Gimatecan. DNA-intercalating drug DNA topoisomerase I inhibitor oncolytic

Drugs of the Future

Volumn 32, Issue 10, 2007, Pages 859-867

  Sorbera, L A ^a   Serradell, N ^a   Bolos J ^a   Rosa, E ^a   Bozzo, J ^a  

^a PROUS SCIENCE   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

ANTHRACYCLINE; BEVACIZUMAB; BORTEZOMIB; CAMPTOTHECIN; DNA TOPOISOMERASE; DNA TOPOISOMERASE INHIBITOR; ERLOTINIB; EVEROLIMUS; GIMATECAN; MITOXANTRONE; TAXANE DERIVATIVE; TOPOTECAN;

ADVANCED CANCER; ANEMIA; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; ASTHENIA; BONE MARROW SUPPRESSION; BREAST CANCER; CANCER MODEL; CANCER RESEARCH; CELL CYCLE; CLINICAL TRIAL; COMBINATION CHEMOTHERAPY; CONTROLLED CLINICAL TRIAL; CYTOTOXICITY; DIARRHEA; DOSAGE SCHEDULE COMPARISON; DRUG ABSORPTION; DRUG DOSE ESCALATION; DRUG DOSE REDUCTION; DRUG DOSE REGIMEN; DRUG EFFICACY; DRUG FORMULATION; DRUG POTENTIATION; DRUG SAFETY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; GASTROINTESTINAL TOXICITY; GLIOBLASTOMA; HUMAN; IN VITRO STUDY; LEIOMYOSARCOMA; LIPOPHILICITY; LUNG NON SMALL CELL CANCER; MELANOMA; MONOTHERAPY; MULTIPLE CYCLE TREATMENT; MYELODYSPLASTIC SYNDROME; NAUSEA; NEUROBLASTOMA; NEUTROPENIA; NONHUMAN; PROSTATE CARCINOMA; RANDOMIZED CONTROLLED TRIAL; THROMBOCYTOPENIA; TUMOR GROWTH; UNSPECIFIED SIDE EFFECT; VOMITING;

EID: 36749088078     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.2007.032.10.1144756     Document Type: Article

References (57)

