abiraterone

Action and Spectrum

Action: 

It targets CYP17A1 (17α-hydroxylase/17,20-lyase). The agents that help in androgenesis like testosterone which promote the growth of the prostate cancer cells. As a result, the overall androgen production is significantly reduced in the testes, adrenal glands and the tumour tissue due to the CYP17A1 inhibition by abiraterone and thus limiting the progression of the tumour. 

Drug Interaction

Adverse Reaction

Frequency defined:  

>10%:  

Edema (25%)  

Hypertension (9%)  

Hot flash (15%)  

Constipation (23%)  

Dyspepsia (6%)  

Urinary tract infection (12%)  

Bruise  

Increased serum alanine aminotransferase  

Fatigue  

Insomnia  

Arthralgia  

Joint swelling  

1%-10%  

Cardiac arrhythmia  

Cardiac failure  

Nocturia  

Headache  

Bone fracture  

Fever  

<1%:  

Adrenocortical insufficiency  

Black Box Warning

Black Box Warning  

None    

Contraindication / Caution

Contraindication /Caution: 

Cautions: 

Cardiovascular Disorders 

Moderate Liver Impairment 

Electrolyte Imbalances 

Diabetes 

Pregnancy / Lactation

Pregnancy/Lactation: 

Pregnancy consideration: Based on animal studies, it may cause harm to patients who can become pregnant.  

Lactation: Excretion of abiraterone in breast milk is not known.  

Pregnancy category:  

Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester.  

Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women.  

Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women  

Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits.  

Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women.  

Category N: There is no data available for the drug under this category.  

Pharmacology

Pharmacology     

Abiraterone is an antiandrogen class of antineoplastic drug. It is used to treat prostate cancer. 

Pharmacodynamics 

It targets CYP17A1 (17α-hydroxylase/17,20-lyase). The agents that help in androgenesis like testosterone which promote the growth of the prostate cancer cells. As a result, the overall androgen production is significantly reduced in the testes, adrenal glands and the tumour tissue due to the CYP17A1 inhibition by abiraterone and thus limiting the progression of the tumour. 

Pharmacokinetics 

Absorption 

The peak plasma time is 2 hours. 

Distribution
Abiraterone has a high affinity for plasma proteins, including albumin, and alpha-1 acid glycoprotein.

Metabolism
It is metabolized mainly in the liver.

Excretion and elimination
The major route of metabolism of abiraterone is through feces, which constitutes 88%, while urinary excretion accounts for 5%.
The terminal half-life of the drug is estimated to be about 12 h for abiraterone. 

Adminstartion

Administration    

The route of administration is oral. 

The drug can be taken with or without a meal. 

Patient Information Leaflet

Generic Name: abiraterone  

Pronounced: ae-bi-ra-te-ron  

Why do we use abiraterone?  

Abiraterone is an antiandrogen class of antineoplastic drug. It is used to treat cancer of the prostate gland.
Abiraterone has been effective for use in combination with prednisone/prednisolone for mCRPC patients who have demonstrated progression after or during receiving chemotherapy as mentioned including at least a period of docetaxel course.
It is also employed in the treatment of mHSPC when used with prednisone or prednisolone (neoadjuvant or concurrent with initial docetaxel).