South San Francisco, CA, United States
South San Francisco, CA, United States

Exelixis is a genomics-based drug discovery company located in South San Francisco, Ca., and the producer of Cometriq, a treatment approved by the U.S. Food and Drug Administration for medullary thyroid cancer with clinical activity in several other types of metastatic cancer. It works on the development of anti-cancer therapies. Exelixis has several compounds in various stages of FDA approval including : XL147 that targets phosphoinositide-3 kinase ; and XL765, which targets PI3K and mTOR, kinases in the PI3K signaling pathway. XL880 The company also has various compounds in phase 1 clinical trials, including XL518 or GDC0973, a small molecule inhibitor of the MEK. Co-developed with Roche. XL228, which targets insulin-like growth factor type 1 receptor, an RTK in a range of human tumors; XL139 that targets Hedgehog; XL413, a small molecule inhibitor of the serine-threonine kinase CDC7; XL888, a synthetic inhibitor of HSP90, a chaperone protein that promotes the activity and stability of a range of regulatory proteins, including kinases.Its lead compound, XL184, has been approved for treatment of medullary thyroid cancer and is currently in a number of clinical trials for prostate, ovarian, brain, melanoma, breast, non-small cell lung, hepatocellular, kidney. During its trial for the treatment of medullary thyroid cancer, XL184 was designated orphan drug status by the FDA and given the generic name, cabozantinib. Cabozantinib is an inhibitor of the tyrosine kinases Met and VEGFR2, and has been shown to abrogate tumor growth, metastasis, and angiogenesis. Wikipedia.


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Patent
Exelixis | Date: 2015-04-27

This invention is directed to the treatment of cancer in a patient, particularly a patient with lung adenocarcinoma, and more particularly a patient with SLC34A2-ROS1, CD74-ROS1, or FIG-ROS1 fusion-positive non-small cell lung cancer, with an inhibitor of MET, VEGFR2, and ROS1 which is a compound of Formula (I): or a pharmaceutically acceptable salt thereof.


Patent
Exelixis | Date: 2015-03-17

The invention relates to administration of various pharmaceutical formulations of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, (cabozantinib) a c-Met inhibitor, and its metabolites, to achieve desirable pharmacokinetic and pharmacodynamic effects.


The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.


The present invention is directed to processes for making and compositions containing quinolines such as formula I or pharmaceutically acceptable salts thereof wherein: X1 is H, Br, Cl, or X2 is H, Br, Cl, or n1 is 1-2; and n2 is 1-2.


Patent
Exelixis | Date: 2017-02-07

Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.


Patent
Exelixis | Date: 2017-01-25

The invention relates to administration of various pharmaceutical formulations of N- (4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N-(4-fluorophenyl)cyclopropane-1,1- dicarboxamide, (cabozantinib) a c-Met inhibitor, and its metabolites, to achieve desirable pharmacokinetic and pharmacodynamic effects.


Patent
Exelixis | Date: 2016-06-07

Compounds, pharmaceutically acceptable salts, isomers, or prodrugs thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.


Patent
Exelixis | Date: 2016-04-20

A process for preparing a compound of Formula I is disclosed, comprising the steps: wherein:


Patent
Exelixis | Date: 2015-11-05

This invention is directed to the treatment of cancer, particularly ocular melanoma, with a dual inhibitor of MET and VEGF such as Compound 1.


Patent
Exelixis | Date: 2016-03-10

The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

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