Effect of inhibition of the FGFR-MAPK signaling pathway on the development of ocular toxicities

Cancer Treatment Reviews

Volumn 39, Issue 6, 2013, Pages 664-672

  Van der Noll, Ruud ^a   Leijen, Suzanne ^a   Neuteboom, Guido H G ^b   Beijnen, Jos H ^b,c   Schellens, Jan H M ^a,c  

^a ANTONI VAN LEEUWENHOEK HOSPITAL   (Netherlands)

^b SLOTERVAART HOSPITAL   (Netherlands)

^c UTRECHT UNIVERSITY   (Netherlands)

Author keywords

Diagnosis; FGFR; MAPK; Monitoring; Ocular toxicity; RD; RVO

Indexed keywords

2 (2 CHLORO 4 IODOANILINO) N CYCLOPROPYLMETHOXY 3,4 DIFLUOROBENZAMIDE; 3,4 DIFLUORO 2 (2 FLUORO 4 IODOANILINO) N (2 HYDROXYETHOXY) 5 [(3 OXO 1,2 OXAZINAN 2 YL)METHYL]BENZAMIDE; AZD 4547; B RAF KINASE INHIBITOR; BEVACIZUMAB; BRIVANIB; BRIVANIB ALANINATE; COBIMETINIB; DABRAFENIB; DACARBAZINE; DOVITINIB; FIBROBLAST GROWTH FACTOR 2; FIBROBLAST GROWTH FACTOR RECEPTOR; LENVATINIB; MITOGEN ACTIVATED PROTEIN KINASE; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; MSC 1936369; N (2,3 DIHYDROXYPROPOXY) 3,4 DIFLUORO 2 (2 FLUORO 4 IODOANILINO)BENZAMIDE; NINTEDANIB; PIMASERTIB; RAF 865; RANIBIZUMAB; RDEA 119; SELUMETINIB; TAK 733; TEMOZOLOMIDE; TRAMETINIB; UNCLASSIFIED DRUG; VEMURAFENIB; XL 281;

ANTINEOPLASTIC ACTIVITY; BLURRED VISION; BRAIN METASTASIS; CELL DIFFERENTIATION; CELL PROLIFERATION; CENTRAL SEROUS RETINOPATHY; DRUG EFFICACY; DRY EYE; EYE TOXICITY; HUMAN; INTRAOCULAR PRESSURE; IRITIS; LASER COAGULATION; MELANOMA; METASTATIC MELANOMA; MOLECULARLY TARGETED THERAPY; OPTICAL COHERENCE TOMOGRAPHY; PATHOPHYSIOLOGY; PHOTOPHOBIA; PIGMENT EPITHELIUM; RETINA DETACHMENT; RETINA FLUORESCEIN ANGIOGRAPHY; RETINA MACULA AGE RELATED DEGENERATION; RETINA VEIN OCCLUSION; REVIEW; SEROUS RETINA DETACHMENT; SIGNAL TRANSDUCTION; TREATMENT RESPONSE; UVEITIS; VISUAL ACUITY; VISUAL DISORDER;

EYE DISEASES; HUMANS; MAP KINASE SIGNALING SYSTEM; MITOGEN-ACTIVATED PROTEIN KINASES; MOLECULAR TARGETED THERAPY; PROTEIN KINASE INHIBITORS; RECEPTOR, FIBROBLAST GROWTH FACTOR, TYPE 1; SIGNAL TRANSDUCTION;

EID: 84878907330     PISSN: 03057372     EISSN: 15321967     Source Type: Journal    
DOI: 10.1016/j.ctrv.2013.01.003     Document Type: Review

References (130)

