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Bis-[(p-methoxybenzyl)cyclopentadienyl] titanium dichloride, better known as Titanocene Y, is a newly synthesized titanium-based anticancer drug. We studied the antitumor activity of Titanocene Y with concentrations of 2.1, 21 and 210 micromol/l against a range of freshly explanted human tumors, using an in-vitro soft agar cloning system. The sensitivity against Titanocene Y was highly remarkable in the case of renal cell, ovarian, nonsmall cell lung and colon cancer. In particular the surprisingly good response of nonsmall cell lung cancer and colon cancer against Titanocene Y at its lowest concentration of 2.1 micromol/l was well comparable or better with respect to cisplatin, given at a concentration of 1.0 micromol/l. Further clinical development of Titanocene Y appears to be warranted because of the broad cytotoxic activity shown and the specific activity of Titanocene Y against renal cell cancer.

Bis-[(p-methoxybenzyl)cyclopentadienyl] titanium dichloride, better known as Titanocene Y, is a newly synthesized transition metal-based anticancer drug. We studied the antitumor activity of Titanocene Y with concentrations of 2.1, 21 and 210 micromol/l against a freshly explanted human breast cancer, using an in-vitro soft agar cloning system. The sensitivity against Titanocene Y was highly remarkable in the breast cancer tumor in the full concentration range. Titanocene Y showed cell death induction at 2.1 micromol/l, well comparable to cisplatin, given at a concentration of 1.0 micromol/l. A further preclinical development of Titanocene Y was warranted and therefore an MCF-7 human breast cancer xenograft nonobese diabetic/severe combined immunodeficient mouse model was used. Titanocene Y was given for 21 days at 30 mg/kg/day (75% of the maximum tolerable dose of Titanocene Y), which resulted in the reduction of the tumor volume to around one-third, whereas no mouse was lost because of the surprisingly low toxicity of Titanocene Y.

[1,2-di(cyclopentadienyl)-1,2-di(p-N,N-dimethylaminophenyl)-ethanediyl] titanium dichloride is a newly synthesized transition metal-based anti-cancer drug. We studied the anti-tumor activity of this drug (final concentrations: 25, 250 and 2,500 micromol/l) against freshly explanted human tumors, using an in vitro soft agar cloning system. A total of eight tumor samples were evaluated using 1-h exposures. Additionally, the breast carcinoma cell line MCF-7 was examined with regard to sensitivity. The tested compound was markedly active against one renal cancer sample, whereas other renal tumors were resistant. Concentration-dependent anti-tumor activity was demonstrated for all samples except for melanoma. At concentrations of 250 micromol/l or less, the compound was less active than cisplatin or equally active at 0.2 microg/ml, whereas at 2,500 micromol/l it showed a significant cytotoxic activity against a wide spectrum of tumor types. The highest activity was observed against renal carcinomas (three of three tumor specimens inhibited at 2,500 micromol/l). Sensitivity was also highly remarkable in the breast cancer cell line MCF-7 inhibited in a range of 25-2,500 micromol/l, whereas melanoma cells seemed to be profoundly resistant. Further clinical development of this drug appears warranted because of the broad cytotoxic activity shown.