1. Sawada, S., Nokata, K., Furuta, T., Yokokura, T., Miyasaka, T. Chemical modification of an antitumor alkaloid camptothecin: Synthesis and antitumor activity of 7-C-substituted camptothecins. Chem Pharm Bull 1991, 39(10): 2574-80.
2. Dallavalle, S., Ferrari, A., Biasotti, B. et al. Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity. J Med Chem 2001, 44(20): 3264-74.
3. Carminati, P., Penco, S., Zunino, F., Merlini, L. (Istituto Nazionale per lo Studio e la Cura dei Tumori; Sigma-Tau Industrie Farmaceutiche Riunite SpA). Camptothecin derivs. having antitumor activity. EP 1044977, JP 2002539128, US 2001008939, US 2004018988, US 6242457, US 6589939, WO 2000053607.
4. Marzi, M., Tinti, M.O., Alpegiani, M. et al. (Sigma-Tau Industrie Farmaceutiche Riunite SpA). Stereoselective process and crystalline forms of a camptothecin. WO 2006067092.
5. Yan, X.-F., Wang, Y., Yu, T., Zhang, Y.H., Dai, S.J. Variation in camptothecin content in Camptotheca acuminata leaves. Bot Bull Acad Sin 2003, 44(2): 99-105.
6. Wall, M.E., Wani, M.C., Cook, C.E., Palmer, K.H., McPhail, H.T., Sim, G.A. Plant antitumor agents. I. The isolation and structure of camptothecin, a novel alkaloidal leukemia and tumor inhibitor from Camptotheca acuminata. J Am Chem Soc 1966, 88(16): 3888-90.
7. Hsiang, Y.H., Hertzberg, R., Hecht, S., Liu, L.F. Camptothecin induces protein-linked DNA breaks via mammalian DNA topoisomerase I. J Biol Chem 1985, 260(27): 14873-8.
8. Tse, Y.C., Kirgaard, K., Wang, J.C. Covalent bonds between protein and DNA. Formation of phosphotyrosine linkage between certain DNA topoisomerases and DNA. J Biol Chem 1980, 255(12): 5560-5.
9. Hsiang, Y.H., Lihou, M.G., Liu, L.F. Arrest of replication forks by drug-stabilized topoisomerase I-DNA cleavable complexes as a mechanism of cell killing by camptothecin. Cancer Res 1989, 49(18): 5077-82.
10. Liu, L.F. DNA topoisomerase poisons as antitumor drugs. Annu Rev Biochem 1989, 58: 351-74.
11. Van der See, A.G., Hollema, H., De Jong, S. et al. P-glycoprotein expression and DNA topoisomerase I and II activity in benign tumors of the ovary and in malignant tumors of the ovary, before and after platinum/ cyclophosphamide chemotherapy. Cancer Res 1991, 51(21): 5915-20.
12. Giovanella, B.C., Stehlin, J.S., Wall, M.E. et al. DNA topoisomerase I - Targeted chemotherapy of human colon cancer xenografts. Science 1989, 246(4933): 1046-8.
13. Liebes, I. et al. Pharmacodynamics of topoisomerase I inhibition: Western blot determination of topoisomerase I and cleavable complex in patients with upper gastrointestinal malignancies treated with topotecan. Clin Cancer Res 1998, 4(3): 545-57.
14. Pommier, Y. Camptothecins and topoisomerase I: A foot in the door. Targeting the genome beyond topoisomerase I with camptothecins and novel anticancer drugs: Importance of DNA replication, repair and cell cycle checkpoints. Curr Med Chem Anticancer Agents 2004, 4(5): 429-34.
15. Muggia, F.M., Creaven, P.J., Hansen, H.H., Cohen, M.H., Selawry, O.S. Phase I clinical trial of weekly and daily treatment with camptothecin (NSC-100880): Correlation with preclinical studies. Cancer Chemother Rep 1972, 56(4): 515-21.
16. Lee, J.H., Lee, J.M., Lim, J.K., Kim, J.K., Ahn, S.K., Bang, Y.J., Hong, C.I. Preclinical and phase I clinical studies with CKD-602, a novel camptothecin derivative. Ann NY Acad Sci 2000, 922: 324-5.
17. Bom, D., Curran, D.P., Kruszewski, S. et al. The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity. J Med Chem 2000, 43(21): 3970-80.
18. Keir, S.T., Hausheer, F., Lawless, A.A., Bigner, D.D., Friedman, H.S. Therapeutic activity of 7-[(2-trimethylsilyl)ethyl)]-20 (S)-camptothecin against central nervous system tumor-derived xenografts in athymic mice. Cancer Chemother Pharmacol 2001, 48(1): 83-7.
19. Kumazawa, E., Jimbo, T., Ochi, Y., Tohgo, A. Potent and broad antitumor effects of DX-8951f, a water-soluble camptothecin derivative, against various human tumors xenografted in nude mice. Cancer Chemother Pharmacol 1998, 42(3): 210-20.