1. Singh P., Singh A. Ocular adverse effects of anti-cancer chemotherapy and targeted therapy. J Cancer Res Ther 2012, 1:1-7.
2. Renouf D.J., Velazquez-Martin J.P., Simpson R., et al. Ocular toxicity of targeted therapies. J Clin Oncol 2012, 30:3277-3286.
3. Leijen S., Middleton M.R., Tresca P., et al. Phase I dose-escalation study of the safety, pharmacokinetics, and pharmacodynamics of the MEK inhibitor RO4987655 (CH4987655) in patients with advanced solid tumors. Clin Cancer Res 2012, 18:4794-4805.
4. Strauss O. The retinal pigment epithelium. Webvision: the organization of the retina and visual system [Internet] PubMed Bookshelf ID: NBK11530 1995, University of Utah Health Sciences Center, Salt Lake City (UT). H. Kolb, E. Fernandez, R. Nelson (Eds.).
5. Fisher S.K., Lewis G.P. Retinal detachment. Ocular disease: mechanisms and management 2010, 554-561. Elsevier. L.A. Levin, D.M. Albert (Eds.).
6. Anderson D.H., Stern W.H., Fisher S.K., et al. The onset of pigment epithelial proliferation after retinal detachment. Invest Ophthalmol Vis Sci 1981, 21:10-16.
7. Liu Y.Y., Chen M., Ishikawa H., et al. Automated macular pathology diagnosis in retinal OCT images using multi-scale spatial pyramid and local binary patterns in texture and shape encoding. Med Image Anal 2011, 15:748-759.
8. Jaffe G.J., Caprioli J. Optical coherence tomography to detect and manage retinal disease and glaucoma. Am J Ophthalmol 2004, 137:156-169.
9. Spaide R.F., Lee J.K., Klancnik J.K., et al. Optical coherence tomography of branch retinal vein occlusion. Retina 2003, 23:343-347.
10. Zayit-Soudry S., Moroz I., Loewenstein A. Retinal pigment epithelial detachment. Surv Ophthalmol 2007, 52:227-243.
11. Campochiaro P.A., Hafiz G., Shah S.M., et al. Ranibizumab for macular edema due to retinal vein occlusions: implication of VEGF as a critical stimulator. Mol Ther 2008, 16:791-799.
12. Noma H., Funatsu H., Harino S., et al. Vitreous inflammatory factors in macular edema with central retinal vein occlusion. Jpn J Ophthalmol 2011, 55:248-255.
13. Yoshimura T., Sonoda K.H., Sugahara M., et al. Comprehensive analysis of inflammatory immune mediators in vitreoretinal diseases. PLoS One 2009, 4:e8158.
14. Norton E.W., Smith J.L., Curtin V.T., et al. Fluorescein fundus photography: an aid in the differential diagnosis of posterior ocular lesions. Trans Am Acad Ophthalmol Otolaryngol 1964, 68:755-765.
15. Aref A.A., Scott I.U. Management of macular edema secondary to branch retinal vein occlusion: an evidence-based update. Adv Ther 2011, 28:28-39.
16. Rehak M., Wiedemann P. Retinal vein thrombosis: pathogenesis and management. J Thromb Haemost 2010, 8:1886-1894.
17. Heier J.S., Campochiaro P.A., Yau L., et al. Ranibizumab for macular edema due to retinal vein occlusions: long-term follow-up in the HORIZON trial. Ophthalmology 2012, 119:802-809.
18. Dionne C.A., Crumley G., Bellot F., et al. Cloning and expression of two distinct high-affinity receptors cross-reacting with acidic and basic fibroblast growth factors. EMBO J 1990, 9:2685-2692.
19. Walsh N., Valter K., Stone J. Cellular and subcellular patterns of expression of bFGF and CNTF in the normal and light stressed adult rat retina. Exp Eye Res 2001, 72:495-501.
20. Wahlin K.J., Adler R., Zack D.J., et al. Neurotrophic signaling in normal and degenerating rodent retinas. Exp Eye Res 2001, 73:693-701.
