Generic Name: Bicalutamide
Class: Antineoplastic Agents
VA Class: AN900
Chemical Name: (±)-N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide
Molecular Formula: C18H14F4N2O4S
CAS Number: 90357-06-5
Antineoplastic agent; a nonsteroidal antiandrogen.1 3 4 14 40 43
Uses for Casodex
Palliative treatment of metastatic (stage D2) prostate cancer; should be used in conjunction with a luteinizing hormone-releasing hormone (LHRH) analog (e.g., goserelin, leuprolide acetate).1 2 3 9 18
Casodex Dosage and Administration
Initiate bicalutamide and LHRH analog concomitantly.1 35 43
Administer orally once daily at the same time each day (morning or evening) without regard to meals.1 35 43
50 mg once daily.1 3 9 40 43 Duration of combined therapy with LHRH analog depends on clinical response.35
Cautions for Casodex
Known hypersensitivity to bicalutamide or any ingredient in the formulation.1
Should not be used in women, particularly for conditions that are not serious or life-threatening.1
Women who are or may become pregnant.1 (See Fetal/Neonatal Morbidity and Mortality under Cautions.)
Fetal/Neonatal Morbidity and Mortality
May cause fetal harm; contraindicated in pregnant women.1
If used during pregnancy or if patient becomes pregnant, apprise of potential fetal hazard.1
Severe liver injury reported, sometimes resulting in hospitalization and/or death;1 26 manifestations generally occurred within first 3–4 months.1
Possible hepatitis or marked increases in serum concentrations of hepatic transaminases.1
Measure serum transaminase concentrations prior to initiation of therapy, at regular intervals during the first 4 months, and periodically thereafter.1
Immediately measure serum transaminase (especially ALT) concentrations if manifestations suggestive of liver dysfunction occur.1
Immediately discontinue if jaundice develops or serum ALT concentration is >2 times ULN; monitor liver function closely thereafter.1
Regularly monitor serum PSA to assess response; if PSA increases, evaluate for possible disease progression.1 17
For patients with objective progression of disease and elevated serum PSA, consider temporarily withdrawing bicalutamide while continuing LHRH analog.1 35 36 37 Withdrawal of bicalutamide may be associated with PSA decrease.31 44
Possible Prescribing and Dispensing Errors
Ensure accuracy of prescription; similarity in spelling of Casodex (the trade name for bicalutamide) and Kapidex (former trade name for dexlansoprazole, a proton-pump inhibitor) may result in errors.217 218 219 223
Category X.1 (See Fetal/Neonatal Morbidity and Mortality and also Contraindications under Cautions.)
Not known whether bicalutamide is distributed into milk;1 use caution.1
Safety and efficacy not established.1
Use with caution in patients with moderate to severe hepatic impairment.1 3
Consider periodic liver function tests in patients with hepatic impairment receiving long-term therapy.1 35
Not intended for use in women, particularly for nonserious or nonlife-threatening conditions.1
Common Adverse Effects
Combined therapy with LHRH analog: hot flashes, pain (including abdominal, back, and pelvic pain), asthenia, constipation, infection, nausea, dyspnea, diarrhea.1
Gynecomastia and breast pain frequent if bicalutamide used as monotherapy.1
Interactions for Casodex
Does not induce CYP isoenzymes.1 Pharmacokinetic interaction unlikely with drugs metabolized by CYP isoenzymes.1
Increased risk of facial flushing41
Avoid alcohol consumption during therapy41
LHRH analog (e.g., goserelin, leuprolide)
Pharmacokinetic interaction unlikely1
Warfarin and other coumarins
Decreased anticoagulant protein binding and increased plasma concentrations; increased anticoagulant effects1
Monitor PT; adjust anticoagulant dosage as needed1
Well-absorbed following oral administration; absolute bioavailability is unknown.1
Food has no clinically important effect on rate or extent of absorption.1
Plasma Protein Binding
Undergoes stereospecific metabolism in the liver.1
Active R-enantiomer is predominantly oxidized to an inactive metabolite followed by glucuronidation.1 Inactive S-enantiomer is principally metabolized by glucuronidation.1
S-enantiomer is rapidly cleared relative to the R-enantiomer; R-enantiomer accounts for about 99% of total steady-state plasma concentrations.1
Both parent and metabolite glucuronides are eliminated in urine and feces.1
Approximately 6 days.1
Half-life of R-enantiomer was increased approximately 76% in patients with severe hepatic impairment.1
A selective antiandrogen with no androgenic or progestational activity in various animal models.12 17 43
Competitively blocks nuclear androgen receptors in target tissues (e.g., adrenal cortex, prostate, seminal vesicles).1 11 12 14 16 34 43
Blockade of androgen receptors in the hormone-sensitive tumor cells may result in growth arrest or transient tumor regression through inhibition of androgen-dependent DNA and protein synthesis.1 11 12 14 16 34 43
Inhibits initial androgenic stimulation and potential exacerbation of symptoms (e.g., bone pain, urinary obstruction, liver pain, impending spinal cord compression) associated with the first month of LHRH analog therapy.8 10 14 16 18 21 23 25 40
Advice to Patients
Risk of potential liver toxicity.1
Risk of facial flushing,1 41 particularly if used in conjunction with alcohol.41 Avoidance of alcohol recommended if flushing occurs.41
Importance of initiating bicalutamide concomitantly with LHRH analog and of not interrupting or discontinuing therapy without consulting a clinician.1
If used in women, importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.1
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as concomitant illnesses.1
Importance of informing patients of other important precautionary information.1 (See Cautions.)
