Bicalutamide

Bicalutamide is an Antiandrogenic agent belonging to the pharmacological class of non-steroidal androgen receptor inhibitors and antineoplastics.

Bicalutamide is approved for the treatment of prostate cancer and works by inhibiting the effects of androgens, such as testosterone, which can contribute to the growth of prostate cancer cells.

Bicalutamide is well absorbed through the gut, taking about 31 hours for peak plasma levels ([R]-enantiomer). It binds significantly to plasma proteins (96%), undergoes liver metabolism, and is eliminated via urine and faeces.

The most common side effects of Bicalutamide include anaemia (low number of red blood cells).

Bicalutamide is available in the form of oral tablets.

The molecule is available in India, the United States, Canada, the United Kingdom, Italy, Australia, Germany, France, Japan and Spain.

Bicalutamide is an Antiandrogenic agent belonging to the pharmacological class of non-steroidal androgen receptor inhibitors and antineoplastics.

Bicalutamide blocks the activity of androgens of adrenal and testicular origin, which encourage the growth of normal and malignant prostatic tissue by competing with androgen to bind testosterone receptors.

The data duration of Bicalutamide action is approximately 6 days after administration.

The onset of Bicalutamide action typically occurs within a few days to weeks after its initial administration.

The Data of Cmax and Tmax of Bicalutamide has yet to be established.

Bicalutamide is available in the form of oral tablets.

Tablets: To be swallowed whole with water/liquid. Do not chew, crush or break it.

As the physician recommends, take the medication orally once daily; it can be taken with or without food as directed.

Bicalutamide can be used in the following health conditions:

By blocking testosterone's ability to bind to prostate cancer cells, bypassing their ability to produce testosterone and preventing their proliferation, bicalutamide suppresses the effects of androgens. Lowering testosterone levels, relieving urinary issues, and decreasing prostate tumours all contribute to slowing down or stopping the proliferation of cancer cells. It treats metastatic prostate cancer in conjunction with radiation therapy, reducing testosterone levels to prevent cancer cells from growing and facilitating urination.

For the treatment of Stage D2 metastatic prostate carcinoma, bicalutamide is indicated in combination therapy with an analogue of luteinizing hormone-releasing hormone (LHRH).

It may also be indicated in off-label conditions such as hirsutism (excessive hair growth), acne, and polycystic ovary syndrome (PCOS) due to its anti-androgenic properties.

Bicalutamide alone or in combination with other medications is not approved.

Orally: Bicalutamide is typically taken orally as a single dose tablet, and it is advised to take it simultaneously every day. The administration of bicalutamide tablets and an LHRH analog should begin simultaneously. If a dose of bicalutamide is missed, take the next dose at the scheduled time. Nevertheless, taking two doses to make up for a missed one is not recommended.

The dosage and duration of treatment should be as per the treating physician's clinical judgment.

Tablet: 50mg

Bicalutamide is available in the form of oral tablets.

Prostate Cancer: The recommended dose is 50 mg orally qDay (morning or evening)

Use in combination with LHRH analog or start at least 3 days before LHRH therapy.

Locally Advanced Prostate Cancer: The recommended dose is 150 mg orally qDay as monotherapy.

Locally advanced, non-metastatic prostate cancer: 150 mg once a day for at least two years or until the condition progresses in those for whom surgical castration or other medical intervention is inappropriate.

It is best to begin this medication's therapy concurrently with an LHRH analog.

Take the subsequent dose at the scheduled time if a dose is missed. Refrain from the missing dose, and don't take two doses simultaneously.

Consuming fish, soy, tomatoes, Brussels sprouts, kale, broccoli, and omega-3 fatty acid-rich oils like olive oil is crucial to lower prostate cancer risk. Avoid grilled and red meat, saturated fats from animal products, and dairy to minimize the risk. Regular exercise aids weight loss, reducing prostate cancer risk associated with obesity. Cease smoking to decrease the likelihood of prostate cancer development.