21. Skaper S.D., Kee W.J., Facci L., et al. The FGFR1 inhibitor PD 173074 selectively and potently antagonizes FGF-2 neurotrophic and neurotropic effects. J Neurochem 2000, 75:1520-1527.
22. Hecquet C., Lefevre G., Valtink M., et al. CAMP inhibits the proliferation of retinal pigmented epithelial cells through the inhibition of ERK1/2 in a PKA-independent manner. Oncogene 2002, 21:6101-6112.
23. Hecquet C., Lefevre G., Valtink M., et al. Activation and role of MAP kinase-dependent pathways in retinal pigment epithelial cells: ERK and RPE cell proliferation. Invest Ophthalmol Vis Sci 2002, 43:3091-3098.
24. Grierson I., Hiscott P., Hogg P., et al. Development, repair and regeneration of the retinal pigment epithelium. Eye (Lond) 1994, 8(Pt 2):255-262.
25. Guillonneau X., Bryckaert M., Launay-Longo C., et al. Endogenous FGF1-induced activation and synthesis of extracellular signal-regulated kinase 2 reduce cell apoptosis in retinal-pigmented epithelial cells. J Biol Chem 1998, 273:22367-22373.
26. Leschey K.H., Hackett S.F., Singer J.H., et al. Growth factor responsiveness of human retinal pigment epithelial cells. Invest Ophthalmol Vis Sci 1990, 31:839-846.
27. Bryckaert M., Guillonneau X., Hecquet C., et al. Both FGF1 and bcl-x synthesis are necessary for the reduction of apoptosis in retinal pigmented epithelial cells by FGF2: role of the extracellular signal-regulated kinase 2. Oncogene 1999, 18:7584-7593.
28. Bryckaert M., Guillonneau X., Hecquet C., et al. Regulation of proliferation-survival decisions is controlled by FGF1 secretion in retinal pigmented epithelial cells. Oncogene 2000, 19:4917-4929.
29. Desire L., Courtois Y., Jeanny J.C. Endogenous and exogenous fibroblast growth factor 2 support survival of chick retinal neurons by control of neuronal neuronal bcl-x(L) and bcl-2 expression through a fibroblast berowth factor receptor 1- and ERK-dependent pathway. J Neurochem 2000, 75:151-163.
30. Soto I., Rosenthal J.J., Blagburn J.M., et al. Fibroblast growth factor 2 applied to the optic nerve after axotomy up-regulates BDNF and TrkB in ganglion cells by activating the ERK and PKA signaling pathways. J Neurochem 2006, 96:82-96.
31. Rios-Munoz W., Soto I., Duprey-Diaz M.V., et al. Fibroblast growth factor 2 applied to the optic nerve after axotomy increases Bcl-2 and decreases Bax in ganglion cells by activating the extracellular signal-regulated kinase signaling pathway. J Neurochem 2005, 93:1422-1433.
32. Faktorovich E.G., Steinberg R.H., Yasumura D., et al. Photoreceptor degeneration in inherited retinal dystrophy delayed by basic fibroblast growth factor. Nature 1990, 347:83-86.
33. Faktorovich E.G., Steinberg R.H., Yasumura D., et al. Basic fibroblast growth factor and local injury protect photoreceptors from light damage in the rat. J Neurosci 1992, 12:3554-3567.
34. Fischer A.J., Scott M.A., Ritchey E.R., et al. Mitogen-activated protein kinase-signaling regulates the ability of Muller glia to proliferate and protect retinal neurons against excitotoxicity. Glia 2009, 57:1538-1552.
35. Qin S., McLaughlin A.P., De Vries G.W. Protection of RPE cells from oxidative injury by 15-deoxy-delta12,14-prostaglandin J2 by augmenting GSH and activating MAPK. Invest Ophthalmol Vis Sci 2006, 47:5098-5105.
36. Malecaze F., Mascarelli F., Bugra K., et al. Fibroblast growth factor receptor deficiency in dystrophic retinal pigmented epithelium. J Cell Physiol 1993, 154:631-642.
