Abirapro works by reducing androgen production in the body. Androgens are male hormones that can promote tumor growth in the prostate gland.
Abirapro is used together with steroid medication (prednisone or methylprednisolone) to treat prostate cancer that has spread to other parts of the body. Abirapro is used in men whose prostate cancer cannot be treated with surgery or other medicines.
Abirapro may also be used for purposes not listed in this medication guide.
An indication is a term used for the list of condition or symptom or illness for which the medicine is prescribed or used by the patient. For example, acetaminophen or paracetamol is used for fever by the patient, or the doctor prescribes it for a headache or body pains. Now fever, headache and body pains are the indications of paracetamol. A patient should be aware of the indications of medications used for common conditions because they can be taken over the counter in the pharmacy meaning without prescription by the Physician.
Abirapro is indicated with prednisone or prednisolone for the treatment of metastatic castration resistant prostate cancer in adult men who are asymptomatic or mildly symptomatic after failure of androgen deprivation therapy in whom chemotherapy is not yet clinically indicated; the treatment of metastatic castration resistant prostate cancer in adult men whose disease has progressed on or after a docetaxel-based chemotherapy regimen.
How should I use Abirapro?
Use Abirapro as directed by your doctor. Check the label on the medicine for exact dosing instructions.
An extra patient leaflet is available with Abirapro. Talk to your pharmacist if you have questions about this information.
Take Abirapro by mouth on an empty stomach at least 1 hour before or 2 hours after eating. Do NOT take it with food. The amount of Abirapro in your body may be increased if you take it with food. This may increase the risk of side effects.
Swallow Abirapro whole with water. Do not break, crush, or chew before swallowing.
If you miss a dose of Abirapro, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once. If you miss more than 1 dose, contact your doctor.
Ask your health care provider any questions you may have about how to use Abirapro.
Uses of Abirapro in details
There are specific as well as general uses of a drug or medicine. A medicine can be used to prevent a disease, treat a disease over a period or cure a disease. It can also be used to treat the particular symptom of the disease. The drug use depends on the form the patient takes it. It may be more useful in injection form or sometimes in tablet form. The drug can be used for a single troubling symptom or a life-threatening condition. While some medications can be stopped after few days, some drugs need to be continued for prolonged period to get the benefit from it.
This medication is used along with prednisone to treat men with prostate cancer that has spread to other areas of the body and has not responded to surgical treatment that lowers testosterone levels. Abirapro belongs to a class of drugs known as anti-androgens (anti-testosterone). Testosterone, a natural hormone, helps prostate cancer to grow and spread. Abirapro works by blocking the production of testosterone, thereby slowing the growth and spread of prostate cancer.
This medication should not be given to women or children.
How to use Abirapro
Read the Patient Information Leaflet if available from your pharmacist before you start taking Abirapro and each time you get a refill. If you have any questions, ask your doctor or pharmacist.
Take this medication by mouth on an empty stomach, as directed by your doctor, usually once daily. Do not eat for at least 2 hours before and 1 hour after taking Abirapro. Taking Abirapro with food greatly increases the amount of this drug in your body and increases the risk of side effects.
Swallow whole. Do not crush or chew before swallowing. Pregnant women should wear gloves if handling the tablets. If the tablet is crushed or broken, women who are pregnant or who may become pregnant should not handle it or breathe the dust from it.
The dosage is based on your medical condition, lab results, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).
Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day. Do not stop any medications for your prostate cancer unless told to do so by your doctor. Stopping your medications could allow the cancer to spread more rapidly.
Tell your doctor if your condition persists or worsens (such as urination becomes more difficult, bone pain increases).
Abirapro is a derivative of steroidal progesterone and is an innovative drug that offers clinical benefit to patients with hormone refractory prostate cancer. Abirapro is administered as an acetate salt prodrug because it has a higher bioavailability and less susceptible to hydrolysis than Abirapro itself. FDA approved on April 28, 2011.
