Generic Name
Abiraterone Acetate
Brand Names
Abiraterone, Zytiga, Akeega, YONSA, Abirtega
FDA approval date: April 28, 2011
Classification: Cytochrome P450 17A1 Inhibitor
Form: Tablet
What is Abiraterone (Abiraterone Acetate)?
Abiraterone acetate tablets are indicated in combination with prednisone for the treatment of patients with Metastatic castration-resistant prostate cancer Metastatic high-risk castration-sensitive prostate cancer Abiraterone acetate tablets are a CYP17 inhibitor indicated in combination with prednisone for the treatment of patients with metastatic castration-resistant prostate cancer . metastatic high-risk castration-sensitive prostate cancer .
Approved To Treat
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Brand Information
Abiraterone (Abiraterone acetate)
1INDICATIONS AND USAGE
Abiraterone acetate tablets are indicated in combination with prednisone for the treatment of patients with
• Metastatic high-risk castration-sensitive prostate cancer (CSPC)
2DOSAGE FORMS AND STRENGTHS
Film-Coated Tablets (250 mg): beige colored, oval shaped, film-coated tablets debossed with “MA” on one side and “21” on other side.
3CONTRAINDICATIONS
None.
4ADVERSE REACTIONS
The following are discussed in more detail in other sections of the labeling:
4.1Clinical Trial Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.
COU-AA-301: Metastatic CRPC Following Chemotherapy
COU-AA-301 enrolled 1195 patients with metastatic CRPC who had received prior docetaxel chemotherapy. Patients were not eligible if AST and/or ALT ≥2.5 x ULN in the absence of liver metastases. Patients with liver metastases were excluded if AST and/or ALT >5 x ULN.
Table 1 shows adverse reactions on the abiraterone acetate arm in COU-AA-301 that occurred with a ≥2% absolute increase in frequency compared to placebo or were events of special interest. The median duration of treatment with abiraterone acetate with prednisone was 8 months.
COU-AA-301 enrolled 1195 patients with metastatic CRPC who had received prior docetaxel chemotherapy. Patients were not eligible if AST and/or ALT ≥2.5 x ULN in the absence of liver metastases. Patients with liver metastases were excluded if AST and/or ALT >5 x ULN.
Table 1 shows adverse reactions on the abiraterone acetate arm in COU-AA-301 that occurred with a ≥2% absolute increase in frequency compared to placebo or were events of special interest. The median duration of treatment with abiraterone acetate with prednisone was 8 months.
Table 1: Adverse Reactions due to Abiraterone acetate in COU-AA-301
4.2Postmarketing Experience
The following additional adverse reactions have been identified during post approval use of abiraterone acetate with prednisone. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Immune System Disorders – Hypersensitivity: anaphylactic reactions (severe allergic reactions that include, but are not limited to difficulty swallowing or breathing, swollen face, lips, tongue or throat, or an itchy rash (urticaria)).
5OVERDOSAGE
Human experience of overdose with abiraterone acetate is limited.
6DESCRIPTION
Abiraterone acetate, the active ingredient of abiraterone acetate tablets USP is the acetyl ester of abiraterone. Abiraterone is an inhibitor of CYP17 (17α-hydroxylase/C17,20-lyase). Each abiraterone acetate tablet USP contains 250 mg or 500 mg of abiraterone acetate. Abiraterone is designated chemically as 17-(Pyridin-3-yl)androsta-5,16-dien-3β-yl acetate and its structure is:
Abiraterone acetate is a white to off-white, non-hygroscopic, crystalline powder. Its molecular formula is C
Abiraterone acetate tablets USP are available in 250 mg and 500 mg film-coated tablets and 250 mg uncoated tablets with the following inactive ingredients:
250 mg uncoated tablets: FDA approved dissolution test specifications differ from USP
250 mg and 500 mg film-coated tablets: Meets USP dissolution test 3
250 mg and 500 mg film-coated tablets: Meets USP dissolution test 3
7CLINICAL STUDIES
The efficacy and safety of abiraterone acetate with prednisone was established in three randomized placebo-controlled international clinical studies. All patients in these studies received a GnRH analog or had prior bilateral orchiectomy. Patients with prior ketoconazole treatment for prostate cancer and a history of adrenal gland or pituitary disorders were excluded from these trials. Concurrent use of spironolactone was not allowed during the study period.
