While the clinical translation of many direct P-gp inhibition strategies has faced significant limitations due to toxicity, unfavorable pharmacokinetic interactions, and lack of sufficient efficacy in clinical trials [8,9,10,11], it is important to note that substantial progress has nonetheless been achieved in the overall treatment of hematological malignancies over the past decades despite the pervasive challenge of P-gp-mediated resistance. The gene discussed is PGP; the disease is hematologic disorder.