37. Wen R., Cheng T., Song Y., et al. Continuous exposure to bright light upregulates bFGF and CNTF expression in the rat retina. Curr Eye Res 1998, 17:494-500.
38. Yoshikawa T., Mizuno A., Yasumuro H., et al. MEK-ERK and heparin-susceptible signaling pathways are involved in cell-cycle entry of the wound edge retinal pigment epithelium cells in the adult newt. Pigment Cell Melanoma Res 2012, 25:66-82.
39. Pittack C., Jones M., Reh T.A. Basic fibroblast growth factor induces retinal pigment epithelium to generate neural retina in vitro. Development 1991, 113:577-588.
40. Pittack C., Grunwald G.B., Reh T.A. Fibroblast growth factors are necessary for neural retina but not pigmented epithelium differentiation in chick embryos. Development 1997, 124:805-816.
41. Spence J.R., Madhavan M., Aycinena J.C., et al. Retina regeneration in the chick embryo is not induced by spontaneous Mitf downregulation but requires FGF/FGFR/MEK/Erk dependent upregulation of Pax6. Mol Vis 2007, 13:57-65.
42. Vergara M.N., Rio-Tsonis K. Retinal regeneration in the Xenopus laevis tadpole: a new model system. Mol Vis 2009, 15:1000-1013.
43. Perry J., Du J., Kjeldbye H., et al. The effects of bFGF on RCS rat eyes. Curr Eye Res 1995, 14:585-592.
44. McLaren M.J., An W., Brown M.E., et al. Analysis of basic fibroblast growth factor in rats with inherited retinal degeneration. FEBS Lett 1996, 387:63-70.
45. Campochiaro P.A., Chang M., Ohsato M., et al. Retinal degeneration in transgenic mice with photoreceptor-specific expression of a dominant-negative fibroblast growth factor receptor. J Neurosci 1996, 16:1679-1688.
46. Geller S.F., Lewis G.P., Fisher S.K. FGFR1, signaling, and AP-1 expression after retinal detachment: reactive Muller and RPE cells. Invest Ophthalmol Vis Sci 2001, 42:1363-1369.
47. Huang W., Yang A.H., Matsumoto D., et al. PD0325901, a mitogen-activated protein kinase kinase inhibitor, produces ocular toxicity in a rabbit animal model of retinal vein occlusion. J Ocul Pharmacol Ther 2009, 25:519-530.
48. Cassidy L., Barry P., Shaw C., et al. Platelet derived growth factor and fibroblast growth factor basic levels in the vitreous of patients with vitreoretinal disorders. Br J Ophthalmol 1998, 82:181-185.
49. La Heij E.C., Van De Waarenburg M.P., Blaauwgeers H.G., et al. Levels of basic fibroblast growth factor, glutamine synthetase, and interleukin-6 in subretinal fluid from patients with retinal detachment. Am J Ophthalmol 2001, 132:544-550.
50. O'Driscoll C., O'Connor J., O'Brien C.J., et al. Basic fibroblast growth factor-induced protection from light damage in the mouse retina in vivo. J Neurochem 2008, 105:524-536.
51. Chen J., Wang L., Chen Y., et al. Phosphatidylinositol 3 kinase pathway and 4-hydroxy-2-nonenal-induced oxidative injury in the RPE. Invest Ophthalmol Vis Sci 2009, 50:936-942.
52. Faghiri Z., Bazan N.G. PI3K/Akt and mTOR/p70S6K pathways mediate neuroprotectin D1-induced retinal pigment epithelial cell survival during oxidative stress-induced apoptosis. Exp Eye Res 2010, 90:718-725.
53. Turner N., Grose R. Fibroblast growth factor signalling: from development to cancer. Nat Rev Cancer 2010, 10:116-129.
54. Dhillon A.S., Hagan S., Rath O., et al. MAP kinase signalling pathways in cancer. Oncogene 2007, 26:3279-3290.
55. Liebmann C. Regulation of MAP kinase activity by peptide receptor signalling pathway: paradigms of multiplicity. Cell Signal 2001, 13:777-785.
