Version July 2025
Dosage guidance:
Safety: Control BP and correct hypokalemia prior to and during treatment.
Dosage form information : Abiraterone acetate is available in different tablet formulations; use caution when selecting dosage form as dosing and food effects vary between products. The formulations are NOT interchangeable; do not substitute between formulations.
Clinical considerations : Patients receiving abiraterone should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently (or have had a bilateral orchiectomy). Refer to "Administration" for information regarding an alternate abiraterone (Zytiga) administration method using a lower dose.
Prostate cancer, metastatic, castration resistant:
Zytiga: Oral: 1,000 mg once daily (in combination with prednisone 5 mg twice daily) (Ref)
or (off-label combination; Zytiga ; BRCA-mutated disease): Oral: 1,000 mg once daily (in combination with olaparib and prednisone or prednisolone) until disease progression or unacceptable toxicity (Ref).
Yonsa (micronized formulation): Oral: 500 mg once daily (in combination with methylprednisolone 4 mg twice daily).
Prostate cancer, synchronous metastatic, castration sensitive (off-label combination): Zytiga: Oral: 1,000 mg once daily (in combination with androgen deprivation, docetaxel [for 6 cycles], and prednisone 5 mg twice daily); continue abiraterone and prednisone until disease progression or unacceptable toxicity (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.
Altered kidney function: No dosage adjustment necessary for any degree of kidney dysfunction (<5% excreted in the urine) (Ref).
Hemodialysis, intermittent (thrice weekly): Unlikely to be dialyzed (highly protein bound): No supplemental dose or dosage adjustment necessary (Ref).
Peritoneal dialysis: Unlikely to be dialyzed (highly protein bound): No dosage adjustment necessary (Ref).
CRRT: No dosage adjustment likely to be necessary (Ref).
PIRRT (eg, sustained, low-efficiency diafiltration): No dosage adjustment likely to be necessary (Ref).
Hepatic impairment prior to treatment initiation:
Mild (Child-Turcotte-Pugh class A): No dosage adjustment necessary.
Moderate (Child-Turcotte-Pugh class B): 250 mg once daily (Zytiga) or 125 mg once daily (Yonsa). Permanently discontinue if ALT and/or AST >5 times the ULN or total bilirubin >3 times ULN occur during treatment in patients with baseline moderate hepatic impairment.
Severe (Child-Turcotte-Pugh class C): Use is not recommended.
Hepatotoxicity during treatment:
ALT and/or AST >5 times ULN or total bilirubin >3 times ULN: Withhold treatment until liver function tests return to baseline or ALT and AST ≤2.5 times ULN and total bilirubin ≤1.5 times ULN, then reinitiate at 750 mg once daily (Zytiga) or 375 mg once daily (Yonsa).
Recurrent hepatotoxicity on 750 mg/day (Zytiga) or 375 mg/day (Yonsa): Withhold treatment until liver function tests return to baseline or ALT and AST ≤2.5 times ULN and total bilirubin ≤1.5 times ULN, then reinitiate at 500 mg once daily (Zytiga) or 250 mg once daily (Yonsa).
Recurrent hepatotoxicity on 500 mg once daily (Zytiga) or 250 mg once daily (Yonsa): Discontinue treatment.
ALT >3 times ULN and total bilirubin >2 times ULN (in the absence of biliary obstruction or other contributing cause responsible for concurrent elevation): Permanently discontinue treatment.
Adrenocortical insufficiency: Increased corticosteroid doses may be required before, during, and after stress.
Hypoglycemia (in patients with diabetes): Antidiabetic medication dosage adjustments may be needed.
Mineralocorticoid excess (due to CYP17 inhibition): Concomitant administration with corticosteroids reduces the incidence and severity of these adverse events (eg, hypertension, hypokalemia, fluid retention). Control BP and correct hypokalemia prior to and during treatment.
Refer to adult dosing.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported for use in combination with a corticosteroid.