Generic name: Abirapro 125mg
Dosage form: tablet
Medically reviewed on June 5, 2018.
The recommended dose of Abirapro is 500 mg (four 125 mg tablets) administered orally once daily in combination with methylprednisolone 4 mg administered orally twice daily.
Important Administration Instructions
To avoid medication errors and overdose, be aware that Abirapro (Abirapro) tablets may have different dosing and food effects than other Abirapro products. Patients receiving Abirapro should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had bilateral orchiectomy.
Abirapro tablets can be taken with or without food. The tablets should be swallowed whole with water. Do not crush or chew tablets.
Dose Modification Guidelines in Hepatic Impairment and Hepatotoxicity
In patients with baseline moderate hepatic impairment (Child-Pugh Class B), reduce the recommended dose of Abirapro to 125 mg once daily. In patients with moderate hepatic impairment monitor ALT, AST, and bilirubin prior to the start of treatment, every week for the first month, every two weeks for the following two months of treatment and monthly thereafter. If elevations in ALT and/or AST greater than 5X upper limit of normal (ULN) or total bilirubin greater than 3X ULN occur in patients with baseline moderate hepatic impairment, discontinue Abirapro and do not re-treat patients with Abirapro.
Do not use Abirapro in patients with baseline severe hepatic impairment (Child-Pugh Class C).
For patients who develop hepatotoxicity during treatment with Abirapro (ALT and/or AST greater than 5X ULN or total bilirubin greater than 3X ULN), interrupt treatment with Abirapro. Treatment may be restarted at a reduced dose of 375 mg once daily following return of liver function tests to the patient’s baseline or to AST and ALT less than or equal to 2.5X ULN and total bilirubin less than or equal to 1.5X ULN. For patients who resume treatment, monitor serum transaminases and bilirubin at a minimum of every two weeks for three months and monthly thereafter.
If hepatotoxicity recurs at the dose of 375 mg once daily, re-treatment may be restarted at a reduced dose of 250 mg once daily following return of liver function tests to the patient’s baseline or to AST and ALT less than or equal to 2.5X ULN and total bilirubin less than or equal to 1.5X ULN.
If hepatotoxicity recurs at the reduced dose of 250 mg once daily, discontinue treatment with Abirapro.
Permanently discontinue Abirapro for patients who develop a concurrent elevation of ALT greater than 3 x ULN and total bilirubin greater than 2 x ULN in the absence of biliary obstruction or other causes responsible for the concurrent elevation.
Dose Modification Guidelines for Strong CYP3A4 Inducers
If a strong CYP3A4 inducer must be co-administered, increase the Abirapro dosing frequency to twice a day only during the co-administration period (e.g., from 500 mg once daily to 500 mg twice a day). Reduce the dose back to the previous dose and frequency, if the concomitant strong CYP3A4 inducer is discontinued.
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
Interactions With Other Drugs: Potential for Other Drugs To Affect Abirapro Exposures: In a clinical pharmacokinetic interaction study of healthy subjects pre-treated with a strong CYP3A4 inducer (rifampicin 600 mg daily for 6 days) followed by a single dose of Abirapro 1,000 mg, the mean plasma AUC∞ of Abirapro was decreased by 55%. Strong inducers of CYP3A4 (eg, phenytoin, carbamazepine, rifampicin, rifabutin, rifapentine, phenobarbital) during treatment with Abirapro are to be avoided or used with careful evaluation of clinical efficacy.
In a separate clinical pharmacokinetic interaction study of healthy subjects, co-administration of ketoconazole, a strong inhibitor of CYP3A4, had no clinically meaningful effect on the pharmacokinetics of Abirapro.
Potential of Abirapro to Affect Exposures to Other Drugs: Abirapro is an inhibitor of the hepatic drug-metabolizing enzymes CYP2D6 and CYP2C8. In the clinical study to determine the effects of Abirapro (plus prednisone) on a single dose of the CYP2D6 substrate dextromethorphan, the systemic exposure (AUC) of dextromethorphan was increased by approximately 200%. The AUC24 for dextrorphan, the active metabolite of dextromethorphan, increased approximately 33%.
