More effective Vidaza in the future

[Birgitta-A]

Hi all,
Now the reseachers perhaps have found an azacytidine (Vidaza) variant with enhanced efficacy. Researchers believe that therapy resistance is frequently caused by the fact that not enough of Vidaza gets into the interior of the cells, because cancer cells lack particular transport molecules in the cell membrane.

A Norwegian company has produced an azacytidine variant with modified chemical properties. It is called CP-4200 and is a coupled product of azacytidine and a fatty acid (elaidic acid). When cancer cells in the culture dish are treated with CP-4200, the amount of methyltransferase molecules in the interior of the cells is reduced.
http://checkorphan.getreelhealth.com...nticancer-drug
Kind regards
Birgitta-A

[Neil Cuadra]

A number of websites picked up that dkfz press release. No word yet on what the next tests for CP-4200 will be.

From their description, it seems to me that the same technique (coupling the drug with a fatty acid) might improve efficacy with decitabine (Dacogen) too, because both are hypomethylating agents.

[Birgitta-A]

Hi Neil,
No, nothing about next step in those press releases but Dr Silverman and Dr Holland at Mount Sinai School of Medicine have a patent application called AZACYTIDINE ANALOGUES AND USES THEREOF dated 08-20-2009.

They write:"...The cytotoxic activity of 5-Aza-C-5'-elaidic acid was not only maintained but increased 50-fold when the hENT1 and hENT2 nucleoside transporters were blocked by the use of dipyridamole. The increased activity in cells where the nucleoside transporters are blocked by dipyridamole is surprising, and may indicate even higher activity in patients with resistance to treatment caused by lack of nucleoside transporters."

They seem to look at both Vidaza and Dacogen.
http://www.faqs.org/patents/app/20090209482
Kind regards
Birgitta-A

[ann]

Wonderful! Any news like this is so great for those who have not had good luck with the treatments they have been getting.

[tonydewitt]

Looks like that company is going at attached the fatty acid not only to Vizada (azacytidine becomes CP-4200), but also to Gemzar (gemcitabine becomes CP-4126). If their research is true, having the fatty acid attached to these known cancer drugs will improve their cellular uptake since they're less dependent on the nucleoside transporters, which supposedly improves their efficacy against various cancers. Hooray!

[lfeinsmith]

Originally Posted by tonydewitt

Looks like that company is going at attached the fatty acid not only to Vizada (azacytidine becomes CP-4200), but also to Gemzar (gemcitabine becomes CP-4126). If their research is true, having the fatty acid attached to these known cancer drugs will improve their cellular uptake since they're less dependent on the nucleoside transporters, which supposedly improves their efficacy against various cancers. Hooray!

Sounds interesting.
I just back from Md anderson .I have MDS since 2006 untreated.Now because my platelet count is lo 20000 and ANC is around 500-600 TREATMENT IS RECOMMENDED.
1) FIRST RECOMMENDATION DECABITINE (DACOGEN) 3 DAYS A WEEK
2) SECOND CHOICE IS AN ORAL FORM OF VIDAZA THIS WOULD BE PHASE 2 TRIAL WHICH STARTS IN AUGUST.

A CONFERENCE CALL IS SET UP FOR MONDAY THE 30TH APRIL (TODAY)
NO MENTION OF CP-4200