>10%:
Cardiovascular: Edema (25% to 27%), hypertension (9% to 37%)
Endocrine & metabolic: Hot flash (15% to 22%), hyperglycemia (57%), hypernatremia (33%), hypertriglyceridemia (63%), hypokalemia (17% to 30%), hypophosphatemia (24%)
Gastrointestinal: Constipation (23%), diarrhea (18% to 22%), dyspepsia (6% to 11%)
Genitourinary: Urinary tract infection (7% to 12%)
Hematologic & oncologic: Bruise (13%), lymphocytopenia (20% to 38%; grades 3/4: 4% to 9%)
Hepatic: Increased serum alanine aminotransferase (11% to 46%), increased serum aspartate aminotransferase (15% to 37%), increased serum bilirubin (7% to 16%)
Nervous system: Fatigue (39%), insomnia (14%)
Neuromuscular & skeletal: Arthralgia (≤30%), joint swelling (≤30%), myalgia (26%)
Respiratory: Cough (7% to 17%), dyspnea (12%), nasopharyngitis (11%), upper respiratory infection (5% to 13%)
1% to 10%:
Cardiovascular: Cardiac arrhythmia (7%), cardiac failure (2% to 3%), chest discomfort (≤4%), chest pain (≤4%)
Dermatologic: Skin rash (8%)
Genitourinary: Groin pain (7%), hematuria (10%), nocturia (6%), urinary frequency (7%)
Nervous system: Falling (6%), headache (8%)
Neuromuscular & skeletal: Bone fracture (6%)
Miscellaneous: Fever (9%)
<1%: Endocrine & metabolic: Adrenocortical insufficiency
Postmarketing:
Hepatic: Acute hepatic failure, fulminant hepatitis
Hypersensitivity: Anaphylaxis
Neuromuscular & skeletal: Myopathy, rhabdomyolysis
Respiratory: Pneumonia
There are no contraindications listed in the manufacturer's US labeling.
Canadian labeling: Hypersensitivity to abiraterone acetate or any component of the formulation or container; patients who are or could become pregnant.
Concerns related to adverse effects:
• Adrenocortical insufficiency: Adrenocortical insufficiency has been reported rarely. Concurrent infection, stress, or interruption of daily corticosteroids are associated with reports of adrenocortical insufficiency. Signs and symptoms of adrenocorticoid insufficiency could be masked by adverse events associated with mineralocorticoid excess.
• Hepatotoxicity: Severe hepatotoxicity (eg, fulminant hepatitis, acute liver failure, and death) has been reported. Significant increases in liver enzymes (including grade 3 and 4 events) have also been observed (higher likelihood in patients with baseline elevations), generally occurring in the first 3 months of treatment. The safety of retreatment after significant elevations (ALT or AST ≥20 times the ULN and/or total bilirubin ≥10 times ULN) has not been evaluated.
• Mineralocorticoid excess: Increased mineralocorticoids due to CYP17 inhibition may result in hypertension, hypokalemia, and fluid retention (including grade 3 and 4 events).
Disease-related concerns:
• Cardiovascular disease: May cause hypertension, hypokalemia, and fluid retention. QT prolongation and torsades de pointes have been observed rarely (postmarketing reports) in patients who developed hypokalemia during abiraterone administration. Monitor patients with cardiovascular disease closely, particularly those with heart failure, recent MI, or ventricular arrhythmia. Patients with left ventricular ejection fraction (LVEF) <50% or NYHA class II, III, or IV heart failure were excluded from clinical trials.
• Diabetes: Use with caution in patients with diabetes; severe hypoglycemia has been reported, particularly in patients receiving concomitant therapy with thiazolidinediones (eg, pioglitazone) or repaglinide.
Concurrent drug therapy issues:
• Radium Ra 223 dichloride: Due to an increased risk of fractures and mortality, the use of abiraterone plus a corticosteroid in combination with radium Ra 223 dichloride is not recommended.
Dosage form specific issues:
• Tablet formulations: Abiraterone acetate is available in different tablet formulations (the conventional formulation [Zytiga] and a micronized [fine particle] formulation [Yonsa]); use caution when selecting dosage form as dosing and food effects vary between products. The formulations are NOT interchangeable; do not substitute between formulations.
Abiraterone acetate is available in different tablet formulations (the conventional formulation and a micronized [fine particle] formulation). The formulations are NOT interchangeable; do not substitute between formulations.