20. Dallavalle, S., Delsoldato, T., Ferrari, A. et al. Novel 7-substituted camptothecins with potent antitumor activity. J Med Chem 2000, 43(21): 3963-9.
21. Liu, W.M., te Poele, R.H. Recent advances and developments in the inhibitors of DNA topoisomerases. Curr Enzyme Inhibition 2007, 3(2): 161-74.
22. Pommier, Y. Topoisomerase I inhibitors: Camptothecins and beyond. Nat Rev Cancer 2006, 6(10): 789-802.
23. Croce, A.C., Bottiroli, G., Supino, R., Favini, E., Zuco, V., Zunino, F. Subcellular localization of the camptothecin analogues, topotecan and gimatecan. Biochem Pharmacol 2004, 67(6): 1035-45.
24. Perego, P., De Cesare, M., De Isabella, P. et al. A novel 7-modified camptothecin analog overcomes breast cancer resistance protein-associated resistance in a mitoxantrone-selected colon carcinoma cell line. Cancer Res 2001, 61(16): 6034-7.
25. Pratesi, G., De Cesare, M., Carenini, N. et al. Pattern of antitumor activity of a novel camptothecin, ST1481, in a large panel of human tumor xenografts. Clin Cancer Res 2002, 8(12): 3904-9.
26. Ulivi, P., Zoli, W., Fabbri, F. et al. Cellular basis of antiproliferative and antitumor activity of the novel camptothecin derivative, gimatecan, in bladder carcinoma models. Neoplasia 2005, 7(2): 152-61.
27. Di Francesco, A.M., Riccardi, A.S., Barone, G. et al. The novel lipophilic camptothecin analogue gimatecan is very active in vitro in human neuroblastoma: A comparative study with SN38 and topotecan. Biochem Pharmacol 2005, 70(8): 1125-36.
28. Nici, L., Monfils, B., Carminati, P., Calabresi, P. Antineoplastic effects of ST1481, a novel camptothecin, on human malignant mesothelioma. Proc Am Assoc Cancer Res (AACR) 2002, 43: Abst 1232.
29. Sartore-Bianchi, A., Nici, L., Porta, C., Chatterjee, D., Mutti, L., Calabresi, P. The combination of the novel camptothecin analogue gimatecan (ST1481) plus the proteasome inhibitor PS341 produces an enhanced pro-apoptotic effect in a malignant mesothelioma cell line. Proc Am Assoc Cancer Res (AACR) 2003, 44(2nd ed): Abst R3729.
30. Zuco, V., Supino, R., De Cesare, M. et al. Cellular bases of the antitumor activity of a 7-substituted camptothecin in hormone-refractory human prostate carcinoma models. Biochem Pharmacol 2003, 65(8): 1281-94.
31. Perego, P., Ciusani, E., Gatti, L., Carenini, N., Corna, E., Zunino, F. Sensitization to gimatecan-induced apoptosis by tumor necrosis factor-related apoptosis inducing ligand in prostate carcinoma cells. Biochem Pharmacol 2006, 71(6): 791-8.
32. Marchetti, S., Oostendorp, R., Pluim, D. et al. ABC-transporter studies of gimatecan (7-tert-butoxyiminomethylcamptothecin) in comparison to topotecan. Proc Am Assoc Cancer Res (AACR) 2006, 47: Abst 611.
33. Gounder, M.K., Nazar, A., Saleem, A., Pungaliya, P., Malegaonkar, D., Versace, R., Rubin, E.H. Effects of drug efflux proteins and topoisomerase I mutations on the anti-proliferative activity of gimatecan. Proc Am Assoc Cancer Res (AACR) 2007, 48: Abst 2307.
34. De Cesare, M., Pratesi, G., Perego, P. et al. Potent antitumor activity and improved pharmacological profile of ST1481, a novel 7-substituted camptothecin. Cancer Res 2001, 61(19): 7189-95.
35. De Cesare, M., Pratesi, G., Veneroni, S., Bergottini, R., Zunino, F. Efficacy of the novel camptothecin gimatecan against orthotopic and metastatic human tumor xenograft models. Clin Cancer Res 2004, 10(21): 7357-64.
36. Petrangolini, G., Pratesi, G., De Cesare, M. et al. Antiangiogenic effects of the novel camptothecin ST1481 (gimatecan) in human tumor xenografts. Mol Cancer Res 2003, 1(12): 863-70.
37. De Cesare, M., Perego, P., Righetti, S.C. et al. Enhanced antitumour efficacy of gimatecan in combination with Bcl-2 antisense oligonucleotide in human melanoma xenografts. Eur J Cancer 2005, 41(8): 1213-22.
38. Poupon, M., Assayag, F., DePlater, L., Marangoni, E., Dieras, V. In vivo efficacy of gimatecan, a Novartis new topoisomerase 1 inhibitor alone or combined with RAD001, bevacizumab or erlotinib in breast, lung and ovary human cancer xenografts. Proc Am Assoc Cancer Res (AACR) 2007, 48: Abst 783.