56. Weinberg R.A. Oncogenes and tumor suppressor genes. CA Cancer J Clin 1994, 44:160-170.
57. Chapman M.S., Miner J.N. Novel mitogen-activated protein kinase kinase inhibitors. Expert Opin Investig Drugs 2011, 20:209-220.
58. Montagut C., Settleman J. Targeting the RAF-MEK-ERK pathway in cancer therapy. Cancer Lett 2009, 283:125-134.
59. Bos J.L. Ras oncogenes in human cancer: a review. Cancer Res 1989, 49:4682-4689.
60. Davies H., Bignell G.R., Cox C., et al. Mutations of the BRAF gene in human cancer. Nature 2002, 417:949-954.
61. Sharpe R., Pearson A., Herrera-Abreu M.T., et al. FGFR signaling promotes the growth of triple-negative and basal-like breast cancer cell lines both in vitro and in vivo. Clin Cancer Res 2011, 17:5275-5286.
62. Kunii K., Davis L., Gorenstein J., et al. FGFR2-amplified gastric cancer cell lines require FGFR2 and Erbb3 signaling for growth and survival. Cancer Res 2008, 68:2340-2348.
63. Lamont F.R., Tomlinson D.C., Cooper P.A., et al. Small molecule FGF receptor inhibitors block FGFR-dependent urothelial carcinoma growth in vitro and in vivo. Br J Cancer 2011, 104:75-82.
64. Weiss J., Sos M.L., Seidel D., et al. Frequent and focal FGFR1 amplification associates with therapeutically tractable FGFR1 dependency in squamous cell lung cancer. Sci Transl Med 2010, 2:62ra93.
65. Wang Y., Becker D. Antisense targeting of basic fibroblast growth factor and fibroblast growth factor receptor-1 in human melanomas blocks intratumoral angiogenesis and tumor growth. Nat Med 1997, 3:887-893.
66. Friday B.B., Adjei A.A. Advances in targeting the Ras/Raf/MEK/Erk mitogen-activated protein kinase cascade with MEK inhibitors for cancer therapy. Clin Cancer Res 2008, 14:342-346.
67. Wang H.L., Lopategui J., Amin M.B., et al. KRAS mutation testing in human cancers: the pathologist's role in the era of personalized medicine. Adv Anat Pathol 2010, 17:23-32.
68. Sebolt-Leopold J.S. Advances in the development of cancer therapeutics directed against the RAS-mitogen-activated protein kinase pathway. Clin Cancer Res 2008, 14:3651-3656.
69. Wellbrock C., Karasarides M., Marais R. The RAF proteins take centre stage. Nat Rev Mol Cell Biol 2004, 5:875-885.
70. Kirkwood J.M., Bastholt L., Robert C., et al. Phase II, open-label, randomized trial of the MEK1/2 inhibitor selumetinib as monotherapy versus temozolomide in patients with advanced melanoma. Clin Cancer Res 2012, 18:555-567.
71. Kim K.B., Lewis K., Pavlick A., et al. A phase II study of the MEK1/MEK2 inhibitor GSK1120212 in metastatic BRAF-V600E or K mutant cutaneous melanoma patients previously treated with or without a BRAF inhibitor. Pigment Cell Melanoma Res 2011, 24. Abstract 1021.
72. Weekes CD, Von Hoff DD, Adjei AA et al. A multi-center phase i, dose-escalation trial to the safety and pharmacokinetics/pharmacodynamics of BAY 86-9766 (RDEA119), a MEK inhibitor, in advanced cancer patients. In: Presented at the 22nd EORTC-NCI-AACR Symposium on " Molecular targets and cancer therapeutics" , Berlin, November 16-19 2010.
73. Awada A., Houedé N., Delord J.P., et al. Clinical pharmacokinetic (PK) and pharmacodynamic (PD) results of first-in-man phase I trial of the orally available MEK-inhibitor MSC1936369 (AS703026) in patients (pts) with advanced solid tumors. European Journal of Cancer 2010, 8(7). Abstract 118.
