Combination of ATP-competitive mammalian target of rapamycin inhibitors with standard chemotherapy for colorectal cancer

Investigational New Drugs

Volumn 30, Issue 6, 2012, Pages 2219-2225

  Atreya, Chloe E ^a   Ducker, Gregory S ^b   Feldman, Morris E ^c   Bergsland, Emily K ^a   Warren, Robert S ^d   Shokat, Kevan M ^b,c  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b UNIVERSITY OF CALIFORNIA   (United States)

^c UNIVERSITY OF CALIFORNIA   (United States)

^d UNIVERSITY OF CALIFORNIA   (United States)

Author keywords

ATP competitive; Colorectal cancer; Combination index; MTOR; PI3K

Indexed keywords

2 (4 AMINO 1 ISOPROPYL 1H PYRAZOLO[3,4 D]PYRIMIDIN 3 YL) 1H INDOL 5 OL; CELL PROTEIN; FIRTECAN; FLUOROURACIL; IRINOTECAN; KRAS PROTEIN; KU 0063794; MAMMALIAN TARGET OF RAPAMYCIN INHIBITOR; OXALIPLATIN; PHOSPHATIDYLINOSITOL 4,5 BISPHOSPHATE 3 KINASE; PROTEIN P53; RAPAMYCIN; UNCLASSIFIED DRUG;

ARTICLE; CANCER RESISTANCE; COLORECTAL CANCER; CONTROLLED STUDY; DRUG ANTAGONISM; DRUG EFFICACY; DRUG POTENTIATION; DRUG SENSITIVITY; DRUG SPECIFICITY; GENE MUTATION; HUMAN; HUMAN CELL; IN VITRO STUDY; PREDICTION; PRIORITY JOURNAL; WILD TYPE;

ADENOSINE TRIPHOSPHATE; ANTINEOPLASTIC AGENTS; CAMPTOTHECIN; CELL LINE, TUMOR; CELL PROLIFERATION; COLORECTAL NEOPLASMS; DRUG COMBINATIONS; FLUOROURACIL; HUMANS; INDOLES; MUTATION; NUCLEAR PROTEINS; ORGANOPLATINUM COMPOUNDS; PROTO-ONCOGENE PROTEINS; PURINES; RAS PROTEINS; TOR SERINE-THREONINE KINASES; TRANSCRIPTION FACTORS;

EID: 84875498652     PISSN: 01676997     EISSN: 15730646     Source Type: Journal    
DOI: 10.1007/s10637-012-9793-y     Document Type: Article

References (35)

