New paper below [1].
As many know [2]:
"Administration {of Abi} with food increases absorption of the drug and thus has the potential to result in increased and highly variable exposures; the drug should be consumed on an empty stomach at least one hour before or two hours after food."
But Abi is expensive &, taken with a high-fat meal, the cost might be reduced by 90%.
"Its low solubility and high lipophilicity lead to poor oral bioavailability (<10%) and a dramatic positive food effect (5 to 10-fold)."
"Specific emphasis of this review is placed on enabling oral formulation strategies that can improve solubilization and bioavailability, reduce the clinical dose and remove the pharmaceutical food effect to ultimately provide prostate cancer patients with a more efficient formulation with greater patient compliance."
Access isn't free. The strategy needs to be made available to the group IMO.
-Patrick
[1] ncbi.nlm.nih.gov/pubmed/319...
Int J Pharm. 2020 Jan 22:119069. doi: 10.1016/j.ijpharm.2020.119069. [Epub ahead of print]
Oral formulation strategies to improve the bioavailability and mitigate the food effect of abiraterone acetate.
Schultz HB1, Meola TR1, Thomas N1, Prestidge CA2.
Author information
1
University of South Australia Cancer Research Institute, Adelaide, South Australia 5000, Australia; ARC Centre of Excellence in Convergent Bio-Nano Science and Technology, University of South Australia, Mawson Lakes Campus, Mawson Lakes 5095, Australia.
2
University of South Australia Cancer Research Institute, Adelaide, South Australia 5000, Australia; ARC Centre of Excellence in Convergent Bio-Nano Science and Technology, University of South Australia, Mawson Lakes Campus, Mawson Lakes 5095, Australia. Electronic address: clive.prestidge@unisa.edu.au.
Abstract
Abiraterone acetate, marketed as Zytiga®, is an antiandrogen medication used in the treatment of prostate cancer. Abiraterone acetate is a BCS Class IV compound associated with several oral delivery challenges. Its low solubility and high lipophilicity lead to poor oral bioavailability (<10%) and a dramatic positive food effect (5 to 10-fold). Hence, a large dose of abiraterone acetate (1000 mg per day) is prescribed to patients who must fast for at least 1 hour before and 2 hours after administration. The recent expiry of Zytiga®s' patent has led to the emergence of publications describing improved oral formulation strategies for abiraterone acetate. This review aims to discuss the characteristics of abiraterone acetate that lead to its unfavorable oral delivery, examine the oral formulation strategies that have been applied, and to describe potential alternative oral formulation strategies that have been used for other BCS Class IV drugs, to determine the most valuable strategies to develop novel and improved alternatives to the current commercial product. Specific emphasis of this review is placed on enabling oral formulation strategies that can improve solubilization and bioavailability, reduce the clinical dose and remove the pharmaceutical food effect to ultimately provide prostate cancer patients with a more efficient formulation with greater patient compliance.
Copyright © 2020. Published by Elsevier B.V.
KEYWORDS:
Abiraterone acetate; bioavailability; food effect; oral delivery; poorly water-soluble drug; prostate cancer
PMID: 31981706 DOI: 10.1016/j.ijpharm.2020.119069