74. Rosen L.S., Galatin P., Fehling J.M., et al. A phase 1 dose-escalation study of XL518, a potent MEK inhibitor administered orally daily to subjects with solid tumors. J Clin Oncol 2008, 26. Abstract 14585.
75. Infante J.R., Fecher L.A., Falchook G.S., et al. Safety, pharmacokinetic, pharmacodynamic, and efficacy data for the oral MEK inhibitor trametinib: a phase 1 dose-escalation trial. Lancet Oncol 2012, 13:773-781.
76. Zelboraf FDA approval; Highlights of prescribing information. 2011.
77. Chapman P.B., Hauschild A., Robert C., et al. Improved survival with vemurafenib in melanoma with BRAF V600E mutation. N Engl J Med 2011, 364:2507-2516.
78. Falchook G.S., Long G.V., Kurzrock R., et al. Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial. Lancet 2012, 379:1893-1901.
79. Kefford R., Arkenau H., Brown M.P., et al. Phase I/II study of GSK2118436, a selective inhibitor of oncogenic mutant BRAF kinase, in patients with metastatic melanoma and other solid tumors. J Clin Oncol 2010, 28(15s). Abstract 8503.
80. Flaherty K.T., Puzanov I., Kim K.B., et al. Inhibition of mutated, activated BRAF in metastatic melanoma. N Engl J Med 2010, 363:809-819.
81. Sosman J.A., Kim K.B., Schuchter L., et al. Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib. N Engl J Med 2012, 366:707-714.
82. Jonker D.J., Rosen L.S., Sawyer M.B., et al. A phase I study to determine the safety, pharmacokinetics and pharmacodynamics of a dual VEGFR and FGFR inhibitor, brivanib, in patients with advanced or metastatic solid tumors. Ann Oncol 2011, 22:1413-1419.
83. Finn R.S., Kang Y.K., Mulcahy M., et al. Phase II, open-label study of brivanib as second-line therapy in patients with advanced hepatocellular carcinoma. Clin Cancer Res 2012, 18:2090-2098.
84. Sarker D., Molife R., Evans T.R., et al. A phase I pharmacokinetic and pharmacodynamic study of TKI258, an oral, multitargeted receptor tyrosine kinase inhibitor in patients with advanced solid tumors. Clin Cancer Res 2008, 14:2075-2081.
85. Kim K.B., Chesney J., Robinson D., et al. Phase I/II and pharmacodynamic study of dovitinib (TKI258), an inhibitor of fibroblast growth factor receptors and VEGF receptors, in patients with advanced melanoma. Clin Cancer Res 2011, 17:7451-7461.
86. Okamoto I., Kaneda H., Satoh T., et al. Phase I safety, pharmacokinetic, and biomarker study of BIBF 1120, an oral triple tyrosine kinase inhibitor in patients with advanced solid tumors. Mol Cancer Ther 2010, 9:2825-2833.
87. Ledermann J.A., Hackshaw A., Kaye S., et al. Randomized phase II placebo-controlled trial of maintenance therapy using the oral triple angiokinase inhibitor BIBF 1120 after chemotherapy for relapsed ovarian cancer. J Clin Oncol 2011, 29:3798-3804.
88. Yamada K., Yamamoto N., Yamada Y., et al. Phase I dose-escalation study and biomarker analysis of E7080 in patients with advanced solid tumors. Clin Cancer Res 2011, 17:2528-2537.
89. Boss D.S., Glen H., Beijnen J.H., et al. A phase I study of E7080, a multitargeted tyrosine kinase inhibitor, in patients with advanced solid tumours. Br J Cancer 2012, 106:1598-1604.
90. Bhide R.S., Cai Z.W., Zhang Y.Z., et al. Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor. J Med Chem 2006, 49:2143-2146.
91. Trudel S., Li Z.H., Wei E., et al. CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood 2005, 105:2941-2948.
92. Roth G.J., Heckel A., Colbatzky F., et al. Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). J Med Chem 2009, 52:4466-4480.