Zytiga 250 mg tablets are produced in film-coated and uncoated tablets; only the uncoated tablets are available in the United States. Zytiga 500 mg tablets are film-coated. Yonsa is a micronized formulation of abiraterone.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Abirtega: 250 mg
Yonsa: 125 mg
Zytiga: 250 mg, 500 mg
Generic: 250 mg, 500 mg
Yes
Tablets (Abiraterone Acetate Oral)
250 mg (per each): $1.20 - $97.21
500 mg (per each): $195.75 - $206.85
Tablets (Abirtega Oral)
250 mg (per each): $1.20
Tablets (Yonsa Oral)
125 mg (per each): $104.57
Tablets (Zytiga Oral)
250 mg (per each): $119.69
500 mg (per each): $239.37
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Zytiga: 250 mg, 500 mg
Generic: 250 mg, 500 mg
Note: Abiraterone acetate is available in different tablet formulations; use caution when selecting dosage form as dosing and food effects vary between products. The formulations are NOT interchangeable; do not substitute between formulations.
Oral:
Swallow tablets whole with water. Do not crush or chew.
Zytiga: Administer on an empty stomach, at least 1 hour before and 2 hours after food (per the manufacturer); no food should be consumed for at least 2 hours before or for at least 1 hour after the dose.
Note: Data from a small, phase 2 study suggest that abiraterone (Zytiga) 250 mg once daily administered with or within 30 minutes of a low-fat breakfast is noninferior to the standard dose (1,000 mg) administered on an empty stomach; prostate-specific antigen and progression-free survival results were similar between the 2 arms, although higher troughs were reported with the standard dose (Ref). Low-dose abiraterone may decrease patient financial burden and improve adherence for those in resource-poor settings; further study is necessary to determine long-term efficacy of this dosing approach.
Yonsa (micronized formulation): May be administered without regard to food.
Hazardous agent (NIOSH 2024 [table 2]).
Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2023; NIOSH 2024; USP-NF 2020).
Note: Facilities may perform risk assessment of some hazardous drugs to determine if appropriate for alternative handling and containment strategies (USP-NF 2020). Refer to institution-specific handling policies/procedures.
Prostate cancer, metastatic:
Treatment of metastatic, castration-resistant prostate cancer (in combination with prednisone [Zytiga] or methylprednisolone [Yonsa])
Treatment of metastatic, high-risk castration-sensitive prostate cancer (in combination with prednisone [Zytiga])
Abiraterone may be confused with apalutamide, darolutamide, niraparib and abiraterone acetate
Zytiga may be confused with Jevtana, Xgeva, Xofigo, Xtandi, Zejula, Zometa, Zydelig
The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drug classes (chemotherapeutic agent, parenteral and oral) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Acute Care Settings).
Dosage formulation issues: Abiraterone acetate is available in different tablet formulations (the conventional formulation [Zytiga] and a micronized [fine particle] formulation [Yonsa]); use caution when selecting dosage form as dosing and food effects vary between products. The formulations are NOT interchangeable; do not substitute between formulations.
Substrate of CYP3A4 (Major with inducers), CYP3A4 (Minor with inhibitors); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits CYP2C8 (Weak), CYP2D6 (Moderate);
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Ajmaline: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Ajmaline. Risk C: Monitor
Amitriptyline: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Amitriptyline. CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of Amitriptyline. Risk C: Monitor
Amoxapine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Amoxapine. Risk C: Monitor
Amphetamines: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Amphetamines. Management: Monitor for amphetamine toxicities (including serotonin syndrome) if used with a moderate CYP2D6 inhibitor. Initiate amphetamine therapy at lower doses, monitor frequently, and adjust doses as needed. Discontinue amphetamines if serotoinin syndrome occurs Risk C: Monitor
Androgens: Hypertension-Associated Agents may increase hypertensive effects of Androgens. Risk C: Monitor
ARIPiprazole Lauroxil: CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of ARIPiprazole Lauroxil. Risk C: Monitor
ARIPiprazole: CYP2D6 Inhibitors (Moderate) may increase serum concentration of ARIPiprazole. Management: Monitor for increased aripiprazole pharmacologic effects. Aripiprazole dose adjustments may or may not be required based on concomitant therapy, indication, or dosage form. Consult full interaction monograph for specific recommendations. Risk C: Monitor
Atomoxetine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Atomoxetine. Risk C: Monitor
