137 A phase I study of an oral vascular endothelial growth factor receptor-2 (VEGFR-2) tyrosine kinase inhibitor, CP-547,632, in patients with advanced solid tumors

Tolcher, A. W.; O’Leary, James J.; deBono, Johann S.; Molpus, Kelly L.; Woodard, C.; Warnat, M.; Liau, Katherine; Noe, Dennis A.; Healey, Diane; Huberman, Mark S.

doi:10.1016/s1359-6349(04)80145-9

Cited by 13 publications

(7 citation statements)

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“…Dose escalation showed no dose-limiting toxicity up to 160 mg/day. Preliminary safety data reveal no serious adverse events under CP-547, 632 therapy (Tolcher et al 2002). Six out of 22 patients had stable disease for more than 8 weeks and one patient had stable disease for more than 24 weeks.…”

Section: Vegf-r Tyrosine Kinase Inhibitorsmentioning

confidence: 91%

The impact of anti-angiogenic agents on cancer therapy

Marmé

2003

Journal of Cancer Research and Clinical Oncology

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Section: Vegf-r Tyrosine Kinase Inhibitorsmentioning

confidence: 91%

The impact of anti-angiogenic agents on cancer therapy

Marmé

2003

Journal of Cancer Research and Clinical Oncology

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“…CP-547,632 is a selective VEGFR-2 receptor tyrosine kinase inhibitor that is currently in phase I studies (Tolcher et al, 2002).…”

Section: Vegf Receptor Tyrosine Kinase Inhibitorsmentioning

confidence: 99%

Angiogenesis inhibitors in clinical development; where are we now and where are we going?

Eskens

2004

Br J Cancer

174

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Angiogenesis is crucial for tumour growth and the formation of metastases. Various classes of angiogenesis inhibitors that are each able to inhibit one of the various steps of this complex process can be distinguished. Results from clinical studies with these agents are summarised. In general, it has been shown that most angiogenesis inhibitors can be safely administered, but that tumour regressions are rare. Combining angiogenesis inhibitors with cytotoxic chemotherapy can enhance anticancer activity. Recently, some promising data with regard to clinical efficacy have been presented. While performing clinical studies with angiogenesis inhibitors, defining biological activity is crucial, but thus far no validated techniques are available. It is conceivable that in the near future various classes of angiogenesis inhibitors will be combined in an attempt to further improve antiangiogenic and anticancer activity.

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“…CP-547.632 is orally bioavailable, welltolerated, and is currently in phase I trials in cancer patients. Preliminary human pharmacokinetics data in advanced cancer patients were recently disclosed: 24 patients receiving oral administration of CP-547.632 at 35 mg for 14 days to 160 mg per day continuously for a median of 2 courses (range 1-7) [18]. Half-life was estimated to be 29 h. No dose-limiting toxicity or treatment discontinuations were observed in either of the dose cohorts except for a transient non-maculopapular rash and dry mouth observed in 2 of 24 patients.…”

Section: Inhibition Of Proangiogenic Cytokinesmentioning

confidence: 99%

Antiangiogenesis: Current Clinical Data and Future Perspectives

Drevs

Laus²,

Medinger³

et al. 2002

Oncol Res Treat

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Neovascularization is a prerequisite for progressive growth of solid tumors and their metastases. This process is tightly regulated by a large number of proangiogenic and antiangiogenic factors such as VEGF, bFGF and matrix-metalloproteinases. The inhibition of angiogenesis is an innovative therapeutic approach and could represent a powerful adjunct to traditional therapy of malignant tumors. Preclinical trials have been very successful but in clinical studies meaningful response rates could only be shown in some cases. This might indicate the existence of different angiogenic phenotypes in humans. It seems that at present only a part of the interactions between the angiogenic cytokines are known. In addition, new receptor/ligand systems which regulate the neovascularization are being described. This article presents an overview of the most important angiogenically active substances, preclinical and clinical data, surrogate markers as well as future perspectives.

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137 A phase I study of an oral vascular endothelial growth factor receptor-2 (VEGFR-2) tyrosine kinase inhibitor, CP-547,632, in patients with advanced solid tumors

Cited by 13 publications

References 0 publications

The impact of anti-angiogenic agents on cancer therapy

The impact of anti-angiogenic agents on cancer therapy

Angiogenesis inhibitors in clinical development; where are we now and where are we going?

Antiangiogenesis: Current Clinical Data and Future Perspectives

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