) and pulmonary embolism (PE).
The use in pregnancy is contraindicated due to the potential for birth defects.
In essence, Megestrol Acetate is a potent synthetic progestin. Its primary clinical value lies in its dual ability to act as a hormonal anti-cancer agent by blocking estrogen-driven tumor growth and as a powerful appetite stimulant to counteract the devastating weight loss seen in cachexia associated with AIDS and cancer. Its use requires careful medical supervision due to significant side effects, particularly its impact on the adrenal gland and risk of blood clots.
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