Brexpiprazole: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Brexpiprazole. Management: If brexpiprazole is to be used together with both a moderate CYP2D6 inhibitor and a strong or moderate CYP3A4 inhibitor, the brexpiprazole dose should be reduced to 25% of the usual dose when treating indications other than major depressive disorder. Risk C: Monitor
Carvedilol: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Carvedilol. Risk C: Monitor
Choline C 11: Antiandrogens may decrease therapeutic effects of Choline C 11. Risk C: Monitor
ClomiPRAMINE: CYP2D6 Inhibitors (Moderate) may increase serum concentration of ClomiPRAMINE. CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of ClomiPRAMINE. Risk C: Monitor
CloZAPine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of CloZAPine. Risk C: Monitor
Codeine: CYP2D6 Inhibitors (Moderate) may decrease therapeutic effects of Codeine. These CYP2D6 inhibitors may prevent the metabolic conversion of codeine to its active metabolite morphine. Risk C: Monitor
CYP3A4 Inducers (Moderate): May decrease serum concentration of Abiraterone Acetate. Risk C: Monitor
CYP3A4 Inducers (Strong): May decrease serum concentration of Abiraterone Acetate. Management: Avoid coadministration with strong CYP3A4 inducers. For patients treated with single-agent abiraterone who require therapy with a strong CYP3A4 inducers, abiraterone frequency may increased to twice daily. See full mono for details. Risk D: Consider Therapy Modification
Daprodustat: CYP2C8 Inhibitors (Weak) may increase serum concentration of Daprodustat. Risk C: Monitor
Desipramine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Desipramine. Risk C: Monitor
Deutetrabenazine: CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of Deutetrabenazine. Risk C: Monitor
Dextromethorphan: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Dextromethorphan. Risk C: Monitor
Doxepin (Systemic): CYP2D6 Inhibitors (Moderate) may increase serum concentration of Doxepin (Systemic). Risk C: Monitor
Doxepin (Topical): CYP2D6 Inhibitors (Moderate) may increase serum concentration of Doxepin (Topical). Risk C: Monitor
DOXOrubicin (Conventional): CYP2D6 Inhibitors (Moderate) may increase serum concentration of DOXOrubicin (Conventional). Risk X: Avoid
Eliglustat: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Eliglustat. Management: Eliglustat dose is 84 mg daily with CYP2D6 inhibitors. Use is contraindicated (COI) when also combined with strong CYP3A4 inhibitors. When also combined with a moderate CYP3A4 inhibitor, use is COI in CYP2D6 EMs or IMs and should be avoided in CYP2D6 PMs. Risk D: Consider Therapy Modification
Flecainide: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Flecainide. Risk C: Monitor
Flotufolastat F18: Coadministration of Antiandrogens and Flotufolastat F18 may alter diagnostic results. Management: Therapies targeting the androgen pathway may result in changes in the uptake of flotufolastat F18 in prostate cancer. The impact of these therapies on the performance of flotufolastat F18 is unknown; consider use of alternative agents. Risk D: Consider Therapy Modification
Gallium Ga 68 PSMA-11: Antiandrogens may decrease therapeutic effects of Gallium Ga 68 PSMA-11. Management: Therapies targeting the androgen pathway may result in changes in the uptake of gallium Ga 68 PSMA-11 (gozetotide) in prostate cancer. The impact on the performance of gallium Ga 68 PSMA-11 (gozetotide) is unknown; consider use of alternative agents. Risk D: Consider Therapy Modification
Haloperidol: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Haloperidol. Risk C: Monitor
HMG-CoA Reductase Inhibitors (Statins): Abiraterone Acetate may increase myopathic (rhabdomyolysis) effects of HMG-CoA Reductase Inhibitors (Statins). Risk C: Monitor
Iboga: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Iboga. Risk C: Monitor
Iloperidone: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Iloperidone. CYP2D6 Inhibitors (Moderate) may decrease active metabolite exposure of Iloperidone. Specifically, concentrations of the metabolite P95 may be decreased. CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of Iloperidone. Specifically, concentrations of the metabolite P88 may be increased. Risk C: Monitor
Imipramine: CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of Imipramine. Concentrations of desipramine may be increased. CYP2D6 Inhibitors (Moderate) may increase serum concentration of Imipramine. Risk C: Monitor
Indium 111 Capromab Pendetide: Coadministration of Antiandrogens and Indium 111 Capromab Pendetide may alter diagnostic results. Risk X: Avoid
Indoramin: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Indoramin. Risk C: Monitor
Lofepramine: CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of Lofepramine. The active metabolite of lofepramine is desipramine. Risk C: Monitor
Mequitazine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Mequitazine. Risk X: Avoid
