Abstract: Provided herein are methods for the treatment of liver cancer. These methods encompass the administration of a compound comprising a modified oligonucleotide, wherein the modified oligonucleotide is targeted to a miRNA. Also provided herein are compositions for the treatment of liver cancer. Such compositions include compounds comprising a modified oligonucleotide, wherein the modified oligonucleotide is targeted to a miRNA. Certain miRNAs have been identified as overexpressed in liver cancer, such as, for example, hepatocellular carcinoma, and are thus selected for targeting by modified oligonucleotides. Further, certain miRNAs have been identified as overexpressed in hepatocellular carcinoma cells exposed to dioxin, and are thus selected for targeting by modified oligonucleotides. Antisense inhibition of certain of these miRNAs has been found to inhibit cell proliferation and induce apoptosis.
Abstract: Described herein are compounds comprising modified oligonucleotides that are complementary to miR-103 and/or miR-107 and methods of treating diseases and disorders using the compounds.
Type:
Application
Filed:
September 25, 2018
Publication date:
May 23, 2019
Applicant:
Regulus Therapeutics Inc.
Inventors:
Balkrishen Bhat, Neil W. Gibson, Diedre MacKenna, Brandee Wagner, David P. Bartel
Abstract: Provided herein are methods for the treatment of poly-cystic kidney disease, including autosomal dominant polycystic kidney disease, using modified oligonucleotides targeted to miR-17.
Type:
Application
Filed:
August 25, 2016
Publication date:
May 23, 2019
Applicants:
Regulus Therapeutics Inc., Board of Regents of the University of Texas System
Inventors:
John R. Androsavich, B. Nelson Chau, Vishal D. Patel
Abstract: Described herein are compositions and methods for the inhibition of miR-122 activity. The compositions have certain nucleoside modifications that yield potent inhibitors of miR-122 activity. The compounds may comprise conjugates to facilitate delivery to the liver. The compositions may be administered to subjects infected with hepatitis C virus, as a treatment for hepatitis C virus and related conditions.
Abstract: Described herein are conjugated modified oligonucleotides that are complementary to a target RNA. The conjugate facilitates cellular uptake of the modified oligonucleotide, resulting improved potency.
Abstract: Compounds, compositions and methods are provided for modulating the expression and function of small non-coding RNAs. The compositions comprise oligomeric compounds, targeted to small non-coding RNAs. Methods of using these compounds for modulation of small non-coding RNAs as well as downstream targets of these RNAs and for diagnosis and treatment of disease associated with small non-coding RNAs are also provided.
Type:
Application
Filed:
September 6, 2018
Publication date:
February 28, 2019
Applicant:
Regulus Therapeutics Inc.
Inventors:
Christine Esau, Bridget Lollo, C. Frank Bennett, Susan M. Freier, Richard H. Griffey, Brenda F. Baker, Timothy A. Vickers, Eric G. Marcusson, Erich Koller, Eric E. Swayze, Ravi Jain, Balkrishen Bhat, Eigen Peralta
Abstract: The disclosure includes methods of determining the activity of an inhibitor of a target microRNA (miRNA) or of a mimic of a target microRNA. Determination of polysome occupancy in treated and control samples followed by comparing the occupancies can be used to determine a displacement value for the inhibitor or mimic of the target miRNA. The displacement value reflects the extent of a change in the levels of the target miRNA (which may include the mimic if applicable) in polysomal and non-polysomal compartments of a sample or a shift of the target miRNA between polysomal and non-polysomal compartments of a sample and can indicate the activity of the inhibitor toward the target miRNA or of the mimic toward a target RNA.
Type:
Application
Filed:
September 2, 2016
Publication date:
December 20, 2018
Applicant:
Regulus Therapeutics Inc.
Inventors:
John R. Androsavich, B. Nelson Chau, Ryan R. Galasso
Abstract: Described herein are compositions and methods for the inhibition of miR-21 activity. The compositions have certain nucleoside modifications that yield potent inhibitors of miR-21 activity. The compounds may comprise conjugates to facilitate delivery to the liver. The compositions may be administered to subjects with liver conditions, such as liver cancer.
Abstract: Described herein are compositions and methods for the inhibition of miR-122 activity. The compositions have certain nucleoside modifications that yield potent inhibitors of miR-122 activity. The compounds may comprise conjugates to facilitate delivery to the liver. The compositions may be administered to subjects infected with hepatitis C virus, as a treatment for hepatitis C virus and related conditions.
Abstract: Described herein are compounds comprising modified oligonucleotides that are complementary to miR-103 and/or miR-107 and methods of treating diseases and disorders using the compounds.
Type:
Grant
Filed:
October 5, 2017
Date of Patent:
November 27, 2018
Assignee:
Regulus Therapeutics Inc.
Inventors:
Balkrishen Bhat, Neil W. Gibson, Diedre MacKenna, Brandee Wagner, David P. Bartel
Abstract: Provided herein are compositions and methods for the modulation of miR-214 for the treatment and/or prevention of fibrosis and fibroproliferative conditions.
