[(T-BU)DSER6, (AZA)GLY10]-LUTEINIZING HORMONE-RELEASING HORMONE
Goserelin acetate
CAS: 145781-92-6
Molecular Formula: C59H84N18O14
[(T-BU)DSER6, (AZA)GLY10]-LUTEINIZING HORMONE-RELEASING HORMONE - Names and Identifiers
| Name | Goserelin acetate |
| Synonyms | Fertilan Goserelin HCl Goserelin acetate ICI-118630 acetate (D-SER(TBU)6,AZAGLY10)-LHRH [(T-BU)DSER6, (AZA)GLY10]-LH-RH (D-Ser(tBu)6,Azagly10)-LHRH acetate salt PYR-HIS-TRP-SER-TYR-D-SER(TBU)-LEU-ARG-PRO-AZAGLY-NH2 GLP-HIS-TRP-SER-TYR-D-SER(TBU)-LEU-ARG-PRO-AZA-GLY-NH2 [(T-BU)DSER6, (AZA)GLY10]-LUTEINIZING HORMONE-RELEASING HORMONE GOSERELIN HCL[PYR-HIS-TRP-SER-TYR-D-SER(T-BU)-LEU-ARG-PRO-AZAGLY-NH2] 1-9-Luteinizing hormone-releasing factor (swine), 6-(o-(1,1-dimethylethyl)-D-serine)-, 2-(aminocarbonyl)hydrazide, acetate (salt) |
| CAS | 145781-92-6 |
| EINECS | 652-995-1 |
| InChI | InChI=1/C59H84N18O14.C2H4O2/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;1-2(3)4/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);1H3,(H,3,4)/t38-,39-,40-,41-,42-,43-,44-,45+,46-;/m0./s1 |
| InChIKey | IKDXDQDKCZPQSZ-JHYYTBFNSA-N |
[(T-BU)DSER6, (AZA)GLY10]-LUTEINIZING HORMONE-RELEASING HORMONE - Physico-chemical Properties
| Molecular Formula | C59H84N18O14 |
| Molar Mass | 1269.41 |
| Melting Point | >190°C (dec.) |
| Boling Point | 1695.5°C at 760 mmHg |
| Flash Point | 979.2°C |
| Solubility | H2O: 20mg/mL, clear, colorless |
| Vapor Presure | 0mmHg at 25°C |
| Appearance | white powder |
| Color | White to Off-White |
| Storage Condition | -20°C |
| Stability | Hygroscopic |
| Physical and Chemical Properties | Solubility: H2O: 20 mg/mL, clear, colorless storage conditions:? 20℃ WGK Germany:3 |
[(T-BU)DSER6, (AZA)GLY10]-LUTEINIZING HORMONE-RELEASING HORMONE - Risk and Safety
| Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
| RTECS | OK6369800 |
| HS Code | 2937190000 |
[(T-BU)DSER6, (AZA)GLY10]-LUTEINIZING HORMONE-RELEASING HORMONE - Reference Information
| pharmacological action | goserelin acetate is a synthetic analog of LHRH, long-term use can inhibit the secretion of luteinizing hormone in the pituitary gland, which can cause the decrease of serum testosterone in men and serum estradiol in women. Male patients after the first medication after 21 days or so, testosterone concentration can be reduced to the level of castration, every 28 days in the course of treatment, the concentration of testosterone was maintained in the concentration range after castration. This testosterone suppression by goserelin acetate leads to regression of prostate tumors and improvement in most patients. In female patients, serum estradiol concentrations were suppressed approximately 21 days after initial administration and were maintained at postmenopausal levels every 28 days thereafter. This inhibition is associated with hormone-dependent breast cancer, endometriosis. |
| pharmacokinetics | goserelin acetate has almost complete bioavailability. The use of an injection of the implant every 4 weeks can maintain the effective blood concentration without tissue accumulation. Zoladex protein binding capacity is poor, in the case of normal renal function, plasma elimination half-life of 2-4 hours, the half-life of patients with renal insufficiency will be prolonged, however, for patients who use implants on a monthly basis, this effect is very small, so there is no need to change the dosage of these patients. There were no significant changes in pharmacokinetics in patients with hepatic insufficiency. |