1. Apsel B, Blair JA, Gonzalez B et al (2008) Targeted polypharma-cology: discovery of dual inhibitors of tyrosine and phosphoinosi-tide kinases. Nat Chem Biol 4:691-699
2. Feldman ME, Apsel B, Uotila A et al (2009) Active site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. PLoS Biology 7:371-383
3. Janes MR, Limon JJ, So L et al (2010) Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor. Nat Med 16:205-213
4. Yu K, Shi C, Toral-Barza L et al (2010) Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2. Cancer Res 70:621-631
5. Chresta CM, Davies BR, Hickson I et al (2010) AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity. Cancer Res 70:288-298
6. Benjamin D, Colombi M, Moroni C, Hall MN (2011) Rapamycin passes the torch: a new generation of mTOR inhibitors. Nat Rev Drug Discov 10:868-880
7. American Cancer Society. Colorectal Cancer Facts & Figures 2011-2013. American Cancer Society, Atlanta, pp. 3, 8
8. Parsons DW, Wang TL, Samuels Y et al (2005) Colorectal cancer: mutations in a signaling pathway. Nature 436:792
9. Allegra CJ, Jessup JM, Somerfield MR et al (2009) American Society of Clinical Oncology provisional clinical opinion: testing for KRAS gene mutations in patients with metastatic colorectal carcinoma to predict response to anti-epidermal growth factor receptor monoclonal antibody therapy. J Clin Oncol 27:2091-2096
10. Guertin DA, Sabatini DM (2007) Defining the role of mTOR in cancer. Canc Cell 12:9-22
11. Sarbassov DD, Guertin DA, Ali SM, Sabatini DM (2005) Phos-phorylation and regulation of AKT/PKB by the rictor-mTOR complex. Science 307:1098-1101
12. O'Reilly KE, Rojo F, She QB et al (2006) mTOR inhibition induces upstream receptor tyrosine kinase signaling and activates AKT. Cancer Res 66:1500-1508
13. Gulhati P, Bowen KA, Liu J et al (2011) mTORC1 and mTORC2 regulate EMT, motility, and metastasis of colorectal cancer via RhoA and Rac1 signaling pathways. Cancer Res 71(9):3246-3256
14. Hsieh AC, Costa M, Zollo O et al (2010) Genetic dissection of the oncogenic mTOR pathway reveals druggable addiction to transla-tional control via 4EBP-eIF4E. Cancer Cell 17:249-261
15. Schlieman MG, Fahy BN, Ramsamooj R, Beckett L, Bold RJ (2003) Incidence, mechanism and prognostic value of activated AKT in pancreas cancer. Br J Cancer 89:2110-2115
16. Ciardiello F, Caputo R, Bianco R et al (2000) Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor. Clin Cancer Res 6:2053-2063
17. Prewett MC, Hooper AT, Bassi R, Ellis LM, Waksal HW, Hicklin DJ (2002) Enhanced antitumor activity of anti-epidermal growth factor receptor monoclonal antibody IMC-C225 in combination with irinotecan (CPT-11) against human colorectal tumor xeno-grafts. Clin Cancer Res 8:994-1003
18. Morelli MP, Cascone T, Troiani T et al (2005) Sequence-dependent antiproliferative effects of cytotoxic drugs and epidermal growth factor receptor inhibitors. Ann Oncol Suppl 4:61-68
19. Cunningham D, Humblet Y, Siena S et al (2004) Cetuximab monotherapy and cetuximab plus irinotecan in irinotecan-refractory metastatic colorectal cancer. N Engl J Med 351:337-345
20. Bokemeyer C, Bondarenko I, Makhson A et al (2009) Fluorouracil, leucovorin, and oxaliplatin with and without cetuximab in the first-line treatment of metastatic colorectal cancer. J Clin Oncol 27:663-671
21. Van Cutsem E, Köhne CH, Hitre E et al (2009) Cetuximab and chemotherapy as initial treatment for metastatic colorectal cancer. N Engl J Med 360:1408-1417
22. Tol J, Koopman M, Cats A et al (2009) Chemotherapy, bevacizumab, and cetuximab in metastatic colorectal cancer. N Engl J Med 360:563-572
23. Zunder ER, Knight ZA, Houseman BT, Apsel B, Shokat KM (2008) Discovery of drug-resistant and drug-sensitizing mutations in the oncogenic PI3K isoform p110 alpha. Canc Cell 14:180-192
24. Chou TC, Talalay P (1984) Quantitative analysis of dose-effect relationships: the combined effects of multiple drugs or enzyme inhibitors. Adv Enzyme Regul 22:27-55
25. Chou TC (2006) Theoretical basis, experimental design, and computerized simulation of synergism and antagonism in drug combination studies. Pharmacol Rev 58:621-681
26. García-Martínez JM, Moran J, Clarke RG et al (2009) Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR). Biochem J 421:29-42
27. Milano G, Spano JP, Leyland-Jones B (2008) EGFR-targeting drugs in combination with cytotoxic agents: from bench to bedside, a contrasted reality. Br J Cancer 99:1-5
28. Perkins G, Lièvre A, Ramacci C et al (2010) Additional value of EGFR downstream signaling phosphoprotein expression to KRAS status for response to anti-EGFR antibodies in colorectal cancer. Int J Cancer 127:1321-1331
29. Sartore-Bianchi A, Martini M, Molinari F et al (2009) PIK3CA mutations in colorectal cancer are associated with clinical resistance to EGFR-targeted monoclonal antibodies. Cancer Res 69 (5):1851-1857
30. De Roock W, Claes B, Bernasconi D et al (2010) Effects of KRAS, BRAF, NRAS, and PIK3CA mutations on the efficacy of cetux-imab plus chemotherapy in chemotherapy-refractory metastatic colorectal cancer: a retrospective consortium analysis. Lancet Oncol (8):753-62
31. Boyer J, McLean EG, Aroori S, Wilson P, McCulla A, Carey PD, Longley DB, Johnston PG (2004) Characterization of p53 wild-type and null isogenic colorectal cancer cell lines resistant to 5-fluorouracil, oxaliplatin, and irinotecan. Clin Cancer Res 10:2158-2167
32. McDermott U, Longley DB, Galligan L, Allen W, Wilson T, Johnston PG (2005) Effect of p53 status and STAT1 on chemotherapy-induced, Fas-mediated apoptosis in colorectal cancer. Cancer Res 65:8951-8960
33. Jacob S, Aguado M, Fallik D, Praz F (2001) The role of the DNA mismatch repair system in the cytotoxicity of the topoisomerase inhibitors camptothecin and etoposide to human colorectal cancer cells. Cancer Res 61:6555-6562
34. Johnson SM, Gulhati P, Rampy BA et al (2010) Novel expression patterns of PI3K/AKT/mTOR signaling pathway components in colorectal cancer. J Am Coll Surg 210(5):767-776, 776-8
35. The Catalogue of Somatic Mutations in Cancer (COSMIC) (2011) Wellcome Trust Sanger Institute, Hinxton, UK. http://www.sanger. ac.uk/genetics/CGP/ cosmic/