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[C@H](NC(=O)[C@@H](COC(C)(C)C)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CO)NC(=O)[C@H](CC1=CNC2=CC=CC=C12)NC(=O)[C@H](CC1=CN=CN1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]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

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

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

Biệt dược thương mại : Zoladex 3.6 mg implant syringe

Giá bán buôn : USD >451.19

Đơn vị tính : syringe
Biệt dược thương mại : Zoladex 10.8 mg implant syringe

Giá bán buôn : USD >1380.65

Đơn vị tính : syringe

Nhà Sản Xuất

Công ty : AstraZeneca

Sản phẩm biệt dược : Zoladex

Đóng gói

Công ty : AstraZeneca Inc.

Website : http://www.astrazeneca.ca

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB00014

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D00573

National Drug Code Directory

http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0310-0951-30

PharmGKB

http://www.pharmgkb.org/drug/PA164747674

Wikipedia

http://en.wikipedia.org/wiki/Goserelin

RxList

http://www.rxlist.com/cgi/generic/goserel.htm

Drugs.com

http://www.drugs.com/cdi/goserelin.html

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