Search results for "Bicalutamide"

Moving Towards Precision Urologic Oncology: Targeting Enzalutamide-resistant Prostate Cancer and Mutated Forms of the Androgen Receptor Using the Nov…

2017

Abstract Darolutamide (ODM-201) is a novel androgen receptor (AR) antagonist with a chemical structure distinctly different from currently approved AR antagonists that targets both wild-type and mutated ligand binding domain variants to inhibit AR nuclear translocation. Here, we evaluate the activity of darolutamide in enzalutamide-resistant castration resistant prostate cancer (CRPC) as well as in AR mutants detected in patients after treatment with enzalutamide, abiraterone, or bicalutamide. Darolutamide significantly inhibited cell growth and AR transcriptional activity in enzalutamide-resistant MR49F cells in vitro, and led to decreased tumor volume and serum prostate-specific antigen l…

MP-03.04 The Combination Treatment of Bicalutamide Plus Carbidopa Significantly Enhances the in vivo Antitumor Activity on LNCaP Castration-resistant…

2011

Spectrophotometric estimation of bicalutamide in tablets

2007

A simple, sensitive, rapid, accurate and precise spectrophotometric method has been developed for the estimation of bicalutamide in bulk and pharmaceutical dosage forms. Bicalutamide shows maximum absorbance at 272 nm with molar absorptivity of 2.3399×10(4) l/mol/cm. Beer's law was obeyed in the concentration range of 1.5-18 μg/ml. The limit of detection and limit of quantification were found to be 0.1 and 0.4 μg/ml, respectively. Results of analysis were validated statistically and by recovery studies.

Preventing bone loss during androgen deprivation therapy for prostate cancer: Early experience with neridronate

2005

Abstract Objective: Androgen-deprivation therapy (ADT) is the usual treatment for locally advanced or metastatic prostate cancer. Osteoporosis is a common complication of ADT. The aim of our study was to evaluate the efficacy of neridronate, a relatively new bisphosphonate to prevent bone loss during androgen ablation. Methods: Sixty patients with prostate cancer and osteoporosis were enrolled and randomly assigned to 2 different treatment regimes: group A (30 patients) treated with maximum androgenic blockage (MAB), and group B (30 patients) treated with bicalutamide 150mg. Each group was divided in 2 subgroups A1–A2 and B1–B2. All patients received calcium and cholecalciferol supplements …

Design, synthesis, and biological evaluation of nonsteroidal cycloalkane[d]isoxazole-containing androgen receptor modulators.

2012

We report here the design, preparation, and systematic evaluation of a novel cycloalkane[d]isoxazole pharmacophoric fragment-containing androgen receptor (AR) modulators. Cycloalkane[d]isoxazoles form new core structures that interact with the hydrophobic region of the AR ligand-binding domain. To systematize and rationalize the structure-activity relationship of the new fragment, we used molecular modeling to design a molecular library containing over 40 cycloalkane[d]isoxazole derivatives. The most potent compound, 4-(3a,4,5,6,7,7a-hexahydrobenzo[d]isoxazol-3-yl)-2-(trifluoromethyl)benzonitrile (6a), exhibits antiandrogenic activity significantly greater than that of the most widely used …

Management of bicalutamide induced gynaecomastia. A randomized study comparing therapy versus prophylaxis with tamoxifen.

2008

Introduction and Objective: Gynaecomastia is a potentially treatment limiting adverse event of antiandrogen monotherapy for prostate cancer. Tamoxifen has shown to be effective in therapy and prophylaxis of gynecomastia and breast pain. However, tamoxifene dosage and treatment duration are not established and debate still exists if prophylaxis is more effective than therapy at the early onset. This randomized study compared the prophylactic activity of tamoxifene at the dose of 10 mg with its therapeutic activity when given at the dose of 20 mg at the early appearance of gynecomastia in patients receiving bicalutamide 150 mg/d for prostate cancer. Methods: Between June 2005 and June 2007, 1…

A randomized trial comparing tamoxifen therapy vs. tamoxifen prophylaxis in bicalutamide-induced gynecomastia.

2012

BACKGROUND: Tamoxifen (TAM) has been shown to be active against the bicalutamide-induced breast events (BEs) gynecomastia, and breast pain in patients with prostate cancer (PC). Optimal doses and schedules are not yet established. Debate still exists about whether prophylaxis with TAM is more effective than treatment of BEs when diagnosed. The results of a randomized study comparing TAM prophylaxis vs. TAM therapy are presented. METHODS: One hundred seventy-six patients with prostate cancer (PC) who were candidates for bicalutamide monotherapy were randomized to receive TAM 20 mg daily orally within 1 month from the onset of BEs (arm A) vs. TAM 10 mg daily starting simultaneously with bical…

Re: Does Oral Antiandrogen Use Before Leuteinizing Hormone-Releasing Therapy in Patients with Metastatic Prostate Cancer Prevent Clinical Consequence…

2010

Oh et al report their experience with 1566 metastatic prostate cancer patients treated with luteinising hormone-releasing hormone (LHRH) agonists in the area of Boston, Massachusetts, USA. Of these patients, 79.5% were given antiandrogens (bicalutamide, flutamide, or nilutamide) before the first LHRH agonist dose. The remaining patients (20.5%) did not receive antiandrogens. In all patients, complications appearing within 30 d and attributable to a flare phenomenon (fractures, spinal cord compression, bladder outlet obstruction, exacerbation of pain) were assessed retrospectively. Such complications were extremely rare ( or =7 d before starting the LHRH analogues) made no difference.The aut…

Neridronate prevents bone loss in patients receiving androgen deprivation therapy for prostate cancer.

2004

Today, androgen deprivation therapy is a cornerstone of treatment for advanced prostate cancer, although it presents important complications such as osteoporosis. Neridronate, a relatively new bisphosphonate, is able to prevent bone loss in patients with prostate cancer during androgen ablation. Introduction: Androgen-deprivation therapy (ADT) is a cornerstone of treatment for advanced prostate cancer. This therapy has iatrogenic complications, such as osteoporosis. The aim of our study was to evaluate the efficacy of neridronate, a relatively new bisphosphonate, to prevent bone loss during androgen ablation. Materials and Methods: Forty-eight osteoporotic patients with prostate cancer, tre…