114828-90-9Relevant articles and documents
TOPICAL COMPOSITIONS AND METHODS FOR TREATMENT
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Page/Page column 87-89, (2019/04/09)
The present disclosure provides novel topical compositions comprising endoxifen and salts and solvates thereof and methods for making the compositions. Certain compounds have been combined to make a stable topical compositions comprising endoxifen. The pr
Endoxifen is a new potent inhibitor of PKC: A potential therapeutic agent for bipolar disorder
Ali, Shoukath M.,Ahmad, Ateeq,Shahabuddin, Syed,Ahmad, Moghis U.,Sheikh, Saifuddin,Ahmad, Imran
body text, p. 2665 - 2667 (2010/07/05)
Protein kinase C (PKC) plays a major role in regulation of both pre and postsynaptic neurotransmission. Excessive activation of PKC results in symptoms related to bipolar disorder. Tamoxifen, a widely used breast cancer drug is known to inhibit PKC and demonstrate antimanic properties in human. We describe herein the synthesis of endoxifen, a tamoxifen active metabolite and compared its PKC inhibitory activity with that of tamoxifen. Endoxifen exhibited fourfold higher potency compared to tamoxifen.
TARGETED DRUG-FORMALDEHYDE CONJUGATES AND METHODS OF MAKING AND USING THE SAME
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Page/Page column 85, (2008/06/13)
The invention provides a prodrug platform technology for improving the therapeutic value of a variety of parent drug compounds by altering and improving drug characteristics such as aqueous solubility, hydrolytic stability, therapeutic index, toxicity profile, pharmacokinetics and selectivity while allowing the potential for synthetic elaboration. The prodrug platform is particularly well suited for targeting therapeutic drugs, including anti-tumor drugs and antibiotics, to specific receptors on target cells (e.g., cancer cells and bacteria). The platform is a technology for providing an improved, preactivated form of a therapeutic drug, and for optionally targeting such drug to target cells or biological molecules. The invention is broadly applicable to many different therapeutic drugs, as well as to a variety of diseases and conditions, including a variety of forms of cancer and bacterial infections.