93. Matsui J., Yamamoto Y., Funahashi Y., et al. E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer 2008, 122:664-671.
94. Chen C.Y., Wong T.Y., Heriot W.J. Intravitreal bevacizumab (Avastin) for neovascular age-related macular degeneration: a short-term study. Am J Ophthalmol 2007, 143:510-512.
95. Gavine P.R., Mooney L., Kilgour E., et al. AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res 2012, 72:2045-2056.
96. Guagnano V., Furet P., Spanka C., et al. Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamin o]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. J Med Chem 2011, 54:7066-7083.
97. Chader G.J. Animal models in research on retinal degenerations: past progress and future hope. Vision Res 2002, 42:393-399.
98. Basti S. Ocular toxicities of epidermal growth factor receptor inhibitors and their management. Cancer Nurs 2007, 30:S10-S16.
99. Bendell J.C., Rodon J., Burris H.A., et al. Phase I, dose-escalation study of BKM120, an oral pan-Class I PI3K inhibitor, in patients with advanced solid tumors. J Clin Oncol 2012, 30:282-290.
100. Burris H., Rodon J., Sharma S., et al. First-in-human phase I study of the oral PI3K inhibitor BEZ235 in patients (pts) with advance solid tumors. J Clin Oncol 2010, 28. Abstract 3005.
101. Munster P.N., van der Noll R., Voest E.E., et al. Phase I first-in-human study of the PI3 kinase inhibitor GSK2126458 (GSK458) in patients with advanced solid tumos (study P3K112826). J Clin Oncol 2011, 29. Abstract 3018.
102. Parodi M.B. Medical treatment of retinal vein occlusions. Semin Ophthalmol 2004, 19:43-48.
103. Marcucci R., Sofi F., Grifoni E., et al. Retinal vein occlusions: a review for the internist. Intern Emerg Med 2011, 6:307-314.
104. Haura E.B., Ricart A.D., Larson T.G., et al. A phase II study of PD-0325901, an oral MEK inhibitor, in previously treated patients with advanced non-small cell lung cancer. Clin Cancer Res 2010, 16:2450-2457.
105. Abouzeid H., Wolfensberger T.J. Macular recovery after retinal detachment. Acta Ophthalmol Scand 2006, 84:597-605.
106. Rinehart J., Adjei A.A., Lorusso P.M., et al. Multicenter phase II study of the oral MEK inhibitor, CI-1040, in patients with advanced non-small-cell lung, breast, colon, and pancreatic cancer. J Clin Oncol 2004, 22:4456-4462.
107. Sebolt-Leopold J.S., Dudley D.T., Herrera R., et al. Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo. Nat Med 1999, 5:810-816.
108. Boasberg P.D., Redfern C.H., Daniels G.A., et al. Pilot study of PD-0325901 in previously treated patients with advanced melanoma, breast cancer, and colon cancer. Cancer Chemother Pharmacol 2011, 68:547-552.
109. Sebolt-Leopold J.S., Herrera R. Targeting the mitogen-activated protein kinase cascade to treat cancer. Nat Rev Cancer 2004, 4:937-947.
110. Adjei A.A., Cohen R.B., Franklin W., et al. Phase I pharmacokinetic and pharmacodynamic study of the oral, small-molecule mitogen-activated protein kinase kinase 1/2 inhibitor AZD6244 (ARRY-142886) in patients with advanced cancers. J Clin Oncol 2008, 26:2139-2146.
111. Yeh T.C., Marsh V., Bernat B.A., et al. Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor. Clin Cancer Res 2007, 13:1576-1583.
112. Banerji U., Camidge D.R., Verheul H.M., et al. The first-in-human study of the hydrogen sulfate (Hyd-sulfate) capsule of the MEK1/2 inhibitor AZD6244 (ARRY-142886): a phase I open-label multicenter trial in patients with advanced cancer. Clin Cancer Res 2010, 16:1613-1623.
