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Volumn 30, Issue 6, 2012, Pages 2334-2343

Phase i study of the safety, tolerability and pharmacokinetics of PHA-848125AC, a dual tropomyosin receptor kinase A and cyclin-dependent kinase inhibitor, in patients with advanced solid malignancies

Author keywords

Cyclin dependent kinase; Investigational agent; PHA 848125AC; Phase I clinical trial; Tropomyosin receptor kinase A

Indexed keywords

CYCLIN DEPENDENT KINASE; CYCLIN DEPENDENT KINASE INHIBITOR; PHA 848125AC; PHOSPHOTRANSFERASE; TROPOMYOSIN RECEPTOR KINASE A; UNCLASSIFIED DRUG;

EID: 84875505550     PISSN: 01676997     EISSN: 15730646     Source Type: Journal    
DOI: 10.1007/s10637-011-9774-6     Document Type: Article
Times cited : (32)

References (37)
  • 1
    • 32644432029 scopus 로고    scopus 로고
    • Clinical relevance of the neurotro-phins and their receptors
    • Allen SJ, Dawbarn D (2006) Clinical relevance of the neurotro-phins and their receptors. Clinical Science 110:175-191
    • (2006) Clinical Science , vol.110 , pp. 175-191
    • Allen, S.J.1    Dawbarn, D.2
  • 2
    • 3343020830 scopus 로고    scopus 로고
    • Epidermal growth factor, neuro-trophins and the metastatic cascade in prostate cancer
    • Montano X, Djamgoz MB (2004) Epidermal growth factor, neuro-trophins and the metastatic cascade in prostate cancer. FEBS Lett 571:1-8
    • (2004) FEBS Lett , vol.571 , pp. 1-8
    • Montano, X.1    Djamgoz, M.B.2
  • 3
    • 0242610430 scopus 로고    scopus 로고
    • Reverse transcription-PCR analysis of laser-captured cells points to potential paracrine and autocrine actions of neurotrophins in pancreatic cancer
    • Ketterer K, Rao S, Friess H, Weiss J, Büchler MW, Korc M (2003) Reverse transcription-PCR analysis of laser-captured cells points to potential paracrine and autocrine actions of neurotrophins in pancreatic cancer. Clin Cancer Res 9:5127-5136
    • (2003) Clin Cancer Res , vol.9 , pp. 5127-5136
    • Ketterer, K.1    Rao, S.2    Friess, H.3    Weiss, J.4    Büchler, M.W.5    Korc, M.6
  • 5
    • 0031872458 scopus 로고    scopus 로고
    • Cell cycle-independent death of prostate adenocar-cinoma is induced by the TRK tyrosine kinase inhibitor CEP-751 (KT6587)
    • Dionne CA, Camoratto AM, Jani JP, Emerson E, Neff N, Vaught JL et al (1998) Cell cycle-independent death of prostate adenocar-cinoma is induced by the TRK tyrosine kinase inhibitor CEP-751 (KT6587). Clin Cancer Res 4:1887-1898
    • (1998) Clin Cancer Res , vol.4 , pp. 1887-1898
    • Dionne, C.A.1    Camoratto, A.M.2    Jani, J.P.3    Emerson, E.4    Neff, N.5    Vaught, J.L.6
  • 6
    • 0032939723 scopus 로고    scopus 로고
    • Neurotrophins and TRK receptors in human pancreatic Ductal adenocarcinoma: Expression patterns and effects on in vitro invasive behavior
    • Miknyoczki SJ, Lang D, Huang L, Klein-Szanto AJ, Dionne CA, Ruggeri BA (1999) Neurotrophins and TRK receptors in human pancreatic Ductal adenocarcinoma: Expression patterns and effects on in vitro invasive behavior. Int J Cancer 81:417-427
    • (1999) Int J Cancer , vol.81 , pp. 417-427
    • Miknyoczki, S.J.1    Lang, D.2    Huang, L.3    Klein-Szanto, A.J.4    Dionne, C.A.5    Ruggeri, B.A.6
  • 8
    • 0037500963 scopus 로고    scopus 로고
    • Expression and activation of the nerve growth factor receptor TRKA in serous ovarian carcinoma
    • Davidson B, Reich R, Lazarovici P, Nesland JM, Skrede M, Risberg B et al (2003) Expression and activation of the nerve growth factor receptor TRKA in serous ovarian carcinoma. Clin Cancer Res 9:2248-2259
    • (2003) Clin Cancer Res , vol.9 , pp. 2248-2259
    • Davidson, B.1    Reich, R.2    Lazarovici, P.3    Nesland, J.M.4    Skrede, M.5    Risberg, B.6
  • 9
    • 30144437331 scopus 로고    scopus 로고
    • Oncogenic rearrangements of the NTRK1/NGF receptor
