The main objective of the current study is to quantitatively characterize the anticancer effects of CIS and CIM as single agents and combinations in two cancer cell lines, OCT2-negative liver cancer cell line, Huh7, and OCT2-positive breast cancer cell line, MDA-MB-468, using a combination of experimental data and in vitro pharmacodynamic (PD) modeling approaches. Here, SLC22A2 is linked to breast carcinoma.