1 p-value is derived from a log-rank test stratified by ECOG performance status score (0-1 vs. 2), pain score (absent vs. present), number of prior chemotherapy regimens (1 vs. 2), and type of disease progression (PSA only vs. radiographic).
2 Hazard Ratio is derived from a stratified proportional hazards model. Hazard ratio <1 favors abiraterone acetate with prednisone.
Figure 1: Kaplan-Meier Overall Survival Curves in COU-AA-301 (Intent-to-Treat Analysis)
2 Hazard Ratio is derived from a stratified proportional hazards model. Hazard ratio <1 favors abiraterone acetate with prednisone.
Figure 1: Kaplan-Meier Overall Survival Curves in COU-AA-301 (Intent-to-Treat Analysis)
COU-AA-302: Patients with metastatic CRPC who had not received prior cytotoxic chemotherapy
In COU-AA-302 (NCT00887198), 1088 patients were randomized 1:1 to receive either abiraterone acetate orally at a dose of 1,000 mg once daily (N=546) or Placebo once daily (N=542). Both arms were given concomitant prednisone 5 mg twice daily. Patients continued treatment until radiographic or clinical (cytotoxic chemotherapy, radiation or surgical treatment for cancer, pain requiring chronic opioids, or ECOG performance status decline to 3 or more) disease progression, unacceptable toxicity or withdrawal. Patients with moderate or severe pain, opiate use for cancer pain, or visceral organ metastases were excluded.
Patient demographics were balanced between the treatment arms. The median age was 70 years. The racial distribution of patients treated with abiraterone acetate was 95% Caucasian, 2.8% Black, 0.7% Asian and 1.1% Other. The ECOG performance status was 0 for 76% of patients, and 1 for 24% of patients. Co-primary efficacy endpoints were overall survival and radiographic progression-free survival (rPFS). Baseline pain assessment was 0-1 (asymptomatic) in 66% of patients and 2-3 (mildly symptomatic) in 26% of patients as defined by the Brief Pain Inventory-Short Form (worst pain over the last 24 hours).
Radiographic progression-free survival was assessed with the use of sequential imaging studies and was defined by bone scan identification of 2 or more new bone lesions with confirmation (Prostate Cancer Working Group 2 criteria) and/or modified Response Evaluation Criteria In Solid Tumors (RECIST) criteria for progression of soft tissue lesions. Analysis of rPFS utilized centrally-reviewed radiographic assessment of progression.
In COU-AA-302 (NCT00887198), 1088 patients were randomized 1:1 to receive either abiraterone acetate orally at a dose of 1,000 mg once daily (N=546) or Placebo once daily (N=542). Both arms were given concomitant prednisone 5 mg twice daily. Patients continued treatment until radiographic or clinical (cytotoxic chemotherapy, radiation or surgical treatment for cancer, pain requiring chronic opioids, or ECOG performance status decline to 3 or more) disease progression, unacceptable toxicity or withdrawal. Patients with moderate or severe pain, opiate use for cancer pain, or visceral organ metastases were excluded.
Patient demographics were balanced between the treatment arms. The median age was 70 years. The racial distribution of patients treated with abiraterone acetate was 95% Caucasian, 2.8% Black, 0.7% Asian and 1.1% Other. The ECOG performance status was 0 for 76% of patients, and 1 for 24% of patients. Co-primary efficacy endpoints were overall survival and radiographic progression-free survival (rPFS). Baseline pain assessment was 0-1 (asymptomatic) in 66% of patients and 2-3 (mildly symptomatic) in 26% of patients as defined by the Brief Pain Inventory-Short Form (worst pain over the last 24 hours).
Radiographic progression-free survival was assessed with the use of sequential imaging studies and was defined by bone scan identification of 2 or more new bone lesions with confirmation (Prostate Cancer Working Group 2 criteria) and/or modified Response Evaluation Criteria In Solid Tumors (RECIST) criteria for progression of soft tissue lesions. Analysis of rPFS utilized centrally-reviewed radiographic assessment of progression.
