| Powder: | Yes |
|---|---|
| Customized: | Non-Customized |
| Certification: | Enterprise Standards |
| Suitable for: | Adult |
| State: | Powder |
| Purity: | >98% |
| Customization: |
|---|
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Abiraterone, the active metabolite of abiraterone acetate, inhibits CYP17A1, which manifests as two enzymes, 17α-hydroxylase (IC50 = 2.5 nM) and 17,20-lyase (IC50 = 15 nM) (approximately 6-fold more selective for inhibition of 17α-hydroxylase over 17,20-lyase) that are expressed in testicular, adrenal, and prostatic tumor tissues. CYP17A1 catalyzes two sequential reactions: (a) the conversion of pregnenolone and progesterone to their 17α-hydroxy derivatives by its 17α-hydroxylase activity, and (b) the subsequent formation of and androstenedion, respectively, by its 17,20-lyase activity. Androstenedion are androgens and precursors of testosteron. Inhibition of CYP17A1 activity by abiraterone acetate thus decreases circulating levels of androgens such as testosteron, and dihydrotestosteron (DHT). Abiraterone acetate, via abiraterone, has the capacity to lower circulating testosteron levels to less than 1 ng/dL (i.e., undetectable) when added to castration. These concentrations are considerably lower than those achieved by castration alone (~20 ng/dL). The addition of abiraterone acetate to castration was found to reduce levels of DHT by 85%, and androstenedion by 77 to 78% relative to castration alone. In accordance with its antiandrogenic action, abiraterone acetate decreases the weights of the prostate gland, seminal vesicles, and testes.
Abiraterone also acts as a partial antagonist of the androgen receptor (AR), and as an inhibitor of the enzymes 3β-hydroxysteroid dehydrogenase (3β-HSD), CYP11B1 (steroid 11β-hydroxylase), CYP21A2 (Steroid 21-hydroxylase), and other CYP450s (e.g., CYP1A2, CYP2C9, and CYP3A4). In addition to abiraterone itself, part of the activity of the drug has been found to be due to a more potent active metabolite, δ4-abiraterone (D4A), which is formed from abiraterone by 3β-HSD. D4A is an inhibitor of CYP17A1, 3β-hydroxysteroid dehydrogenase/Δ5-4 isomerase, and 5α-reductase, and has also been found to act as a competitive antagonist of the AR reportedly comparable to the potent antagonist enzalutamide. However, the initial 5α-reduced metabolite of D4A, 3-keto-5α-abiraterone, is an agonist of the AR, and promotes prostate cancer progression. Its formation can be blocked by the coadministration of dutasteride, a potent and selective 5α-reductase inhibitor.
| Product Name | tianeptine sulfate |
| CAS Number |
1224690-84-9
|
| Molecular Formula | C42H56Cl2N4O14S3 |
| Molecular Weight | 1008.01 |
| Purity | 99% |
There has been interest in the use of abiraterone acetate for the treatment of breast cancer due to its ability to lower estrogen levels. However, abiraterone has been found to act as a direct agonist of the estrogen receptor, and induces proliferation of human breast cancer cells in vitro. If abiraterone acetate is used in the treatment of breast cancer, it should be combined with an estrogen receptor antagonist like fulves trant. In spite of its antiandrogenic and estrogenic properties, abiraterone acetate does not appear to produce gynecomastia as a side effect.
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