Drug reference

Abiraterone

Hormonal Anticancer Agent · Treatment for metastatic castration-resistant prostate cancer

Also known as Abiraterone acetate

Hormonal Anticancer AgentTreatment for metastatic castration-resistant prostate cancerATC null

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

AmiodaroneSevereDatabaseDDInter
AmisulprideSevereDatabaseDDInter
AnagrelideSevereDatabaseDDInter
ApalutamideSevereDatabaseDDInter

Mechanism

It functions as an anti-androgen.

Indications

Metastatic castration-resistant prostate cancer in patients whose disease has progressed during or after treatment with a docetaxel-containing chemotherapy regimen (in combination with prednisone or prednisolone)Metastatic castration-resistant prostate cancer in patients who are asymptomatic or mildly symptomatic after failure of androgen deprivation therapy (in combination with prednisone or prednisolone) and before chemotherapy is indicatedMetastatic prostate cancer (castration-sensitive and castration-resistant)Prolongs survival in metastatic CRPC (chemotherapy-naïve or in those who have received previous docetaxel)Prolongs overall survival in men with metastatic castration-sensitive prostate cancer (in conjunction with ADT)

Dosing

Adult: indication] can be used, initially for up to 10 weeks, to manage troublesome hot ﬂushes caused by long-term androgen suppression; cyproterone acetate can be considered as an alternative if medroxyprogesterone acetate is not effective or not tolerated.…

Pharmacokinetics

Onset

Continuous administration increases adrenocorticotropic hormone levels, resulting in mineralocorticoid excess, necessitating coadministration with prednisone.

Bioavailability

Food significantly increases Cmax and AUC.

Metabolism

Metabolized by CYP3A4. Abiraterone acetate inhibits the highly polymorphic CYP2D6 and CYP2C8.

Side effects

Common

FatigueArthralgiaHypertensionNauseaEdemaHypokalemiaHot flushDiarrheaVomitingUpper respiratory tract infectionCoughHeadache

Serious

Mineralocorticoid excess (due to increased adrenocorticotropic hormone levels)
Increased risk of short-term mortality in elderly men with preexisting cardiovascular comorbidities
Anemia
Elevated alkaline phosphatase
Hypertriglyceridemia
Lymphopenia
Hypercholesterolemia
Hyperglycemia