OY-101, an orally active compound, serves as a potent and specific inhibitor of P-glycoprotein (P-gp). It has the capability to sensitize drug-resistant tumors and counteract tumor multidrug resistance efficiently. Compared to Tetrandrine [1], OY-101 demonstrates enhanced water-solubility, cytotoxicity, and reversal activity.

OY-101与Vincristine在耐药性Eca109/VCR细胞中展现出卓越的协同抗癌效果，其IC50值为9.9 ± 1.3 nM^[1]。在0-5 μM浓度范围内，OY-101对Eca109/VCR细胞的毒性不显著，能够显著提升其对Vincristine的敏感性^[1]。

OY-101（每2天30 mg/kg，灌胃，连续3周）能提高机体对长春新碱的敏感性，同时未观察到明显毒性反应[1]。无论是静脉注射（3 mg/kg）还是口服（30 mg/kg），OY-101均展现出了优良的药代动力学特性[1]。