1.What is Exemestane?
Definition:
Exemestane is a steroidal aromatase inhibitor used in the treatment of advanced breast cancer in postmenopausal women whose disease has progressed after treatment with tamoxifen.
Postmenopausal women with estrogen receptor-positive early breast cancer are switched to Exemestane for a total of five years of adjuvant hormonal therapy after two to three years of tamoxifen.
Aromasin® is the brand name for exemestane and is available as a tablet in one strength: 25 mg, which is taken at the same time once daily.
It can be used alone or in combination with other medications, and the US FDA approved it in October 1999.
Chemical & Physical properties:
Chemical structure:
Molecular weight: 296.41
Molecular formula: C20H24O2
CAS (Chemical Abstracts Service) number: 107868-30-4
IUPAC name: (8R,9S,10R,13S,14S)-10,13-dimethyl-6-methylidene-7,8,9,11,12,14,15,16-octahydrocyclopenta[a]phenanthrene-3,17-dione
DrugBank accession number: DB00990
Powder Color: White to slightly yellow crystalline powder
Melting point: 155.13 °C
Water Solubility: Non-soluble
Brand names: Aromasin®
2. Mechanism of action
Exemestane binds irreversibly to the active site of the enzyme aromatase, causing it to be permanently inhibited and preventing cholesterol conversion to pregnenolone as well as peripheral aromatization of androgenic precursors into estrogens.
As a result, the body produces less estrogen, which can slow or stop some breast tumors that require estrogen to grow.
3. Forms and specifications
Exemestane tablets （25mg)
Each Aromasin® Tablet is round, biconvex, and contains 25 mg of the active ingredient, exemestane, which is white to slightly yellow crystalline powder with a molecular weight of 296.41.
The tablets are approved for use in the treatment of advanced breast cancer in postmenopausal women.
4.Exemestane vs Arimidex
Exemestane (Aromasin®) and anastrozole (Arimidex®) are both aromatase inhibitors (medications that reduce the production of the hormone estrogen) used in the treatment of postmenopausal women with breast cancer.
Females whose cancer has progressed despite taking tamoxifen are frequently given both drugs.
Both medications work in the same way as aromatase inhibitors and have similar side effects.
5.Exemestane vs Letrozole
Both exemestane (Aromasin®) and letrozole (Femara®) are third-generation aromatase inhibitors used to lower estrogen levels and thus reduce the risk of tumor progression in females with certain types of cancer.
Femara's off-label use includes increasing fertility in females with polycystic ovary syndrome (PCOS) by inducing ovulation. In contrast, Aromasin's off-label use includes adjuvant treatment of estrogen receptor-positive early breast cancer in postmenopausal women.
Both medications are available as oral tablets that must be taken daily.
6.Uses
Breast cancer
Aromasin® is a steroidal aromatase inhibitor that effectively treats advanced breast cancer in postmenopausal women.
Exemestane-based hormone therapy may help fight cancer by preventing tumor cells from using estrogen or reducing estrogen in the body.
Gynecomastia
Aromatase inhibitors may be used to treat gynecomastia (male breast growth) caused by an imbalance in androgen and estrogen action.
The drug, however, has not been approved by the FDA for this use.
7.Dosage
One 25 mg tablet taken once daily after a meal is the recommended dose in early and advanced breast cancer.
8.Side effects
Hot flashes, nausea, fatigue, arthralgia, headache, insomnia, and increased sweating are possible side effects.
9.Manufacturing process
The in-active ingredients in each Aromasin® Tablet are as follows: mannitol, crospovidone, polysorbate 80, hypromellose, colloidal silicon dioxide, microcrystalline cellulose, sodium starch glycolate, magnesium stearate, simethicone, polyethylene glycol 6000, sucrose, magnesium carbonate, titanium dioxide, methylparaben, and polyvinyl alcohol.
10.Exemestane Active Pharmaceutical Ingredient (API) price
The average price is 5.8k (USD/KGS).
11.Exemestane Active Pharmaceutical Ingredient (API) manufacturers in China
Below are some professional pharmaceutical ingredients manufacturers in China.
QILU PHARMACEUTICAL
Qilu Pharmaceutical is a large modern pharmaceutical enterprise in China that can supply high-quality products and services like API, chemical synthesis, fermentation, and biological technology.
The products have been certified by drug regulators in the United States, the European Union, Australia, the United Kingdom, South Africa, and other countries.
The major manufacturing equipment and instruments are purchased from the world's leading professional pharmaceutical equipment manufacturers.
Qilu Pharma Spain is the European subsidiary of Qilu Pharmaceutical.
