Horsholm, Denmark
Horsholm, Denmark

Santaris Pharma AS has become a leading clinical-stage biopharmaceutical company that develops RNA-targeted medicines using a Locked Nucleic Acid Drug Platform and Drug Development Engine.The company was acquired by Roche in August 2014. Santaris has the worldwide exclusive intellectual property rights to the therapeutic applications of locked nucleic acid technology. This includes ownership of over 60 patent types, which range from the chemistry to manufacturing and from therapeutic uses to drug design.With their LNA technology, Santaris works on developing drugs for a wide range of diseases using microRNA and mRNA. Their research focuses on infectious disease and metabolic disorders. They also work on collaborations with pharmaceuticals to develop drugs for rare genetic disorders, cancers, cardiovascular disease, and immune and inflammatory diseases. Wikipedia.

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Van Rooij E.,Miragen Therapeutics | Purcell A.L.,Cooley LLP | Levin A.A.,Santaris Pharma
Circulation Research | Year: 2012

Rarely a new research area has gotten such an overwhelming amount of attention as have microRNAs. Although several basic questions regarding their biological principles still remain to be answered, many specific characteristics of microRNAs in combination with compelling therapeutic efficacy data and a clear involvement in human disease have triggered the biotechnology community to start exploring the possibilities of viewing microRNAs as therapeutic entities. This review serves to provide some general insight into some of the current microRNAs targets, how one goes from the initial bench discovery to actually developing a therapeutically useful modality, and will briefly summarize the current patent landscape and the companies that have started to explore microRNAs as the next drug target. © 2011 American Heart Association, Inc.


The present invention relates to compositions and methods for preparing splice variants of TNFalpha receptor (TNFR) in vivo or in vitro, and the resulting TNFR protein variants. Such variants may be prepared by controlling the splicing of pre-mRNA molecules and regulating protein expression with splice switching oligonucleotides or splice switching oligomers (SSOs). The preferred SSOs according to the invention target exon 7 or 8 of TNFR1 (TNFRSF1A) or TNFR2 (TNFRSF1A) pre-mRNA, typically resulting in the production of TNFR variants which comprise a deletion in part or the entire exon 7 or 8 respectfully. SSOs targeting exon 7 are found to result in a soluble form of the TNFR, which has therapeutic benefit for treatment of inflammatory diseases. The SSOs are characterized in that they are substantially incapable or incapable of recruiting RNaseH.


Patent
Santaris Pharma and Enzon Pharmaceuticals | Date: 2013-04-30

The invention provides the combination use of antisense oligomers targeting androgen receptor mRNA and androgen receptor binding inhibitors that reduce androgen receptor activity for the treatment of androgen receptor related medical disorders, such as cancers, particularly prostate cancers and breast cancers.


Patent
Santaris Pharma | Date: 2014-07-09

A class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. Novel oligonucleotides have improved antisense properties. The oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides.


Patent
Santaris Pharma | Date: 2013-03-15

A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides.


Patent
Santaris Pharma | Date: 2014-10-29

The present invention relates to very short heavily modified oligonucleotides which target and inhibit microRNAs in vivo, and their use in medicaments and pharmaceutical compositions.


Patent
Santaris Pharma | Date: 2014-02-11

The present invention is directed to novel double-stranded short interfering (siRNA) analogues comprising locked nucleic acid (LNA) monomers. Such compounds induces sequence-specific post-transcriptional gene silencing in many organisms by a process known as RNA interference (RNAi). The compounds disclosed herein has improved properties compared to non-modified siRNAs and may, accordingly, be useful as therapeutic agents, e.g., in the treatment of various cancer forms. More particularly, the present invention is directed to siRNA analogues comprising a sense strand and an antisense strand, wherein each strand comprises 12-35 nucleotides and wherein the siRNA analogues comprise at least one locked nucleic acid (LNA) monomer.


Methods and compositions are disclosed for controlling expression of TNF receptors (TNFR1 and TNFR2) and of other receptors in the TNFR superfamily using compounds that modulate splicing of pre-mRNA encoding these receptors. More specifically these compounds cause the removal of the transmembrane domains of these receptors and produce soluble forms of the receptor which act as an antagonist to reduce TNF- activity or activity of the relevant ligand. Reducing TNF- activity provides a method of treating or ameliorating inflammatory diseases or conditions associated with TNF- activity. Similarly, diseases associated with other ligands can be treated in like manner. In particular, the compounds of the invention are splice-splice switching oligomers (SSOs) which are small molecules that are stable in vivo, hybridize to the RNA in a sequence specific manner and, in conjunction with their target, are not degraded by RNAse H.


The invention provides pharmaceutical compositions comprising short single stranded oligonucleotides, of length of between 8 and 26 nucleobases which are complementary to human microRNAs selected from the group consisting of miR19b, miR21, miR122a, miR155 and miR375. The short oligonucleotides are particularly effective at alleviating miRNA repression in vivo. It is found that the incorporation of high affinity nucleotide analogues into the oligonucleotides results in highly effective anti-microRNA molecules which appear to function via the formation of almost irreversible duplexes with the miRNA target, rather than RNA cleavage based mechanisms, such as mechanisms associated with RNaseH or RISC.


The invention provides oligonucleotides 8 - 22 nucleotides in length, for inhibition of a microRNA target in a cell, which comprise a high proportion of high affinity nucleotide analogue units as well as LNA units. The oligonucleotides are particularly effective at alleviating miRNA repression in vivo. It is found that the incorporation of high affinity nucleotide analogues into the oligonucleotides results in highly effective anti-microRNA molecules which appear to function via the formation of almost irreversible duplexes with the miRNA target, rather than RNA cleavage based mechanisms, such as mechanisms associated with RNaseH or RISC.

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