Enzalutamide

BRAND NAMES

Xtandi: Patients with metastatic castration-sensitive prostate cancer and those with castration-resistant prostate cancer can be treated with it. The suggested dosage for Xtandi is 160 mg, which can be taken orally once a day as two 80 mg tablets or four 40 mg capsules or tablets. You can take Xtandi with or without meals.

MECHANISM OF ACTION

It is generally accepted that androgen receptor signaling suppression might cause prostate cancer to respond. The course of the disease is nevertheless encouraged by this receptor's signaling even at low or undetectable serum androgen levels. Nuclear localization and DNA binding are necessary for the androgen receptor to stimulate the development of tumor cells. Even in situations where androgen receptor overexpression is present, as well as in prostate cancer cells resistant to androgen therapy, enzalutamide competitively inhibits androgen binding to androgen receptors, nuclear translocation of activated receptors, and the association of the activated androgen receptor with DNA. Prostate cancer cell proliferation is inhibited by enzalutamide treatment, which can also cause cancer cell death and tumor regression. Enzalutamide does not exhibit androgen receptor agonist action in preclinical research.

PHARMACOKINETICS

Absorption

Patients' plasma concentrations of enzalutamide reach their peak 1 to 2 hours after injection. According to mass balance research in humans, oral absorption of enzalutamide is expected to be at least 84.2%. Food has no clinically meaningful effect on the level of absorption. In clinical trials, Xtandi was given without concern for diet.

Distribution

The average apparent volume of distribution of enzalutamide in patients following a single oral dose is 110 L. The volume of distribution of enzalutamide exceeds the volume of total body water, indicating widespread extravascular distribution.

Metabolism

Enzalutamide is extensively metabolized. Human plasma contains two primary metabolites: N-desmethyl enzalutamide and a carboxylic acid derivative. Enzalutamide is metabolized by CYP2C8 and, to a lesser extent, by CYP3A4/5, both of which contribute to the synthesis of the active metabolite. In vitro, N-desmethyl enzalutamide is metabolized to a carboxylic acid by carboxylesterase 1, which also plays a minor role in enzalutamide metabolism to the carboxylic acid metabolite. CYPs did not metabolize N-desmethyl enzalutamide in vitro. Under clinical conditions, enzalutamide is a strong inducer of CYP3A4, a moderate inducer of CYP2C9 and CYP2C19, and has no clinically significant effect on CYP2C8.

Excretion

Enzalutamide is mostly removed by hepatic metabolism. 71% of the dosage is recovered in urine, whereas 14% is recovered in feces.

PHARMACODYNAMICS

Enzalutamide is a second-generation antiandrogen that inhibits the activity of androgens and androgen receptors in prostate cancer. Enzalutamide can cause a decrease in serum PSA for at least 12 weeks. However, this reaction can be transient, leading to enzalutamide resistance. When compared to placebo, patients using enzalutamide had a 37% lower risk of mortality.

ADMINISTRATION

Enzalutamide can be consumed orally. The dose should be taken as advised by your physician. Don't cut, crush, or chew this medication. Swallow the capsule whole. Consume with or without food.

DOSAGE AND STRENGTHS

Enzalutamide is available in 40 mg capsules and tablets of 40 mg and 80 mg under the brand name Xtandi. The suggested dose is 160mg taken orally once daily.

Capsule-40 mg

Tablets: 40 mg and 80 mg.

DRUG INTERACTIONS

Drug interactions of Enzalutamide includes

• Anti-coagulants- Apixaban
• Psoriasis and psoriatic arthritis—Avemilast
• Cancer drugs: Bosutinib, Dasatanib
• Anti-depressants- Citalopram,Escitalopram
• Immunomodulating medications: Fingolimod
• Opiate analgesics: hydrocodone
• Antibiotics- Moxifloxacin

CONTRAINDICATIONS

Ezelutamide may be hazardous to a fetus if administered to a pregnant woman due to the way it functions. It is not advised for women to use enzalutamide. Enzalutamide should not be taken by women who are pregnant or may become pregnant. Tell the patient that if this medicine is taken during pregnancy or if the patient becomes pregnant while taking it, there may be risks for fetal damage and pregnancy loss.

SIDE EFFECTS

A medication may have some undesirable side effects in addition to its intended ones.

• Back discomfort
• Chest ache
• Facial swelliness or bloating
• Feeling cold
• Mucus-filled cough
• High temperature
• Bladder loss
• Pounding sensation in the ears
• Sore throat
• unable to move the legs
• A typical weight increase or decrease

OVERDOSE

For enzalutamide, there is no known counteradote. If an overdose occurs, enzalutamide treatment should be discontinued and general supportive measures should be started while keeping in mind the medication's 5.8-day half-life. After taking an overdose, patients may be more susceptible to seizures.

STORAGE CONDITIONS

Keep the medication in a closed container at ambient temperature, away from moisture, humidity, and sunlight. Storage at 20°-25°C (68°-77°F).