A Phase I Pharmacokinetic and Pharmacodynamic Study of the Farnesyl Transferase Inhibitor BMS-214662 in Combination with Cisplatin in Patients with Advanced Solid Tumors

Clinical Cancer Research

Volumn 10, Issue 8, 2004, Pages 2636-2644

  Mackay, Helen J ^a   Hoekstra, Ronald ^b   Eskens, Ferry A L M ^b   Loos, Walker J ^b   Crawford, Donna ^a   Voi, Maurizio ^c   Van Vreckem, Anne ^c   Evans, T R Jeffrey ^a,d   Verweij, Jaap ^b  

^a IMPERIAL CANCER RESEARCH FUND   (United Kingdom)

^b ERASMUS MEDICAL CENTER   (Netherlands)

^c BRISTOL MYERS SQUIBB   (United States)

^d BEATSON INSTITUTE FOR CANCER RESEARCH   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

3 BENZYL 7 CYANO 2,3,4,5 TETRAHYDRO 1 (1H IMIDAZOL 4 YLMETHYL) 4 (2 THIENYLSULFONYL) 1H 1,4 BENZODIAZEPINE; AMINOTRANSFERASE; CISPLATIN; PROTEIN FARNESYLTRANSFERASE; PROTEIN FARNESYLTRANSFERASE INHIBITOR;

ADULT; ADVANCED CANCER; AGED; ANEMIA; ARTICLE; BLEEDING; BLOOD SAMPLING; CANCER CHEMOTHERAPY; CANCER PATIENT; CHEMOTHERAPY INDUCED EMESIS; CLINICAL TRIAL; COHORT ANALYSIS; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DIARRHEA; DOSE RESPONSE; DOSE TIME EFFECT RELATION; DRUG INFUSION; DRUG RESPONSE; EDEMA; ENZYME ACTIVITY; ENZYME INHIBITION; FATIGUE; FEBRILE NEUTROPENIA; FEMALE; HUMAN; INFECTION; INHIBITION KINETICS; KIDNEY FAILURE; KIDNEY FUNCTION; LEUKOPENIA; LIVER FUNCTION; MALE; NAUSEA; NEUTROPENIA; PHARMACODYNAMICS; PHASE 1 CLINICAL TRIAL; PRIORITY JOURNAL; SENSORY NEUROPATHY; SIDE EFFECT; SOLID TUMOR; THROMBOCYTOPENIA; TIME; TOXICITY; URINALYSIS;

ADULT; AGED; ALKYL AND ARYL TRANSFERASES; ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS; AREA UNDER CURVE; BENZODIAZEPINES; CISPLATIN; COHORT STUDIES; DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYME INHIBITORS; FARNESYLTRANSTRANSFERASE; FEMALE; HUMANS; IMIDAZOLES; LEUKOCYTES, MONONUCLEAR; MALE; MIDDLE AGED; NEOPLASMS; TIME FACTORS; TREATMENT OUTCOME;

EID: 1942502426     PISSN: 10780432     EISSN: None     Source Type: Journal    
DOI: 10.1158/1078-0432.CCR-03-0327     Document Type: Article

References (34)

