Bicalon50 mg

Approved Indication

Bicalon is indicated, in combination with a luteinizing hormone-releasing hormone (LHRH) analog, for the treatment of Stage D2 metastatic carcinoma of the prostate.

Guideline-Supported / Additional Uses

• Combination therapy with an LHRH analog (as part of combined androgen blockade) for locally advanced, non-metastatic prostate cancer, including alongside radiotherapy, per specialist oncology guidelines.
• Use as monotherapy in certain specialist-directed regimens, under close monitoring for gynecomastia and breast pain; this is not an FDA-approved use of the 150 mg strength.

Bicalon is not indicated for use in women and has no established role outside the management of prostate cancer.

Each film-coated tablet contains Bicalutamide as the active pharmaceutical ingredient, commonly available in a 50 mg strength (150 mg is used in some specialist-directed regimens outside the approved indication). Tablets also contain standard pharmaceutical excipients such as lactose, povidone, sodium starch glycollate, magnesium stearate, and film-coating agents.

Bicalon is a non-steroidal antiandrogen used in the management of prostate cancer. It works by blocking the action of androgens (male hormones) at the androgen receptor in prostate tissue, thereby slowing the growth of hormone-sensitive prostate cancer cells. Bicalon is typically administered once daily by mouth, usually in combination with an LHRH analog as part of combined androgen blockade therapy.

Bicalon belongs to the therapeutic class of non-steroidal antiandrogens (hormonal antineoplastic agents), used in the hormonal management of prostate cancer.

Mechanism

Bicalutamide is a racemic mixture; its antiandrogenic activity resides almost entirely in the R-enantiomer, which competitively binds to and inhibits the androgen receptor in prostate cancer cells, blocking the stimulatory effect of androgens (testosterone and dihydrotestosterone) on tumor growth. When combined with an LHRH analog, Bicalutamide blocks the transient rise in testosterone ("flare") that can occur at the start of LHRH therapy.

Pharmacokinetics

• Absorption: Well absorbed orally; not significantly affected by food.
• Distribution: Highly protein-bound (approximately 96%).
• Metabolism: Undergoes stereospecific metabolism via oxidation and glucuronidation, mainly in the liver.
• Elimination: Long elimination half-life of the active R-enantiomer (approximately 5.8 days), supporting once-daily dosing; excreted via urine and feces.

Bicalon tablets should be swallowed whole with a glass of water, with or without food, at the same time each day to maintain consistent blood levels. Do not stop taking Bicalon or change the dose without consulting the prescribing physician, even if symptoms improve.

Anticoagulants (e.g., Warfarin)

Bicalon can displace coumarin-type anticoagulants from plasma protein binding sites, increasing anticoagulant effect and bleeding risk. Prothrombin time/INR should be closely monitored when starting or stopping Bicalon in patients on these agents, with the anticoagulant dose adjusted as needed.

CYP3A4 Substrates

Bicalon inhibits the CYP3A4 enzyme (with weaker effects on CYP2C9, CYP2C19, and CYP2D6) and may increase plasma levels of drugs metabolized by this pathway (e.g., midazolam). Caution is advised when Bicalon is co-administered with narrow-therapeutic-index CYP3A4 substrates.

Inform your physician of all other medicines, including over-the-counter drugs and supplements, before starting Bicalon.

Very Common

Hot flashes, generalized pain, back pain, weakness (asthenia), pelvic pain, constipation, and gynecomastia/breast tenderness (especially with monotherapy).

Common

Nausea, peripheral edema, shortness of breath, nocturia, blood in urine, anemia, and infection.

Serious (Less Common but Important)

• Liver injury (elevated liver enzymes, jaundice, hepatitis) - see Precautions and Warnings.
• Interstitial lung disease, presenting as new or worsening cough and shortness of breath.
• Increased bleeding risk in patients on anticoagulants (see Interactions).

Patients taking Bicalon should seek prompt medical attention for yellowing of the skin/eyes, severe abdominal pain, unusual bleeding, or breathing difficulty.

Bicalon is contraindicated in pregnancy; it is not intended for use in women, and animal data show it can affect male fetal genital development if a partner becomes pregnant during treatment. Men receiving Bicalon whose partner is or may become pregnant should use effective contraception during treatment and for a period after stopping Bicalon, as advised by a physician. Bicalon is not used in breastfeeding women; there is no established role for its use during lactation. Any exposure during pregnancy should be discussed immediately with a physician.

Liver Function

Rare but sometimes severe liver injury has been reported with Bicalon. Liver function tests should be checked before starting treatment, periodically during the first few months, and thereafter as clinically indicated. Bicalon should be discontinued if significant liver injury or jaundice occurs.

Gynecomastia and Breast Pain

Gynecomastia and breast tenderness are common with Bicalon, particularly with monotherapy. Discuss preventive options with your specialist if this is a concern.

Lung Disease

Rare cases of interstitial lung disease, including fatal cases, have been reported. Report new or worsening cough, chest pain, or breathlessness promptly.

Bleeding Risk with Anticoagulants

See the Interactions field for details on increased bleeding risk with coumarin-type anticoagulants.

Disease Monitoring

Regular clinical evaluation, including PSA monitoring, is recommended to assess response to Bicalon therapy and detect disease progression.

Not for Use in Women

Bicalon must not be used in female patients (see Contraindications).

There is limited clinical experience with overdose of Bicalon; doses up to 200 mg daily have been tolerated in trials without life-threatening effects. There is no specific antidote. In case of a suspected overdose, seek immediate medical attention or contact a poison control center. Management is supportive and symptomatic. Bicalon is highly protein-bound and extensively metabolized, so dialysis is not expected to be effective in removing the drug.

Store Bicalon at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

Pediatric Use

Safety and efficacy of Bicalon have not been established in children. It is not indicated for routine pediatric use, except in rare specialist-directed circumstances (e.g., certain precocious puberty conditions) managed by a pediatric endocrinology or oncology specialist.

Geriatric Use

Bicalon is commonly used in older men, the typical population for prostate cancer; no dose adjustment based on age alone is required, though age-related hepatic or renal changes should be considered.

Renal Impairment

No dosage adjustment of Bicalon is required in renal impairment.

Hepatic Impairment

Bicalon should be used with caution in patients with moderate-to-severe hepatic impairment, with periodic monitoring of liver function, as elimination may be prolonged (see Precautions and Warnings).

Duration of Bicalon therapy is determined by the treating oncologist/urologist based on disease stage, response to treatment, and tolerability. It is generally continued long-term as part of ongoing hormonal management of prostate cancer unless disease progression, unacceptable side effects, or physician advice indicates otherwise.

Non-steroidal antiandrogen; hormonal antineoplastic agent (androgen receptor inhibitor).

Bicalutamide acts by competitively binding to androgen receptors in prostate tissue, blocking the binding and action of endogenous androgens (testosterone and dihydrotestosterone). This inhibits androgen-driven stimulation of prostate cancer cell growth. When used with an LHRH analog, Bicalutamide also blocks the initial testosterone surge ("flare") associated with starting LHRH therapy.

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Safety and efficacy of Bicalon have not been established in the general pediatric population. Limited specialist experience exists in select conditions (e.g., certain forms of precocious puberty) under close endocrinology/oncology supervision, but routine pediatric use of Bicalon is not recommended outside such specialist settings.