"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.
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.
I would not suggest anyone try to experiment on their own with this drug. I had a very severe reaction last spring which lasted all summer. I can not attribute it directly to Zytiga but I had just changed to the generic. Drug reactions can lead to a drug induced Lupus and trust me if that is what it was you do not want to go there. Follow the label until they have some scientific guidance that works for 90 percent of the population and remember we are all different ! What works for one may not work for all.
Agree and I wish we would not have experimented with the reduced dose. Only because of postings/opinions on here and due to threat of losing good insurance coverage late last year did we try reduction. Reduced dose with food did not work. If it’s working don’t mess with it.
Searching for Zytiga prices on the Internet produces crazy results. Typically they are above $11,000 per month, but then I saw a price for Zytiga at CVS pharmacy listed on WellRx for "as low as" $2,735 for 120 pills, and the same in India for $1,265. And of course there are different prices depending on whether you pay cash or use insurance.
In the specific case of Zytiga, it seems to me that one big problem highlighted by the article that Patrick cited is that the the solubility and bioavailability of Zytiga isn't just a matter of whether you take it with food or not. It matters hugely which food you take it with. The effective dose of the drug taken with one food might be double the dose on an empty stomach, but with another food it might be 10 times the dose on an empty stomach. So what we really want is for the drug to be formulated with a specific dose of a specific food built right into the tablet or capsule, together with rules on what else may or may not be eaten and when, so that the lower dose can be taken safely.
Of course all of this only works if 1) the price of the drug is actually proportional to the dosage (does it really cost 4 times as much to manufacture one gram of Zytiga as it costs to manufacture 250 mg? Or is the drug price mostly made up of marketing costs, profits, research costs, payments for loans, etc.), and 2) we have a rational system for pricing drugs in the United States. Neither of these conditions obtain. Manufacturing cost and pricing algorithms for drugs are buried as deep as the drug companies can bury them, and rationality in drug pricing is probably years away, if that.
Depotdoug raised this topic a month ago and the discussion and references were very informative for anyone wanting to get up to speed. This may be a good advance. Thanks PJ.
Not sure how to do that. Have just read it and while its an interesting paper and above my full understanding, it's not really relevant to us. It's about the techniques to make abi more absorbable from the manufacturer's view, not how patients can take less by modifying the conditions under which they take it. When I get the time I'll message you and Patrick to arrange a copy. Give me a day, I've got a bit on.
This is a US issue. Most of the rest of the civilised world get it free. I’ve been on 1000mg for the last eight years all free of charge.
I understand you Americans don’t believe in free healthcare for all for some crazy reason, but when taking Zytiga, and the possible fluctuations in dosage through taking it with food, it shows how desperate you are for cheap meds. To pay $10,000+ for a drug available in India for $500 is a disgrace. You’re being taken for a ride my friends.
The "dramatic positive food effect (5 to 10-fold)" is based on low-fat & high-fat meals. Since fat is the key to absorption, it makes sense to shoot for the 10-fold response, using 10% of the regular dose.
For men faced with high out-of-pocket cost, this approach is very attractive, but the authors also point out that that reducing the dose by 90% would also reduce side effects, as well as the burden on the body.
They cite the precedent of non-oncology drugs, where 8 out of 9 of those where uptake is enhanced by food, are labeled to be taken with food.
The bulk of the paper deals with approaches that the manufacturer might use, in order to increase uptake & lower the dose. I doubt that the price would change much.
For men interested in dosing with food, a supportive doctor is essential IMO.
Yes, careful monitoring is necessary. The problem is that although a dose of 25% (250mg) with a cup of full fat yoghurt is probably ok for most, (and if that does't work, in the absence of side effects, slowly increasing dose), for a percentage of men it could result in severe side effects due to over-dosing. Probably the best way is to start at a dosage of 10% (100mg) and slowly increasing while monitoring for PSA reaction and side effects.
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