39. Stano, P., Bufali, S., Pisano, C. et al. Novel camptothecin analogue (gimatecan)-containing liposomes prepared by the ethanol injection method. J Liposome Res 2004, 14(1-2): 87-109.
40. Zucchetti, M., Pace, S., Frapolli, R. et al. Clinical pharmacokinetic profile of gimatecan (ST 1481), a new oral campthotecin derivative. Proc Am Soc Clin Oncol (ASCO) 2002, 21(Part 1): Abst 476.
41. 14C gimatecan (LBQ707) after oral administration in patients with advanced cancer. J Clin Oncol [43rd Annu Meet Am Soc Clin Oncol (ASCO) (June 1-5, Chicago) 2007] 2007, 25(18, Suppl.): Abst 2564.
42. Alderson, L., Supko, J., Maestri, X. et al. Phase I/II trial of gimatecan in patients with recurrent malignant glioma. Proc Am Soc Clin Oncol (ASCO) 2003, 22: Abst 416.
43. Hochberg, F.H., Supko, J., Amato, A., Salem, N., Carminati, P., Wen, P. Phase I trial and pharmacokinetic study of oral gimatecan in adults with malignant glioma. 42nd Annu Meet Am Soc Clin Oncol (ASCO) (June 3-6, Atlanta) 2006, Abst 1559.
44. Zucchetti, M., Frapolli, R., Moliterni, A. et al. Pharmacokinetic of the novel oral camptothecin gimatecan in women with pretreated advanced breast cancer. Eur J Cancer - Suppl [18th EORTC-NCI-AACR Symp Mol Targets Cancer Ther (Nov 7-10, Prague) 2006] 2006, 4(12): Abst 442.
45. Zanna, C., Calabresi, P., Corsi, M. et al. Potent and less schedule-dependent antitumor activity of the oral camptothecin derivative ST 1481. Proc Am Soc Clin Oncol (ASCO) 2001, 20(Part 1): Abst 406.
46. Lucreziotti, M.R., Mazue, G., De Angelis, C. et al. Toxicology profile of the novel oral camptothecin analog ST 1481. Toxicol Lett 2001, 123(Suppl. 1): Abst 380.
47. Sessa, C., Credsta, S., Cerny, T. et al. Concerted escalation of dose and dosing duration in a phase I study of the oral camptothecin gimatecan (ST1481) in patients with advanced solid tumors. Ann Oncol 2007, 18(3): 561-8.
48. Zhu, A.X., Ready, N.E., Clark, J.W. et al. Phase I trial of gimatecan given orally once a week for 3 of 4 weeks in patients with advanced solid tumors. Proc Am Soc Clin Oncol (ASCO) 2003, 22: Abst 557.
49. Mariani, P., Moliterni, A., Da Prada, G. et al. A phase II trial of the novel oral camptothecin gimatecan (G) in women with anthracycline (A) and taxane (T) pre-treated advanced breast cancer. 42nd Annu Meet Am Soc Clin Oncol (ASCO) (June 3-6, Atlanta) 2006, Abst 662.
50. Pecorelli, S., Ray-Coquard, I., Colombo, N. et al. A phase II study of oral gimatecan (ST1481) in women with progressing or recurring advanced epithelial ovarian, fallopian tube and peritoneal cancers. 42nd Annu Meet Am Soc Clin Oncol (ASCO) (June 3-6, Atlanta) 2006, Abst 5088.
51. Biron, P., Reichardt, P., Grosso, F. et al. A phase II study of gimatecan as salvage treatment in patients with advanced or metastatic soft tissue sarcoma (STS) relapsing after anthracy-cline/ifosfamide-based chemotherapy regimens. J Clin Oncol [43rd Annu Meet Am Soc Clin Oncol (ASCO) (June 1-5, Chicago) 2007] 2007, 25(18, Suppl.): Abst 10063.
52. A phase I dose escalation study of LBO707 (gimatecan) administered orally twice per week to Japanese patients with advanced solid tumors (NCT00487058). ClinicalTrials.gov Web site, October 8, 2007.
53. An extension trial to a phase I dose escalation study of gimatecan administered orally 5 consecutive days to Japanese patients with advanced solid tumor (NCT00441610). ClinicalTrials.gov Web site, October 8, 2007.
54. Dose-escalation study of gimatecan administered in two different schedules in adult patients with advanced solid tumors (NCT00420485). ClinicalTrials.gov Web site, October 8, 2007.
55. Extension to dose-escalation study of gimatecan administered in two different schedules in adult patients with advanced solid tumors (NCT00462163). ClinicalTrials.gov Web site, October 8, 2007.
56. This is an early study to investigate the effect of gimatecan in adults with malignant glioma (NCT00032903). ClinicalTrials.gov Web site, October 8, 2007.
57. Phase I study of gimatecan in patients with myelodysplastic syndromes (NCT00493571). ClinicalTrials.gov Web site, October 8, 2007.