8HOW SUPPLIED/STORAGE AND HANDLING
Abiraterone Acetate Tablets USP are available in the strengths and packages listed below:
Storage and Handling
Store at 20°C to 25°C (68°F to 77°F); excursions permitted in the range from 15°C to 30°C (59°F to 86°F) [ see USP Controlled Room Temperature].Keep out of reach of children.
Based on its mechanism of action, abiraterone acetate may harm a developing fetus. Women who are pregnant or women who may be pregnant should not handle abiraterone acetate 250 mg uncoated tablets or other abiraterone acetate tablets if broken, crushed, or damaged without protection, e.g., gloves [see Use in Specific Populations (8.1)].
Store at 20°C to 25°C (68°F to 77°F); excursions permitted in the range from 15°C to 30°C (59°F to 86°F) [ see USP Controlled Room Temperature].Keep out of reach of children.
Based on its mechanism of action, abiraterone acetate may harm a developing fetus. Women who are pregnant or women who may be pregnant should not handle abiraterone acetate 250 mg uncoated tablets or other abiraterone acetate tablets if broken, crushed, or damaged without protection, e.g., gloves [see Use in Specific Populations (8.1)].
9PATIENT COUNSELING INFORMATION
Advise the patient to read the FDA-approved patient labeling (Patient Information)
Hypokalemia, Fluid Retention,
• Inform patients that abiraterone acetate is associated with hypertension, hypokalemia, and peripheral edema that may lead to QT prolongation and Torsades de Pointes in patients who develop hypokalemia while taking abiraterone acetate. Advise patients that their blood pressure, serum potassium and signs and symptoms of fluid retention will be monitored clinically at least monthly. Advise patients to adhere to corticosteroids and to report symptoms of hypertension, hypokalemia, or edema to their healthcare provider [
Adrenocortical Insufficiency
• Inform patients that abiraterone acetate with prednisone is associated with adrenal insufficiency. Advise patients to report symptoms of adrenocortical insufficiency to their healthcare provider [
Hepatotoxicity
• Inform patients that abiraterone acetate is associated with severe hepatotoxicity. Inform patients that their liver function will be monitored using blood tests. Advise patients to immediately report symptoms of hepatotoxicity to their healthcare provider [
Hypokalemia, Fluid Retention,
• Inform patients that abiraterone acetate is associated with hypertension, hypokalemia, and peripheral edema that may lead to QT prolongation and Torsades de Pointes in patients who develop hypokalemia while taking abiraterone acetate. Advise patients that their blood pressure, serum potassium and signs and symptoms of fluid retention will be monitored clinically at least monthly. Advise patients to adhere to corticosteroids and to report symptoms of hypertension, hypokalemia, or edema to their healthcare provider [
Adrenocortical Insufficiency
• Inform patients that abiraterone acetate with prednisone is associated with adrenal insufficiency. Advise patients to report symptoms of adrenocortical insufficiency to their healthcare provider [
Hepatotoxicity
• Inform patients that abiraterone acetate is associated with severe hepatotoxicity. Inform patients that their liver function will be monitored using blood tests. Advise patients to immediately report symptoms of hepatotoxicity to their healthcare provider [
Hypoglycemia
• Inform patients that severe hypoglycemia has been reported when abiraterone acetate was administered to patients with pre-existing diabetes who were receiving medications containing thiazolidinediones (including pioglitazone) or repaglinide, antidiabetic drugs. Advise patients with diabetes to monitor glucose levels during and after treatment with abiraterone acetate [see Warnings and Precautions (5.6) andDrug Interactions (7.2)].
Use in Combination with Radium Ra 223 Dichloride
• Advise patients that radium Ra 223 dichloride showed an increase in mortality and an increased rate of fracture when used in combination with abiraterone acetate plus prednisone/prednisolone. Inform patients to speak with their healthcare provider about any other medications or treatment they are currently taking for prostate cancer [
Dosing and Administration
• Inform patients that abiraterone acetate is taken once daily with prednisone (once or twice daily according to their healthcare provider's instructions) and to not interrupt or stop either of these medications without consulting their healthcare provider.
