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【求助】一药物状况
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| 请教一药物Panomifene的情况，是否已经上市了？？？？ |
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nkbeholder
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clkk216(金币+1,VIP+0):谢谢诶参与虫友讨论~！ 5-6 10:23
clkk216(金币+1,VIP+0):谢谢诶参与虫友讨论~！ 5-6 10:23
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我也不知道是什么情况。你自己看看？ Drug: Panomifene Synonyms: EGIS 5650; GYKl 13504 Chemical Name: Ethanol, 2-((2-(4((3,3,3-trifluoro- 1,2-diphenyl-1-propenyl) phenoxy)ethyl)amino-, (E)- Molecular Formula: C25H24F3NO2 CAS® Registry Number: 77599-17-8 Related CAS Registry Number: 77600-10-3 Therapeutic Class: Anti-estrogens Cytostatic anti-oestrogens Mechanism of Action: Estrogen receptor antagonists Originator Company: IVAX Drug Research Institute (Hungary) Parent Company: IVAX Corporation Licensee: Fujimoto Pharmaceutical Other Company: Egis Pharmaceuticals Highest Phase: No Development Reported Development Status: No Development Reported, Hungary, Breast cancer Introduction: Panomifene (EGIS 5650, GYK1 13504) is the most active antiestrogen of a series of triphenylethylene derivatives. It was synthesised by the Institute for Drug Research, Budapest, Hungary, and was in phase II trials with Egis for the treatment of breast cancer. Panomifene is licensed to Fujimoto Pharmaceutical in Japan. In October 1999, the Institute for Drug Research was purchased by IVAX Corporation. In 2001, the Institute for Drug Research was renamed as the IVAX Drug Research Institute. No recent development of panomifene has been reported. Adis Evaluation: Breast cancer 72 (PO). Pharmacology Overview: Pharmacodynamics: Longer lasting antiestrogen effect than tamoxifen Mechanism of action: Estrogen receptor antagonists ------------------------------- tmax (h) (oral) 3.55 (Adult) t (1/2) beta (h) 69.6 (Adult) ------------------------------- Clinical Overview: Route(s) of Administration: PO Administration Freq.(per day): od Adverse events: most frequent: Flushing. occasional: Abdominal pain, Dizziness, Drowsiness, Headache, Heat sensation, Hyperhidrosis, Skin eruptions. Drug Interactions: Unknown. Adverse Events: 13 healthy postmenopausal women received oral panomifene 3-120mg. Lower abdominal pain occurred in 1 patient after panomifene 120mg and in 2 after panomifene 24mg. Hot flushes of uncertain relationship to the study drug occurred in 3 patients. Other occasional adverse events, which were not dose-dependent, were dizziness, drowsiness, headache, rashes, heat sensation and sweating/1/. In 10 healthy postmenopausal volunteers, daily oral doses of panomifene 3-120 mg/day were well tolerated in 9/10 volunteers at the highest dose level of 120 mg/day. One volunteer experienced abdominal pain after the 120mg dose which became more severe when the dose was repeated. Hot flushes occurred in 3 volunteers, and 1 case of spot bleeding was observed. Other adverse events seen occasionally were drowsiness, rashes and headache; these were not dose-dependent/2/. Pharmacokinetics: The pharmacokinetics of oral panomifene 24mg were investigated in 13 healthy postmenopausal women. The t sub(1/2) was 69.6h, C sub(max) was 67.7 ng/ml, t sub(max) was 3.55h and AUC was 4814 ng x h x ml sup(-1). There was considerable interpatient variability in the pharmacokinetics of panomifene at all dose levels. There was a medium correlation between dose and AUC (r = 0.876). The data could be fitted to a 1-compartment model in 6 patients and a 2-compartment model in 4 patients. No biotransformation products of panomifene were detected. The plasma C sub(max) concentrations (25.2-290.4 ng/ml) were dose- dependent and were within the range which caused a 50% proliferation inhibition on MCF-7 cells in an in vitro study/1/. Pharmacodynamics (Cancer): Preclinical studies: the duration and dose-dependence of the antiestrogenic effects of panomifene and tamoxifen in an immature rat uterus stimulated by estrogen were recently reported. Rats received either a single oral dose of panomifene 0.3-10 mg/kg or tamoxifen. 24h after treatment there was no difference in uterine weight or RNA, DNA and protein content. The estrogen-mediated rise in nucleic acid incorporation was inhibited by panomifene at 72-96h, and at 144h panomifene still showed significant antiestrogenic activity. At 96h the antiestrogenic effect of tamoxifen could not be observed. Both compounds had similar antiuterotrophic activity/3/. Drug Update Information: 26-Oct-1999: IVAX Corporation has acquired the Institute for Drug Research 26-Sep-1997: A clinical study has been added to the pharmacokinetics and adverse events sections (612835) 27-May-1997: Phase-II clinical trials for Breast cancer in Hungary (PO) 05-May-1995: A preclinical study has been added to the pharmacodynamics section (308623) 22-Sep-1994: New profile References: 1. Erdelyi-Toth V, Gyergyay F, et al. Pharmacokinetics of panomifene in healthy volunteers at phase 1/a study. Anti-Cancer Drugs. 8: 603-609, Jul 1997. (English). 800612835 2. Gyergyay F, Erdelyi-Toth V, et al. Phase I/a study on panomifene in healthy volunteers. Annals of Oncology. 3 (Suppl. 5): 54, Nov 1992. (English). 3. Hermann I, Borvendeg J. Comparative studies on antiestrogenic effects of a new triphenylethylene derivative, panomifene and tamoxifen. European Journal of Endocrinology. 130 (Suppl. 2): 165, Jun 1994. (English). Revision Date: August 9, 2002 Adis R&D Insight © 2009 Adis International Limited. All rights reserved. Dialog® File Number 107 Accession Number 002127 |
2楼2009-05-06 09:46:13
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karl2100(金币+1,VIP+0):3Q 5-6 22:08
karl2100(金币+1,VIP+0):3Q 5-6 22:08
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DR panomifene SUMMARY OVERVIEW DRUG NAME BREAKING NEWS LICENSING SUMMARY No data for any portlets within this tab SUMMARY Drug name panomifene Company EGIS Gyogyszergyar RT (Servier) Highest dev status Discontinued Therapy areas Cancer Actions Anticancer; Estrogen receptor antagonist Target Estrogen receptor Update date 05-MAR-2002 Reason for update indexing updated Top OVERVIEW Egis has discontinued development of panomifene, an estrogen antagonist which had reached phase I clinical trials as a potential treatment for cancer [231757]. Top DRUG NAME Names associated with this drug Name Type panomifene USAN, INN 77599-17-8 CAS RN EGIS-5650 Research Code panomifine Top BREAKING NEWS No news items found. Disclaimer | Terms of Use | Privacy Policy | Copyright © 2009 THOMSON REUTERS [ Last edited by acdmail1 on 2009-5-6 at 13:04 ] |
3楼2009-05-06 13:02:13
4楼2009-06-20 01:35:35