Representative steroidal aromatase ingbitorov third generation is exemestane, which, entering into covalent interaction with aromatase during the first cycle of oxidation leads to an effective selective irreversible inactivation of the enzyme reduces and estrogen synthesis in the body by 97%. Like anastrazole and letrozole, it is well tolerated by patients. Produced for receiving per os in form of tablets of 25 mg, and the daily dose is in the treatment of metastatic breast cancer in postmenopausal women. Exemestane, which is approved in the USA and is used as a drug in the oncology first-line endocrine therapy for breast cancer after receiving Imre class of drugs so far in the clinical setting has not been studied. However, it found that with respect to the process of accumulation and the extent of aromatization of estrogens it has an activity higher than tamoxifen, but less high than anastrozole (AS TO comparative study, 2002).
Clinical trials have shown that the metastatic breast cancer exemestane more pronounced compared to tamoxifen, slow disease progression, but does not affect the process of metastasis. Randomized MA-17, Research ATAS, IES showed that it differs from the spectrum of toxicity of non-steroidal aromatase inhibitor, but the therapeutic value of this data has not been studied. The drug is subjectively very well tolerated; the most common side effects are hot flushes (19%) and nausea (21%). According to the severity of impact on the development of osteoporosis and the incidence of pathological fractures in patients treated with exemestane, letrozole is not inferior. The risk of pathological fractures compared with the control group (placebo) for exemestane is increased by 60%! Arthralgia accompany the drug in 4.5% of cases, which is higher than that of tamoxifen (3.6%). However, the risk of endometrial cancer, as well as arterial and venous thrombosis significantly lower for exemestane (and also letrozole) than tamoxifen. The frequency of appearance of dryness and itching of the urogenital region when receiving exemestane above, and vaginal discharge – lower than tamoxifen.
Action exemestane on mental ability tests in the above MA-17, ATAS, the IES has not been studied. However, all taking anti-estrogen drugs, you should think about the fact that a lack of endogenous estrogen, even against the background replacement therapy significantly increases the risk of developing dementia in the future.
This product is available in the following variations:
- Exedrol by Balkan Pharmaceuticals