Prostaxen Tablet
Apalutamide
60 mg
Everest Pharmaceuticals Ltd.
| Pack size | 30s in HDPE container |
|---|---|
| Dispensing mode | |
| Source | |
| Agent | |
| Retail Price | 500.00 AED |
Indications
Prostaxen Tablet is used for:
Prostate Cancer
Adult Dose
Prostate Cancer
Indicated for nonmetastatic, castration-resistant prostate cancer (NM-CRPC)
240 mg (ie, four 60-mg tablets) once daily
Child Dose
Renal Dose
Renal impairment
Mild-to-moderate (eGFR 30-89 mL/min/1.73 m2): No clinical significant difference in pharmacokinetics
Severe (eGFR <30 mL/min/1.73 m2): Pharmacokinetics unknown
Administration
May take with or without food
Take at the same time each day
Contra Indications
Pregnancy
Precautions
Cerebrovascular and ischemic cardiovascular events occurred in patients receiving Apalutamide. Monitor for signs and symptoms of cerebrovascular disorders and ischemic heart disease. Optimize management of cardiovascular risk factors.
Fractures occurred in patients receiving Apalutamide. Evaluate patients for fracture risk and treat patients with bone-targeted agents according to established guidelines.
Falls occurred in patients receiving Apalutamide with increased incidence in the elderly. Evaluate patients for fall risk.
Seizures occurred in 0.4% of patients receiving Apalutamide. Permanently discontinue Apalutamide in patients who develop a seizure during treatment.
Embryo-Fetal Toxicity: Apalutamide can cause fetal harm. Advise males with female partners of reproductive potential to use effective contraception.
Pregnancy-Lactation
Pregnancy
Contraindicated during pregnancy
Based on its mechanism of action, the drug can cause fetal harm and potential loss of pregnancy
There are no available data regarding use in pregnant women
The drug is not indicated for use in females, so animal embryo-fetal developmental toxicology studies were not conducted
Contraception
Based on the mechanism of action and findings in an animal reproduction study, advise male patients with female partners of reproductive potential to use effective contraception during treatment and for 3 months after the last dose
Infertility
Based on animal studies, may impair fertility in males of reproductive potential
Lactation
Not indicated for use in females
No data are available on presence in human milk or effect on the breastfed child or on milk production
Interactions
Strong CYP2C8 or CYP3A4 inhibitors
Coadministration with strong CYP2C8 or CYP3A4 inhibitors is predicted to increase the steady-state exposure of the active apalutamide moieties
No initial dose adjustment is necessary; however, reduce dose based on tolerability
Mild or moderate CYP2C8 or CYP3A4 inhibitors are not expected to affect apalutamide levels
CYP3A4, CYP2C9, CYP2C19, and UGT substrates
Apalutamide is a strong inducer of CYP3A4 and CYP2C19, a weak inducer of CYP2C9, and it induces UDP-glucuronosyltransferase (UGT)
Drugs primarily metabolized by CYP3A4, CYP2C19, or CYP2C9 can result in lower exposure to these medications; use alternate medications when possible or evaluate for loss of activity if medication is continued
Caution if UGT substrates must be coadministered with apalutamide and evaluate for loss of activity
P-gp, BCRP, or OATP1B1 substrates
Apalutamide is a weak inducer of P-gp, BCRP, and OATP1B1 clinically
Coadministration of apalutamide with these substrates can result in lower exposure of these drugs; caution if these substrates must be coadministered with apalutamide and evaluate for loss of activity
Contraindicated (11)
cabotegravir
doravirine
fostemsavir
isavuconazonium sulfate
lenacapavir
lonafarnib
lorlatinib
mavacamten
nirmatrelvir
nirmatrelvir/ritonavir
praziquantel
Adverse Effects
Side effects of Apalutamide :
>10% All Grades
Hypercholesterolemia, nonfasting (76%)
Anemia (70%)
Hyperglycemia (70%)
Hypertriglyceridemia, nonfasting (67%)
Leukopenia (47%)
Lymphopenia (41%)
Fatigue (39%)
Hyperkalemia (32%)
Hypertension (25%)
Rash (24%)
Diarrhea (20%)
Nausea (18%)
Arthralgia (16%)
Fall (16%)
Weight decreased (16%)
Hot flush (14%)
Fracture (12%)
Decreased appetite (12%)
Peripheral edema (11%)
>10% Grades 3-4
Hypertension (14%)
1-10%
Hypothyroidism (8%)
Pruritus (6.2%)
Ischemic heart disease (3.7%)
Heart failure (2.2%)
1-10% Grades 3-4
Rash (5%)
Fracture (3%)
Fall (2%)
Hypertriglyceridemia, nonfasting (2%)
Lymphopenia (2%)
Hyperkalemia (2%)
Hyperglycemia (2%)
Fatigue (1%)
Weight decreased (1%)
Diarrhea (1%)
Mechanism of Action
Androgen receptor (AR) inhibitor that binds directly to the ligand-binding domain of the AR; inhibits AR nuclear translocation, inhibits DNA binding, and impedes AR-mediated transcription
Administration caused decreased tumor cell proliferation and increased apoptosis, leading to decreased tumor volume in mouse xenograft models of prostate cancer
Note
Prostaxen 60 mg Tablet manufactured by Everest Pharmaceuticals Ltd.. Its generic name is Apalutamide. Prostaxen is availble in Bangladesh.
Farmaco BD drug index information on Prostaxen Tablet is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.