Can Abiraterone cure prostate cancer? Where to buy & What Cost

Abiraterone 250 mg is a targeted drug for the fight against prostate cancer in the last stages. It is the official generic of the original drug Zytiga, with the active ingredient abiraterone acetate .

The drug is used in cases of the ineffectiveness of an appropriately solution, or in case of cancer metastases to other parts of the patient's body. Abiraterone zytiga suppresses the production of hormones, as a result of which the tumor becomes smaller and stops spreading.

abiraterone zytiga is an inhibitor of androgen biosynthesis. In particular, abiraterone zytiga selectively inhibits the activity of the 17α-hydroxylase / C17,20-lyase (CYP17) enzyme. This enzyme is essential for the biosynthesis of androgens in the testes, adrenal glands, and prostate tumor cells.
CYP17 catalyzes the conversion of pregnenolone and progesterone by 17α-hydroxylation and cleavage of the C17,20 bond to testosterone precursors: dehydroepiandrosterone and androstenedione, respectively. The inhibition of CYP17 activity is also accompanied by an increase in the synthesis of mineralocorticoids in the adrenal glands.

Antiandrogen therapy, such as the use of luliberin agonists or orchiectomy, attenuates androgen synthesis in the testes, but does not affect androgen synthesis in the adrenal glands and tumors. The use of abiraterone zytiga in conjunction with luliberin agonists (or orchidectomy) reduces the concentration of testosterone in the blood serum to a level below the detection threshold. Prostate-specific antigen (PSA) concentration serves as a biomarker in patients with prostate cancer.

Pharmacokinetics:
When administered orally, the prodrug abiraterone acetate is converted to the active metabolite abiraterone zytiga, which has antiandrogenic activity. Joint intake with food increases the absorption of the drug and, therefore, can increase and greatly change the effect of the drug, therefore, abiraterone zytiga should be taken on an empty stomach. The drug binds well to proteins (> 99%) and is metabolized in the liver with the participation of CYP3A4 and SULT2A1 to inactive metabolites. abiraterone zytiga is excreted in feces (~ 88%) and urine (~ 5%). The final half-life is 12 ± 5 hours.

Indications:
In combination with prednisolone for the treatment of metastatic castration-resistant prostate cancer in patients with disease progression during or after chemotherapy, including docetaxel.

Contraindications:
- severe liver dysfunction;
- children and adolescents up to 18 years old;
- hypersensitivity to abiraterone zytiga.

With caution:
- patients with severe renal impairment, since there are no clinical data on the use in this category of patients.
- patients whose condition may worsen with an increase in blood pressure or the development of hypokalemia, for example, with heart failure, recent myocardial infarction or ventricular arrhythmia; with a left ventricular ejection fraction of less than 50%, heart failure of III-IV functional class according to NYHA classification;
- lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
- patients with excessive production of mineralocorticoids;
- patients with adrenal insufficiency.

Pregnancy and lactation:
The FDA category of action on the fetus is N.
abiraterone zytiga is not intended for use in women. There are no data on the use of the drug in pregnant women. abiraterone zytiga is contraindicated in pregnant women and women capable of becoming pregnant. It is not known whether the drug or its metabolites are excreted in milk.
To prevent accidental exposure, pregnant women or women of childbearing age should not handle abiraterone zytiga without gloves.
It is not known if cost of abiraterone or its metabolites are present in semen. During treatment, it is necessary to use a condom if intercourse with a pregnant woman is planned. If intercourse is planned with a woman of childbearing age, it is necessary to use a condom along with other effective methods of contraception.

Method of administration and dosage:
It is intended for oral administration.
As part of combination therapy with prednisone or prednisolone in low doses, the recommended daily dose of abiraterone zytiga is 1 g (4 tablets, 250 mg each) 1 time / day 1 hour before meals or 2 hours after meals. abiraterone zytiga should not be taken with food. Food intake is not recommended within 1 hour after taking the drug.
If you miss the next daily dose of abiraterone zytiga or prednisolone the next day, you should take the usual dose of the missed drug.

Side effects:
Most often: peripheral edema, hypokalemia, arterial hypertension and urinary tract infections.
From the liver: hepatotoxicity, accompanied by an increase in the activity of ALT, ACT and total bilirubin (the mechanism of development of hepatotoxicity is currently unknown).
Infectious diseases: very often - urinary tract infections.
From the endocrine system: rarely - adrenal insufficiency.
On the part of laboratory parameters: very often - hypokalemia; often - hypertriglyceridemia, increased ALT activity.
From the side of the cardiovascular system: very often - arterial hypertension; often - heart failure, incl. acute heart failure, left ventricular failure, decreased left ventricular ejection fraction, angina pectoris, arrhythmia, atrial fibrillation, tachycardia.
On the part of the musculoskeletal system and connective tissue: often - fractures (except for pathological fractures).
From the side of the kidneys and urinary tract: often - hematuria.
Disturbances from the gastrointestinal tract: often - dyspepsia.
General disorders: very often - peripheral edema.

Overdose:
Data on overdose with abiraterone zytiga are limited. There is no specific antidote. In case of overdose, the drug should be discontinued and general supportive measures should be taken, including arrhythmia control. Liver function should also be monitored.
Side effects during therapy with abiraterone zytiga
For any side effects, especially those causing discomfort, you must inform your doctor.
• Diarrhea, vomiting, nausea;
• Painful urination;
• General weakness of the body;
• Elevated temperature;
• Hematomas in the body;
• Shortness of breath;
• Anemia;
• Lowered level of blood enzymes;
• Increased sugar levels;
• Jumping blood pressure.

Contraindications for taking Abirapro and Xbira
The drug should be taken with caution with the following disorders in the body:
• Liver disease;
• High blood pressure;
• Postponed heart attack, myocardial infarction.
It is forbidden to take the drug to persons who have not reached the age of 18, women who are pregnant and breastfeeding. The manufacturer recommends the use of reliable contraceptives during therapy, since the components of the drug can negatively affect the fetus.

Interaction:
Taking the drug simultaneously with food significantly increases the absorption of abiraterone zytiga. The effectiveness and safety of the drug taken with food has not been established, therefore, joint administration is unacceptable.
It is recommended to use buy abiraterone with caution in patients receiving drugs that are metabolized with the participation of CYP2D6, especially for drugs with a narrow therapeutic index. In such cases, consideration should be given to reducing the dose of drugs, incl. dextromethorphan, metoprolol, propranolol, desipramine, venlafaxine, haloperidol, risperidone, propafenone, flecainide, codeine, oxycodone, and tramadol.
Based on in vitro data, abiraterone zytiga is a substrate of the CYP3A4 isoenzyme. Caution is needed when taken concomitantly with strong inhibitors of the CYP3A4 isoenzyme (ketoconazole, itraconazole, clarithromycin, atazanavir, nefazodone, saquinavir, telithromycin, ritona) voriconazole), rifalinabitin, rifalbitin
There are no clinical data on the use of abiraterone zytiga with drugs that are particularly of the CYP2C8 isoenzyme (for example, with paclitaxel and repaglidin).