Methadone: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Methadone. Risk C: Monitor
Metoclopramide: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Metoclopramide. Risk C: Monitor
Metoprolol: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Metoprolol. Risk C: Monitor
Nebivolol: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Nebivolol. Risk C: Monitor
Nortriptyline: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Nortriptyline. Risk C: Monitor
Oliceridine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Oliceridine. Risk C: Monitor
Olmutinib: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Olmutinib. Risk C: Monitor
PARoxetine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of PARoxetine. Risk C: Monitor
Perhexiline: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Perhexiline. Risk C: Monitor
Perphenazine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Perphenazine. Risk C: Monitor
Piflufolastat F18: Coadministration of Antiandrogens and Piflufolastat F18 may alter diagnostic results. Management: Therapies targeting the androgen pathway may result in changes in the uptake of piflufolastat F18 in prostate cancer. The impact of these therapies on the performance of piflufolastat F18 is unknown; consider use of alternative agents. Risk D: Consider Therapy Modification
Pimozide: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Pimozide. Risk C: Monitor
Pitolisant: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Pitolisant. Risk C: Monitor
Propafenone: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Propafenone. Risk C: Monitor
Propranolol: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Propranolol. Risk C: Monitor
Protriptyline: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Protriptyline. Risk C: Monitor
Radium Ra 223 Dichloride: May increase adverse/toxic effects of Abiraterone Acetate. Specifically, the risk for fractures and death may be increased. Risk X: Avoid
Repaglinide: CYP2C8 Inhibitors (Weak) may increase serum concentration of Repaglinide. Risk C: Monitor
Rifabutin: May decrease serum concentration of Abiraterone Acetate. Risk C: Monitor
Rifapentine: May decrease serum concentration of Abiraterone Acetate. Risk C: Monitor
RisperiDONE: CYP2D6 Inhibitors (Moderate) may increase serum concentration of RisperiDONE. Risk C: Monitor
Sertindole: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Sertindole. Risk C: Monitor
Sofpironium: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Sofpironium. Risk C: Monitor
Solriamfetol: May increase hypertensive effects of Hypertension-Associated Agents. Risk C: Monitor
Spironolactone: May decrease therapeutic effects of Abiraterone Acetate. Management: Consider alternatives to the combined use of spironolactone and abiraterone. If combined, monitor the clinical response to abiraterone closely, looking specifically for signs of clinical failure and/or disease progression. Risk D: Consider Therapy Modification
Tamoxifen: CYP2D6 Inhibitors (Moderate) may decrease active metabolite exposure of Tamoxifen. Specifically, CYP2D6 inhibitors may decrease the metabolic formation of highly potent active metabolites. Management: Consider alternatives to the use of moderate CYP2D6 inhibitors with tamoxifen when possible, as the combination may be associated with reduced clinical effectiveness of tamoxifen. Risk D: Consider Therapy Modification
Tamsulosin: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Tamsulosin. Risk C: Monitor
Tetrabenazine: CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of Tetrabenazine. Specifically, concentrations of the active alpha- and beta-dihydrotetrabenazine metabolites may be increased. Risk C: Monitor
Thiazolidinediones: Abiraterone Acetate may increase hypoglycemic effects of Thiazolidinediones. Risk C: Monitor
Thioridazine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Thioridazine. Risk X: Avoid
Timolol (Systemic): CYP2D6 Inhibitors (Moderate) may increase serum concentration of Timolol (Systemic). Risk C: Monitor
TraMADol: CYP2D6 Inhibitors (Moderate) may increase serum concentration of TraMADol. CYP2D6 Inhibitors (Moderate) may decrease active metabolite exposure of TraMADol. Risk C: Monitor
Trimipramine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Trimipramine. Risk C: Monitor
Valbenazine: CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of Valbenazine. Risk C: Monitor
Vortioxetine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Vortioxetine. Risk C: Monitor
Zuclopenthixol: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Zuclopenthixol. Risk C: Monitor
Taking abiraterone with a high-fat meal may increase systemic exposure (up to 10-fold [Zytiga] or up to ~4-fold [Yonsa]). Management: Do not administer with food (Zytiga). According to the manufacturer, abiraterone (Zytiga) must be taken on an empty stomach, at least 1 hour before and 2 hours after food. Abiraterone micronized (Yonsa) may be administered with or without food.
