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Metabolites of N-(4-{[6,7-Bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

a technology of phenyl)n and phenyl)n, which is applied in the field of metabolites of n(4 6, 7bis (methyloxy) quinolin4yloxy ) phenyl)n ′(4fluorophenyl) cyclopropane1, 1dicarboxamide, can solve problems such as altered cellular properties

Pending Publication Date: 2021-01-07
EXELIXIS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Benefits of technology

The patent text describes compounds that can be used in various methods to determine the activity of protein kinases. These compounds can also be used as internal standards in related methods.

Problems solved by technology

Since protein kinases and their ligands play critical roles in various cellular activities, deregulation of protein kinase enzymatic activity can lead to altered cellular properties, such as uncontrolled cell growth associated with cancer.

Method used

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  • Metabolites of N-(4-{[6,7-Bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
  • Metabolites of N-(4-{[6,7-Bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
  • Metabolites of N-(4-{[6,7-Bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

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Identification of Cabozantinib Metabolites

[0117]The objective of this study was to profile and identify metabolites of cabozantinib in human plasma, urine, and feces. The plasma, urine and fecal samples were collected from a mass balance study of cabozantinib following a single 175 mg oral administration of cabozantinib (L-malate salt) containing [14C] cabozantinib (100 μCi) in healthy male subjects.

Study Design and Plasma, Urine, and Feces Sampling

[0118]Eight male subjects participated in the study, and each subject received a single oral dose of 175 mg of cabozantinib (L-malate salt) containing [14C]-cabozantinib (100 μCi). The plasma, urine, and fecal samples were collected from the 8 subjects for the metabolite profiling.

Plasma samples were collected at pre-dose, 0.5, 1, 2, 3, 4, 5, 8, 14, 24, 72, 168, 336, 504 and 648 hours post-dose; urine samples were collected at pre-dose, 0-8 hours, 8-24 hours, at 24-hour intervals to 480 hours post-dose, and at greater than 48-hour interva...

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Abstract

The invention relates to metabolites of cabozantinib (I) as well as uses thereof.

Description

PRIORITY CLAIM[0001]This application claims priority to U.S. Ser. No. 61 / 792,413, filed Mar. 15, 2013. The entire contents of the aforementioned application are incorporated herein.TECHNICAL FIELD[0002]This disclosure relates to metabolites of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy})phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, a c-Met inhibitor.BACKGROUND[0003]Traditionally, dramatic improvements in the treatment of cancer are associated with identification of therapeutic agents acting through novel mechanisms. One mechanism that can be exploited in cancer treatment is the modulation of protein kinase activity because signal transduction through protein kinase activation is responsible for many of the characteristics of tumor cells. Protein kinase signal transduction is of particular relevance in, for example, thyroid, gastric, head and neck, lung, breast, prostate, and colorectal cancers, as well as in the growth and proliferation of brain tumor cells.[0004]Protei...

Claims

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Application Information

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IPC IPC(8): C07D215/22C07C305/24C07C233/60C07D215/60G01N33/487
CPCC07D215/22C07C305/24C07C233/60G01N2570/00G01N33/487C07C2601/02C07D215/60A61P35/00
Inventor AFTAB, DANA T.NAGANATHAN, SRIRAMXU, WEILACY, STEVENNGUYEN, LINH
Owner EXELIXIS INC