• Kestava indications
• Uses of Kestava in details
• Kestava description
• Kestava dosage
• Kestava interactions
• Kestava side effects
• Kestava contraindications

What is Kestava?

Note: Women of childbearing potential should not use or handle Kestava tablets without protection (e.g., gloves).

Kestava is used in combination with prednisone to treat patients with metastatic castration-resistant prostate cancer (prostate cancer that is resistant to medical or surgical treatments that lower testosterone and has already spread to other parts of the body). Kestava is used in patients who have received cancer treatments, such as docetaxel.

Kestava is available only with your doctor's prescription.

Kestava indications

Kestava 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 Kestava?

Use Kestava as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• An extra patient leaflet is available with Kestava. Talk to your pharmacist if you have questions about this information.
• Take Kestava 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 Kestava in your body may be increased if you take it with food. This may increase the risk of side effects.
• Swallow Kestava whole with water. Do not break, crush, or chew before swallowing.
• If you miss a dose of Kestava, 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 Kestava.

Uses of Kestava in details

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. Kestava belongs to a class of drugs known as anti-androgens (anti-testosterone). Testosterone, a natural hormone, helps prostate cancer to grow and spread. Kestava 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 Kestava

Read the Patient Information Leaflet if available from your pharmacist before you start taking Kestava 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 Kestava. Taking Kestava 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).

Kestava description

Kestava is a derivative of steroidal progesterone and is an innovative drug that offers clinical benefit to patients with hormone refractory prostate cancer. Kestava is administered as an acetate salt prodrug because it has a higher bioavailability and less susceptible to hydrolysis than Kestava itself. FDA approved on April 28, 2011.

Kestava dosage

Kestava Dosage

Generic name: Kestava ACETATE 125mg

Dosage form: tablet

Medically reviewed on June 5, 2018.

Recommended Dosage

The recommended dose of Kestava 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 Kestava (Kestava acetate) tablets may have different dosing and food effects than other Kestava acetate products. Patients receiving Kestava should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had bilateral orchiectomy.

Kestava 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

Hepatic Impairment

In patients with baseline moderate hepatic impairment (Child-Pugh Class B), reduce the recommended dose of Kestava 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 Kestava and do not re-treat patients with Kestava acetate.

Do not use Kestava in patients with baseline severe hepatic impairment (Child-Pugh Class C).

Hepatotoxicity

For patients who develop hepatotoxicity during treatment with Kestava (ALT and/or AST greater than 5X ULN or total bilirubin greater than 3X ULN), interrupt treatment with Kestava. 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 Kestava acetate.

Permanently discontinue Kestava 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

Avoid concomitant strong CYP3A4 inducers (e.g., phenytoin, carbamazepine, rifampin, rifabutin, rifapentine, phenobarbital) during Kestava treatment.

If a strong CYP3A4 inducer must be co-administered, increase the Kestava 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.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Medical Disclaimer

More about Kestava (Kestava)

• Kestava Side Effects
• During Pregnancy
• Drug Interactions
• Pricing & Coupons
• En Español
• Drug class: miscellaneous antineoplastics

Consumer resources

• Kestava
• Kestava (Advanced Reading)

Other brands: Kestava

Professional resources

• Kestava (FDA)
• Kestava Acetate (AHFS Monograph)

Related treatment guides

• Prostate Cancer

Kestava interactions

See also:
What other drugs will affect Kestava?

Drugs That Inhibit Or Induce CYP3A4 Enzymes

Based on in vitro data, Kestava is a substrate of CYP3A4.

In a dedicated drug interaction trial, co-administration of rifampin, a strong CYP3A4 inducer, decreased exposure of Kestava by 55%. Avoid concomitant strong CYP3A4 inducers during Kestava treatment. If a strong CYP3A4 inducer must be co-administered, increase the Kestava dosing frequency.

In a dedicated drug interaction trial, co-administration of ketoconazole, a strong inhibitor of CYP3A4, had no clinically meaningful effect on the pharmacokinetics of Kestava.

Effects Of Kestava On Drug Metabolizing Enzymes

Kestava is an inhibitor of the hepatic drug-metabolizing enzymes CYP2D6 and CYP2C8. In a CYP2D6 drug-drug interaction trial, the Cmax and AUC of dextromethorphan (CYP2D6 substrate) were increased 2.8-and 2.9-fold, respectively, when dextromethorphan was given with Kestava acetate 1,000 mg daily and prednisone 5 mg twice daily. Avoid co-administration of Kestava acetate with substrates of CYP2D6 with a narrow therapeutic index (e.g., thioridazine). If alternative treatments cannot be used, exercise caution and consider a dose reduction of the concomitant CYP2D6 substrate drug.