113. Dummer R., Robert C., Chapman P., et al. AZD6244 (ARRY-142886) vs temozolomide in patients with advanced melanoma: an open-label, randomized, multicenter, phase II study. J Clin Oncol 2008, 26. Abstract 9033.
114. Infante J.R., Fecher L.A., Nallapareddy S., et al. Safety and efficacy results from the first-in-human study of the oral MEK 1/2 inhibitor GSK1120212. J Clin Oncol 2010, 28(15). Abstract 2503.
115. Yamaguchi T., Kakefuda R., Tajima N., et al. Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int J Oncol 2011, 39:23-31.
116. Falchook G.S., Lewis K.D., Infante J.R., et al. Activity of the oral MEK inhibitor trametinib in patients with advanced melanoma: a phase 1 dose-escalation trial. Lancet Oncol 2012, 13:782-789.
117. Tolcher A.W., Bendell J.C., Patnaik A., et al. A phase Ib study of the MEK inhibitor GSK1120212 combined with gemcitabine i patients with solid tumors: Interim results. J Clin Oncol 2011, 29(4). Abstract 278.
118. Kim K.B., Kefford R., Pavlick A.C., et al. Phase II study of the MEK1/MEK2 inhibitor trametinib in patients with metastatic BRAF-mutant cutaneous melanoma previously treated with or without a BRAF inhibitor. J Clin Oncol 2013, 31:482-489.
119. Isshiki Y., Kohchi Y., Iikura H., et al. Design and synthesis of novel allosteric MEK inhibitor CH4987655 as an orally available anticancer agent. Bioorg Med Chem Lett 2011, 21:1795-1801.
120. Johnston S. XL518, a potent selevtive orally bioavailable MEK1 inhibitor, downregulates the RAS/RAF/MEK/ERK pathway in vivo, resulting in tumor growth inhibition and regression in pre-clinical models. Mol Cancer Ther 2007, 6. Abstract 3595s.
121. Iverson C., Larson G., Lai C., et al. RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer. Cancer Res 2009, 69:6839-6847.
122. Dong Q., Dougan D.R., Gong X., et al. Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer. Bioorg Med Chem Lett 2011, 21:1315-1319.
123. Hoffman-La Roche Limited. Zelboraf Product Monograph. 2012 Feb 2012.
124. Ribas A., Kim K.B., Schuchter L.M., et al. BRIM-2: an open-label, multicenter phase II study of vemurafenib in previously treated patients with BRAF V600E muttion-positive metastatic melanoma. J Clin Oncol 2001, 29. Abstract 8509.
125. King A.J., Patrick D.R., Batorsky R.S., et al. Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885. Cancer Res 2006, 66:11100-11105.
126. Trefzer U., Minor D., Ribas A., et al. BREAK-2: a phase IIA trial of the selective BRAF kinase inhibitor GSK2118436 in patients with BRAF mutation-positive (V600E/K) metastatic melanoma. Pigment Cell Melanoma Res 2011, 24. Abstract 1020.
127. Schwartz G.K., Robertson S., Shen A., et al. A phase I study of XL281, a selective oral RAF kinase inhibitor, in patients (Pts) with advanced solid tumors. J Clin Oncol 2009, 27. Abstract 3513.
128. Zambon A., Niculescu-Duvaz I., Niculescu-Duvaz D., et al. Small molecule inhibitors of BRAF in clinical trials. Bioorg Med Chem Lett 2012, 22:789-792.
129. Sharfman W.H., Hodi F.S., Lawrence D.P., et al. Results from the first-in-human (FIH) phase I study of the oral RAF inhibitor RAF265 administered daily to patients with advanced cutaneous melanoma. J Clin Oncol 2011, 29(15). Abstract 8508.
130. Yamaguchi Y., Otani T., Kishi S. Tomographic features of serous retinal detachment with multilobular dye pooling in acute Vogt-Koyanagi-Harada disease. Am J Ophthalmol 2007, 144:260-265.