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
Tablets, film- coated
AHFS DI Essentials. © Copyright 2018, Selected Revisions August 1, 2010. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
1. AstraZeneca. Casodex (bicalutamide) tablets prescribing information. Wilmington, DE; 2002 Sep.
2. Anon. Drugs of choice for cancer chemotherapy. Med Lett Drugs Ther. 2000; 42: 83-92.
3. Blackledge G. Casodexmechanisms of action and opportunities for usage. Cancer. 1993; 72(Suppl):3830-3. [PubMed 7504578]
4. Cockshott ID, Sotaniemi EA, Cooper KJ et al. The pharmacokinetics of Casodex enantiomers in subjects with impaired liver function. Br J Clin Pharmacol. 1993; 36:339-43. [PubMed 12959312]
5. Wilson JD. Androgens. In: Gilman AG, Rall TW, Nies AS et al, eds. Goodman and Gilman’s the pharmacological basis of therapeutics. 8th ed. New York: Pergamon Press; 1990:1413-1430.
6. Prostate cancer. From: CancerNet/PDQ. Physician data query (database). Bethesda, MD: National Cancer Institute; 2001 Oct.
7. Schering. Eulexin (flutamide) capsules prescribing information (dated 1994 Jul). In: Physicians’ desk reference. 49th ed. Montvale, NJ: Medical Economics Company Inc; 1995:2253-4.
8. Crawford ED, Eisenberger MA, McLeod DG et al. A controlled trial of leuprolide with and without flutamide in prostatic carcinoma. N Engl J Med. 1989; 321:419-24. [PubMed 2503724]
9. Schellhammer P, Sharifi R, Block N et al et al. A controlled trial of bicalutamide versus flutamide, each in combination with luteinizing hormone-releasing hormone analogue therapy, in patients with advanced prostate cancer. Urology. 1995; 45:745-52. [PubMed 7538237]
10. Dole EJ, Holdsworth MT. Nilutamide: an anitandrogen for the treatment of prostate cancer. Ann Pharmacother. 1997; 31: 65-75.
11. Geller J. Basis for hormonal management of advanced prostate cancer. Cancer. 1993; 71(Suppl):1039-45. [PubMed 7679038]
12. McLeod DG. Antiandrogenic drugs. Cancer. 1993; 71(Suppl):1046-9. [PubMed 8428326]
13. Migliari R, Muscas G, Usai E. Effect of Casodex on sleep-related erections in patients with advanced prostate cancer. J Urol. 1992; 148:338-41. [PubMed 1378907]
14. Denis L. Prostate cancer: primary hormonal treatment. Cancer. 1993; 71(Suppl):1050-8. [PubMed 8428327]
15. Smith PH. Deferred therapy in patients with advanced disease. Cancer. 1993; 71(Suppl):1074-7. [PubMed 8428330]
16. Daneshgari F, Crawford ED. Endocrine therapy of advanced carcinoma of the prostate. Cancer. 1993; 71(Suppl):1089-97. [PubMed 8428333]
17. Soloway MS, Matzkin H. Antiandrogenic agents as monotherapy in advanced prostatic carcinoma. Cancer. 1993; 71(Suppl):1083-8. [PubMed 8428332]
18. Mahler C. Is disease flare a problem? Cancer. 1993; 72(Suppl):3799-802. (IDIS 323226)
19. Sagalowsky AI, Wilson JD. Hyperplasia and carcinoma of the prostate. In: Wilson JD, Braunwald E, Isselbacher KJ et al, eds. Harrison’s principles of internal medicine. 12th ed. New York: McGraw-Hill Company; 1991: 1629-33.
20. Brendler CB. Diseases of the prostate. In: Wyngaarden JB, Smith LH Jr, Bennett JC, eds. Cecil textbook of medicine. 19th ed. Philadelphia: WB Saunders Company; 1992:1351-5.
