Prostaxen (Apalutamide) 60 Mg – 30 Tablets

Description

Prostaxen Tablet: Each film coated tablet contains Apalutamide INN 60 mg.

Product Features:

Indication and Usage

Prostaxen 60 mg is an androgen receptor inhibitor indicated for the treatment of patients with:

metastatic castration-sensitive prostate cancer
non-metastatic castration-resistant prostate cancer.

Pharmacology

Prostaxen is an orally administered, selective Androgen Receptor (AR) inhibitor that binds directly to the ligand-binding domain of the AR. Aslo prevents AR nuclear translocation, inhibits DNA binding, impedes AR-mediated transcription, and lacks androgen receptor agonist activity. Apalutamide treatment decreases tumor cell proliferation and increases apoptosis leading to potent antitumor activity.

Dosage and Administration

The recommended dose of Apalutamide is 240 mg (four 60 mg tablets) administered orally once daily. Swallow the tablets whole. Prostaxen 60 mg take with or without food.

Patients should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had a bilateral orchiectomy.

Warnings and Precautions

 Seizure: Do not recommend Apalutamide for patients with a history of seizures or other predisposing factors, including underlying brain injury, recent stroke (within the past year), primary brain tumors, or brain metastases. Discontinue the treatment permanently if a seizure develops during Apalutamide therapy. In two randomized studies (SPARTAN and TITAN), seizure occurred in 0.4% of patients receiving apalutamide and in 0.2% of patients treated with placebo. These studies excluded patients with a history of seizure or predisposing factors for seizure.

Falls and fractures: Patients receiving apalutamide experienced falls and fractures. Before starting apalutamide, healthcare providers should evaluate patients for fracture and fall risk. They should continue monitoring and managing patients according to established treatment guidelines.

Ischemic heart disease: Ischemic heart disease, including events leading to death, occurred in patients treated with Apalutamide. The majority of patients had cardiac risk factors. Monitor patients for signs and symptoms of ischemic heart disease and optimize management of cardiovascular risk factors according to standard of care, such as hypertension, diabetes, or dyslipidemia.

Concomitant use with other medicinal products

Prostaxen acts as a strong enzyme inducer and may decrease the effectiveness of many commonly used medications. Avoid the simultaneous use of aplutamide with drugs that are sensitive substrates of many metabolizing enzymes or transporters if their therapeutic effect is significant for the patient and if dose adjustment based on efficacy or plasma concentration is not easily performed.

Avoid co-administration of aplutamide with warfarin and coumarin-type anticoagulants. If you co-administer Apalutamide with an anticoagulant metabolized by CYP2C9 (such as warfarin or acenocoumarol), conduct additional international normalized ratio (INR) monitoring.

Recent cardiovascular disease

Clinical studies excluded patients with clinically significant cardiovascular disease in the past 6 months, including severe or unstable angina, myocardial infarction, symptomatic congestive heart failure, arterial or venous thromboembolic events (eg, pulmonary embolism, cerebrovascular accidents with transient ischemic attacks), ventricular Arrhythmias. Consequently, the safety of aplutamide in these patients remains uncertain.

If a healthcare provider prescribes Apalutamide, they should monitor patients with clinically significant cardiovascular disease for risk factors such as hypercholesterolemia, hypertriglyceridemia, or other cardio-metabolic disorders. Treat this condition according to established treatment guidelines after starting aplutamide.

Androgen deprivation therapy may prolong the QT interval

In patients with a history of or risk factors for QT prolongation and in patients receiving concomitant medicinal products that might prolong the QT interval, physicians should assess the benefit-risk ratio including the potential for Torsade de pointes prior to initiating Apalutamide.

Side effects

• Endocrine disorders: Hypothyroidism
• Metabolism and nutrition disorders: hypercholesterolemia, hypertriglyceridemia
• Nervous system disorders: Dysgeusia, seizure
• Cardiac disorders: ischemic heart disease
• Vascular disorders: hot flush, hypertension
• Gastrointestinal disorders: diarrhea
• Skin and subcutaneous tissue disorders: skin rash, pruritus
• Musculoskeletal and connective tissue disorders: fracture, arthralgia, muscle spasm
• General disorders and administration site conditions: fatigue
• Investigations: weight decreased
• Injury, poisoning and procedural complications: fall, fracture

Drug Interactions

Effect of Other Drugs on Apalutamide

CYP2C8 plays a role in the elimination of Apalutamide and in the formation of its active metabolite. In a drug-drug interaction study, the Cmax of Apalutamide decreased by 21% while AUC increased by 68% following co-administration of Apalutamide 240 mg single dose with gemfibrozil (strong CYP2C8 inhibitor). For the active moieties (sum of apalutamide plus the potency adjusted active metabolite), Cmax decreased by 21% while AUC increased by 45%. No initial dose adjustment is necessary when Apalutamide is co-administered with a strong inhibitor of CYP2C8 (e.g., gemfibrozil, clopidogrel) however, a reduction of the Apalutamide dose based on tolerability should be considered . Mild or moderate inhibitors of CYP2C8 are not expected to affect the exposure of Apalutamide.

Medicinal products that Inhibit CYP3A4

CYP3A4 is involved in the elimination of aplutamide and the formation of its active metabolite. In a drug-drug interaction study, co-administration of aplutamide (240 mg single dose) with itraconazole, a strong CYP3A4 inhibitor, led to a 22% decrease in the Cmax of aplutamide, while the AUC remained the same. For active ingredients (sum of apalutamide and energy-modulating active metabolites), Cmax decreased by 22%, and AUC remained unchanged. Do not require an initial dose adjustment when co-administering Apalutamide with a strong CYP3A4 inhibitor (e.g., ketoconazole, ritonavir, clarithromycin). Consider reducing the Apalutamide dose based on tolerability. Expect mild or moderate CYP3A4 inhibitors to have minimal effect on Apalutamide exposure.

Medicinal products that Induce CYP3A4 or CYP2C8

The effects of CYP3A4 or CYP2C8 inducers on the pharmacokinetics of aplutamide have not been evaluated in vivo. However, based on the results of drug-drug interaction studies with strong CYP3A4 and CYP2C8 inhibitors, researchers do not expect CYP3A4 or CYP2C8 inducers to have a clinically relevant effect on the pharmacokinetics of aplutamide and its active ingredients. Therefore, no dose adjustment is necessary during co-administration of aplutamide with inducers of CYP3A4 or CYP2C8.

Use in specific population

Pregnancy: Prostaxen is contraindicated in women who are or may become pregnant. Based on its mechanism of action, Apalutamide may cause fatal harm when administered during pregnancy. There are no data available from the use of Apalutamide in pregnant women. Animal reproductive studies have not been conducted with Apalutamide.

Fertility: Based on animal studies, Apalutamide may decrease fertility in males of reproductive potential.

Breast-feeding: Exclude the use of apalutamide during breastfeeding to avoid any risk to the suckling child.

Overdose

There is no known specific antidote for apalutamide overdose. In the event of an overdose, stop Apalutamide, undertake general supportive measures until clinical toxicity has been diminished or resolved.

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