Drug | Target | Influx | Metabolisma | Efflux | Refs. |
---|---|---|---|---|---|
Cytarabine (Ara-C) | DNA polymerases | ENT1, CNT3, OCTN1 | Activation: dCK, dCMPK, NDK. Inactivation: CDA, dCMPD, PN-I. | MRP4,7,8 | |
Daunorubicin (DNR) | DNA, Topoisomerase II | Passive diffusion | Â | P-gp, MRP1,7, BCRP | |
Mitoxantrone (MX) | DNA, Topoisomerase II | Passive diffusion | Â | P-gp, MRP1, BCRP | |
Etoposide (VP-16) | Topoisomerase II | Passive diffusion | Â | P-gp, MRP1-3,6, BCRP | |
Methotrexate (MTX) | DHFR, TS, AICARFT | RFC, PCFT | Aldehyde oxidase, FPGS (polyglutamylation) | P-gp, MRP1-5, BCRP | |
Venetoclax (VEN) | Bcl-2 | Passive diffusion | Â | P-gp | |
Gemtuzumab Ozogamicin (GO) | DNA | Ab-mediated endocytosis | Lysosomal Calicheamicin cleavage from Ab, glutathione | P-gp, MRP1 |