• Inform patients receiving GnRH therapy that they need to maintain this treatment during the course of treatment with abiraterone acetate.
• Instruct patients to take abiraterone acetate tablets as a single dose once daily on an empty stomach. Instruct patients to not eat food 2 hours before and 1 hour after taking abiraterone tablets. Abiraterone tablets taken with food causes increased exposure and may result in adverse reactions. Instruct patients to swallow tablets whole with water and not to crush or chew the tablets [
• Inform patients that if they miss a dose of abiraterone acetate or prednisone, they should take their normal dose the following day. If more than one daily dose is skipped, inform patients to contact their healthcare provider [
• Inform patients that severe hypoglycemia has been reported when abiraterone acetate was administered to patients with pre-existing diabetes who were receiving medications containing thiazolidinediones (including pioglitazone) or repaglinide, antidiabetic drugs. Advise patients with diabetes to monitor glucose levels during and after treatment with abiraterone acetate [see Warnings and Precautions (5.6) andDrug Interactions (7.2)].
Use in Combination with Radium Ra 223 Dichloride
• Advise patients that radium Ra 223 dichloride showed an increase in mortality and an increased rate of fracture when used in combination with abiraterone acetate plus prednisone/prednisolone. Inform patients to speak with their healthcare provider about any other medications or treatment they are currently taking for prostate cancer [
Dosing and Administration
• Inform patients that abiraterone acetate is taken once daily with prednisone (once or twice daily according to their healthcare provider's instructions) and to not interrupt or stop either of these medications without consulting their healthcare provider.
• Inform patients receiving GnRH therapy that they need to maintain this treatment during the course of treatment with abiraterone acetate.
• Instruct patients to take abiraterone acetate tablets as a single dose once daily on an empty stomach. Instruct patients to not eat food 2 hours before and 1 hour after taking abiraterone tablets. Abiraterone tablets taken with food causes increased exposure and may result in adverse reactions. Instruct patients to swallow tablets whole with water and not to crush or chew the tablets [
• Inform patients that if they miss a dose of abiraterone acetate or prednisone, they should take their normal dose the following day. If more than one daily dose is skipped, inform patients to contact their healthcare provider [
Embryo-Fetal Toxicity
• Inform patients that abiraterone acetate may harm a developing fetus and can cause loss of pregnancy.
• Advise males with female partners of reproductive potential to use effective contraception during treatment and for 3 weeks after the final dose of abiraterone acetate [
• Advise females who are pregnant or women who may be pregnant not to handle abiraterone acetate 250 mg uncoated tablets or other abiraterone acetate tablets if broken, crushed, or damaged without protection, e.g., gloves [andHow Supplied/Storage and Handling (16)].
Infertility
• Advise male patients that abiraterone acetate may impair fertility [
• Inform patients that abiraterone acetate may harm a developing fetus and can cause loss of pregnancy.
• Advise males with female partners of reproductive potential to use effective contraception during treatment and for 3 weeks after the final dose of abiraterone acetate [
• Advise females who are pregnant or women who may be pregnant not to handle abiraterone acetate 250 mg uncoated tablets or other abiraterone acetate tablets if broken, crushed, or damaged without protection, e.g., gloves [andHow Supplied/Storage and Handling (16)].
Infertility
• Advise male patients that abiraterone acetate may impair fertility [
Manufactured by:
MSN Laboratories Private Limited
Telangana – 509 228,
INDIA
MSN Laboratories Private Limited
Telangana – 509 228,
INDIA
Distributed by:
MSN Pharmaceuticals Inc.
Piscataway, NJ 08854-3714
MSN Pharmaceuticals Inc.
Piscataway, NJ 08854-3714
Issued on: May 2024
10PACKAGE LABEL.PRINCIPAL DISPLAY PANEL
250mg-container-label-120's-count
Abiraterone-film-coated-tablets-250mg-120's-count-container-label
Abiraterone-film-coated-tablets-250mg-500's-count-container-label
Abiraterone-film-coated-tablets-500mg-60's-count-container-label
Abiraterone-film-coated-tablets-500mg-500's-count-container-label
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