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Hi all!
Does anyone have any suggestions for inhibitors of BCRP efflux
transport that can be dosed in animals?
I know of a couple: Iressa (gefitinib) and a non commercial GSK
compound (GF 120918). ....Sigma does not seem to sell either..
Does anyone have suggestions for obtaining these compounds? Does
anyone have ideas for other inhibitors of this transporter that
we have not come across?
Thanks in advance for your help!
-Rachel Mandell
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Dear Rachell
The following drugs are effective inhibitirs of BCRP:
1. Imatinib
2. 4-anilino quinazolines
3. Flavanoids like chrysin, biochanin A and Benzoflavone
4. HIV protease inhibitors like Ritonavir, Saquinavir and Nelfinavir
5. Cyclosporin A, Tacrolimus and Sirolimus
6. Dihydropyridines like niguldipine, nicardipine and nitrendipine
i think you may go for the best one as for your experimental objective
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The following message was posted to: PharmPK
Rachel,
look at: Mol Cancer Ther. 2002 Apr;1(6):417-25. Potent and specific
inhibition of the breast cancer resistance protein multidrug
transporter in
vitro and in mouse intestine by a novel analogue of fumitremorgin C.
Allen
JD, van Loevezijn A, Lakhai JM, van der Valk M, van Tellingen O, Reid G,
Schellens JH, Koomen GJ, Schinkel AH.
Prof G Koomen is the person to get in touch with for request of the
Bcrp1
inhibitor used in the above study/publication. He has retired from the
University of Amsterdam (Laboratory of Organic Chemistry, Institute of
Molecular Chemistry, University of Amsterdam, Amsterdam, the
Netherlands)
but as far as I know he is the key person to ask for Ko143, a pretty
strong
and selective Bcrp1/ BCRP inhibitor
Regards
Hans
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The following message was posted to: PharmPK
Dear Rachel
Try out with cyclosporin A, tacrolimus and sirolimus,
(immunosuppressants), if in case GF 120918, Iressa (gefitinib) are
unavailable as several recent studies have demonstrated significant
BCRP-mediated efflux inhibitory activity of immunosuppresants.
Regards
Shravan Kumar.Eduru
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