BICALUTAMIDE- bicalutamide tablet, film coated
Dava Pharmaceuticals, Inc.
Bicalutamide Tablets, USP 50 mg daily are indicated for use in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analog for the treatment of Stage D2 metastatic carcinoma of the prostate.
Bicalutamide Tablets, USP 150 mg daily are not approved for use alone or with other treatments [see Clinical Studies (14.2)].
The recommended dose for Bicalutamide Tablets, USP therapy in combination with an LHRH analog is one 50 mg tablet once daily (morning or evening), with or without food. It is recommended that Bicalutamide Tablets, USP be taken at the same time each day. Treatment with Bicalutamide Tablets, USP should be started at the same time as treatment with an LHRH analog.
No dosage adjustment is necessary for patients with renal impairment [see Use in Specific Populations (8.7)].
No dosage adjustment is necessary for patients with mild to moderate hepatic impairment. In patients with severe liver impairment (n=4), although there was a 76% increase in the half-life (5.9 and 10.4 days for normal and impaired patients, respectively) of the active enantiomer of bicalutamide no dosage adjustment is necessary [see Use in Specific Populations (8.6)].
Bicalutamide Tablets, USP 50 mg Tablets for oral administration.
Bicalutamide Tablets, USP are contraindicated in any patient who has shown a hypersensitivity reaction to the drug or any of the tablet’s components. Hypersensitivity reactions including angioneurotic edema and urticaria have been reported [see Adverse Reactions (6.2)].
Bicalutamide Tablets, USP have no indication for women, and should not be used in this population.
Bicalutamide Tablets, USP may cause fetal harm when administered to a pregnant woman. Bicalutamide Tablets, USP are contraindicated in women, including those who are or may become pregnant. There are no studies in pregnant women using Bicalutamide Tablets, USP. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be appraised of the potential hazard to the fetus [see Use in Specific Populations ( 8.1)].
Rare cases of death or hospitalization due to severe liver injury have been reported post-marketing in association with the use of Bicalutamide Tablets, USP. Hepatotoxicity in these reports generally occurred within the first three to four months of treatment. Hepatitis or marked increases in liver enzymes leading to drug discontinuation occurred in approximately 1% of Bicalutamide Tablets, USP patients in controlled clinical trials.
Serum transaminase levels should be measured prior to starting treatment with Bicalutamide Tablets, USP, at regular intervals for the first four months of treatment, and periodically thereafter. If clinical symptoms or signs suggestive of liver dysfunction occur (e.g., nausea, vomiting, abdominal pain, fatigue, anorexia, “flu-like” symptoms, dark urine, jaundice, or right upper quadrant tenderness), the serum transaminases, in particular the serum ALT, should be measured immediately. If at any time a patient has jaundice, or their ALT rises above two times the upper limit of normal, Bicalutamide Tablets, USP should be immediately discontinued with close follow-up of liver function.
In clinical trials with Bicalutamide Tablets, USP 150 mg as a single agent for prostate cancer, gynecomastia and breast pain have been reported in up to 38% and 39% of patients, respectively.
A reduction in glucose tolerance has been observed in males receiving LHRH agonists. This may manifest as diabetes or loss of glycemic control in those with pre-existing diabetes. Consideration should therefore be given to monitoring blood glucose in patients receiving Bicalutamide Tablets, USP in combination with LHRH agonists.
Regular assessments of serum Prostate Specific Antigen (PSA) may be helpful in monitoring the patient’s response. If PSA levels rise during Bicalutamide Tablets, USP therapy, the patient should be evaluated for clinical progression. For patients who have objective progression of disease together with an elevated PSA, a treatment-free period of antiandrogen, while continuing the LHRH analog, may be considered.
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
In patients with advanced prostate cancer treated with Bicalutamide Tablets, USP in combination with an LHRH analog, the most frequent adverse reaction was hot flashes (53%).