Abstract: Described herein are compositions and methods for the inhibition of miR-21 activity. The compositions have certain nucleoside modification patterns that yield potent inhibitors of miR-21 activity. The compositions may be used to inhibit miR-21, and also to treat diseases associated with abnormal expression of miR-21, such as fibrosis and cancer.
Abstract: Provided herein are methods for the treatment of Alport Syndrome, using modified oligonucleotides targeted to miR-21. In certain embodiments, a modified oligonucleotide targeted to miR-21 improves kidney function and/or reduces fibrosis in subjects having Alport Syndrome. In certain embodiments, administration of a modified oligonucleotide targeted to miR-21 delays the onset of end-stage renal disease in a subject having Alport Syndrome. In certain embodiments, a modified oligonucleotide targeted to miR-21 delays the need for dialysis or kidney transplant in a subject having Alport Syndrome.
Type:
Application
Filed:
April 9, 2018
Publication date:
October 18, 2018
Applicant:
Regulus Therapeutics Inc.
Inventors:
Jeremy Duffield, Balkrishen Bhat, Deidre MacKenna
Abstract: Compounds, compositions and methods are provided for modulating the expression and function of small non-coding RNAs. The compositions comprise oligomeric compounds, targeted to small non-coding RNAs. Methods of using these compounds for modulation of small non-coding RNAs as well as downstream targets of these RNAs and for diagnosis and treatment of disease associated with small non-coding RNAs are also provided.
Type:
Grant
Filed:
April 4, 2017
Date of Patent:
October 9, 2018
Assignee:
Regulus Therapeutics Inc.
Inventors:
C. Frank Bennett, Susan M. Freier, Richard H. Griffey
Abstract: Compounds, compositions and methods are provided for modulating the expression and function of small non-coding RNAs. The compositions comprise oligomeric compounds, targeted to small non-coding RNAs. Methods of using these compounds for modulation of small non-coding RNAs as well as downstream targets of these RNAs and for diagnosis and treatment of disease associated with small non-coding RNAs are also provided.
Type:
Grant
Filed:
July 31, 2017
Date of Patent:
September 11, 2018
Assignee:
Regulus Therapeutics Inc.
Inventors:
C. Frank Bennett, Susan M. Freier, Richard H. Griffey
Abstract: Described herein are compounds comprising modified oligonucleotides that are complementary to miR-103 and/or miR-107 and methods of treating diseases and disorders using the compounds.
Type:
Application
Filed:
October 5, 2017
Publication date:
June 21, 2018
Applicant:
Regulus Therapeutics Inc.
Inventors:
Balkrishen Bhat, Neil W. Gibson, Diedre MacKenna, Brandee Wagner, David P. Bartel
Abstract: Methods are provided for the treatment of cardiovascular or metabolic diseases characterized by elevated serum total cholesterol, elevated serum LDL-cholesterol, or elevated serum triglycerides, through the administration of an oligomeric compound which modulates the levels or activity of miR-122a. Further provided are methods for reducing hepatic steatosis or liver tissue triglyceride accumulation through the administration of an oligomeric compound which modulates the levels or activity of miR-122a. Such methods employ oligomeric compounds which hybridize with or sterically interfere with nucleic acid molecules comprising or encoding miR-122a. Such oligomeric compounds may include one or more modifications thereon, which may improve the activity, stability, or nuclease resistance of the oligomeric compound. These modified oligomeric compounds are used as single compounds or in compositions, including pharmaceutical compositions, to modulate or mimic the targeted nucleic acid comprising or encoding miR-122a.
Abstract: Described herein are compositions and methods for the inhibition of miR-21 activity. The compositions have certain nucleoside modifications that yield potent inhibitors of miR-21 activity. The compounds may comprise conjugates to facilitate delivery to the liver. The compositions may be administered to subjects with liver conditions, such as liver cancer.
Abstract: Described herein are compositions and methods for the inhibition of miR-21 activity. The compositions have certain nucleoside modification patterns that yield potent inhibitors of miR-21 activity. The compositions may be used to inhibit miR-21, and also to treat diseases associated with abnormal expression of miR-21, such as fibrosis and cancer.
Abstract: Provided herein are methods for the treatment of Alport Syndrome, using modified oligonucleotides targeted to miR-21. In certain embodiments, a modified oligonucleotide targeted to miR-21 improves kidney function and/or reduces fibrosis in subjects having Alport Syndrome. In certain embodiments, administration of a modified oligonucleotide targeted to miR-21 delays the onset of end-stage renal disease in a subject having Alport Syndrome. In certain embodiments, a modified oligonucleotide targeted to miR-21 delays the need for dialysis or kidney transplant in a subject having Alport Syndrome.
Type:
Grant
Filed:
May 26, 2017
Date of Patent:
May 15, 2018
Assignee:
Regulus Therapeutics Inc.
Inventors:
Jeremy Duffield, Balkrishen Bhat, Deidre MacKenna