21. Chrisp P, Goa KL. Goserelin: a review of its pharmacodynamic and pharmacokinetic properties, and clinical use in sex hormone-related conditions. Drugs. 1991; 41:254-88. [PubMed 1709853]
22. Vogelzang NJ, Kennealey GT. Recent developments in endocrine treatment of prostate cancer. Cancer. 1992; 70:966-76. [PubMed 1386283]
23. Santen RJ. Endocrine treatment of prostate cancer. J Clin Endocrinol Metab. 1992; 75:685-9. [PubMed 1517354]
24. Tyrrell CJ, Altwein JE, Klippel F et al et al. A multicenter randomized trial comparing the luteinizing hormone-releasing hormone analogue goserelin acetate alone and with flutamide in the treatment of advanced prostate cancer. J Urol. 1991; 146:1321-6. [PubMed 1834864]
25. Kuhn JM, Billebaud T, Navratil H et al. Prevention of a gonadotropin-releasing hormone analogue (buserelin) in metastatic prostatic carcinoma by administration of an antiandrogen (nilutamide). N Engl J Med. 1989; 321:413-8. [PubMed 2503723]
26. Dawson LA, Chow E, Morton G. Fulminant hepatic failure associated with bicalutamide. Urology. 1997; 49:283-4. [PubMed 9037299]
27. Soloway MS. Newer methods of hormonal therapy for prostate cancer. Urology. 1984; 24(Suppl):30-8. [PubMed 6437034]
28. Paulson DF. Management of metastatic prostatic cancer. Urology. 1985; 25:(Suppl):49-52.
29. Tolis G, Ackman D, Stellos A et al. Tumor growth inhibition in patients with prostatic carcinoma treated with luteinizing hormone-releasing hormone agonists. Med Sci. 1982; 79:1658-62.
30. Elder JS, Catalona WJ. Management of newly diagnosed metastatic carcinoma of the prostate. Urol Clin North Am. 1984; 11:283-95. [PubMed 6428022]
31. Nieh PT. Withdrawal phenomenon with the antiandrogen casodex. J Urol. 1995; 153:1070-2. [PubMed 7531785]
32. Crawford ED. Withdrawal phenomenon with the antiandrogen Casodex: editorial comments. J Urol. 1995; 153:1072.
33. Scher HI, Kelly WK. Withdrawal phenomenon with the antiandrogen Casodex: editorial comments. J Urol. 1995; 153:1072-3.
34. Kennealey GT, Furr BJA. Use of the nonsteroidal anti-androgen Casodex in advanced prostatic carcinoma. Urol Clin North Am. 1991; 18:99-110. [PubMed 1992575]
35. Zeneca Pharmaceuticals, Wilmington, DE: Personal communication.
36. Cersosimo RJ, Carr D. Prostate cancer: current and evolving strategies. Am J Health-Syst Pharm. 1996; 53:381-96. [PubMed 8673658]
37. McLeod DG, Kolvenbag GJCM. Defining the role of antiandrogens in the treatment of prostate cancer. Urology. 1996; 47(Suppl 1A):85-9. [PubMed 8560682]
39. Erlichman C, Loprinzi CL. Hormonal therapies. In: DeVita VT Jr, Hellman S, Rosenberg SA, eds. Cancer: principles and practice of oncology. 5th ed. Philadelphia, PA: J. B. Lippincott; 1997:395-405.
40. Anon. Bicalutamide for prostate cancer. Med Lett Drugs Ther. 1996; 38:56-7. [PubMed 8657047]
41. Kirschenbaum A. Management of hormonal treatment effects. Cancer. 1995; 75:1983-6.
42. Schellhammer PF, Sharifi R, Block NL et al. Clinical benefits of bicalutamide compared with flutamide in combined androgen blockade for patients with advanced prostatic carcinoma: final report of a double-blind, randomized, multicenter trial. Casodex Combination Study Group. Urology. 1997; 50:330-6. [PubMed 9301693]
43. Goa KL, Spencer CM. Bicalutamide in advanced prostate cancer: a review. Drugs Aging. 1998; 12:401-22. [PubMed 9606617]
44. Culig Z, Hoish A, Hittmair A et al. Androgen receptor gene mutations in prostate cancer: implications for disease progression and therapy. Drug Aging. 1997; 10:50-8.
217. US Food and Drug Administration. FDA approves name change for heartburn drug Kapidex. Rockville, MD; 2010 Mar 4. News release from FDA website ().
218. Institute for Safe Medication Practices. Kapidex-Casodex confusion. ISMP Medication Safety Alert! Community/Ambulatory Care edition. Horsham, PA; 2009 Jul. From ISMP website ().
219. Institute for Safe Medication Practices. ISMP quarterly action agenda July–September 2009. ISMP Medication Safety Alert! Acute Care edition. Horsham, PA; 2009 Oct 8. From ISMP website ().
222. Takeda Pharmaceuticals America. Dexilant (dexlansoprazole) delayed-release capsules prescribing information. Deerfield, IL; 2010 Mar.
223. Institute for Safe Medication Practices. Progress with preventing name confusion errors. ISMP Medication Safety Alert! Acute Care edition. Horsham, PA; 2007 Aug 9. From ISMP website ().
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