Tìm theo
Goserelin
Các tên gọi khác (4 ) :
  • Goserelin
  • Goserelin acetate
  • ICI-118630
  • Zoladex
Thuốc chống ung thư và tác động vào hệ thống miễn dịch
Thuốc Gốc
Small Molecule
CAS: 65807-02-5
ATC: L02AE03
ĐG : AstraZeneca Inc. , http://www.astrazeneca.ca
CTHH: C59H84N18O14
PTK: 1269.4105
Goserelin is a synthetic hormone. In men, it stops the production of the hormone testosterone, which may stimulate the growth of cancer cells. In women, goserelin decreases the production of the hormone estradiol (which may stimulate the growth of cancer cells) to levels similar to a postmenopausal state. When the medication is stopped, hormone levels return to normal.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C59H84N18O14
Phân tử khối
1269.4105
Monoisotopic mass
1268.641439486
InChI
InChI=1S/C59H84N18O14/c1-31(2)22-40(49(82)68-39(12-8-20-64-57(60)61)56(89)77-21-9-13-46(77)55(88)75-76-58(62)90)69-54(87)45(29-91-59(3,4)5)74-50(83)41(23-32-14-16-35(79)17-15-32)70-53(86)44(28-78)73-51(84)42(24-33-26-65-37-11-7-6-10-36(33)37)71-52(85)43(25-34-27-63-30-66-34)72-48(81)38-18-19-47(80)67-38/h6-7,10-11,14-17,26-27,30-31,38-46,65,78-79H,8-9,12-13,18-25,28-29H2,1-5H3,(H,63,66)(H,67,80)(H,68,82)(H,69,87)(H,70,86)(H,71,85)(H,72,81)(H,73,84)(H,74,83)(H,75,88)(H4,60,61,64)(H3,62,76,90)/t38-,39-,40-,41-,42-,43-,44-,45+,46-/m0/s1
InChI Key
InChIKey=BLCLNMBMMGCOAS-URPVMXJPSA-N
IUPAC Name
(2S)-1-[(2S)-2-[(2S)-2-[(2R)-3-(tert-butoxy)-2-[(2S)-2-[(2S)-3-hydroxy-2-[(2S)-2-[(2S)-3-(1H-imidazol-5-yl)-2-{[(2S)-5-oxopyrrolidin-2-yl]formamido}propanamido]-3-(1H-indol-3-yl)propanamido]propanamido]-3-(4-hydroxyphenyl)propanamido]propanamido]-4-methylpentanamido]-5-[(diaminomethylidene)amino]pentanoyl]-N-(carbamoylamino)pyrrolidine-2-carboxamide
Traditional IUPAC Name
(2S)-1-[(2S)-2-[(2S)-2-[(2R)-3-(tert-butoxy)-2-[(2S)-2-[(2S)-3-hydroxy-2-[(2S)-2-[(2S)-3-(3H-imidazol-4-yl)-2-{[(2S)-5-oxopyrrolidin-2-yl]formamido}propanamido]-3-(1H-indol-3-yl)propanamido]propanamido]-3-(4-hydroxyphenyl)propanamido]propanamido]-4-methylpentanamido]-5-[(diaminomethylidene)amino]pentanoyl]-N-(carbamoylamino)pyrrolidine-2-carboxamide
SMILES
CC(C)C[[email protected]](NC(=O)[[email protected]@H](COC(C)(C)C)NC(=O)[[email protected]](CC1=CC=C(O)C=C1)NC(=O)[[email protected]](CO)NC(=O)[[email protected]](CC1=CNC2=CC=CC=C12)NC(=O)[[email protected]](CC1=CN=CN1)NC(=O)[[email protected]@H]1CCC(=O)N1)C(=O)N[[email protected]@H](CCCN=C(N)N)C(=O)N1CCC[[email protected]]1C(=O)NNC(N)=O
Độ hòa tan
Soluble
logP
-2
logS
-4.7
pKa (strongest acidic)
9.27
pKa (Strongest Basic)
10.82
PSA
495.89 Å2
Refractivity
325.84 m3·mol-1
Polarizability
131.22 Å3
Rotatable Bond Count
33
H Bond Acceptor Count
18
H Bond Donor Count
17
Physiological Charge
2
Number of Rings
6
Bioavailability
0
MDDR-Like Rule
true
Dược Lực Học : The pharmacokinetics of goserelin have been determined in both male and female healthy volunteers and patients. In these studies, goserelin was administered as a single 250µg (aqueous solution) dose and as a single or multiple 3.6 mg depot dose by subcutaneous route.
Cơ Chế Tác Dụng : Goserelin is a synthetic hormone. In men, it stops the production of the hormone testosterone, which may stimulate the growth of cancer cells. In women, goserelin decreases the production of the hormone estradiol (which may stimulate the growth of cancer cells) to levels similar to a postmenopausal state. When the medication is stopped, hormone levels return to normal. Goserelin is a synthetic decapeptide analogue of LHRH. Goserelin acts as a potent inhibitor of pituitary gonadotropin secretion when administered in the biodegradable formulation. The result is sustained suppression of LH and serum testosterone levels.
Dược Động Học :
▧ Absorption :
Inactive orally, rapidly absorbed following subcutaneous administration.
▧ Volume of Distribution :
* 44.1 ± 13.6 L [subcutaneous administration of 250 mcg]
▧ Protein binding :
27.3%
▧ Metabolism :
Hepatic
▧ Route of Elimination :
Clearance of goserelin following subcutaneous administration of a radiolabeled solution of goserelin was very rapid and occurred via a combination of hepatic and urinary excretion. More than 90% of a subcutaneous radiolabeled solution formulation dose of goserelin was excreted in urine.
▧ Half Life :
4-5 hours
▧ Clearance :
* 121 +/- 42.4 mL/min [prostate cancer with 10.8 mg depot]
Độc Tính : No experience of overdosage from clinical trials.
Chỉ Định : Used to treat hormone-sensitive cancers of the breast (in pre- and peri- menopausal women) and prostate, and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning). In addition, goserelin is used in assisted reproduction and in the treatment of precocious puberty.
Liều Lượng & Cách Dùng : Implant - Subcutaneous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Zoladex
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