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Background: Androgen deprivation therapy (ADT) is indispensable part of treatment for metastatic prostate cancer (MPC) patients. There is documented association between ADT and adverse cardiovascular (CV) events, with variability between the different modes. However, there is dearth of evidence on the background CV risk factors of these group of patients at diagnosis. Aims and Objectives: We envisaged this retrospective observational study in the department of oncology to document the background CV risk factors of MPC patients at diagnosis, to help us better select the available ADTs based on their CV risks. Materials and Methods: Over a period of 2 years, all patients registered for treatment with a diagnosis of MPC, indicated for ADT, and available detailed history and background cardiological evaluation at presentation, were included in the study. As indirect indicators of CV risks, history of smoking, presence and treatment of dyslipidemia, and type 2 diabetes mellitus (T2DM), were documented. As direct indicators of CV risks, presence and treatment of hypertension, ischemic heart disease (IHD), congestive cardiac failure (CCF), ECG, and echocardiography changes suggesting cardiac morbidity were documented and the data were analyzed using descriptive statistical methods. Results: Indirect indicators: dyslipidemia, habit of smoking, and T2DM were found in 74%, 29.3%, and 13.3% patients, respectively. Direct indicators: Presence of hypertension, IHD, CCF, abnormalities in ECG, and echocardiography were found in 38.7%, 10.6%, 4%, 28%, and 34.6% patients, respectively. ST-T changes on ECG, low EF, and IHD on echocardiography were seen in 28.5%, 23%, and 26.9%, respectively. Conclusions: MPC patients have a substantial pre-existing CV risk at diagnosis. Our findings warrant a meticulous screening of all MPC patients for CV risk factors, to help in judicious selection of their ADT.
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Objective To investigate the effect of bicalutamide on migration and invasion of androgen receptor(AR) positive breast cancer cells and related mechanism, and the effect of mTOR inhibitor everolimus combined with bicalutamide on the proliferation of MDA-MB-453 cells. Methods Western blot was used to detect the expression change of mTOR, p-mTOR and p-S6 in breast cancer cell lines before and after bicalutamide treatment. Transwell assay was used to detect the cell viability. MTT assay was used to detect the proliferation of MDA-MB-453 cells treated by the combination of bicalutamide and everolimus. The combined effect of the two drugs was calculated by Jin Zhengjun's method. Results After six days of bicalutamide treatment, the expression of mTOR, p-mTOR and p-S6 were decreased in MDA-MB-453 cells (Ρ =0.034, 0.05, 0.03). The invasion and migration were inhibited in MDA-MB-453 cells (migration: t =4.88, P =0.001, invasion: t =2.684, P =0.028). The proliferation of MDA-MB-453 cells was inhibited after the treatment of bicalutamide combined with everolimus, and the Q value were all greater than 1.15. Conclusion Bicalutamide could inhibit the invasion and migration of MDA-MB-453, and the inhibition effect is affected by the expression level of AR. The combination of bicalutamide and everolimus could synergistically inhibit the proliferation of AR positive breast cancer cells.
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OBJECTIVE: To investigate therapeutic efficacy of Goserelin acetate sustained-release implants combined with bicalutamide in the treatment of elderly (≥70 years old) prostate cancer patients, and its effects on cognitive function and short-term survival rate. METHODS: A total of 56 prostate cancer patients treated in our hospital from Nov. 2014 to Nov. 2016 were divided into observation group and control group according to random number table, with 28 cases in each group. Observation group was given maximal androgen blokage (MAB) treatment which was Goserelin acetate sustained-release implant (subcutaneous injection of abdominal wall, 3. 6 mg/ times, once) combined with Bicalutamide tablet (orally, 50 mg/times, qd). Control group received surgical castration, and then was given docetaxel (intravenous dripping on 1st day) combined with Prednisone acetate tablets (lst-21st day, orally, 5 mg/time, bid) after surgery for adjuvant therapy. Treatment course of 2 groups lasted for 3 weeks, and all patients were followed up for 12 months. Clinical efficacy, Montreal cognitive function assessment table (MoCA) score, serum prostate specific antigen (PSA) levels and 12-month survival rate were observed in 2 groups. RESULTS: The total response rate of observation group was significantly higher than that of control group, with statistical significance (P<0. 05). Before treatment, there was no statistical significance in MoCA score and serum PSA levels between 2 groups (P>0. 05). After treatment, MoCA scores of 2 groups were decreased significantly, and the observation group was higher than the control group, with statistical significance (P<0. 05). 6 and 12 months after treatment, serum PSA levels of 2 groups were decreased significantly, and the observation group was significantly lower than the control group, with statistical significance (P<0. 05); 12-month survival rate of observation group (92. 86％) was significantly higher than that of control group (64. 29％), with statistical significance (P< 0. 05). CONCLUSIONS: Nonsteroidal anti-androgen drugs show significant therapeutic efficacy for elderly prostate cancer, reduce cognitive function damage, improve serum PSA levels, therapeutic efficacy and short-term survival rate.