The dietary restriction should be individualized as per patient requirements.

Bicalutamide may be contraindicated in the following conditions:-

The adverse reactions related to Bicalutamide can be categorized as

Common Adverse Effects: Hot flashes, general pain, back pain, asthenia, constipation, pelvic pain, infection, nausea, dyspnea, oedema, diarrhoea, hematuria, nocturia, abdominal pain, anaemia.

Less Common Adverse Effects: Gynecomastia, rash, urinary tract infection, chest pain, hypertension, vomiting, flu-like symptoms, headache, elevation in liver function tests, weight loss, anorexia, breast pain, anxiety, and arthritis.

Rare Adverse Effects: Severe allergic reactions (such as anaphylaxis), interstitial lung disease, and liver toxicity (hepatotoxicity).

Disorders of the respiratory system: Interstitial lung disease, which can be fatal in some instances, such as pulmonary fibrosis and interstitial pneumonitis, usually occurs when a dose exceeds 50 mg.

Haemorrhage: Higher PT/INR due to Bicalutamide and coumarin anticoagulants interaction. There have been reports of severe bleeding.

Disorders of the skin and subcutaneous tissue: Photosensitivity

The clinically relevant drug interactions of Bicalutamide are briefly summarized here.

Pregnancy Category X (FDA): The risks outweigh the potential benefits. Safer alternatives exist.

It is not indicated for women and should not be used in this population because it can cause fetal harm.

There are no human data on the use of Bicalutamide in pregnant women.

Lactating women are not advised to use Bicalutamide. Evidence about the presence of Bicalutamide in human milk, its effects on nursing infants, or its impact on milk supply is not currently available. Rat milk has been found to contain bicalutamide.

As per the FDA, safety and effectiveness in the pediatric population have not been established.

The safety and efficacy of Bicalutamide in geriatric patients have yet to be extensively studied. Dosage adjustments may not be necessary based on age alone. Caution and close monitoring for potential adverse effects are recommended in this population.

Renal impairment: No dosage adjustment is required.

Mild-moderate hepatic impairment: No dosage adjustment is necessary.

The physician should be vigilant about the knowledge pertaining to identifying and treating overdosage of Bicalutamide.

Overconsumption of Bicalutamide could lead to dizziness, fainting, breast enlargement, reduced libido, and other hormonal-related effects.

There is no specific antidote or treatment for excessive Bicalutamide intake, so treatment typically involves symptomatic and supportive measures. Measures may include gastric lavage or induced emesis to remove unabsorbed medication, followed by supportive care to maintain vital functions. Monitoring for potential side effects, such as hormonal imbalances or adverse reactions, is essential. Hemodialysis might not be beneficial due to Bicalutamide's extensive protein binding and large volume of distribution. Continuous observation, along with appropriate medical interventions to address specific symptoms or complications, is recommended.

Bicalutamide is a pure, non-steroidal antiandrogen that has an affinity for androgen receptors but not for glucocorticoid, progestogen, or estrogen receptors. As a result, Bicalutamide inhibits the growth of both malignant and normal prostatic tissue by blocking the activity of androgens originating from the adrenal and testicular regions. Castration, either surgical or chemical, is one treatment option for prostate cancer, which is primarily androgen dependent. Castration has not been demonstrated to be comparable to antiandrogen monotherapy on an ongoing schedule to date.

Bicalutamide is efficiently absorbed from the gastrointestinal tract, reaching peak plasma concentration around 31 hours for the active [R]-enantiomer.

It exhibits a high plasma protein binding of 96%.

Metabolism occurs notably in the liver, where the active (R)-enantiomer undergoes oxidation to inactive compounds before glucuronidation. Meanwhile, the inactive (S)-enantiomer primarily undergoes glucuronidation.

Elimination involves excretion through urine and faeces. The elimination half-life for the [R]-enantiomer, the active form, is approximately one week, marking its sustained presence in the system after administration.