Megestrol
(Synonyms: 甲地孕酮) 目录号 : GC38660
Megestrol, a synthetic progestin, is approved for the treatment of anorexia, cachexia, or an unexplained significant weight loss in patients with an acquired immunodeficiency syndrome diagnosis. Megestrol acetate (Megace) is one of the first progestational agents to be evaluated for use in the hormonal therapy of advanced breast cancer.
Cas No.:3562-63-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Megestrol, a synthetic progestin, is approved for the treatment of anorexia, cachexia, or an unexplained significant weight loss in patients with an acquired immunodeficiency syndrome diagnosis. Megestrol acetate (Megace) is one of the first progestational agents to be evaluated for use in the hormonal therapy of advanced breast cancer.
[1] Jose M Garcia, Tatyana A Shamliyan. Am J Med. 2018 Jun;131(6):623-629.e1. [2] S M Sedlacek. Semin Oncol. 1988 Apr;15(2 Suppl 1):3-13.
| Cas No. | 3562-63-8 | SDF | |
| 别名 | 甲地孕酮 | ||
| Canonical SMILES | CC([C@@]1(O)CC[C@@]2([H])[C@]3([H])C=C(C)C4=CC(CC[C@]4(C)[C@@]3([H])CC[C@]12C)=O)=O | ||
| 分子式 | C22H30O3 | 分子量 | 342.47 |
| 溶解度 | DMSO: 70 mg/mL (204.40 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.92 mL | 14.5998 mL | 29.1996 mL |
| 5 mM | 0.584 mL | 2.92 mL | 5.8399 mL |
| 10 mM | 0.292 mL | 1.46 mL | 2.92 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Efficacy and Safety of Megestrol in the Hospitalized Older Person
Sr Care Pharm 2022 Jul 1;37(7):284-292.PMID:35752918DOI:10.4140/TCP.n.2022.284.
Objectives To evaluate the efficacy and safety of Megestrol for off-label use in older patients with weight loss. Design Retrospective, nonblinded cohort study. Setting Upstate University Hospital is a 420-bed facility and academic medical center with a level 1 trauma center. Upstate Community Hospital is a 314-bed acute care/hospital/ambulatory care center and long-term care hospital that also provides teaching services. Participants Patients 65 years of age and older without malignancy or acquired immunodeficiency syndrome who were initiated and continued Megestrol therapy at the Upstate University hospitals for at least two weeks were included. Of the 1,290 patients initially screened, 16 patients on Megestrol were evaluated. An age- and gender-matched control group of 16 patients was utilized for comparison of changes in weight and other variables. Interventions Patients in the Megestrol group have received daily doses of Megestrol between 160 mg to 800 mg for an average duration of 19 days. Patients in the control group had no history or current use of Megestrol utilization. Main Outcome Measurements The primary outcome was an increase in weight. Secondary outcome measures included albumin and thromboembolic events. Changes in weight and albumin were also compared with the control group. Results At a mean duration of 19 days, there was no significant difference in weight gain (0.95 kg, OR = 1.33 [95% CI -1.615-3.527]). Albumin decreased by (0.4 g/dL OR = 0.916 [95% CI 0.12-0.78]) and none of the patients developed a thromboembolic event. Conclusion In older hospitalized patients, Megestrol did not increase weight, and did not improve albumin. No thromboembolic events were observed, but this may be because of a limited duration of observation of therapy and the routine use of anticoagulation prophylaxis in the inpatient setting.
Megestrol acetate in cachexia and anorexia
Int J Nanomedicine 2006;1(4):411-6.PMID:17722275DOI:10.2147/nano.2006.1.4.411.
The aim is to review major clinical trials that have used Megestrol acetate (MA) in the treatment of cachexia across several disease states. A review of general usage and potential side-effects are discussed. A theory that the newly approved nanocrystal formation of MA can better deliver this potent medication for treatment will also be reviewed.
Megestrol acetate in the treatment of metastatic carcinoma of the prostate
Oncology 1992;49 Suppl 2:22-7.PMID:1461622DOI:10.1159/000227123.
Although current hormonal therapy of prostate cancer may not appear to have altered survival appreciably, there have been considerable changes that may significantly affect the future management of this disease. A number of new hormonal agents have been introduced that still require definition of their therapeutic efficacy. Megestrol acetate, a hormonal agent with multiple sites of action in androgen metabolism, has recently been investigated in the treatment of patients with metastatic and locally advanced disease, and in those patients whose disease progresses with other hormonal therapies. Megestrol acetate plus mini-dose diethylstilbestrol (DES) is associated with fewer side effects than standard-dose DES and has equivalent therapeutic efficacy in the treatment of patients with metastatic disease. In patients with locally advanced disease that may benefit from hormonal cytoreduction, Megestrol acetate is effective and well tolerated. Megestrol acetate has a role in the palliation of patients with progressive disease despite initial hormonal therapy. Considerable controversy surrounds the therapy of carcinoma of the prostate; further studies are required to define optimal hormonal therapy.
[Megestrol acetate: a systematic review usefulness about the weight gain in neoplastic patients with cachexia]
Med Clin (Barc) 2002 Jul 6;119(5):166-70.PMID:12200017DOI:10.1016/s0025-7753(02)73352-6.
Background: The clinical efficacy of Megestrol acetate in the treatment of cachexia in cancer patients has not been clearly demonstrated. A systematic review and meta-analysis have been performed to ascertain its effectiveness on weight gain in patients with cancer-associated cachexia. Material and method: A systematic review of randomized clinical trials comparing Megestrol acetate with placebo in cancer patients was performed. The outcome measure used was weight gain expressed as the difference in weight at the outset compared with that at the end of treatment. Trials analyzed were those that allowed for this calculation, or those whose authors provided information for the above calculation. Results: Patients treated with placebo had an average weight loss of 1.090 kg (CI 95%, 1.620 to 0.561), whereas patients treated with Megestrol acetate gained an average 0.423 kg (CI 95%, 0.078-0.769). A weight gain of 0.448 kg (CI 95%, 0.021-0.874) was observed with acetate Megestrol doses # 240 mg. No statistically significant effect was observed when using higher doses: 0.358 kg (CI 95%, 0.135-0.85). Conclusions: Megestrol acetate doses equal to or lower than 240 mg/day lead to slight weight gain in patients with cancer-associated cachexia. The majority of studies have a low methodological quality. Further, well-designed studies comparing Megestrol acetate with placebo are warranted.
Megestrol-induced Cushing syndrome
Ann Pharmacother 2001 Oct;35(10):1208-10.PMID:11675847DOI:10.1345/aph.10197.
Objective: To report a case of Cushing syndrome associated with Megestrol acetate therapy in a patient with renal insufficiency. Summary: A 17-year-old boy with renal insufficiency due to unilateral renal agenesis developed Cushing syndrome and worsening of his renal function after Megestrol acetate therapy. The diagnosis was based on clinical and analytical evaluation. Discussion: Megestrol acetate is indicated for the treatment of cachexia associated with AIDS and malignancy. Due to its glucocorticoid activity, Megestrol use has resulted in the occurrence of Cushing syndrome in both patient groups. We report the case of a young patient with renal insufficiency due to unilateral renal agenesis who developed Cushing syndrome two months after administration of high-dose (900-mg/d) Megestrol acetate for an eating disorder. Conclusions: The risk of megestrol-induced Cushing syndrome, especially with high doses of the medication, should be considered as a possible adverse effect in patents with renal insufficiency.