    • Pierotti MA, Greco A (2006) Oncogenic rearrangements of the NTRK1/NGF receptor. Cancer Lett 232:90-98
    • (2006) Cancer Lett , vol.232 , pp. 90-98
    • Pierotti, M.A.1    Greco, A.2
  • 10
    • 8644219655 scopus 로고    scopus 로고
    • Living with or without cyclins and cyclin-dependent kinases
    • Sherr CJ, Roberts JM (2004) Living with or without cyclins and cyclin-dependent kinases. Genes Dev 18:2699-2711
    • (2004) Genes Dev , vol.18 , pp. 2699-2711
    • Sherr, C.J.1    Roberts, J.M.2
  • 11
    • 0035754080 scopus 로고    scopus 로고
    • To cycle or not to cycle: A critical decision in cancer
    • Malumbres M, Barbacid M (2001) To cycle or not to cycle: a critical decision in cancer. Nat Rev Cancer 1:222-231
    • (2001) Nat Rev Cancer , vol.1 , pp. 222-231
    • Malumbres, M.1    Barbacid, M.2
  • 12
  • 13
    • 0347917093 scopus 로고    scopus 로고
    • Cell-cycle targeted therapies
    • Swanton C (2004) Cell-cycle targeted therapies. Lancet Oncol 5:27-36
    • (2004) Lancet Oncol , vol.5 , pp. 27-36
    • Swanton, C.1
  • 14
    • 0034092911 scopus 로고    scopus 로고
    • Regulation of the cdk inhibitor p27 and its deregulation in cancer
    • Slingerland J, Pagano M (2000) Regulation of the cdk inhibitor p27 and its deregulation in cancer. J Cell Physiol 183:10-17
    • (2000) J Cell Physiol , vol.183 , pp. 10-17
    • Slingerland, J.1    Pagano, M.2
  • 15
    • 0034030234 scopus 로고    scopus 로고
    • P27: A pleiotropic regulator of cellular phenotype and a target for cell cycle dysregulation in cancer
    • Desdouets C, Bréchot C (2000) p27: a pleiotropic regulator of cellular phenotype and a target for cell cycle dysregulation in cancer. Pathol Biol (Paris) 48:203-210
    • (2000) Pathol Biol (Paris) , vol.48 , pp. 203-210
    • Desdouets, C.1    Bréchot, C.2
  • 16
    • 0035095973 scopus 로고    scopus 로고
    • Regulation of the retinoblastoma tumor suppressor protein by cyclin/cdks
    • Adams PD (2001) Regulation of the retinoblastoma tumor suppressor protein by cyclin/cdks. Biochim Biophys Acta 1471: M123-M133
    • (2001) Biochim Biophys Acta , vol.1471
    • Adams, P.D.1
  • 17
    • 0041854279 scopus 로고    scopus 로고
    • Cyclin-dependent kinase 2 is essential for meiosis but not for mitotic cell division in mice
    • Epub 2003 Aug 17
    • Ortega S, Prieto I, Odajima J, Martín A, Dubus P, Sotillo R et al (2003) Cyclin-dependent kinase 2 is essential for meiosis but not for mitotic cell division in mice. Nat Genet 35:25-31, Epub 2003 Aug 17
    • (2003) Nat Genet , vol.35 , pp. 25-31
    • Ortega, S.1    Prieto, I.2    Odajima, J.3    Martín, A.4    Dubus, P.5    Sotillo, R.6
  • 19
    • 0041828595 scopus 로고    scopus 로고
    • Cell proliferation without cyclin E-CDK2
    • Méndez J (2003) Cell proliferation without cyclin E-CDK2. Cell 114(4):398-399
    • (2003) Cell , vol.114 , Issue.4 , pp. 398-399
    • Méndez, J.1
  • 21
    • 69049103115 scopus 로고    scopus 로고
    • Identification of N 1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl) phenyl]amino}-4,5-dihydro-1H-pyrazolo [4,3-h]quinazoline-3-carboxamide (PHA-848125) a potent orally available cyclin dependent kinase inhibitor
    • Brasca MG, Amboldi N, Ballinari D, Cameron A, Casale E, Cervi G et al (2009) Identification of N, 1, 4, 4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl) phenyl]amino}-4, 5-dihydro-1H-pyrazolo [4, 3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor. J Med Chem 52:5152-5163
    • (2009) J Med Chem , vol.52 , pp. 5152-5163
    • Brasca, M.G.1    Amboldi, N.2    Ballinari, D.3    Cameron, A.4    Casale, E.5    Cervi, G.6
  • 22
    • 0034594628 scopus 로고    scopus 로고
    • New guidelines to evaluate the response to treatment in solid tumors. European Organization for Research and Treatment of Cancer, National Cancer Institute of the United States, National Cancer Institute of Canada