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Maximum androgen blockade is the standard endocrine treatment for advanced prostate cancer. Interstitial lung disease in different degrees of severity, with low mortality and excellent response to treatment may appear with its use. We report a 77 years old patient with advanced prostate cancer who developed severe and progressive respiratory failure associated to bilateral pulmonary infiltrates, attributed to the direct effect of maximum androgen blockade. Despite the therapeutic efforts, the patient died. Lung pathology revealed Usual Interstitial Pneumonia.
Subject(s)
Humans , Male , Aged , Lung Diseases, Interstitial/chemically induced , Androgen Antagonists/adverse effects , Antinematodal Agents/adverse effects , Prostatic Neoplasms/drug therapy , Tosyl Compounds/adverse effects , Biopsy , Adenocarcinoma/drug therapy , Tomography, X-Ray Computed , Lung Diseases, Interstitial/pathology , Fatal Outcome , Disease Progression , Anilides/adverse effects , Nitriles/adverse effectsABSTRACT
The role of adjuvant hormonal therapy and optimized regimens for high-risk localized prostate cancer after radical prostatectomy remains controversial. Herein, the clinical trial CU1005 prospectively evaluated two regimens of maximum androgen blockage or bicalutamide 150 mg daily as immediate adjuvant therapy for high-risk localized prostate cancer. Overall, 209 consecutive patients were recruited in this study, 107 of whom received 9 months of adjuvant maximum androgen blockage, whereas 102 received 9 months of adjuvant bicalutamide 150 mg. The median postoperative follow-up time was 27.0 months. The primary endpoint was biochemical recurrence. Of the 209 patients, 59 patients developed biochemical recurrence. There was no difference between the two groups with respect to clinical characteristics, including age, pretreatment prostate-specific antigen, Gleason score, surgical margin status, or pathological stages. The maximum androgen blockage group experienced longer biochemical recurrence-free survival (P = 0.004) compared with the bicalutamide 150 mg group. Side-effects in the two groups were similar and could be moderately tolerated in all patients. In conclusion, immediate, 9-month maximum androgen blockage should be considered as an alternative to bicalutamide 150 mg as adjuvant treatment for high-risk localized prostate cancer patients after radical prostatectomy.
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Objective:To establish a headspace GC method for the determination of 7 kinds of residual solvents in bicalutamide, including dichloromethane, n-hexane, tetrahydrofuran, ethanol, ether, acetone and ethyl acetate. Methods: The residual solvents in the substance were determined by GC equipped with an FID detector and linked with an Agilent DB-624 capillary column (30. 0 m × 0. 25 mm × 1. 4 m). The inlet temperature was 200℃ and the FID detector temperature was 250℃. The column temperature was raised by program:the initial temperature was 35℃, maintained for 13 min, raised to 180℃ with a rate of 100℃/min, and maintained for 5 min. The carrier gas was nitrogen and the flow rate was 1. 2 ml·min-1. The heated temperature of the headspace oven was 90℃, the heated time lasted 30 min, and the injection volume was 1. 0 ml. The solution medium was dimethyl sulphoxide (DMSO). Results:Each solvent could be completely separated, and the calibration curve of each solvent showed good linear relationship with good accuracy. Conclusion:The method can be applied for the determination of residual solvents in bicalutamide.
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PURPOSE: We compared the efficacy, survival rate, and adverse events between bicalutamide 150-mg monotherapy and combined androgen blockade (CAB) in men with locally advanced prostate cancer. MATERIALS AND METHODS: From March 2003 to July 2012, we retrospectively included 74 patients who were treated for more than 3 months and were followed up for more than 6 months. 25 men were treated with bicalutamide 150-mg only (group 1) and 49 men received CAB (group 2). Serum prostate-specific antigen (PSA) change, survival rate, and adverse events were compared between the 2 groups. RESULTS: The PSA levels before and after treatment were 37.0+/-32.8 ng/mL and 9.5+/-27.0 ng/mL in group 1 (p<0.001) and 50.2+/-40.0 ng/mL and 20.0+/-35.8 ng/mL in group 2 (p<0.001). Mean survival rates were 78.9% in group 1 and 52.3% in group 2 (p=0.055). There were no statistically significant differences in adverse events between the 2 groups (p=0.304). The International Index of Erectile Function 5 (IIEF-5) score before treatment was 19.3+/-5.9 in group 1 and 18.3+/-5.8 in group 2 (p=0.487). The IIEF-5 score after treatment was 17.1+/-6.3 in group 1 and 14.0+/-6.1 in group 2, which was a statistically significant difference (p=0.036). CONCLUSIONS: The PSA change, mean survival rate, and adverse events in patients with locally advanced prostate cancer treated with bicalutamide 150-mg and CAB did not differ significantly. However, sexual function was better in the bicalutamide 150-mg group. Therefore, bicalutamide 150-mg monotherapy could be considered as a treatment for locally advanced prostate cancer in patients concerned about sexual function.
