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Polymorphism in Drug
Transporters - Pgp
MDR1 is the gene that codes P-glycoprotein.
15 mutations in MDR1
C3435T polymorphism correlates w/ Pgp expression in
the intestine.
C/C = high expression of intestinal Pgp
C/C is prevalent in West Africans (83%) and African
Americans (61%), and less so in caucasians (26%)
and Japanese (34%).
High intestinal Pgp causes reduced bioavailability of
certain Pgp substrates: HIV drugs nelfinavir, ritonavir,
and saquinavir; also cyclosporine.
AAPS Newsmagazine, January 2002.
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