Caution is advised when Abirapro is administered with drugs activated by or metabolized by CYP2D6, particularly with drugs that have a narrow therapeutic index. Dose reduction of narrow therapeutic index drugs metabolized by CYP2D6 should be considered.
In the same study to determine the effects of Abirapro (plus prednisone) on a single dose of the CYP1A2 substrate theophylline, no increase in systemic exposure of theophylline was observed.
In a CYP2C8 drug-drug interaction trial in healthy subjects, the AUC of pioglitazone was increased by 46% and the AUCs for M-III and M-IV, the active metabolites of pioglitazone, each decreased by 10%, when pioglitazone was given together with a single dose of Abirapro 1,000 mg. Although these results indicate that no clinically meaningful increases in exposure are expected when Abirapro is combined with drugs that are predominantly eliminated by CYP2C8, patients should be monitored for signs of toxicity related to a CYP2C8 substrate with a narrow therapeutic index if used concomitantly with Abirapro.
Effect of Food on Abirapro: Administration of Abirapro with food significantly increases the absorption of Abirapro. The efficacy and safety of Abirapro given with food has not been established. Abirapro must not be taken with food.
The most common adverse reactions seen with Abirapro are peripheral edema, hypokalemia, urinary tract infection and hypertension.
Abirapro may cause hypertension, hypokalemia and fluid retention as a pharmacodynamic consequence of its mechanism of action. In a phase 3 study anticipated mineralocorticoid effects were seen more commonly in patients treated with Abirapro versus patients treated with placebo: Hypokalemia 21% versus 11%, hypertension 16% versus 11% and fluid retention (peripheral edema) 26% versus 20%, respectively. In patients treated with Abirapro, grades 3 and 4 hypokalemia and grades 3 and 4 hypertension were observed in 4% and 2% of patients, respectively. Mineralocorticoid effects generally were able to be successfully managed medically. Concomitant use of a corticosteroid reduces the incidence and severity of these adverse drug reactions.
In studies of patients with metastatic advanced prostate cancer who were using a LHRH agonist, or were previously treated with orchiectomy, Abirapro was administered at a dose of 1 g daily in combination with low-dose prednisone or prednisolone (10 mg daily). Patients were intolerant to or had failed up to 2 prior chemotherapy regimens, 1 of which contained a taxane.
Adverse drug reactions due to Abirapro that occurred at a rate of ≥1% (all grades) are shown in Table 4.
The adverse drug reaction, adrenal insufficiency, occurred in the phase 3 clinical study at a rate of <0.5 % in taking Abirapro and at a rate of 0.2% in patients taking placebo.
Cardiovascular Effects: Both phase 3 studies excluded patients with uncontrolled hypertension, clinically significant heart disease as evidenced by myocardial infarction, arterial thrombotic events in the past 6 months, severe or unstable angina, NYHA class III or IV heart disease (study 301) or class II to IV heart failure (study 302) or cardiac ejection fraction measurement of <50%. All patients enrolled (both active and placebo-treated patients) were concomitantly treated with androgen deprivation therapy, predominantly with the use of LHRH agonists, which has been associated with diabetes, myocardial infarction, cerebrovascular accident and sudden cardiac death. The incidence of cardiovascular adverse reactions in the phase 3 studies in patients taking Abirapro versus patients taking placebo were as follows: Atrial fibrillation 3.4% versus 3.4%, tachycardia 2.7% versus 1.7%, angina pectoris 1.9% versus 0.9%, cardiac failure 1.9% versus 0.6% and arrhythmia 1.1% versus 0.4%.
