Product name: Exemestane
Alias: Aromasin ; Exemestan;Exemestane
Product Category: Pharmaceutical raw materials and intermediates
Assay: 98%min
CAS Registry Number:107868-30-4
Molecular formula: C20H24O2
Appearance: White or Almost White Crystalline Powder
Grade : Pharmaceutical Grade
Storage: Shading, confined preservation
Usage: Developed to help fight breast cancer, Aromasin is one of the most powerful estrogen suppressing compounds
Other drugs in same class: Anastrozole,Letrozole,Tamoxifen citrate,Exemestane
Description.
Exemestane is an oral steroidal aromatase inhibitor that is used in ER-positive breast cancer in addition to surgery and/or radiation in post-menopausal women.
The main source of estrogen is the ovaries in premenopausal women, while in post-menopausal women most of the body's estrogen is produced via the conversion of androgens into estrogen by the aromatase enzyme in the peripheral tissues (i.e. adipose tissue like that of the breast) and a number of sites in the brain. Estrogen is produced locally via the actions of the aromatase enzyme in these peripheral tissues where it acts locally. Any circulating estrogen in post-menopausal women as well as men is the result of estrogen escaping local metabolism and entering the circulatory system.
Applications
Exemestane is an oral steroidal aromatase inhibitor that is used in ER-positive breast cancer in addition to surgery and/or radiation in post-menopausal women.
The main source of estrogen is the ovaries in premenopausal women, while in post-menopausal women most of the body's estrogen is produced via the conversion of androgens into estrogen by the aromatase enzyme in the peripheral tissues (i.e. adipose tissue like that of the breast) and a number of sites in the brain. Estrogen is produced locally via the actions of the aromatase enzyme in these peripheral tissues where it acts locally. Any circulating estrogen in post-menopausal women as well as men is the result of estrogen escaping local metabolism and entering the circulatory system.
Exemestane is an irreversible, steroidal aromatase inactivator, structurally related to the natural substrate androstenedione. It acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme causing its inactivation, an effect also known as "suicide inhibition." By being structurally similar to enzyme targets, Exemestane permanently binds to the enzymes, preventing them from converting androgen into estrogen.
Exemestane is taken in tablet form once a day. Patients can experience side effects like nausea, anxiety, shortness of breath, abdominal pain, bone pain, and chest pain. Side effects vary widely between patients and patients should report the side effects they experience to their doctors, as some may be indicators of dangerous complications. Shortness of breath and chest pain in particular are causes for concern in patients taking exemestane.
Aromasin is used to fight breast cancer and raise testosterone in the body.
Exemestane blocks the process of aromatisation. So it lowers the amount of oestrogen in the body. In early breast cancer, taking exemestane can help to stop breast cancer coming back. In advanced breast cancer the cancer cells may grow more slowly or stop growing completely.
Hormones are chemical substances that are produced by glands in the body, which enter the bloodstream and cause effects in other tissues. For example, the hormone testosterone made in the testicles and is responsible for male characteristics such as deepening voice and increased body hair. The use of hormone therapy to treat cancer is based on the observation that receptors for specific hormones that are needed for cell growth are on the surface of some tumor cells. Hormone therapies work by stopping the production of a certain hormone, blocking hormone receptors, or substituting chemically similar agents for the active hormone, which cannot be used by the tumor cell. The different types of hormone therapies are categorized by their function and/or the type of hormone that is affected.
Specification
COA:
TEST ITEMS | SPECIFICATION | RESULTS |
Description | White Crystalline Powder | White Powder |
Identification | Positive | Positive |
Assay(by HPLC) | 98.0~102.0% | 99.04% |
Absorbance(E1cm) | 465~495 | 482.5 |
Melting Point | 191~195°C | 193.5~195.0°C |
Loss On Drying | 0.5%max | 0.19% |
Specific Rotation | +288°~ +298° | +290.2° |
Residue On Ignition | 0.1%max | 0.03% |
Related Substances | Total:1.5%max | <1.3% |
Single | 0.5%max | <0.4% |
Residue Solvents | 0.2%max | 0.10% |
Heavy Metals | 20PPm max | <10PPm |
Conclusion | The specification conform with enterprise standard. |