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Abiraterone: Drug information

Abiraterone: Drug information
(For additional information see "Abiraterone: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Yonsa;
  • Zytiga
Brand Names: Canada
  • APO-Abiraterone;
  • JAMP Abiraterone;
  • JAMP-Abiraterone;
  • MAR-Abiraterone;
  • NAT-Abiraterone;
  • PMS-Abiraterone;
  • REDDY-Abiraterone;
  • Sandoz Abiraterone;
  • Zytiga
Pharmacologic Category
  • Antiandrogen;
  • Antineoplastic Agent, Antiandrogen
Dosing: Adult

Note: Patients receiving abiraterone should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently (or have had a bilateral orchiectomy). Control BP and correct hypokalemia prior to and during treatment. 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. Refer to "Administration" for information regarding an alternate abiraterone (Zytiga) administration method using a lower dose.

Prostate cancer, metastatic, castration-resistant

Prostate cancer, metastatic, castration-resistant:

Zytiga: Oral: 1,000 mg once daily (in combination with prednisone 5 mg twice daily) (Ref).

Yonsa (micronized formulation): Oral: 500 mg once daily (in combination with methylprednisolone 4 mg twice daily).

Prostate cancer, metastatic, high-risk, castration-sensitive

Prostate cancer, metastatic, high-risk, castration-sensitive: Zytiga: Oral: 1,000 mg once daily (in combination with prednisone 5 mg once daily) (Ref)

or (off-label combination; Zytiga) Oral: 1,000 mg once daily (in combination with prednisolone 5 mg once daily) (Ref).

Prostate cancer, synchronous metastatic, castration-sensitive

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], filgrastim, 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.

Dosing: Kidney Impairment: Adult

No dosage adjustment necessary.

Dosing: Hepatic Impairment: Adult

Hepatic impairment prior to treatment initiation:

Mild (Child-Pugh class A): No dosage adjustment necessary.

Moderate (Child-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-Pugh class C): Do not use.

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.

Dosing: Older Adult

Refer to adult dosing.

Dosing: Adjustment for Toxicity: Adult

Adrenocortical insufficiency: Increased corticosteroid doses may be required before, during, and after stress.

Hepatotoxicity: Refer to "Dosing: Hepatic Impairment".

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.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Yonsa: 125 mg

Zytiga: 250 mg, 500 mg

Generic: 250 mg, 500 mg

Generic Equivalent Available: US

Yes

Dosage Forms Considerations

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.

Dosage Forms: Canada

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

Administration: Adult

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 Drugs Handling Considerations

Hazardous agent (NIOSH 2016 [group 1]).

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 2016; USP-NF 2020).

Use: Labeled Indications

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])

Medication Safety Issues
Sound-alike/look-alike issues:

Abiraterone may be confused with apalutamide

Zytiga may be confused with Jevtana, Xgeva, Xofigo, Xtandi, Zometa, Zydelig

Other safety concerns:

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.

Adverse Reactions

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

Contraindications

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.

Warnings/Precautions

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. Increased corticosteroid doses may be required before, during, and after stress.

• 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). Concomitant administration with corticosteroids reduces the incidence and severity of these adverse 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. Monitor at least monthly for hypertension, hypokalemia, and fluid retention.

• 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. Antidiabetic medication dosage adjustments may be needed.

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.

Other warnings/precautions:

• Food: The manufacturer for abiraterone (Zytiga) recommends administering on an empty stomach (administer at least 1 hour before and 2 hours after any food); abiraterone AUC (exposure) may be increased up to 10-fold if administered with a meal. Abiraterone micronized (Yonsa) may be administered without regard to food.

Metabolism/Transport Effects

Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits CYP2C8 (weak), CYP2D6 (moderate)

Drug Interactions

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 Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Ajmaline: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Ajmaline. Risk C: Monitor therapy

Amitriptyline: CYP2D6 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of Amitriptyline. CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Amitriptyline. Risk C: Monitor therapy

Amoxapine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Amoxapine. Risk C: Monitor therapy

Amphetamines: CYP2D6 Inhibitors (Moderate) may increase the 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 therapy

Androgens: Hypertension-Associated Agents may enhance the hypertensive effect of Androgens. Risk C: Monitor therapy

ARIPiprazole: CYP2D6 Inhibitors (Moderate) may increase the 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 therapy

ARIPiprazole Lauroxil: CYP2D6 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of ARIPiprazole Lauroxil. Risk C: Monitor therapy

Atomoxetine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Atomoxetine. Risk C: Monitor therapy

Brexpiprazole: CYP2D6 Inhibitors (Moderate) may increase the 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 therapy

Carvedilol: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Carvedilol. Risk C: Monitor therapy

