Casodex
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Casodex
BicalutamideSystematic (IUPAC) nameN--3--2-hydroxy-2-methylpropanamideIdentifiersCAS number90357-06-5ATC codeL02BB03PubChem56069DrugBankAPRD00042ChemSpider2284Chemical dataFormulaC18H14F4N2O4S Mol. mass430.373 g/molSMILESeMolecules & PubChemPharmacokinetic dataBioavailabilitywell absorbedProtein binding96%MetabolismhepaticHalf life5.8 daysExcretion ?Therapeutic considerationsPregnancy cat.X(US)Legal status℞ Prescription onlyRoutesOralBicalutamide (marketed as Casodex, Cosudex, Calutide, Kalumid) is an oral non-steroidal anti-androgen used in the treatment of prostate cancer and hirsutism. It was first launched in 1995 as a combination treatment (with surgical or medical castration) for advanced prostate cancer and subsequently launched as monotherapy for the treatment of earlier stages of the disease.Bicalutamide is marketed by AstraZeneca with the brand names Casodex and Cosudex. It is recommended 50 mg once daily in combination with a luteinizing hormone-releasing hormone analogue or surgical castration.// Description and mechanism of actionBicalutamide is an oral non-steroidal anti-androgen with the empirical formula C18H14F4N2O4S and is an off-white powder that is practically insoluble in water.Bicalutamide acts as a pure anti-androgen by binding to the androgen receptor (AR) and preventing the activation of the AR and subsequent upregulation of androgen responsive genes by androgenic hormones. In addition, bicalutamide accelerates the degradation of the androgen receptor. Indications and useBicalutamide is indicated for the treatment of stage D2 metastatic prostate cancer in combination with a luteinizing hormone-releasing hormone analogue or as a monotherapy. It has also been used in clinical trials for ovarian cancer. It has also been used in combination with castration.Most advanced prostate cancer patients eventually become resistant to antiandrogen including bicalutamide therapy. Contraindications and precautionsBicalutamide is contraindicated in females and children and must not be given to any patient who has shown a hypersensitivity reaction to its use. Adverse reactionsAdverse reactions include reproductive system and breast disorders, breast tenderness, gynaecomastia, hot flushes, gastrointestinal disorders, diarrhoea, nausea, hepatic changes (elevated levels of transaminases, jaundice), asthenia and pruritus. PhysiologyIn adult males blocking the androgen receptors by bicalutamide, and eliminating the effect of testosterone and the other androgens from binding and stimulating the cellular effects of androgens, bicalutamide may cause a decline in sperm count and sexual difficulties. Nevertheless bicalutamide monotherapy appears to have minimal effect on sexual activity.Blockade of androgens receptors by bicalutamide in the brain will eliminate the negative feedback loop of testosterone on the release of luteinizing hormone (LH). This in turn will lead to a dramatic increase in testosterone and estrogen levels. Bicalutamide treatment will block the effects of rising testosterone levels but the effect of rising estrogen levels will remain unopposed and lead to feminizing effects most notably gynecomastia which is often painful.If bicalutamide is combined with an LHRH agonist or surgical castration then the elevation of estrogen levels will be prevented and the risks of excessive estrogen will be reduced. However since both testosterone and estrogens are essential for normal bone metabolism, reducing the anabolic bone effects of both androgens (which increase bone formation by stimulating osteoblasts) and estrogens (which reduce bone resorption by inhibiting osteoclasts) will increase bone loss and promote osteoporosis.
He showed biologic rationale that IAS in mice had prolonged time to progress and delay in onset of AI disease. The MHRA has issued a drug alert to recall this product from the market, to minimise the risk to patients.org/product/casodex. It works by blocking the effects of certain chemicals that are necessary for the cancer cells to live. The data show a potential significant reduction in risk of death by 20% (95% CI, 2% to 34%) for prostate cancer patients, achieved by adding the non-steroidal anti-androgen âCasodexâ (bicalutamide 50mg)Updated data from the Early Prostate Cancer (EPC) programme on the use of the nonsteroidal anti-androgen bicalutamide (Casodex) in comparison with standard care were presented during several sessions today,CASODEX (BICALUTAMIDE) Tablets for oral administration contain 50 mg of BICALUTAMIDE, a non-steroidal antiandrogen with no other known endocrine activity. In men with localized or locally advanced prostate cancer, treatment with the antiandrogen bicalutamide (Casodex; AstraZeneca, Wilmington, Delaware), either alone or as part of a curative regimen, significantly reduces the risk of disease progression, according to a recent report.This submission is based upon the first analysis of the combined efficacy and tolerability data from the three trials forming part of the largest international
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Learn about the prescription medication Casodex (Bicalutamide), drug uses, dosage, side effects, drug interactions, warnings, and patient labeling.
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