A letrozole-based dual aromatase–sulphatase inhibitor with in vivo activity
Paul M. WoodL. W. Lawrence WooAnna HumphreysSurinder K. ChanderAtul PurohitMichael ReedBarry V. L. Potter
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Letrozole
Aromatase inhibitor
Letrozole
Exemestane
Anastrozole
Aromatase inhibitor
Antiestrogen
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Letrozole is a novel potent nonsteroidal aromatase inhibitor,which has been shown to be useful as first-line therapy in postmenopausal women with advanced breast cancer(ABC).It was well tolerated and produced potent,selective and long-lasting inhibition of aromatase.Letrozole is an effective and safe agent for treatment of ABC.The advances in the research of the synthesis and clinical studies of Letrozole were reviewed in this paper.
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Aromatase inhibitor
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Recent investigations of novel aromatase inhibitors have addressed several important questions related to the biochemical effects of this class of drugs. While aromatase inhibitors such as aminoglutethimide, formestane (given by the oral and i.m. route), rogletimide and fadrozole administered at different doses have been found to inhibit in vivo aromatization by 60–93%, the novel aromatase inhibitors, letrozole and anastrozole, are shown to inhibit in vivo aromatization by about 98%. Contrary to previous studies on aromatase inhibitors reporting plasma oestrogens sustained at 30–50% of their control levels letrozole and anastrozole suppress plasma oestrone sulphate by approximately 95%. Future studies should explore cross-resistance of aromatase inhibitors and steroidal antioestrogens and between different types of aromatase inhibitors. A major goal is to evaluate alterations in tissue oestrogen concentration as well as growth factor expression in response to oestrogen deprivation with aromatase inhibitors.
Letrozole
Aminoglutethimide
Anastrozole
Aromatase inhibitor
Aromatization
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Letrozole
Aromatase inhibitor
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Letrozole
Aromatase inhibitor
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Aromatase inhibitor provides the best suitable approach at present for the treatment of many estrogen dependent diseases. The estrogen dependent diseases like breast cancer and endometriosis can be treated more effectively with new third generation aromatase inhibitors. As in case of breast cancer after mastectomy (removal of breast) regression of advance breast cancer is observed and in case of endometriosis even after total hysterectomy (removal of uterus and ovary) the reoccurrence of endometriosis is observed. So estrogen deprivation remains a main key as a therapeutic approach to cure estrogen dependent diseases. The third generation aromatase inhibitors are available in the preparations like Letrozole, Anastrazole, Vorazole and some more preparations are available. Among these preparations of aromatase inhibitor Letrozole is consider to be a better therapeutic agent. As it is found that patient using Letrozole as an aromatase inhibitor are having lower plasma estrogen level as compared to another third generation aromatase inhibitor and more over calcium reabsorption in bone is also seen with Letrozole. In this study we have designed some new aromatase inhibitor and reported them as potentially new aromatase inhibitor by comparing their pharmagological properties with Letrozole and some synthesized derivatives of Letrozole (Downloaded from Zinc data base with 90% structural similarity) (http://zinc.docking.org/search/structure) by using molecular docking analysis and various free internet based Insilco tools.
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Aromatase inhibitor
Anastrozole
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Drug Development
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Aromatase inhibitor
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Aromatase inhibitor
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Supplementary Figure 1 from Sensitivity to the Aromatase Inhibitor Letrozole Is Prolonged After a “Break” in Treatment
Letrozole
Aromatase inhibitor
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