abiraterone acetate

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abiraterone acetate


Pharmacologic class: CYP17 inhibitor

Therapeutic class: Antineoplastic

Pregnancy risk category X


Converts from abiraterone acetate in vivo to abiraterone, an androgen biosynthesis inhibitor that inhibits 17α-hydroxylase/C17,20-lyase (CYP17), an enzyme that's expressed in testicular, adrenal, and prostatic tumor tissues and is required for androgen biosynthesis, thereby causing androgen-sensitive prostatic carcinoma to respond to such treatment that decreases androgen levels


Tablets: 250 mg

Indications and dosages

Metastatic castration-resistant prostate cancer in combination with prednisone in patients who have received prior chemotherapy containing docetaxel

Adults: 1,000 mg P.O. daily in combination with prednisone 5 mg P.O. b.i.d.

Dosage adjustment

• Baseline moderate hepatic impairment (Child-Pugh Class B)


• Pregnancy

• Women of childbearing age


Use cautiously in:

• mild to moderate hepatic disease, mineralocorticoid excess, adrenocortical insufficiency, CV disease

• co-administration of CYP2D6 substrates with a narrow therapeutic index (avoid use or if alternative treatments can't be used, consider a dosage reduction of the concomitant CYP2D6 substrate)

• co-administration of strong inhibitors and inducers of CYP3A4 (avoid or use with caution)

• breastfeeding women

• children (safety and efficacy not established).


Be aware that pregnant women and women of childbearing age shouldn't handle drug without wearing gloves.

• Control hypertension and correct hypokalemia before starting drug.

• Give tablets whole and be aware that patient shouldn't eat for at least 2 hours before drug is administered and for at least 1 hour after drug is administered.

Don't use in patients with baseline severe hepatic impairment (Child-Pugh Class C).

• Withhold drug in patients who develop hepatotoxicity during treatment until recovery. May restart drug at a reduced dosage.

Discontinue drug if patient develops severe hepatotoxicity.

• Be aware that safety isn't established in patients with left ventricular ejection fraction less than 50% or New York Heart Association Class III or IV heart failure.

Adverse reactions

CV: hypertension, arrhythmia, heart failure

GI: diarrhea, dyspepsia

GU: urinary tract infection, urinary frequency, nocturia

Hepatic: hepatotoxicity

Metabolic: hypokalemia, mineralocorticoid excess with fluid retention, adrenocortical insufficiency,

hyperosmolar coma or death Musculoskeletal: joint swelling or discomfort, muscle discomfort, fractures, musculoskeletal and connective tissue disorders

Respiratory: cough, upper respiratory tract infection

Other: fluid retention, edema, hot flushes, chest pain or discomfort


Drug-drug. CYP2D6 substrates with a narrow therapeutic index (such as thioridazine): increased CYP2D6 substrate Cmax and area under the curve (AUC) CYP3A4 inducers (such as carbamazepine, phenobarbital, phenytoin, rifabutin, rifapentine, rifampin): unknown effects Strong CYP3A4 inhibitors (such as atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole): unknown effects

Drug-diagnostic tests. ALT, AST, triglycerides, total bilirubin): increased levels

Potassium: reduced level

Drug-food. Any food: increased abiraterone AUC

Patient monitoring

• Monitor hepatic function tests closely and modify, interrupt, or discontinue dosing as prescribed.

• Monitor blood pressure, serum potassium level, and signs and symptoms of fluid retention at least monthly.

• Monitor patient for signs and symptoms of adrenocortical insufficiency (such as hypoglycemia, hypotension, orthostatic hypotension, dehydration, weight loss, and nausea and vomiting); be aware that increased dosage of corticosteroids may be indicated before, during, and after stressful situations.

Patient teaching

• Tell patient to swallow tablets whole with water on an empty stomach (don't eat for at least 2 hours before taking drug and for at least 1 hour after taking drug).

• Instruct patient to take drug with prednisone as prescribed and not to interrupt or stop either drug without consulting prescriber.

• Instruct patient to report joint or muscle discomfort, urinary or respiratory tract infection, urinating more frequently or during the night, dizziness on standing, extreme thirst, or weight loss.

Advise pregnant women and women of childbearing age not to handle drug without wearing gloves.

