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Related Concept Videos

Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
Selectins01:25

Selectins

Cell adhesion is  an essential aspect of multicellularity. While stable cell interactions usually occur between cells of the same type, transient cell interactions occur between cells of different tissue types, such as between neutrophils and endothelial cells. Selectins are one class of cell adhesion molecules (CAMs) that bind carbohydrate ligands to form transient cell adhesion. They are rod-like proteins with a long extracellular part of variable length ending with the lectin domain, which...
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Tissue-Drug Binding: Localization of Drugs and its Significance

Body tissues, comprising approximately 40% of the body weight, are crucial in drug distribution and localization. These tissues can serve as drug storage sites, competing with plasma binding sites for drug molecules.
Drugs can bind to different tissue components, enhancing their distribution and localization. The factors influencing drug localization in tissues include the drug's lipophilicity, structural characteristics, tissue perfusion rate, and pH differences. These factors determine the...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
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Dose-Response Relationship: Selectivity and Specificity01:25

Dose-Response Relationship: Selectivity and Specificity

Drugs exert their therapeutic effects by interacting with receptors, enzymes, or ion channels that are present throughout the human body. The strength and duration of the interaction between a drug and its target receptor are characterized by the selectivity and specificity of the drug. Selectivity refers to a drug's strong preference for its intended target over other targets. For instance, isoprenaline, a non-selective β-adrenergic agonist, interacts with both β1- and β2-adrenergic receptors...
Tissues01:18

Tissues

Cells with similar structure and function are grouped into tissues. A group of tissues with a specialized function is called an organ. There are four main types of tissue in vertebrates: epithelial, connective, muscle, and nervous.

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Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer
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Tissue-selective agents: selective estrogen receptor modulators and the tissue-selective estrogen complex.

James H Pickar1, Sebastián Mirkin

  • 1Obstetrics and Gynecology, Columbia University Medical Center, New York, NY, USA. jhpickar@me.com

Menopause International
|October 20, 2010
PubMed
Summary

Tissue-selective estrogen complexes (TSECs) combining bazedoxifene (BZA) and conjugated estrogens (CEs) effectively treat menopausal symptoms and prevent bone loss. This new treatment paradigm offers benefits with improved tolerability for postmenopausal women.

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Area of Science:

  • Reproductive Endocrinology
  • Pharmacology
  • Bone Biology

Background:

  • Menopause is linked to vasomotor symptoms, vaginal atrophy, and osteoporosis.
  • Selective estrogen receptor modulators (SERMs) aim to alleviate symptoms and prevent bone loss without adverse effects.
  • No SERM has fully achieved these therapeutic goals to date.

Purpose of the Study:

  • To evaluate the safety and efficacy of a tissue-selective estrogen complex (TSEC) combining bazedoxifene (BZA) and conjugated estrogens (CEs).
  • To assess the TSEC's potential in treating menopausal symptoms and preventing osteoporosis in postmenopausal women.
  • To determine if BZA/CE provides endometrial protection against estrogenic stimulation.

Main Methods:

  • The Selective estrogen Menopause And Response to Therapy (SMART) trials were multicenter, randomized, double-blind, placebo- and active-controlled phase 3 studies.
  • Healthy postmenopausal women were treated with varying doses of BZA/CE.
  • Safety and efficacy endpoints included symptom relief, bone mass maintenance, and endometrial effects.

Main Results:

  • BZA/CE demonstrated endometrial protection, relieved hot flushes, and maintained bone mass in over 3400 women.
  • Adverse event rates were similar to placebo, including amenorrhea and breast pain.
  • BZA 20 mg was the lowest effective dose for endometrial protection and bone mass maintenance when combined with CE 0.625 mg or 0.45 mg.

Conclusions:

  • The TSEC containing BZA/CE represents a novel therapeutic approach for managing menopausal symptoms.
  • This combination therapy is effective in preventing osteoporosis and protecting the endometrium.
  • BZA/CE offers a promising new paradigm for postmenopausal hormone therapy with improved tolerability.