Although silibinin might become a new candidate to clinically manage the undesirable lorlatinib-induced hypercholesterolemic and hyperlipidemic effects in human hepatic cells, further studies will be required to fully define the inhibitory potential of silibinin against the lorlatinib-metabolizing CYP3A4 isoenzyme when used as specific orally bioavailable formulations (e.g., Eurosil 85®) before suggesting its therapeutic combination with lorlatinib in a clinical setting with ALK-rearranged lung cancer patients. Here, ALK is linked to lung cancer.