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Casodex is an antiandrogenic non-steroidal agent. By binding to receptors having an affinity for androgens, it inhibits the activity of androgens. As a result of such an activity, the regression of a prostate tumor is detected. It does not obtain other types of endocrine activity.


After oral administration, Casodex is well absorbed. Meals do not affect its bioavailability.

Plasma protein binding is 96%. It is intensively metabolized in the liver by oxidation and the formation of glucuronide conjugates. It is excreted in the form of metabolites with urine and bile in approximately equal proportions.

Cumulation of bicalutamide in the body is possible.


Prostate cancer – as part of combination therapy with an analog of GnRH or with surgical castration.

Dosage and administration

Intended for an oral administration.

Adult men (including the elderly):

  • with advanced prostate cancer in combination with a GnRH analog or surgical castration: 50 mg once a day. Treatment with bicalutamide should be started at the same time as the intake of GnRH analog or surgical castration.
  • for locally advanced prostate cancer: 150 mg once a day. Bicalutamide should be taken for a long time, at least for 2 years. If signs of disease progression appear, the drug should be discontinued.

Disorders of kidney function: dose adjustment is not required.

Liver dysfunction: dose adjustment is not required in the case of mild impairment of liver function. In patients with moderate and severe hepatic impairment, increased accumulation of bicalutamide may be detected.


  • Hypersensitivity to any component of the drug;
  • Simultaneous administration with terfenadine, astemizole, cisapride;
  • Lactase deficiency, lactose intolerance, glucose-galactose malabsorption (the drug contains lactose);
  • Childhood;
  • Female patients.

Side effects

The pharmacological effect of Casodex may cause the following side effects:

  • very often (> 10%): gynecomastia (may persist even after therapy discontinuation, especially if the drug is taken for a long time), tenderness of the mammary glands, face flushing;
  • often (> 1%): diarrhea, nausea, a transient increase in the activity of “liver” transaminases, cholestasis and jaundice, itching, asthenia; when using the drug in a daily dose of 150 mg – alopecia or restoration of hair growth, decreased sex drive, sexual dysfunctions, weight gain may be observed.
  • rarely (> 0.1%): hypersensitivity reactions, including angioedema and urticaria, interstitial lung diseases; angina pectoris, prolongation of the QT interval, cardiac arrhythmias; when using the drug in a daily dose of 150 mg – abdominal pain, depression, dyspepsia, hematuria may be found.
  • very rarely (> 0.01% – vomiting, dry skin (when using the drug in a daily dose of 150 mg, dry skin is often observed), liver failure (a causal relationship with bicalutamide has not been reliably established), thrombocytopenia.


Cases of an overdose in humans are not described. There is no specific antidote. The treatment is symptomatic. Dialysis is not effective since bicalutamide is firmly bound to proteins and is not excreted by the kidneys unchanged. General supportive therapy and monitoring of vital functions of the body are prescribed.


  • There are no data on pharmacokinetic or pharmacodynamic interactions between bicalutamide and GnRH analogs.
  • In vitro studies have shown that the (11) -enantiomer of bicalutamide inhibits CYP ZA4, to a lesser extent affecting the activity of CYP 2C9, 2C19, and 2D6. The potential ability of bicalutamide to interact with other drugs was not found, however, when using bicalutamide for 28 days while taking midazolam, the area under the concentration-time (AUC) curve of midazolam increases by 80%.
  • Incompatible with terfenadine, astemizole, cisapride.
  • Be cautious prescribing bicalutamide simultaneously with cyclosporine or calcium channel blockers. It may be necessary to reduce the dose of these drugs, especially in the case of potentiation or the development of side effects. After the start of the use or cancellation of bicalutamide, it is recommended to carefully monitor the plasma concentration of cyclosporine and the patient’s clinical condition.
  • The simultaneous use of bicalutamide and drugs that inhibit microsomal oxidation of drugs, for example, with cimetidine or ketoconazole, can result in an increase in the concentration of bicalutamide in the blood plasma and, possibly, in an increase in the incidence of side effects. It enhances the effect of coumarin anticoagulants, including warfarin (competition for protein binding).