Using intraluminal perfusion of “in situ” ileum in anaesthetized rats bearing catheters into the portal vein and the common bile duct that permitted portal blood and bile sample collection, and in conscious rats in which a permanent intraarterial catheter had been implanted to carry out sequential blood sampling, the existence of enterohepatic circulation of the cytostatic drug Bamet-H2–Na[Pt(cholylgycinate- O, N) (cholylgycinate- O) Cl]–was investigated. Total platinum in serum, bile, ileum, liver, urine and feces was measured by flameless atomic absorption spectroscopy. After i.v. and i.g., 1 μmol Bamet-H2 or cisplatin administration, model-independent methods based on the theory of statistical moments were used in order to characterize the pharmacokinetics of Bamet-H2. The area under the curve from 0 to 168 h after i.v. administration (AUC 168) was significantly higher (+27%) for Bamet-H2 than for cisplatin. However, extrapolation from 0 to infinity indicated that AUC ∞ was lower for Bamet-H2 (−23%) than for cisplatin. The clearance (Cl ∞) for cisplatin was consistently lower (−23%) than for Bamet-H2. Ultrafiltration of serum collected at 168 h revealed that an important part of the Bamet-H2 (67%) and cisplatin (53%) remaining in the serum at this time was in the nonultrafiltrable form, i.e. probably bound, in part irreversibly, to serum macromolecules. When the rats received i.g. 1 μmol cisplatin or Bamet-H2, peak in serum concentrations of total platinum were markedly higher (6-fold) after Bamet-H2 than after cisplatin administration. The area under the curve was, also in this case, significantly higher for Bamet-H2 than for cisplatin (+98%). This was in part due to the enhanced intestinal absorption of Barnet-H2, as confirmed in experiments on perfused rat ileum, where an increase in portal serum Bamet-H2 concentrations was found. Moreover, markedly higher amount of the drug was found in ileum, liver and bile after perfusion with media containing Bamet-H2 as compared with experiments where cisplatin instead of Bamet-H2 was added to perfusion media. Moreover, after i.v. administration to conscious rats, excretion of Bamet-H2 by the kidney was lower (−51%) than that of cisplatin, while elimination of the former compound into feces was higher (+189%) than that of the latter. In sum, these results indicate that in addition to the previously reported cytostatic activity of Bamet-H2, this complex has interesting cholephilic characteristics, such as reduced urinary excretion together with enhanced intestinal absorption and biliary secretion, which are probably endowed by one or both cholylglycyl moieties bound to the platinum(II) atom in the Bamet-H2 molecule.