Choline C 11: Antiandrogens may diminish the therapeutic effect of Choline C 11. Risk C: Monitor therapy

ClomiPRAMINE: CYP2D6 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of ClomiPRAMINE. CYP2D6 Inhibitors (Moderate) may increase the serum concentration of ClomiPRAMINE. Risk C: Monitor therapy

CloZAPine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of CloZAPine. Risk C: Monitor therapy

Codeine: CYP2D6 Inhibitors (Moderate) may diminish the therapeutic effect of Codeine. These CYP2D6 inhibitors may prevent the metabolic conversion of codeine to its active metabolite morphine. Risk C: Monitor therapy

CYP3A4 Inducers (Moderate): May decrease the serum concentration of Abiraterone Acetate. Risk C: Monitor therapy

CYP3A4 Inducers (Strong): May decrease the serum concentration of Abiraterone Acetate. Management: Avoid when possible. If the combination cannot be avoided, increase abiraterone acetate dosing frequency from once daily to twice daily during combined use. Reduce abiraterone dose back to the prior dose and frequency once strong inducer is discontinued. Risk D: Consider therapy modification

Daprodustat: CYP2C8 Inhibitors (Weak) may increase the serum concentration of Daprodustat. Risk C: Monitor therapy

Desipramine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Desipramine. Risk C: Monitor therapy

Deutetrabenazine: CYP2D6 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of Deutetrabenazine. Risk C: Monitor therapy

Dextromethorphan: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Dextromethorphan. Risk C: Monitor therapy

Doxepin (Systemic): CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Doxepin (Systemic). Risk C: Monitor therapy

Doxepin (Topical): CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Doxepin (Topical). Risk C: Monitor therapy

DOXOrubicin (Conventional): CYP2D6 Inhibitors (Moderate) may increase the serum concentration of DOXOrubicin (Conventional). Risk X: Avoid combination

Eliglustat: CYP2D6 Inhibitors (Moderate) may increase the 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 the serum concentration of Flecainide. Risk C: Monitor therapy

Gallium Ga 68 PSMA-11: Antiandrogens may diminish the therapeutic effect 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 the serum concentration of Haloperidol. Risk C: Monitor therapy

HMG-CoA Reductase Inhibitors (Statins): Abiraterone Acetate may enhance the myopathic (rhabdomyolysis) effect of HMG-CoA Reductase Inhibitors (Statins). Risk C: Monitor therapy

Iboga: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Iboga. Risk C: Monitor therapy

Iloperidone: CYP2D6 Inhibitors (Moderate) may decrease serum concentrations of the active metabolite(s) of Iloperidone. Specifically, concentrations of the metabolite P95 may be decreased. CYP2D6 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of Iloperidone. Specifically, concentrations of the metabolite P88 may be increased. CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Iloperidone. Risk C: Monitor therapy

Imipramine: CYP2D6 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of Imipramine. Concentrations of desipramine may be increased. CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Imipramine. Risk C: Monitor therapy

Indium 111 Capromab Pendetide: Antiandrogens may diminish the diagnostic effect of Indium 111 Capromab Pendetide. Risk X: Avoid combination

Indoramin: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Indoramin. Risk C: Monitor therapy

Lofepramine: CYP2D6 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of Lofepramine. The active metabolite of lofepramine is desipramine. Risk C: Monitor therapy

Mequitazine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Mequitazine. Risk X: Avoid combination

Metoclopramide: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Metoclopramide. Risk C: Monitor therapy

Metoprolol: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Metoprolol. Risk C: Monitor therapy

Nebivolol: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Nebivolol. Risk C: Monitor therapy

Nortriptyline: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Nortriptyline. Risk C: Monitor therapy

Oliceridine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Oliceridine. Risk C: Monitor therapy

Olmutinib: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Olmutinib. Risk C: Monitor therapy

PARoxetine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of PARoxetine. Risk C: Monitor therapy

Perhexiline: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Perhexiline. Risk C: Monitor therapy

Perphenazine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Perphenazine. Risk C: Monitor therapy

Piflufolastat F18: Antiandrogens may diminish the diagnostic effect of Piflufolastat F18. 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 the serum concentration of Pimozide. Risk C: Monitor therapy

Pitolisant: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Pitolisant. Risk C: Monitor therapy

Propafenone: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Propafenone. Risk C: Monitor therapy

Propranolol: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Propranolol. Risk C: Monitor therapy

Protriptyline: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Protriptyline. Risk C: Monitor therapy

Radium Ra 223 Dichloride: May enhance the adverse/toxic effect of Abiraterone Acetate. Specifically, the risk for fractures and death may be increased. Risk X: Avoid combination

Repaglinide: CYP2C8 Inhibitors (Weak) may increase the serum concentration of Repaglinide. Risk C: Monitor therapy

