Combinations of cabozantinib and atezolizumab to treat cancer

A technology of atezolizumab and a combination, applied in the field of combination of cabozantinib and atezolizumab for the treatment of cancer

Pending Publication Date: 2019-10-18
EXELIXIS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Despite these advances, there is still room for improvement

Method used

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  • Combinations of cabozantinib and atezolizumab to treat cancer
  • Combinations of cabozantinib and atezolizumab to treat cancer
  • Combinations of cabozantinib and atezolizumab to treat cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach 1

[0194] Embodiment 1. A method of treating locally advanced or metastatic solid tumors comprising administering a compound of formula I to a patient in need of such treatment:

[0195]

[0196] Or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising a compound of formula I or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier, wherein:

[0197] R 1 is halo;

[0198] R 2 is halo; and

[0199] Q is CH or N;

[0200] In combination with atezolizumab.

[0201] Embodiment 2. The method of Embodiment 1, wherein the compound of Formula I is Compound 1 or a pharmaceutically acceptable salt thereof.

[0202]

[0203] Embodiment 3. The method of Embodiment 2, wherein Compound 1 is administered as the L-malate salt.

[0204] Embodiment 4. The method of Embodiment 2, wherein Compound 1 is administered as the S-malate salt.

[0205] Embodiment 5. The method of embodiments 2-4, wherein atezolizumab is administere...

Embodiment 1

[0261] Example 1. Summary of an experimental clinical trial investigating the combination of cabozantinib (XL184) and atezolizumab in subjects with locally advanced or metastatic solid tumors such as advanced UC, RCC, CRPC and NSCLC

[0262] Fundamental

[0263] Multitargeted tyrosine kinase inhibitors (TKIs) and immune checkpoint inhibitors (ICIs) represent two systemic modalities that have made recent advances in anticancer therapy in recent years. Both classes of therapy have shown broad clinical efficacy, resulting in new approved treatment options in multiple tumor types including: Renal Cell Carcinoma (RCC), Urothelial Carcinoma (UC), Melanoma, Non-Small Cell Lung Cancer (NSCLC) and so on. The success of these therapy types as single agents with distinct mechanisms of action has naturally drawn attention to the evaluation of combinations of TKIs and ICIs in search of further, possibly synergistic, anticancer clinical effects.

[0264] Atezolizumab is a humanized immu...

Embodiment 2

[0465] Example 2. Phase Ib Study of Cabozantinib and Atezolizumab for the Treatment of Locally Advanced or Metastatic Solid Tumors

[0466] 1. Background and Rationale

[0467] 1.1 Background

[0468] Multitargeted tyrosine kinase inhibitor (TKI) and immune checkpoint inhibitor (ICI) immunotherapy represent two systemic modalities that have contributed to recent advances in anticancer therapy. Both classes of therapy have shown broad clinical efficacy, resulting in new approved treatment options in multiple tumor types including: Renal Cell Carcinoma (RCC), Urothelial Carcinoma (UC), Melanoma, Non-Small Cell Lung Cancer (NSCLC) and so on. The success of these therapy types as single agents with distinct mechanisms of action has naturally drawn attention to the evaluation of combinations of TKIs and ICIs in search of further, possibly synergistic, anticancer clinical effects.

[0469] 1.1.1 Atezolizumab

[0470] Atezolizumab is a humanized immunoglobulin (Ig) G1 monoclonal ...

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Abstract

This invention relates to the combination of cabozantinib and atezolizumab to treat locally advanced or metastatic solid tumors, particularly advanced urothelial cancer or renal cell carcinoma.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit and priority of U.S. Provisional Application 62 / 448,869, filed January 20, 2017, and U.S. Provisional Application 62 / 458,447, filed February 13, 2017, the disclosures of which are incorporated by reference in their entirety Incorporated into this article. [0003] field of invention [0004] The present invention relates to the combination of cabozantinib and atezolizumab for the treatment of locally advanced or metastatic solid tumors. [0005] Background of the invention [0006] Multitargeted tyrosine kinase inhibitors (TKIs) and immune checkpoint inhibitors (ICIs) represent two systemic modalities that have made recent advances in anticancer therapy in recent years. Both classes of therapy have shown broad clinical efficacy, resulting in new approved treatment options in multiple tumor types including: Renal Cell Carcinoma (RCC), Urothelial Carcinoma (UC), Melanoma, Non-Small Cell...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/47A61K9/00A61K45/06A61P35/00A61P35/04
CPCA61K39/39558A61K45/06A61K9/2018A61K31/47C07K16/2827A61K2039/545C07K2317/76A61P35/00A61P35/04A61K2300/00A61K2039/505
Inventor G·施瓦布C·谢佛德C·海塞尔
Owner EXELIXIS INC
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