Patients with partners who could become pregnant should use effective contraception during treatment and for 3 weeks after the last abiraterone dose.
Abiraterone is available in uncoated and film-coated tablets and in micronized tablets; the manufacturer recommends patients who could become pregnant wear gloves if handling uncoated tablets, micronized tablets, or tablets that are broken, crushed, or damaged.
Based on the mechanism of action and adverse effects observed in animal reproduction studies, abiraterone may cause fetal harm or fetal loss if administered during pregnancy. Abiraterone is not indicated for use in females.
Abiraterone is available in uncoated and film-coated tablets and in micronized tablets; the manufacturer recommends patients who are pregnant wear gloves if handling uncoated tablets, micronized tablets, or tablets that are broken, crushed, or damaged.
It is not known if abiraterone is present in breast milk. Abiraterone is not indicated for use in females.
ALT, AST, and bilirubin prior to treatment, every 2 weeks for 3 months and monthly thereafter; if baseline moderate hepatic impairment (Child-Turcotte-Pugh class B), monitor ALT, AST, and bilirubin prior to treatment, weekly for the first month, every 2 weeks for 2 months, then monthly thereafter. If hepatotoxicity develops during treatment (and only after therapy is interrupted and liver function tests have returned to safe levels), monitor ALT, AST, and bilirubin every 2 weeks for 3 months and monthly thereafter. Monitoring of testosterone levels is not necessary. Serum potassium (prior to treatment and at least monthly). Monitor blood glucose (in patients with diabetes) during and after discontinuation of abiraterone therapy. Monitor BP and monitor for fluid retention (prior to treatment and at least monthly).
Monitor closely for signs/symptoms of adrenocorticoid insufficiency (if clinically indicated, consider appropriate diagnostics to confirm adrenal insufficiency) and signs/symptoms of hepatotoxicity (evaluate liver function promptly with signs or symptoms of hepatotoxicity). Monitor adherence.
Cardiovascular monitoring for patients with prostate cancer: Comprehensive assessment prior to treatment including a history and physical examination, screening for cardiovascular disease risk factors such as hypertension, diabetes, dyslipidemia, obesity, and smoking; baseline and serial ECGs are recommended in patients at risk of QTc prolongation during androgen deprivation therapy (ADT); estimate 10-year cardiovascular disease risk in patients without cardiovascular disease at baseline; assess cardiovascular risk annually during ADT (ASCO [Armenian 2017]; ESC [Lyon 2022]).
Abiraterone selectively and irreversibly inhibits CYP17 (17 alpha-hydroxylase/C17,20-lyase), an enzyme required for androgen biosynthesis which is expressed in testicular, adrenal, and prostatic tumor tissues. Inhibits the formation of the testosterone precursors dehydroepiandrosterone (DHEA) and androstenedione.
Distribution: Vdss: 19,669 ± 13,358 L
Protein binding: >99%; to albumin and alpha1-acid glycoprotein
Metabolism: Abiraterone acetate is hydrolyzed to the active metabolite abiraterone; further metabolized to inactive metabolites abiraterone sulphate and N-oxide abiraterone sulphate via CYP3A4 and SULT2A1
Bioavailability: Systemic exposure is increased by food
Half-life elimination: 14.4 to 16.5 hours (Acharya 2012); prolonged in patients with mild and moderate hepatic impairment, ~18 and ~19 hours, respectively
Time to peak: 2 hours (Acharya 2012)
Excretion: Feces (~88%); urine (~5%)
Hepatic function impairment: After a single oral 1,000 mg dose (Zytiga), systemic exposure increased ~1.1- and 3.6-fold in subjects with mild and moderate hepatic impairment, respectively. The mean half-life was prolonged to ~18 hours and ~19 hours in subjects with mild and moderate impairment, respectively. Systemic exposure of abiraterone increased by 7- fold and the fraction of free drug increased by 2-fold in subjects with severe baseline hepatic impairment. Mean protein binding was found to be lower in patients with severe hepatic impairment.