    • Therasse P, Arbuck SG, Eisenhauer EA, Wanders J, Kaplan RS, Rubinstein L et al (2000) New guidelines to evaluate the response to treatment in solid tumors. European Organization for Research and Treatment of Cancer, National Cancer Institute of the United States, National Cancer Institute of Canada. J Natl Cancer Inst 92:205-216
    • (2000) J Natl Cancer Inst , vol.92 , pp. 205-216
    • Therasse, P.1    Arbuck, S.G.2    Eisenhauer, E.A.3    Wanders, J.4    Kaplan, R.S.5    Rubinstein, L.6
  • 23
    • 44849096697 scopus 로고    scopus 로고
    • The MERITO Study: A multicentre trial of the analgesic effect and tolerability of normal-release oral morphine during 'titration phase' in patients with cancer pain
    • De Conno F, Ripamonti C, Fagnoni E, Brunelli C, Luzzani M, Maltoni M et al (2008) The MERITO Study: a multicentre trial of the analgesic effect and tolerability of normal-release oral morphine during 'titration phase' in patients with cancer pain. Palliat Med 22:214-221
    • (2008) Palliat Med , vol.22 , pp. 214-221
    • De Conno, F.1    Ripamonti, C.2    Fagnoni, E.3    Brunelli, C.4    Luzzani, M.5    Maltoni, M.6
  • 24
    • 84875494106 scopus 로고    scopus 로고
    • Phase i study of the oral CDK-TRKA inhibitor PHA-848125 administered with prolonged schedule of administration
    • suppl; abstr 3065
    • Cresta S, SessaC, Del Conte G, Locatelli A, Gallerani E, FiorentiniF, et al. Phase I study of the oral CDK-TRKA inhibitor PHA-848125 administered with prolonged schedule of administration. J Clin Oncol 28:15 s, 2010 (suppl; abstr 3065)
    • J Clin Oncol , vol.28 , Issue.15 S , pp. 2010
    • Cresta, S.1    Sessac Del Conte, G.2    Locatelli, A.3    Fiorentinif, G.E.4
  • 25
    • 77955495586 scopus 로고    scopus 로고
    • Dual targeting of CDK and tropomyosin receptor kinase families by the oral inhibitor PHA-848125, an agent with broad-spectrum antitumor efficacy
    • Albanese C, Alzani R, Amboldi N, Avanzi N, Ballinari D, Brasca MG et al (2010) Dual targeting of CDK and tropomyosin receptor kinase families by the oral inhibitor PHA-848125, an agent with broad-spectrum antitumor efficacy. Mol Cancer Ther 9:2243-2254
    • (2010) Mol Cancer Ther , vol.9 , pp. 2243-2254
    • Albanese, C.1    Alzani, R.2    Amboldi, N.3    Avanzi, N.4    Ballinari, D.5    Brasca, M.G.6
  • 26
    • 20844444589 scopus 로고    scopus 로고
    • Phase i trial of orally administered CEP-701, a novel neurotrophin receptor-linked tyrosine kinase inhibitor
    • Marshall JL, Kindler H, Deeken J, Bhargava P, Vogelzang NJ, Rizvi N et al (2005) Phase I trial of orally administered CEP-701, a novel neurotrophin receptor-linked tyrosine kinase inhibitor. Invest New Drugs 23:31-37
    • (2005) Invest New Drugs , vol.23 , pp. 31-37
    • Marshall, J.L.1    Kindler, H.2    Deeken, J.3    Bhargava, P.4    Vogelzang, N.J.5    Rizvi, N.6
  • 27
    • 0033375469 scopus 로고    scopus 로고
    • Flavopiridol: The first cyclin-dependent kinase inhibitor in human clinical trials
    • Senderowicz AM (1999) Flavopiridol: the first cyclin-dependent kinase inhibitor in human clinical trials. Invest New Drugs 17:313-320
    • (1999) Invest New Drugs , vol.17 , pp. 313-320
    • Senderowicz, A.M.1
  • 28
    • 0031670668 scopus 로고    scopus 로고
    • Phase i trial of continuous infusion flavopiridol, a novel cyclin-dependent kinase inhibitor, in patients with refractory neoplasms
    • Senderowicz AM, Headlee D, Stinson SF, Lush RM, Kalil N, Villalba L et al (1998) Phase I trial of continuous infusion flavopiridol, a novel cyclin-dependent kinase inhibitor, in patients with refractory neoplasms. J Clin Oncol 16:2986-2999
    • (1998) J Clin Oncol , vol.16 , pp. 2986-2999
    • Senderowicz, A.M.1    Headlee, D.2    Stinson, S.F.3    Lush, R.M.4    Kalil, N.5    Villalba, L.6
  • 29
    • 20344387478 scopus 로고    scopus 로고
    • Chronic lymphocytic leukemia: A niche for flavopiridol?
