Aims Capmatinib, an orally bioavailable, highly potent and selective MET inhibitor, was recently approved to treat adult patients with metastatic non-small cell lung cancer with METex14 skipping mutations. The study investigated the effect of capmatinib on the pharmacokinetics of a single oral dose of digoxin and rosuvastatin, administered orally as a two-drug cocktail in patients with MET-dysregulated advanced solid tumors. Methods This was a multicenter, open-label, single-sequence study. An oral drug cocktail containing 0.25 mg digoxin and 10 mg rosuvastatin was administered to adult patients with MET-dysregulated advanced solid tumors on Day 1, and then on Day 22 with capmatinib. Between Days 11 and 32, capmatinib 400 mg was administered twice daily to ensure the attainment of steady state for drug-drug interaction (DDI) assessment. Pharmacokinetics of cocktail drugs and safety of capmatinib were evaluated. Results Thirty-two patients (median age: 61.5 years) were enrolled. Co-administration of capmatinib increased digoxin Cmax, and AUCinf by 74%, and 47%, respectively. Co-administration of capmatinib increased rosuvastatin Cmax, and AUCinf by 204%, and 108%, respectively. Most frequent adverse events (AEs; ≥25% for all grades) were nausea (56.3%), asthenia (43.8%), constipation and vomiting (40.6%, each), peripheral edema (28.1%) and pyrexia (25%). Most frequent Grade 3/4 AEs (≥5%) were anemia and pulmonary embolism (9.4%, each), asthenia, dyspnea, nausea and vomiting (6.3%, each). Conclusion This study demonstrated that capmatinib is an inhibitor of P-gp as well as BCRP transporters, with clinically relevant DDI potential. Capmatinib was well-tolerated and no unexpected safety concerns were observed.