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Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Lasofoxifene is a nonsteroidal SERM developed by Pfizer for the prevention and treatment of osteoporosis and for the treatment of vaginal atrophy. There is also evidence based on meta-analyses that it can reduce the risk of breast cancer in women. It was approved for the treatment of osteoporosis in postmenopausal women by the FDA (under the name OporiaTM) and by the EMEA (under the name FablynTM) in 2005 and 2009, respectively. The closely related ormeloxifene (also known as centchroman) has an oxygen in its tetrahydronaphthalene ring system and is estrogenic in some parts of the body (e.g., bones) but antiestrogenic in others (e.g., uterus and breasts). It has been available in India for use as a weekly nonhormonal oral contraceptive since the early 1990s and is currently marketed under the trade names SaheliTM or ChhayaTM. However, there is evidence that it may also be effective for dysfunctional uterine bleeding (menorrhagia), mastalgia, fibro-adenoma, and advanced breast cancer.
Plasma protein binding, metabolism, reaction phenotyping and toxicokinetic studies of fenarimol after oral and intravenous administration in rats
Published in Xenobiotica, 2021
Kajal Karsauliya, Ashish Kumar Sonker, Manisha Bhateria, Isha Taneja, Anshuman Srivastava, Manu Sharma, Sheelendra Pratap Singh
FNL (CAS no. 60168-88-9, purity ≥ 98.0%) was procured from Sigma Aldrich (St Louis, MO) whereas, Centchroman (internal standard, IS) was a generous gift from CSIR-Central Drug Research Institute, Lucknow, India. The chemical structures of FNL and IS are represented in Figure 1. Propranolol, ethylenediaminetetraacetic acid (EDTA), ketoconazole, LC grades of acetonitrile and formic acid were supplied by Sigma Aldrich (St. Louis, Germany). Dipotassium hydrogen phosphate anhydrous and potassium dihydrogen phosphate were purchased from Merck Life Sciences Pvt. Ltd (Mumbai, India). Magnesium chloride was procured from Loba Chemie Pvt. Ltd (Mumbai, India). NADPH was procured from SRL Pvt. Ltd (Mumbai, India). Liver microsomes (Catalogue number: RTMCPL (rat liver microsomes) and HMMCPL (human liver microsomes)) and recombinant human CYP450 isoforms (1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, 3A4) were purchased from Invitrogen (Thermo Fisher Scientific, Bangalore, India). Milli Q water was obtained from a Millipore gradient water purification system (Millipore India Pvt. Ltd, New Delhi, India). MultiScreen Solvinert Filter Plate (96-well device with 0.45 µm PTFE membranes) were purchased from Millipore Corporation (Milford, CT). Blank plasma was obtained from healthy adult Wistar rats procured from the animal facility of the CSIR-Indian Institute of Toxicology Research, Lucknow, India. For maintenance, experimental studies, euthanasia, and disposal of the carcass, prior approval was taken from Institutional Animal Ethics Committee (IITR/IAEC/03/19). Human blank plasma was offered by healthy volunteers.
Effectiveness of Matricaria chamomilla (chamomile) extract on pain control of cyclic mastalgia: a double-blind randomised controlled trial
Published in Journal of Obstetrics and Gynaecology, 2018
N. Saghafi, H. Rhkhshandeh, N. Pourmoghadam, L. Pourali, M. Ghazanfarpour, A. Behrooznia, F. Vafisani
A variety of therapies have been recommended to lessen mastalgia. Such therapies include prescription of vitamin B2, B6, E and C, non-steroidal inflammatory drugs (NSAIDs), diuretics, thyroxin, progestational agents, Tamoxifen, Centchroman, Danazol, Bromocriptine and plant extracts like vitexagnus castus, evening primrose oil (EPO) (Kataria et al. 2014). However, given the side effects of hormonal treatment (Sharifi et al. 2014), many women have developed a propensity towards the use of herbal medicine.