    • Brown JR (2005) Chronic lymphocytic leukemia: a niche for flavopiridol? Clin Cancer Res 11:3971-3973
    • (2005) Clin Cancer Res , vol.11 , pp. 3971-3973
    • Brown, J.R.1
  • 30
    • 33846254185 scopus 로고    scopus 로고
    • A phase i trial of the selective oral cyclin-dependent kinase inhibitor seliciclib (CYC202; R-Roscovitine), administered twice daily for 7 days every 21 days
    • Epub 2006 Dec 19
    • Benson C, White J, De Bono J, O'Donnell A, Raynaud F, Cruickshank C et al (2007) A phase I trial of the selective oral cyclin-dependent kinase inhibitor seliciclib (CYC202; R-Roscovitine), administered twice daily for 7 days every 21 days. Br J Cancer 96:29-37, Epub 2006 Dec 19
    • (2007) Br J Cancer , vol.96 , pp. 29-37
    • Benson, C.1    White, J.2    De Bono, J.3    O'Donnell, A.4    Raynaud, F.5    Cruickshank, C.6
  • 31
    • 77951944979 scopus 로고    scopus 로고
    • Safety, tolerability, pharmacokinetics and pharmacodynamics of the oral cyclin-dependent kinase inhibitor AZD5438 when administered at intermittent and continuous dosing schedules in patients with advanced solid tumours
    • Epub 2009 Oct 13
    • Boss DS, Schwartz GK, Middleton MR, Amakye DD, Swaisland H, Midgley RS et al (2010) Safety, tolerability, pharmacokinetics and pharmacodynamics of the oral cyclin-dependent kinase inhibitor AZD5438 when administered at intermittent and continuous dosing schedules in patients with advanced solid tumours. Ann Oncol 21:884-894, Epub 2009 Oct 13
    • (2010) Ann Oncol , vol.21 , pp. 884-894
    • Boss, D.S.1    Schwartz, G.K.2    Middleton, M.R.3    Amakye, D.D.4    Swaisland, H.5    Midgley, R.S.6
  • 32
    • 84875531325 scopus 로고    scopus 로고
    • Phase i study of the CDK inhibitor dinaciclib (SCH 727965) in patients (pts) with relapsed/refractory CLL
    • suppl; abstr 6623
    • Flynn JM, Jones JA, Andritsos L, Blum KA, Johnson AJ, Hessler J, et al. (2011) Phase I study of the CDK inhibitor dinaciclib (SCH 727965) in patients (pts) with relapsed/refractory CLL. J Clin Oncol 29: (suppl; abstr 6623)
    • (2011) J Clin Oncol , vol.29
    • Flynn, J.M.1    Jones, J.A.2    Andritsos, L.3    Blum, K.A.4    Johnson, A.J.5    Hessler, J.6
  • 35
    • 0032055497 scopus 로고    scopus 로고
    • Flavopiridol induces apoptosis of normal lymphoid cells, causes immunosuppression, and has potent antitumor activity in vivo against human and leukemia xenografts
    • Arguello F, Alexander M, Sterry J, Tudor G, Smith EM, Kalavar NT et al (1998) Flavopiridol induces apoptosis of normal lymphoid cells, causes immunosuppression, and has potent antitumor activity in vivo against human and leukemia xenografts. Blood 91:2482-2490
    • (1998) Blood , vol.91 , pp. 2482-2490
    • Arguello, F.1    Alexander, M.2    Sterry, J.3    Tudor, G.4    Smith, E.M.5    Kalavar, N.T.6
  • 36
    • 25144438475 scopus 로고    scopus 로고
    • Expression of neurotrophin receptors in surgically resected thymic epithelial tumors
    • Kim DJ, Yang WI, Kim SH, Park IK, Chung KY (2005) Expression of neurotrophin receptors in surgically resected thymic epithelial tumors. Eur J Cardiothorac Surg 28:611-616
    • (2005) Eur J Cardiothorac Surg , vol.28 , pp. 611-616
    • Kim, D.J.1    Yang, W.I.2    Kim, S.H.3    Park, I.K.4    Chung, K.Y.5
  • 37
    • 77957941177 scopus 로고    scopus 로고
    • A synthetic cell-penetrating peptide antagonizing TrkA function suppresses neuropathic pain in mice
    • Epub 2010 Aug 11
    • Ma WY, Murata E, Ueda K, Kuroda Y, Cao MH, Abe M, et al. A synthetic cell-penetrating peptide antagonizing TrkA function suppresses neuropathic pain in mice. J Pharmacol Sci 2010;114:79-84. Epub 2010 Aug 11.
    • (2010) J Pharmacol Sci , vol.114 , pp. 79-84
    • Ma, W.Y.1    Murata, E.2    Ueda, K.3    Kuroda, Y.4    Cao, M.H.5    Abe, M.6


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