Nandrolone decanoate is hydrolyzed to [nandrolone], possibly by PDE7B. Nandrolone is further metabolized to the urinary metabolites 19-norandrosterone, 19-noretiocholanolone, and 19-norepiandrosterone. 19-norandrosterone is 3-O-glucuronidated by UGT2B7, UGT 1A4, UGT2B4, UGT1A3, and UGT1A1. 19-noretiocholanolone is 3-O-glucuronidated by UGT2B7, UGT2B4, UGT1A4, UGT1A10, UGT1A3, and UGT1A1.
参考文献：M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. 美国食品药品监督管理局批准的药物标签用于研究药物诱导的肝损伤，《药物发现今日》，16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007
M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank：按人类发展药物诱导肝损伤风险排名的最大参考药物清单。《药物发现今日》2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015
References:M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. FDA-Approved Drug Labeling for the Study of Drug-Induced Liver Injury, Drug Discovery Today, 16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007
M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. Drug Discov Today 2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015
A 50 mg intramuscular dose of nandrolone decanoate reaches a mean Cmax 2.14 ng/mL, with a mean Tmax of 30 hours, and a mean AUC of 400 h\*ng/mL. A 100 mg intramuscular dose of nandrolone decanoate reaches a mean Cmax 4.26 ng/mL, with a mean Tmax of 30 hours, and a mean AUC of 862 h\*ng/mL. A 150 mg intramuscular dose of nandrolone decanoate reaches a mean Cmax 5.16 ng/mL, with a mean Tmax of 72 hours, and a mean AUC of 1261 h\*ng/mL.
Nandrolone decanoate is eliminated as urinary metabolites, however data regarding elimination in the feces are not readily available. Data in cattle shows that [nandrolone] is 30% eliminated in the feces.
诺龙 、 正癸酸 、 N,N'-二环己基碳二亚胺 、 溶剂黄146 在
4-二甲氨基吡啶 、 对甲苯磺酸 作用下，
以
二氯甲烷 、 水合甲醇 为溶剂，
反应 5.0h，
以The same work-up procedure as in Example 6 gives 7.6 g of pure 19-nortestosterone decanoate (88% yield) as white crystals from methanol/water的产率得到癸酸诺龙
[EN] ASH1L INHIBITORS AND METHODS OF TREATMENT THEREWITH<br/>[FR] INHIBITEURS DE ASH1L ET MÉTHODES DE TRAITEMENT AU MOYEN DE CEUX-CI
申请人：UNIV MICHIGAN REGENTS
公开号：WO2017197240A1
公开（公告）日：2017-11-16
Provided herein are small molecule inhibitors of ASH1L activity and small molecules that facilitate ASH1L degradation and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.
[EN] PEPTIDE-BASED MULTIPLE-DRUG DELIVERY VEHICLE<br/>[FR] VÉHICULE D'ADMINISTRATION DE MÉDICAMENTS MULTIPLES À BASE DE PEPTIDES
申请人：ARIEL-UNIVERSITY RES AND DEV COMPANY LTD
公开号：WO2017068577A1
公开（公告）日：2017-04-27
A molecular structure comprising a targeting moiety, a multi-functional peptide platform and a plurality of controllably released bioactive agents attached thereto is provided herein.
本文提供了一种包括靶向基团、多功能肽平台和附着在其上的多种可控释放的生物活性剂的分子结构。
ANDROGEN MODULATORS
申请人：Boys Mark Laurence
公开号：US20090170886A1
公开（公告）日：2009-07-02
The present invention is directed to a new class of benzonitriles and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth.
Provided herein is a drug delivery (DD) system for ratiometric luminescence determination of drug release degree in drug delivery monitoring, which includes a drug, a switchable reporter and non-switchable reporter providing two distinguishable signals for detection; or a single switchable reporter providing two distinguishable signals for detection, and a cleavable linker connecting a drug to a switchable reporter, as well as a method for ratiometric luminescence determination of drug release in a target in vivo or in vitro), which is effected by administering the DD system provided herein that is capable of releasing a drug from the DD system, measuring two luminescent signals provided by the switchable reporter and the non-switchable reporter, or the single switchable reporter, determining the ratio between these two luminescence signals, and determining the drug release degree through the ratio between the two luminescence signals.
[EN] SUBSTITUTED TRICYCLIC COMPOUNDS AND METHODS OF USE THEREOF<br/>[FR] COMPOSÉS TRICYCLIQUES SUBSTITUÉS ET LEURS PROCÉDÉS D'UTILISATION
申请人：BAYER HEALTHCARE AG
公开号：WO2009033581A1
公开（公告）日：2009-03-19
This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly cancer.
