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Method of Treating Cancer and Bone Cancer Pain

a bone cancer and cancer technology, applied in the field of cancer treatment, can solve the problems of abnormal deposition of unstructured bone, morbidity and mortality in crpc, and modest improvement in survival, so as to prolong the overall survival of patients and prevent bone metastases.

Inactive Publication Date: 2014-06-26
EXELIXIS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patent describes a new treatment for bone pain and cancer that uses a compound called Compound of Formula I. The patent describes methods for treating or minimizing bone pain associated with lung cancer, breast cancer, melanoma, renal cell carcinoma, or thyroid cancer, as well as methods for extending the overall survival in patients with these cancers. The treatment involves administering a pharmaceutical formulation containing Compound of Formula I or its malate salt to patients in need of such treatment.

Problems solved by technology

Despite progress in systemic therapy for CRPC, improvements in survival are modest, and virtually all patients succumb to this disease with a median survival of about 2 years.
The primary cause of morbidity and mortality in CRPC is metastasis to the bone, which occurs in about 90% of cases.
Although most CRPC patients with bone metastases display features of both types of lesions, prostate cancer bone metastases are often osteoblastic, with abnormal deposition of unstructured bone accompanied by increased skeletal fractures, spinal cord compression, and severe bone pain.

Method used

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  • Method of Treating Cancer and Bone Cancer Pain
  • Method of Treating Cancer and Bone Cancer Pain
  • Method of Treating Cancer and Bone Cancer Pain

Examples

Experimental program
Comparison scheme
Effect test

embodiments

[0048]In one embodiment the compound of Formula I is the compound of Formula Ia:

or a pharmaceutically acceptable salt thereof, wherein:

[0049]R1 is halo;

[0050]R2 is halo; and

[0051]Q is CH or N.

[0052]In another embodiment, the compound of Formula I is Compound 1:

or a pharmaceutically acceptable salt thereof. As indicated previously, compound I is referred to herein as N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide. WO 2005 / 030140 discloses Compound 1 and describes how it is made (Example 12, 37, 38, and 48) and also discloses the therapeutic activity of this compound to inhibit, regulate and / or modulate the signal transduction of kinases, (Assays, Table 4, entry 289). Example 48 is on paragraph [0353] in WO 2005 / 030140.

[0053]In other embodiments, the compound of Formula I, Ia, or Compound 1, or a pharmaceutically acceptable salt thereof, is administered as a pharmaceutical composition, wherein the pharmaceutical composition additio...

case study 1

[0136]Compound 1 is an orally bioavailable multitargeted tyrosine kinase inhibitor with potent activity against MET and VEGFR2. Compound 1 suppresses MET and VEGFR2 signaling, rapidly induces apoptosis of endothelial cells and tumor cells, and causes tumor regression in xenograft tumor models. Compound 1 also significantly reduces tumor invasiveness and metastasis and substantially improves overall survival in a murine pancreatic neuroendocrine tumor model. In a phase 1 clinical study, Compound 1 was generally well-tolerated, with fatigue, diarrhea, anorexia, rash, and palmar-plantar erythrodysesthesia being the most commonly observed adverse events.

[0137]Based on target rationale and observed antitumor activity in clinical studies, an adaptive phase 2 trial was undertaken in multiple indications including CRPC (http: / / clinicaltrials.gov / ct2 / results?term=NCT00940225 for Study NCT00940225 last visited Sep. 20, 2011)), in which Compound 1 was administered as a 100 mg dose to patients....

case study 2

[0149]In a phase 2 adaptive randomized discontinuation trial (RDT), Compound 1 resulted in resolution or stabilization of metastatic bone lesions on bone scan in 82 of 108 (76 percent) patients evaluable by this method. The majority of patients treated with Compound 1 reported reduced bone pain and reduced reliance upon narcotic pain medication. A total of 83 patients had bone metastases and bone pain reported at baseline, and at least one post-baseline assessment of pain status. Of these patients, 56 (68%) had pain improvement at either Week 6 or 12. Narcotic analgesic medication was required at baseline for control of bone pain in 67 patients assessable for post-baseline review of narcotic consumption. Of these 67 patients, 47 (70%) were able to decrease or discontinue narcotic medication for bone pain. Data on bone pain and narcotic use, as assessed by the investigator, were collected retrospectively. These results suggest that Compound 1 can be used to treat and ameliorate bone ...

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Abstract

This invention is directed to the treatment of cancer, particularly lung cancer, breast cancer, melanoma, renal cell carcinoma, thyroid cancer that has metastasized to the bone. The invention is also directed to a method for treating bone cancer pain in an individual in need of such treatment comprising administering to the individual an effective amount of a compound of Formula I.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims the benefit of priority of U.S. Provisional Application No. 61 / 481,682, filed May 2, 2011, and U.S. Provisional Application No. 61 / 557,366, filed Nov. 8, 2011, all of which are incorporated herein by reference.FIELD OF THE INVENTION[0002]This invention is directed to the treatment of cancer, particularly to cancers where bone disease is common. These cancers include breast cancer, melanoma, renal cell carcinoma, and thyroid cancer, as well as others, using a compound of Formula I as disclosed herein. In addition to treating these forms of cancer, the compound of Formula I can be used to treat the pain associated with bone metastases. The ability of the compound of Formula I to treat these and other forms of cancer and the associated bone pain can be monitored using imaging technologies, including magnetic resonance imaging, among other methods.BACKGROUND OF THE INVENTION[0003]Bone disease is common in patients with...

Claims

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Application Information

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IPC IPC(8): C07D215/233
CPCC07D215/233A61K31/536A61P19/00A61P25/04A61P35/00A61P35/04A61K31/517A61K31/47
Inventor SCHWAB, GISELAAFTAB, DANA T.
Owner EXELIXIS INC
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