Subject(s)
Humans , Male , Prostate-Specific Antigen , Prostatic Neoplasms , Retrospective Studies , Survival RateABSTRACT
In cancer chemotherapy, it is very important to take into account the patient’s background. In recent years, a simple suspension method has attracted increased attention as a method that prevents changes in the stability and safety of various drugs. However, of 135 oral anticancer drugs, only 28 have been examined using this method, as of April 2013. In this study, we carefully investigated whether 53 oral anticancer drugs could be adapted to the simple suspension method, except for the 28 drugs that had already been previously reported. The results showed that most of these oral anticancer drugs could be adapted to the simple suspension method. Of seven drugs that were not adapted, six were generic drugs. In addition, it was clear that the evaluation of bicalutamide tablets was significantly different from our expected results. In conclusion, we were able to qualitatively assess all 53 oral anticancer drugs. This is equivalent to half of 107 untested drugs. These results provide useful information to cancer patients using oral anticancer drugs prepared using the simple suspension method.
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Objective: To study the pharmacokinetic characteristics and bioequivalence of bicalutamide tablets n healthy volunteers. Methods: A single oral dose of 50 mg bicalutamide test(domestic) or control(import) tablets was given to 20 healthy volunteers n an open randomized cross-over study. The concentrations of bicalutamide were determined with HPLC. The pharmacokinetic parameters were calculated with 3P97 and the bioequivalent test was performed with SAS. Results: The main pharmacokinetic parameters of the test and control drug were as follows: Cmax, 691. 50 vs 697. 30 μg/L; Tmax, 20.65 vs 24. 10 h; AUC0-∞, 148 124 vs 153 782 μg · h/L; t 1/2, 127. 46 vs 131. 06 h,respectively. The relative bioavailability was 99. 43%. Conclusion: The test bicalutamide tablet is bioequivalent to the control formulation.
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Androgen deprivation therapy, which is the standard treatment for metastatic prostate cancer, includes nonsteroidal antiandrogenic drugs, such as flutamide, nilutamide and bicalutamide. Of them, bicalutamide rarely induces interstitial pneumonia. We report a case of bicalutamide-induced interstitial pneumonia. A 68-year old male diagnosed with prostate cancer and multiple bone metastases presented with dry cough and low grade fever for 3 days. He had taken bicalutamide (50 mg/day) for 13 months. High resolution computed tomography revealed ground glass opacity in his right upper lung. The laboratory studies showed no eosinophilia in the serum and bronchoalveolar lavage fluid. Despite the use of antimicrobial agents for 2 weeks, the extent of the lung lesions increased to the left upper and right lower lung. He had no environmental exposure, collagen vascular disease and microbiological causes. Under the suspicion of bicalutamide-induced interstitial pneumonia, bicalutamide was stopped and prednisolone (1 mg/kg/day) was initiated. The symptoms and radiologic abnormalities were resolved with residual minimal fibrosis.
Subject(s)
Humans , Male , Anilides , Anti-Infective Agents , Bronchoalveolar Lavage Fluid , Collagen , Cough , Environmental Exposure , Eosinophilia , Fever , Fibrosis , Flutamide , Glass , Imidazolidines , Lung , Lung Diseases, Interstitial , Neoplasm Metastasis , Nitriles , Prednisolone , Prostatic Neoplasms , Tosyl Compounds , Vascular DiseasesABSTRACT
vides com-parable efficacy with medical castration in regard of decreasing PSA level and reducing prostate vol-ume. It is a safe and well tolerated treatment option as well.
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PURPOSE: Nonsteroidal antiandrogen monotherapy may be a treatment option for some patients with locally advanced prostate cancer. We report the efficacy, advantage, and adverse events of bicalutamide monotherapy in patients with locally advanced prostate cancer. MATERIALS AND METHODS: We retrospectively reviewed 13 patients with locally advanced prostate cancer who were treated with bicalutamide 150mg monotherapy. Serum PSA reduction was evaluated with periodic PSA follow-ups. If clinical progression was suspected, pelvic CT or bone scan was performed for the evaluation of disease progression. The changes of sexual function were assessed with the IIEF questionnaires prior to treatment and after 6 months of medication. RESULTS: Serum PSA declined to less than 2ng/ml within 3 months after treatment in most patients. A high serum PSA level was maintained in only 1 patient, and this patient showed disease progression. There were no significant differences between the mean scores of the pretreatment and post-treatment erectile function, orgasmic function, sexual desire, intercourse satisfaction, and overall satisfaction (p>0.05). Of the 13 patients, 2 patients (15.5%) showed adverse events, such as breast pain and gynecomastia. However, the symptoms were mild to moderate. There was no withdrawal to medication due to drug-related adverse events. CONCLUSIONS: From the viewpoint of the fall in serum PSA levels after 3 months, bicalutamide monotherapy was effective in the treatment of locally advanced prostate cancer. There were benefits to the patients in terms of the quality of life parameters, sexual function, and tolerability, which make bicalutamide monotherapy an attractive treatment option for patients with locally advanced prostate cancer. (Korean J Urol 2004;45: 108-113)