Product CAS Number: 107868-30-4
The company contact number: +86-531-83127726
Factory Location: Jinan Shandong, China
Main Sales Markets: America, Europe, Australasia, Asia (e.g., India), Middle East, and Africa.
Sichuan Xieli Pharmaceutical Co., Ltd.
Xieli Pharma is a leading manufacturer with 17 high-quality products registered in over 100 countries, including intermediates, APIs, and formulations.
Business Type: Manufacturing and trading company
Product CAS Number: 107868-30-4
Product Purity: 98.5%d
Contact Number: +86-28-85312818
Factory Location: Chengdu Sichuan, China
Main Sales Markets: America, Europe, Australasia, Asia (e.g., India), Middle East, and Africa
HuNan Kerey Pharmaceutical Co., Ltd.
HuNan Kerey Pharmaceutical Co., Ltd. is one of China's leading pharmaceutical companies, receiving the "Private Technology Development Contribution Award" in 2010 and quality system certification.
They can supply high-quality pharmaceutical intermediates manufacture and pharmaceutical intermediates.
Main Product Categories: Active Pharmaceutical Ingredients, Intermediates.
Product CAS Number: 107868-30-4
Product Purity: 99%
The company contact number: +86-739-3669978
Factory Location: Shao yang Hu nan, China
Main Sales Markets: America, Europe, Australasia, Asia (e.g., India), Middle East, and Africa.
HUBEI GOTO BIOPHARM CO., LTD.
Hubei Goto Biopharm Co., Ltd. is one of China's largest manufacturers and suppliers of steroid hormone API and intermediates.
They have two factories, one specializing in high-quality starting materials and intermediates of steroid hormones and the other in chemical synthesis of steroid hormone API and intermediates.
Product CAS Number: 107868-30-4
Contact Number: +86-710-3423122-815
Email: info@gotochem.com
Factory Location: Xiangyang Hubei, China
Main Sales Markets: America, Europe, Australasia, Asia (e.g., India), Middle East, and Africa.
GUANGDONG VTR BIO-TECH CO., LTD.
Business Type: Manufacturer
Product CAS Number: 107868-30-4
Contact Number: +86-756-8676888
Email: vtr@vtrbio.com
Factory Location: Liuyang Hunan, China
Main Sales Markets: America, Europe, Australasia, Asia (e.g., India), Middle East, and Africa.
12.FAQ:
What is the market size of exemestane?
The global exemestane API market report (2021-2027) identifies various key manufacturers of the market divided geographically into North America, Europe, Asia-Pacific (e.g., China, India), South America, and the Middle East and Africa.
Is exemestane a chemotherapy drug?
Aromatase inhibitors are antineoplastic (anticancer) agents and standard hormone therapy used in the adjuvant treatment of postmenopausal breast cancer.
They work by decreasing the amount of estrogen produced by the body, which can slow or stop some breast tumors that require estrogen to grow.
What is an exemestane half-life?
The half-life is approximately 24 hours.
What is the use of exemestane in bodybuilding?
Aromasin®, which lowers estrogen levels and increases testosterone in the body, is used by some bodybuilders to reduce the side effects of anabolic steroids, increase muscle mass, and improve athletic performance.
However, in some cases, males may experience side effects due to disrupting hormone production in the body; therefore, using Aromasin® for bodybuilding purposes is considered a drug misuse.
What is the difference between anastrozole and exemestane?
Both medications are aromatase inhibitors, which treat cancer in postmenopausal females by inhibiting aromatase enzymes. Likewise, both have FDA approval to treat cancer.
However, the steroidal aromatase inhibitor Aromasin® is the only aromatase inhibitor that causes androgenic side effects instead of the non-steroidal aromatase inhibitor anastrozole (Arimidex®), which causes less bone loss in females and thus appears to maintain an advantage in bone health.
References:
1. https://pubchem.ncbi.nlm.nih.gov/compound/Exemestane
2. https://go.drugbank.com/drugs/DB00990
3. https://www.rxlist.com/aromasin-drug.htm#description
4. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020753s020lbl.pdf
5. https://www.medicalnewstoday.com/articles/aromasin#aromasin-vs-arimidex
6. https://www.drugs.com/medical-answers/aromasin-exemestane-femara-letrozole-compare-3545307/
7. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3143915/
8. https://www.marketwatch.com/press-release/exemestane-api-market-size-share-2021-global-growth-trends-industry-analysis-key-players-and-forecast-2027-2021-04-01
9. https://www.healthline.com/health/drugs/aromasin-dosage#fa-qs
10. https://www.researchgate.net/post/How-can-I-choose-between-Aromatase-inhibitors-in-postmenopausal-hormone-positive-breast-cancer
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