• Advise male patient of child-producing age to use a condom and another effective contraceptive during therapy if having sex with a woman of childbearing potential.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and food mentioned above.

McGraw-Hill Nurse's Drug Handbook, 7th Ed. Copyright © 2013 by The McGraw-Hill Companies, Inc. All rights reserved

Lockerbie Bomber's cancer drug

A popular term for an anti-androgenic agent which results in a 36% increase in average survival and reduced pain in men with advanced castration-resistant metastatic prostate cancer.

Adverse effects
Joint swelling and discomfort, hypokalaemia, oedema, muscle discomfort, hypophosphataemia, hot flushing, diarrhoea, urinary tract infection, cough.
Segen's Medical Dictionary. © 2012 Farlex, Inc. All rights reserved.
References in periodicals archive ?
(Nasdaq: TROV), a clinical-stage, Precision Cancer Medicine oncology therapeutics company developing drugs that target cell division (mitosis), for the treatment of various cancers including prostate, colorectal and leukemia, today announced the presentation of positive clinical data from its ongoing Phase 2 clinical trial of onvansertib in combination with Zytiga (abiraterone acetate)/prednisone, an androgen-receptor signaling (ARS) inhibitor, in metastatic Castration-Resistant Prostate Cancer (mCRPC), at the 20th Asia-Pacific Prostate Cancer Conference in Melbourne, Australia.
Trovagene announced the presentation of positive clinical data from its ongoing Phase 2 clinical trial of onvansertib in combination with Zytiga (abiraterone acetate)/prednisone, an androgen-receptor signaling inhibitor, in metastatic Castration-Resistant Prostate Cancer, at the 20th Asia-Pacific Prostate Cancer Conference in Melbourne, Australia.
Previously, she served as global regulatory lead at Baxter Biosciences, leading Vonvendi (recombinant von Willebrand Factor) approval/launch, senior director Regulatory Affairs at Ambit Biosciences, and director Regulatory Affairs at Cougar Biotechnology, a unit of Johnson and Johnson Ortho Biotech Oncology, where she led the approval of Zytiga, abiraterone acetate, for the treatment of patients with metastatic castrate-resistant prostate cancer.
13, 2019 (HealthDay News) -- Elderly prostate cancer patients with preexisting cardiovascular diseases (CVDs) using abiraterone acetate (AA) or enzalutamide (ENZ) have higher short-term mortality compared with their counterparts without CVDs, according to a study published online Aug.
ZYTIGA (abiraterone acetate), an oral, once-daily medication for use in combination with prednisone for the treatment of metastatic, castration-resistant prostate cancer due to biosimilar and generic entrants.
Active pharmaceutical ingredients (API) company MSN Labs, the parent company of Novadoz Pharmaceuticals, reported on Monday the receipt of US FDA approval to market Abiraterone Acetate 250mg tablets in 120 tablet count bottles for the treatment of prostate cancer with a steroid medication (prednisone or methylprednisolone).
(30) A significant improvement in median OS was seen for ADT plus abiraterone acetate and prednisone (AAP) compared to ADT plus placebo (not yet reached [NYR] vs.
In 2011, abiraterone acetate (abiraterone) was approved by the United States Food and Drug Administration for the treatment of metastatic CRPC.
Ileana et al., "Antitumour activity of abiraterone acetate against metastatic castration-resistant prostate cancer progressing after docetaxel and enzalutamide (MDV3100)," Annals of Oncology, vol.
Chen et al., "Indirect comparison between abiraterone acetate and enzalutamide for the treatment of metastatic castration-resistant prostate cancer: a systematic review," Asian Journal of Andrology, vol.
Singapore, Singapore, February 29, 2016 --(PR.com)-- Scientists in Germany have discovered additional ways that hormone therapy using steroid synthesis inhibitor abiraterone acetate (AA) could deliver great help in treating advanced prostate cancer (PC) patients.
APP-111 is a first-in-class oral, antitubulin targeting agent for the potential treatment for the form of castration resistant prostate cancer that does not respond or becomes resistant to currently available androgen receptor antagonists like Xtandi (enzalutamide) and testosterone reducing agents like Zytiga (abiraterone acetate and prednisone).