| adverse reactions | goserelin acetate may have the following adverse reactions: ① endocrine and metabolic system: common facial Fever, flushing. Swelling of the breast was also seen. In addition, women visible decreased libido, vaginal dryness, menstrual disorders, men visible impotence. ② cardiovascular system: Foreign Reports of venous thrombosis in patients with metastatic prostate cancer after medication. ③ central nervous system: visible Head Pain, reports of epidural spinal cord compression after foreign useful drugs. The digestive system: visible Nausea, rare taste disorders, Diarrhea, Abdominal Pain, gingival atrophy. (5) genitourinary system: a small number of patients with early visible hematuria and urethral obstruction aggravated. Reports of lymphocyte infiltration in uterine leiomyoma occasionally abroad. The skin: visible rash, skin itching, injection site pain, individual may occur polychondritis. Bone: The initial stage of the drug treatment of prostate cancer can be aggravated, manifested as bone pain, sometimes visible lower limb weakness and paresthesia. |
| precautions | goserelin acetate should be used with caution: ① patients with renal injury caused by ureteral obstruction. ②Patients with spinal cord compression. ③ patients with a history of treatment and risk factors leading to decreased bone mineral density. (2) the commonly used injection site is the upper abdominal wall, but it can also be in the lower abdominal midline, and the local anesthetic can be used before injection. (3) the treatment of advanced prostate cancer in men can be started with Flutamide (Flutamide). (4) the implant formulation of goserelin 10.8mg is not suitable for women. (5) daily administration of 0.2 ~ Fever mg Clonidine can treat of facial adverse reactions. |
| peptides | AstraZeneca's Zoladex (goserelin acetate) it is a luteinizing hormone releasing hormone analog for injection. For the palliative treatment of advanced prostate cancer; And the treatment of premenopausal and perimenopausal advanced breast cancer, endometriosis and uterine fibroids. AstraZeneca's global sales of Zoladex reached US $1.1 billion in 2011. In the Chinese market, the former United Kingdom of Great Britain and Northern Ireland were imported and sold in 1999. AstraZeneca continued to be imported and sold by AstraZeneca after the merger of AstraZeneca and AstraZeneca. From 2007 to 30%, the use of goserelin acetate in sample hospitals of 16 key cities in China maintained a high growth rate. Although it slowed down slightly in, the growth rate remained above, in 0.19 billion, the drug use of goserelin acetate in sample hospitals of 16 key cities in China was RMB. |
| biological activity | Goserelin is a luteinizing hormone releasing hormone (LHRH) agonist used to inhibit the production of sex hormones. |
Last Update：2024-04-10 22:29:15
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View History
[(T-BU)DSER6, (AZA)GLY10]-LUTEINIZING HORMONE-RELEASING HORMONE
TERT-BUTYL 1-(5-AMINOPYRIDIN-2-YL)PIPERIDIN-4-YLCARBAMATE
对甲苯磺酰基异腈 (TOSMIC)
1-BUTYL-3-NITRO-1-NITROSOGUANIDINE
Butylsuccinic acid bis[2-(2-butoxyethoxy)ethyl] ester
(S)-1-[(2-氨基-1,1-二甲基乙基)氨基乙酰基]吡咯烷-2-甲氰盐酸盐
环己基2-氰基丙烯酸酯
三仲丁基硼氢化钾
(2-氟嘧啶-5-基)硼酸
T-BUTYLDIMETHYLSILYLIMIDAZOLE
TERT-BUTYL 1-(5-AMINOPYRIDIN-2-YL)PIPERIDIN-4-YLCARBAMATE
对甲苯磺酰基异腈 (TOSMIC)
1-BUTYL-3-NITRO-1-NITROSOGUANIDINE
Butylsuccinic acid bis[2-(2-butoxyethoxy)ethyl] ester
(S)-1-[(2-氨基-1,1-二甲基乙基)氨基乙酰基]吡咯烷-2-甲氰盐酸盐
环己基2-氰基丙烯酸酯
三仲丁基硼氢化钾
(2-氟嘧啶-5-基)硼酸
T-BUTYLDIMETHYLSILYLIMIDAZOLE