The first-in-human study of the solid oral dosage form of AZD6244 (ARRY-142886): A phase I trial in patients (pts) with advanced cancer

Agarwal, Raksheeth; Banerji, Udai; Camidge, D. Ross; Brown, Kathryn H.; Cantarini, Mireille; Morris, Clive; Desar, Ingrid M.E.; Herpen, Carla M. van

doi:10.1200/jco.2008.26.15_suppl.3535

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Mek Inhibitors1

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Cited by 5 publications

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“…In a Phase I study comparing the freebase suspension with the capsule, the new formulation was shown to be a viable successor to the free-base suspension based on its pharmacokinetic and safety profiles [18,19]. Combination regimens using the new formulation are currently being evaluated in Phase II clinical trials.…”

Section: Laboratory and Clinical Parametersmentioning

confidence: 99%

A Phase II, open-label, randomised study to assess the efficacy and safety of the MEK1/2 inhibitor AZD6244 (ARRY-142886) versus capecitabine monotherapy in patients with colorectal cancer who have failed one or two prior chemotherapeutic regimens

et al. 2010

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Section: Laboratory and Clinical Parametersmentioning

confidence: 99%

A Phase II, open-label, randomised study to assess the efficacy and safety of the MEK1/2 inhibitor AZD6244 (ARRY-142886) versus capecitabine monotherapy in patients with colorectal cancer who have failed one or two prior chemotherapeutic regimens

et al. 2010

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“…Several MEK and ERK inhibitors have been tested in cancer treatment. AZD6244 is a potent, selective, non-competitive inhibitor of MEK1/2 that has been studied in a number of solid tumors and has shown interesting activity against thyroid cancer in phase I clinical trials [35]. A multicenter phase II clinical trial is ongoing with AZD6244 in advanced DTC patients (NCT00559949).…”

Section: Mek Inhibitorsmentioning

confidence: 99%

Targeted therapies in thyroid cancer

et al. 2009

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Differentiated thyroid carcinoma is the most frequent neoplasm of the endocrine system. Although thyroid cancer usually has an excellent prognosis, no therapeutic options are available for patients that develop metastases and are or became resistant to radioiodine therapy. The deeper knowledge of molecular aberrations that characterize tumor growth has provided novel targets in cancer therapy. Several proteins have been implicated as having a crucial role in the carcinogenesis of differentiated thyroid cancer, such as those involved in RET/PTC-RAS-RAF-MAPK pathway. Moreover, vascular aberrations and angiogenesis equilibrium have also been related to tumor growth. The development of new, targeted therapies and their encouraging initial results have opened a hopeful opportunity of treatment for these orphan therapy tumor patients.

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Discovery of Allosteric MEK Inhibitors

Wallace

Blake

2009

Kinase Inhibitor Drugs

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The first-in-human study of the solid oral dosage form of AZD6244 (ARRY-142886): A phase I trial in patients (pts) with advanced cancer

Cited by 5 publications

References 0 publications

A Phase II, open-label, randomised study to assess the efficacy and safety of the MEK1/2 inhibitor AZD6244 (ARRY-142886) versus capecitabine monotherapy in patients with colorectal cancer who have failed one or two prior chemotherapeutic regimens

A Phase II, open-label, randomised study to assess the efficacy and safety of the MEK1/2 inhibitor AZD6244 (ARRY-142886) versus capecitabine monotherapy in patients with colorectal cancer who have failed one or two prior chemotherapeutic regimens

Targeted therapies in thyroid cancer

Discovery of Allosteric MEK Inhibitors

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