1. Bos JL. Ras oncogenes in human cancer: a review. Cancer Res 1989;49:4682-9.
2. Boguski MS, McCormick F. Proteins regulating Ras and its relatives. Nature 1993;366:643-54.
3. Medema RH, Bos JL. The role of p21ras in receptor tyrosine kinase signaling. Crit Rev Oncog 1993;4:615-61.
4. McCormick F. Activators and effectors of ras p21 proteins. Cuff Opin Genet Dev 1994;4:71-6.
5. Kato K, Cox AD, Hisaka MM, Graham SM, Buss JE, Der CJ. Isoprenoid addition to ras protein is the critical modification for its membrane association and transforming activity. Proc Natl Acad Sci USA 1992;89:6403-7.
6. Manne V, Roberts D, Tobin, A, et al. Identification and preliminary characterization of protein-cysteine farnesyltransferase Proc Natl Acad Sci USA 1990;87:7541-5.
7. Sepp-Lorenzino L, Ma Z, Rands E, et al. A peptidomimetic inhibitor of farnesylprotein transferase blocks the anchorage-dependent and -independent growth of human tumor cell lines. Cancer Res 1995;55:5302-9.
8. Reuter CWM, Morgan MA, Bergman L. Targeting Ras signalling pathway: a rational, mechanism-based treatment for hematologic malignancies. Blood 2000;96:1655-99.
9. Cox AD, Der CJ. Farnesyltransferase inhibitors and cancer treatment: targeting simply Ras? Biochim Biophys Acta 1997;1333:F51-71.
10. Adjei AA. Protein farnesyltransferase as a target for the development of anticancer agents. Drugs of the future 2000;25:1069-79.
11. Lebowitz PF, Prendergast GC. Non-Ras targets of farnesyltransferase inhibitors: focus on Rho. Oncogene 1998;17:1439-45.
12. Ashar HR, James L, Gray K, et al. FTIs block the farnesylation of CENP-E and CENP-F and alter the association of CENP-E with the microtubules. J Biol Chem 2000;275:30451-7.
13. Jiang K, Coppola D, Crespo NC, et al. The phosphoinositide 3-OH kinase AKt2 pathway as a critical target for farnesyltransferase inhibitor-induced apoptosis. Mol Cell Biol 2000;20:139-48.
14. Hunt JT, Ding CZ, Bartosky R, et al. Discovery of (R)-7-cyano-2,3,4,5-tetrahydro-1-(1 H- imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1, 4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity. J Med Chem 2000;43:3587-95.
15. Rose WC, Lee FYF, Fairchild CR, et al. Preclinical antitumour activity of BMS-214662, a highly apoptotic and novel farnesyltransferase inhibitor. Cancer Res 2001;61:7507-17.
16. Bailey HH, Marnocha R, Arzoomanian R, et al. Phase I trial of weekly paclitaxel and BMS-214662 in patients with advanced solid tumors [abstract]. Proc Am Soc Clin Oncol 20:79a (A314), 2001.
17. Piccart-Gebhart MJ, Branle F, de Valeriola D, et al. A phase I, clinical and pharmacokinetic (PK) trial of the farnesyl transferase inhibitor (FTI) R 115777 + docetaxel: a promising combination in patients (PTS) with solid tumors [abstract]. Proc Am Soc Clin Oncol, 20:80a (A318), 2001.
18. Johnson SW, Stevenson JP, O'Dwyer PJ. Cisplatin and its analogues. In: De Vita VT, Hellman S, Rosenberg SA, editors. Cancer: principles and practice of oncology (Ed. 6). Philadelphia: Lippincott, Williams and Wilkins, 2001. pp. 376-87
19. Eastman A. Activation of programmed cell death by anticancer agents: cisplatin as a model system. Cancer Cells 1990;2:275-80.
20. Segal-Bendirdjian E, Jacquemin-Sablon A. Cisplatin resistance in a murine leukaemia cell line is associated with a defective apoptotic process. Exp Cell Res 1995;218:201-12.
21. Isonishi S, Andrews PA, Howell SB. Increased sensitivity to cisdiammine dichloroplatinum (II) in human ovarian carcinoma cells in response to treatment with 12-O-tetradecanoylphorbol 13-acetate. J Biol Chem 1990;265:3623-7.
22. Levy E, Baroche C, Barret JM, et al. Activated ras oncogene and specifically acquired resistance to cisplatin in human mammary epithelial cells: induction of DNA cross-links and their repair. Carcinogenesis 1994;15:845-50.
23. Isonishi S, Hom DK, Thiebaut FB, et al. Expression of the c-Ha-ras oncogene in mouse NIH 3T3 cells induces resistance to cisplatin. Cancer Res 1991;51:5903-9.
24. Ferguson PJ. Mechanisms of resistance of human tumours to anti-cancer drugs of the platinum family: a review. J Otolaryngol 1995;24:242-52.
25. Yao KS, Godwin AK, Johnson SW, Ozols RF, O'Dwyer PJ, Hamilton TC. Evidence for altered regulation of gamma-glutamylcysteine synthetase gene expression among cisplatin-sensitive and cisplatin resistant human ovarian cancer cell lines. Cancer Res 1995;55:4367-74.
26. Shinohara N, Ogiso Y, Arai T, et al. Differential Na+ K+ -ATPase activity and cisplatin sensitivity between transformants induced by H-ras and those induced by k-ras. Int J Cancer 1994;58:672-7.
27. Adjei AA, Davis JN, Bruzek LM, Erlichman C, Kaufmann SH. Synergy of the protein farnesyltransferase inhibitor SCH 66336 and cisplatin in human cancer cell lines. Clin Cancer Res 2001;7:1438-45.
28. Liu M, Bryant MS, Chen J, et al. Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice. Cancer Res 1998;58:4947-56.
29. Ryan DP, Eder JP, Supko JG, et al. Phase I clinical trial of the farnesyltransferase (FT) inhibitor BMS-214662 in patients with advanced solid tumors [abstract]. Proc Am Soc Clin Oncol 2000;19:185a (720).
30. Miller AB, Hoogstraten B, Staquet M, Winkler A. Reporting results of cancer treatment. Cancer 1981;47:207-14.
31. Sonnichsen D, Damle B, Manning J, et al. Pharmacokinetics (PK) and pharmacodynamics (PD) of the farnesyltransferase (FT) inhibitor BMS-214662 in patients with advanced solid tumors. Proc Am Soc Clin Oncol 2000;19:178a (691).
32. Tabernero J, Sonnichsen D, Albanell J, et al. A phase I pharmacokinetic (PK) and serial tumor and PMBC pharmacodynamic (PD) study of weekly BMS-214662, a farnesyltransferase (FT) inhibitor, in patients with advanced solid tumors [abstract]. Proc Am Soc Clin Oncol 2001;20:77a, (304).
33. Zhu AX, Supko JG, Ryan DP, Clark JW, Butkiewiez L. Eder JP. A phase I clinical, pharmacokinetic and pharmacodynamic study of the farnesyltransferase inhibitor BMS-214662 given as a 24 hour continuous intravenous (IV) infusion once weekly x 3 in patients with advanced solid tumors [abstract]. Proc Am Soc Clin Oncol 2002;21:366.
34. Prendergast GC, Davide JP, deSolms SJ, et al. Farnesyltransferase inhibition causes morphological reversion of ras-transformed cells by a complex mechanism that involves regulation of the actin cytoskeleton. Mol Cell Biol 1994;14:4193-202.