Rifabutin: May decrease the serum concentration of Abiraterone Acetate. Risk C: Monitor therapy

Rifapentine: May decrease the serum concentration of Abiraterone Acetate. Risk C: Monitor therapy

RisperiDONE: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of RisperiDONE. Risk C: Monitor therapy

Sertindole: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Sertindole. Risk C: Monitor therapy

Solriamfetol: May enhance the hypertensive effect of Hypertension-Associated Agents. Risk C: Monitor therapy

Spironolactone: May diminish the therapeutic effect 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 serum concentrations of the active metabolite(s) 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 the serum concentration of Tamsulosin. Risk C: Monitor therapy

Tetrabenazine: CYP2D6 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of Tetrabenazine. Specifically, concentrations of the active alpha- and beta-dihydrotetrabenazine metabolites may be increased. Risk C: Monitor therapy

Thiazolidinediones: Abiraterone Acetate may enhance the hypoglycemic effect of Thiazolidinediones. Risk C: Monitor therapy

Thioridazine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Thioridazine. Risk X: Avoid combination

Timolol (Systemic): CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Timolol (Systemic). Risk C: Monitor therapy

TraMADol: CYP2D6 Inhibitors (Moderate) may decrease serum concentrations of the active metabolite(s) of TraMADol. CYP2D6 Inhibitors (Moderate) may increase the serum concentration of TraMADol. Risk C: Monitor therapy

Trimipramine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Trimipramine. Risk C: Monitor therapy

Valbenazine: CYP2D6 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of Valbenazine. Risk C: Monitor therapy

Vortioxetine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Vortioxetine. Risk C: Monitor therapy

Zuclopenthixol: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Zuclopenthixol. Risk C: Monitor therapy

Food Interactions

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.

Reproductive Considerations

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.

Pregnancy Considerations

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.

Breastfeeding Considerations

It is not known if abiraterone is present in breast milk. Abiraterone is not indicated for use in females.

Monitoring Parameters

ALT, AST, and bilirubin prior to treatment, every 2 weeks for 3 months and monthly thereafter; if baseline moderate hepatic impairment (Child-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.

Mechanism of Action

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.

Pharmacokinetics (Adult Data Unless Noted)

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%)

Pharmacokinetics: Additional Considerations (Adult Data Unless Noted)

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.

Pricing: US

Tablets (Abiraterone Acetate Oral)

250 mg (per each): $1.60 - $97.21

500 mg (per each): $195.51 - $206.85

Tablets (Yonsa Oral)

125 mg (per each): $100.54

Tablets (Zytiga Oral)

250 mg (per each): $108.87

500 mg (per each): $217.74

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.

Brand Names: International
  • Abiratred (TH, TW);
  • Abiron (LK);
  • Aizerone (LK);
  • Xbira (IN);
  • Zytica (ZW);
  • Zytiga (AE, AR, AT, AU, BB, BE, BH, BR, BZ, CH, CL, CN, CO, CR, CY, CZ, DE, DK, DO, EC, EE, EG, ES, FI, FR, GB, GR, GT, HK, HN, HR, HU, ID, IE, IL, IS, JO, JP, KR, KW, LB, LK, LT, LU, LV, MT, MX, MY, NI, NL, NO, NZ, PA, PH, PL, PT, QA, RO, RU, SA, SE, SG, SI, SK, SV, TH, TR, TW, VN);
  • Zytix (BD);
  • Zyvalyx (EC)


For country code abbreviations (show table)
  1. <800> Hazardous Drugs–Handling in Healthcare Settings. United States Pharmacopeia and National Formulary (USP 43-NF 38). Rockville, MD: United States Pharmacopeia Convention; 2020:74-92.
  2. Acharya M, Bernard A, Gonzalez M, et al. Open-Label, Phase I, Pharmacokinetic Studies of Abiraterone Acetate in Healthy Men. Cancer Chemother Pharmacol. 2012;69(6):1583-1590. [PubMed 22526411]
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  20. Yonsa (abiraterone acetate) [prescribing information]. Cranbury, NJ: Sun Pharmaceutical Industries Inc; June 2018.
  21. Yonsa (abiraterone acetate) [prescribing information]. Cranbury, NJ: Sun Pharmaceutical Industries Inc; March 2022.
  22. Zytiga (abiraterone) [prescribing information]. Horsham, PA: Janssen Biotech Inc; October 2020.
  23. Zytiga (abiraterone) [prescribing information]. Horsham, PA: Janssen Biotech Inc; August 2021.
  24. Zytiga (abiraterone) [product monograph]. Toronto, Ontario, Canada: Janssen Inc; November 2021.
Topic 16083 Version 414.0

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