Hepatotoxicity: Drug-associated hepatotoxicity with elevated ALT, aspartate transaminase (AST) and total bilirubin has been reported in patients treated with Abirapro. Across all clinical studies, liver function test elevations (ALT or AST increases of >5 times ULN or bilirubin increases >1.5 times ULN) were reported in approximately 4% of patients who received Abirapro, typically during the first 3 months after starting treatment. In the 301 clinical study, patients whose baseline ALT or AST was elevated were more likely to experience liver function test elevations than those beginning with normal values. When elevations of either ALT or AST >5 times ULN, or elevations in bilirubin >3 times ULN were observed, Abirapro was withheld or discontinued. In 2 instances marked increases in liver function tests occurred. These 2 patients with normal baseline hepatic function, experienced ALT or AST elevations >5 times ULN or elevations in bilirubin >3 times ULN were observed, Abirapro was withheld or discontinued. In 2 instances marked increases in liver function tests occurred. These 2 patients with normal baseline hepatic function, experienced ALT or AST elevations 15-40 times ULN and bilirubin elevations 2-6 times ULN. Upon discontinuation of Abirapro, both patients had normalization of their liver function tests and 1 patient was retreated with Abirapro without recurrence of the elevations. In study 302, grade 3 or 4 ALT or AST elevations were observed in 35 (6.5%) patients treated with Abirapro. Aminotransferase elevations resolved in all but 3 patients (2 with new multiple liver metastases and 1 with AST elevation approximately 3 weeks after the last dose of Abirapro. Treatment discontinuations due to ALT and AST increases were reported in 1.7% and 1.3% of patients treated with Abirapro and 0.2% and 0% of patients treated with placebo, respectively. No deaths were reported due to hepatotoxicity event.
In clinical trials, the risk for hepatotoxicity was mitigated by exclusion of patients with baseline hepatitis or significant abnormalities of liver function tests. In the 302 trial, patients with liver metastases were not eligible and patients with baseline ALT and AST ≥2.5 times ULN were excluded. Abnormal liver function tests developing in patients participating in clinical trials were vigorously managed by requiring treatment interruption and permitting re-treatment only after return of liver function tests to the patient’s baseline. Patients with elevations of ALT or AST >20 times ULN were not retreated. The safety of re-treatment in such patients is unknown. The mechanism for hepatotoxicity associated with Abirapro is not understood.
You should not use this medication if you are allergic to Abirapro, if you have severe liver disease, or if you are pregnant.
Before you take Abirapro, tell your doctor if you have liver disease, low levels of potassium in your blood, any type of infection, high blood pressure, congestive heart failure, or a history of heart disease, fluid retention, recent heart attack, or problems with your adrenal gland or pituitary gland.
Although Abirapro is not for use by women, this medicine can harm an unborn baby or cause birth defects. Abirapro tablets should not be handled by a woman who is pregnant or who may become pregnant.
While you are taking Abirapro and for at least 1 week after your treatment ends: Use a condom to prevent transfer of this medication to your sexual partner if she is pregnant. Use a condom plus another form of effective birth control if your sexual partner could become pregnant.
DTP/NCI. "Abiraterone: The NCI Development Therapeutics Program (DTP) provides services and resources to the academic and private-sector research communities worldwide to facilitate the discovery and development of new cancer therapeutic agents.". https://dtp.cancer.gov/dtpstandard/s... (accessed September 17, 2018).
The results of a survey conducted on ndrugs.com for Abirapro are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Abirapro. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.
Consumer reported useful
No survey data has been collected yet
Consumer reported price estimates
No survey data has been collected yet
3 consumers reported time for results
To what extent do I have to use Abirapro before I begin to see changes in my health conditions? As part of the reports released by ndrugs.com website users, it takes > 3 month and a few days before you notice an improvement in your health conditions. Please note, it doesn't mean you will start to notice such health improvement in the same time frame as other users. There are many factors to consider, and we implore you to visit your doctor to know how long before you can see improvements in your health while taking Abirapro. To get the time effectiveness of using Abirapro drug by other patients, please click here.
> 3 month
4 consumers reported age
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Information checked by Dr. Sachin Kumar, MD Pharmacology