In the multicenter, double-blind, controlled clinical trial comparing Bicalutamide Tablets, USP 50 mg once daily with flutamide 250 mg three times a day, each in combination with an LHRH analog, the following adverse reactions with an incidence of 5% or greater, regardless of causality, have been reported.
|Body System Adverse Reaction||Treatment GroupNumber of Patients (%)|
|Bicalutamide Tablets, USPPlus LHRH Analog(n=401)||FlutamidePlus LHRH Analog(n=407)|
|Body as a Whole|
|Pain (General)||142 (35)||127 (31)|
|Back Pain||102 (25)||105 (26)|
|Asthenia||89 (22)||87 (21)|
|Pelvic Pain||85 (21)||70 (17)|
|Infection||71 (18)||57 (14)|
|Abdominal Pain||46 (11)||46 (11)|
|Chest Pain||34 (8)||34 (8)|
|Headache||29 (7)||27 (7)|
|Flu Syndrome||28 (7)||30 (7)|
|Hot Flashes||211 (53)||217 (53)|
|Hypertension||34 (8)||29 (7)|
|Constipation||87 (22)||69 (17)|
|Nausea||62 (15)||58 (14)|
|Diarrhea||49 (12)||107 (26)|
|Increased Liver Enzyme Test *||30 (7)||46 (11)|
|Dyspepsia||30 (7)||23 (6)|
|Flatulence||26 (6)||22 (5)|
|Anorexia||25 (6)||29 (7)|
|Vomiting||24 (6)||32 (8)|
|Hemic and Lymphatic|
|Anemia †||45 (11)||53 (13)|
|Metabolic and Nutritional|
|Peripheral Edema||53 (13)||42 (10)|
|Weight Loss||30 (7)||39 (10)|
|Hyperglycemia||26 (6)||27 (7)|
|Alkaline Phosphatase Increased||22 (5)||24 (6)|
|Weight Gain||22 (5)||18 (4)|
|Bone Pain||37 (9)||43 (11)|
|Myasthenia||27 (7)||19 (5)|
|Arthritis||21 (5)||29 (7)|
|Pathological Fracture||17 (4)||32 (8)|
|Dizziness||41 (10)||35 (9)|
|Paresthesia||31 (8)||40 (10)|
|Insomnia||27 (7)||39 (10)|
|Anxiety||20 (5)||9 (2)|
|Depression||16 (4)||33 (8)|
|Dyspnea||51 (13)||32 (8)|
|Cough Increased||33 (8)||24 (6)|
|Pharyngitis||32 (8)||23 (6)|
|Bronchitis||24 (6)||22 (3)|
|Pneumonia||18 (4)||19 (5)|
|Rhinitis||15 (4)||22 (5)|
|Skin and Appendages|
|Rash||35 (9)||30 (7)|
|Sweating||25 (6)||20 (5)|
|Nocturia||49 (12)||55 (14)|
|Hematuria||48 (12)||26 (6)|
|Urinary Tract Infection||35 (9)||36 (9)|
|Gynecomastia||36 (9)||30 (7)|
|Impotence||27 (7)||35 (9)|
|Breast Pain||23 (6)||15 (4)|
|Urinary Frequency||23 (6)||29 (7)|
|Urinary Retention||20 (5)||14 (3)|
|Urinary Impaired||19 (5)||15 (4)|
|Urinary Incontinence||15 (4)||32 (8)|
Other adverse reactions (greater than or equal to 2%, but less than 5%) reported in the Bicalutamide Tablets, USP-LHRH analog treatment group are listed below by body system and are in order of decreasing frequency within each body system regardless of causality.
Body as a Whole: Neoplasm; Neck Pain; Fever; Chills; Sepsis; Hernia; Cyst
Cardiovascular: Angina Pectoris; Congestive Heart Failure; Myocardial Infarct; Heart Arrest; Coronary Artery Disorder; Syncope
Digestive: Melena; Rectal Hemorrhage; Dry Mouth; Dysphagia; Gastrointestinal Disorder; Periodontal Abscess; Gastrointestinal Carcinoma
Metabolic and Nutritional: Edema; BUN Increased; Creatinine Increased; Dehydration; Gout; Hypercholesteremia
Musculoskeletal: Myalgia; Leg Cramps
Nervous: Hypertonia; Confusion; Somnolence; Libido Decreased; Neuropathy; Nervousness
Respiratory: Lung Disorder; Asthma; Epistaxis; Sinusitis
Skin and Appendages: Dry Skin; Alopecia; Pruritus; Herpes Zoster; Skin Carcinoma; Skin Disorder
Special Senses: Cataract specified
Urogenital: Dysuria; Urinary Urgency; Hydronephrosis; Urinary Tract Disorder
Abnormal Laboratory Test Values:
Laboratory abnormalities including elevated AST, ALT, bilirubin, BUN, and creatinine and decreased hemoglobin and white cell count have been reported in both Bicalutamide Tablets, USP-LHRH analog treated and flutamide-LHRH analog treated patients.
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