Tìm theo
Exemestane
Các tên gọi khác (4 ) :
  • 6-Methyleneandrosta-1,4-diene-3,17-dione
  • Exemestane
  • Exemestano
  • Exemestanum
Thuốc chống ung thư và tác động vào hệ thống miễn dịch
Thuốc Gốc
Small Molecule
CAS: 107868-30-4
ATC: L02BG06
ĐG : Pfizer Inc. , http://www.pfizer.com
CTHH: C20H24O2
PTK: 296.4034
Exemestane is an oral steroidal aromatase inhibitor used in the adjuvant treatment of hormonally-responsive (also called hormone-receptor-positive, estrogen-responsive) breast cancer in postmenopausal women. 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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
296.4034
Monoisotopic mass
296.177630012
InChI
InChI=1S/C20H24O2/c1-12-10-14-15-4-5-18(22)20(15,3)9-7-16(14)19(2)8-6-13(21)11-17(12)19/h6,8,11,14-16H,1,4-5,7,9-10H2,2-3H3/t14-,15-,16-,19+,20-/m0/s1
InChI Key
InChIKey=BFYIZQONLCFLEV-DAELLWKTSA-N
IUPAC Name
(1S,2R,10R,11S,15S)-2,15-dimethyl-8-methylidenetetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-diene-5,14-dione
Traditional IUPAC Name
exemestane
SMILES
[H][[email protected]@]12CCC(=O)[[email protected]@]1(C)CC[[email protected]@]1([H])[[email protected]@]2([H])CC(=C)C2=CC(=O)C=C[[email protected]]12C
Độ tan chảy
155.13 °C
Độ hòa tan
Non-soluble
logP
3.7
logS
-4.6
pKa (strongest acidic)
19.96
pKa (Strongest Basic)
-5
PSA
34.14 Å2
Refractivity
89.03 m3·mol-1
Polarizability
33.71 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Aromatase is an enzyme that converts hormones to estrogen in the body's adrenal glands. The aromatase inhibitors (AIs) are drugs that reduce estrogen levels by blocking the action of aromatase in the adrenal glands. The selective AIs (SAIs) selectively reduce levels of estrogen without interfering with levels of other steroid hormones that are produced by the adrenal gland. Drugs in this class include anastrozole (Arimidex ™), letrozole (Femara ™) and exemestane (Aromasin ™).
Cơ Chế Tác Dụng : Exemestane is an oral steroidal aromatase inhibitor used in the adjuvant treatment of hormonally-responsive (also called hormone-receptor-positive, estrogen-responsive) breast cancer in postmenopausal women. 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. Breast cancer cell growth may be estrogen-dependent. Aromatase (exemestane) is the principal enzyme that converts androgens to estrogens both in pre- and postmenopausal women. While the main source of estrogen (primarily estradiol) is the ovary in premenopausal women, the principal source of circulating estrogens in postmenopausal women is from conversion of adrenal and ovarian androgens (androstenedione and testosterone) to estrogens (estrone and estradiol) by the aromatase enzyme in peripheral tissues. Estrogen deprivation through aromatase inhibition is an effective and selective treatment for some postmenopausal patients with hormone-dependent breast cancer. 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". Exemestane significantly lowers circulating estrogen concentrations in postmenopausal women, but has no detectable effect on the adrenal biosynthesis of corticosteroids or aldosterone. This reduction in serum and tumor concentrations of estrogen delays tumor growth and disease progression. Exemestane has no effect on other enzymes involved in the steroidogenic pathway up to a concentration at least 600 times higher than that inhibiting the aromatase enzyme.
Dược Động Học :
▧ Absorption :
42%
▧ Protein binding :
90% (mainly α1-acid glycoprotein and albumin)
▧ Metabolism :
Hepatic
▧ Half Life :
24 hours
Độc Tính : Convulsions
Chỉ Định : For the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy.
Tương Tác Thuốc :
  • Etravirine Exemestane, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to increase the dosage of exemestane and to closely monitor therapy for efficacy and toxicity.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Aromasin 25 mg tablet
    Giá bán buôn : USD >13.77
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Aromasin
  • Công ty :
    Sản phẩm biệt dược : Exemestance
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