HER2 Support Group Forums - View Single Post - understanding what limits/allows the brain penetration of lapatinib(tykerb)

Lani · 12-08-2008, 01:18 PM

pGP and BCRP work like pumps at interfaces allowing in some compounds and rejecting and pumping back out others

various parts of the body where what is let in makes a life and death difference have specialized cells which contain them eg, cells in the absorbing parts of the gastrointestinal system, cells lining the airways (often NKT cells in those two loations) as well as the blood-brain barrier.

This study bred mice to lack either one or the other or both and found that when both were not available one had the most penetration of lapatinib, with more of it being pumped out and unavailable to the brain if only one or the other were lacking in the mice and the least penetration if both pGp and BRCP were present ie, not genetically bred out.

Hope this helps!

12-08-2008, 01:18 PM	#7
Lani Senior Member Join Date: Mar 2006 Posts: 4,783	pGP and BCRP work like pumps at interfaces allowing in some compounds and rejecting and pumping back out others various parts of the body where what is let in makes a life and death difference have specialized cells which contain them eg, cells in the absorbing parts of the gastrointestinal system, cells lining the airways (often NKT cells in those two loations) as well as the blood-brain barrier. This study bred mice to lack either one or the other or both and found that when both were not available one had the most penetration of lapatinib, with more of it being pumped out and unavailable to the brain if only one or the other were lacking in the mice and the least penetration if both pGp and BRCP were present ie, not genetically bred out. Hope this helps!