Tìm theo
Testolactone
Các tên gọi khác (11 ) :
  • (4AS,4br,10ar,10bs,12as)-10a,12a-dimethyl-3,4,4a,5,6,10a,10b,11,12,12a-decahydro-2H-naphtho[2,1-F]chromene-2,8(4bh)-dione
  • 1-Dehydrotestololactone
  • 1,2-Didehydrotestololactone
  • 13-Hydroxy-3-oxo-13,17-secoandrosta-1,4-dien-17-oic acid delta-lactone
  • D-Homo-17a-oxaandrosta-1,4-diene-3,17-dione
  • delta(1)-Testololactone
  • Teslac
  • Testolactona
  • Testolactone
  • Testolactonum
  • Testolattone
Thuốc điều trị ung thư
Thuốc Gốc
Small Molecule
CAS: 968-93-4
ĐG : B&B Pharmaceuticals , http://www.bandbpharmaceuticals.com
CTHH: C19H24O3
PTK: 300.3921
An antineoplastic agent that is a derivative of progesterone and used to treat advanced breast cancer. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H24O3
Phân tử khối
300.3921
Monoisotopic mass
300.172544634
InChI
InChI=1S/C19H24O3/c1-18-9-7-13(20)11-12(18)3-4-14-15(18)8-10-19(2)16(14)5-6-17(21)22-19/h7,9,11,14-16H,3-6,8,10H2,1-2H3/t14-,15+,16+,18+,19+/m1/s1
InChI Key
InChIKey=BPEWUONYVDABNZ-DZBHQSCQSA-N
IUPAC Name
(1R,2S,7S,10S,11R)-7,11-dimethyl-6-oxatetracyclo[8.8.0.0^{2,7}.0^{11,16}]octadeca-12,15-diene-5,14-dione
Traditional IUPAC Name
testolactone
SMILES
[H][C@@]12CCC3=CC(=O)C=C[C@]3(C)[C@@]1([H])CC[C@]1(C)OC(=O)CC[C@@]21[H]
Độ tan chảy
218.5 °C
Độ hòa tan
Slightly soluble (27.4 mg/L)
logP
3.7
logS
-4.1
pKa (strongest acidic)
18.84
pKa (Strongest Basic)
-5
PSA
43.37 Å2
Refractivity
85.79 m3·mol-1
Polarizability
33.42 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 : Testolactone is a synthetic anti-neoplastic agent that is structurally distinct from the androgen steroid nucleus in possessing a six-membered lactone ring in place of the usual five-membered carbocyclic D-ring. Despite some similarity to testosterone, testolactone has no in vivo androgenic effect. No other hormonal effects have been reported in clinical studies in patients receiving testolactone.
Cơ Chế Tác Dụng : An antineoplastic agent that is a derivative of progesterone and used to treat advanced breast cancer. [PubChem] Although the precise mechanism by which testolactone produces its clinical antineoplastic effects has not been established, its principal action is reported to be inhibition of steroid aromatase activity and consequent reduction in estrone synthesis from adrenal androstenedione, the major source of estrogen in postmenopausal women. Based on in vitro studies, the aromatase inhibition may be noncompetitive and irreversible. This phenomenon may account for the persistence of testolactone's effect on estrogen synthesis after drug withdrawal.
Dược Động Học :
▧ Absorption :
Testolactone is well absorbed from the gastrointestinal tract.
▧ Protein binding :
~85%
▧ Metabolism :
Hepatic. Metabolized to several derivatives in the liver, all of which preserve the lactone D-ring.
▧ Route of Elimination :
No clinical effects in humans of testolactone on adrenal function have been reported; however, one study noted an increase in urinary excretion of 17-ketosteroids in most of the patients treated with 150 mg/day orally. It is metabolized to several derivatives in the liver, all of which preserve the lactone D-ring. These metabolites, as well as some unmetabolized drug, are excreted in the urine.
Độc Tính : Oral LD50s in mouse and dog are 1630 mg/kg and 593-926 mg/kg, respectively.
Chỉ Định : For palliative treatment of advanced breast cancer in postmenopausal women.
Tương Tác Thuốc :
  • Acenocoumarol The androgen, Testolactone, may incrase the anticoagulant effect of the Vitamin K antagonist, Acenocoumarol. Monitor for changes in the therapeutic effect of Acenocoumarol if Testolactone is initiated, discontinued or dose changed.
  • Cyclosporine The androgen, Testolactone, may increase the hepatotoxicity of Cyclosporine. Testolatone may also elevate serum concentrations of Cyclosporine. Consider alternate therapy or monitor for signs of renal and hepatic toxicity.
  • Warfarin Testolactone may increase the serum concentration and anticoagulant effect of warfarin. Monitor for changes in prothrombin time and therapeutic effects of warfarin if testolactone is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00894
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=13769
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508076
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C02197
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00153
ChemSpider
http://www.chemspider.com/Chemical-Structure.13172.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0003-0690-50
PharmGKB
http://www.pharmgkb.org/drug/PA164743056
RxList
http://www.rxlist.com/cgi/generic2/testolactone.htm
Drugs.com
http://www.drugs.com/cdi/testolactone.html
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