In a CYP2C8 drug-drug interaction trial in healthy subjects, the AUC of pioglitazone (CYP2C8 substrate) was increased by 46% when pioglitazone was given together with a single dose of 1,000 mg Kestava acetate. Therefore, patients should be monitored closely for signs of toxicity related to a CYP2C8 substrate with a narrow therapeutic index if used concomitantly with Kestava.

Kestava side effects

See also:
What are the possible side effects of Kestava?

The most common adverse reactions seen with Kestava are peripheral edema, hypokalemia, urinary tract infection and hypertension.

Kestava 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 Kestava 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 Kestava, 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, Kestava 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 Kestava 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 Kestava 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 Kestava 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 Kestava. 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 Kestava, 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, Kestava 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, Kestava 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 Kestava, both patients had normalization of their liver function tests and 1 patient was retreated with Kestava 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 Kestava. 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 Kestava. Treatment discontinuations due to ALT and AST increases were reported in 1.7% and 1.3% of patients treated with Kestava 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 Kestava is not understood.

Kestava contraindications

See also:
What is the most important information I should know about Kestava?

You should not use this medication if you are allergic to Kestava, if you have severe liver disease, or if you are pregnant.

Before you take Kestava, 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 Kestava is not for use by women, this medicine can harm an unborn baby or cause birth defects. Kestava tablets should not be handled by a woman who is pregnant or who may become pregnant.

While you are taking Kestava 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.

Kestava must be taken on an empty stomach.

Active ingredient matches for Kestava:

Abiraterone in Argentina.

List of Kestava substitutes (brand and generic names)	Sort by popularity
Unit description / dosage (Manufacturer)	Price, USD
Aberic (Argentina)
Abiranova (Argentina)
ABIRAPRO (India)
ABIRAPRO 250MG TABLET 1 packet / 60 tablets each (Glenmark)	$ 677.59
ABIRAPRO 250MG TABLET 1 packet / 120 tablets each (Glenmark)	$ 1273.66
ABIRAPRO 250MG TABLET 1 strip / 30 tablets each (Glenmark)	$ 327.02
ABIRAPRO tab 250 mg x 120's (Glenmark)	$ 1273.67
ABIRAPRO tab 250 mg x 30's (Glenmark)	$ 343.37
ABIRAPRO tab 250 mg x 60's (Glenmark)	$ 668.67
Abirapro 250mg Tablet (Glenmark)	$ 10.61
Abiraterona (Peru)
abiraterone (France, Germany, Ireland, Portugal, Sweden, Switzerland, United Kingdom, United States)
Abiraterone-Humanity (Georgia)
Abitera (Russian Federation)
Adyard (Argentina)
Birat (Argentina)
Bitera (Argentina)
Kigar (Argentina)
Prosterona (Argentina)
Roterona (Argentina)
Tebiran (Argentina)
Yonsa
Zytiga (France, Germany, Ireland, Portugal, Sweden, Switzerland, United Kingdom, United States)
ZYTIGA 250 MG TABLET 1 packet / 120 tablets each (Janssen)	$ 1807.23
Zytiga tab 250 mg 120's (Janssen)
ZYTIGA tab 250 mg x 120's (Janssen)
Zytiga tablet 250 mg (Janssen)
Zytiga tablet 250 mg/1 (Janssen)
Zytiga tablet 500 mg (Janssen)
Zytiga 250mg Tablet (Janssen)	$ 15.06
Zytiga 250mg (Austria, Germany, Luxembourg, Switzerland)
Zytiga 500mg (Austria, Germany, Switzerland)
Zyvalix (Argentina)

References

1. PubChem. "Abiraterone". https://pubchem.ncbi.nlm.nih.gov/com... (accessed September 17, 2018).
2. DrugBank. "Abiraterone". http://www.drugbank.ca/drugs/DB05812 (accessed September 17, 2018).
3. 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).

Reviews

The results of a survey conducted on ndrugs.com for Kestava 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 Kestava. 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.

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Information checked by Dr. Sachin Kumar, MD Pharmacology