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Topic: GPR174 Omeros' start into cancer treatment

The patent application relates the Mode(S) of action of GPR174 and why an inhibitor of it will successfully treat cancer by affecting the immune system in multiple ways. Most therapeutic agent has a single MOA or perhaps 2. GPR174i has about 6 last I counted.

"The present inventors have identified chemical compounds that functionally interact with GPR174 and inhibit one or more GPR174-mediated signaling pathways and, additionally, have characterized the GPR174 receptor signaling profile, which includes the Gs signaling pathway. The inventors have demonstrated that representative GPR174 inhibitory compounds are capable of reducing the fraction of highly suppressive regulatory T cells or "T-Regs" (FoxP3+Helios+) in human peripheral blood mononuclear cells (PBMCs), as described in Examples 6, 8, and 9. The inventors have further determined that GPR174 inhibition stimulates IL-2 production in a dose-dependent manner in PBMCs, as described in Examples 6-11. The inventors have also determined that GPR174 inhibition reduces immune-cell associated programmed death-ligand 1 (PD-L1) expression, cytotoxic T-lymphocyte-associated antigen 4 (CTLA4) expression, T cell immunoreceptor with Ig and ITIM domains (TIGIT) expression and amphiregulin (AREG) expression, as described in Example 13 and 14. Therefore, the GPR174 inhibitory compounds can be used as drugs for use in stimulating an immune response in a mammalian subject and can form the basis for additional therapeutic agents. Based on these discoveries, the present disclosure is related to in vivo and in vitro methods for inhibiting the GPR174 receptor and thereby stimulating an immune response, particularly in a subject suffering from a non-malignant neoplasm or a malignant neoplasm (i.e., cancer)."

original content ©2020 to 2021 by Alan Robert Ross
Founder, Trust Intelligence
The foregoing is not investment advice.

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Re: GPR174 Omeros' start into cancer treatment

I hope I am reading this correctly.  It seems to me that Omeros is taking the same approach to cancer as it did to transplant rejection and Covid.  That is to say, the drug is concerned with the pathway(s) that the human body uses to fight cancer, or by which caner is expressed in the human body.  The drug does not fight the cancer directly, which seems to me is and has been the approach of cancer drug research to date.  If the pathways in the human body are what is(are) used by cancer, then I can see GPR174 hopefully being of use against many types of cancer, not just one type.  Am I reading correctly?

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Re: GPR174 Omeros' start into cancer treatment

yes

original content ©2020 to 2021 by Alan Robert Ross
Founder, Trust Intelligence
The foregoing is not investment advice.

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Re: GPR174 Omeros' start into cancer treatment

Seems like Greg is a bit of a visionary......

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Re: GPR174 Omeros' start into cancer treatment

This is the kind of drug that works synergistically with GPR174
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Arcus rolls out PhI data on adenosine blocker for CRC
Kyle Blankenship Managing Editor
Arcus Biosciences’ adenosine blocker etrumadenant showed some benefit in extending patients’ lives as part of a Phase I/Ib trial in third-line-or-later colorectal cancer patients, according to data presented Saturday at the virtual AACR annual meeting.

Etrumadenant, a dual adenosine A2aR/A2b receptor antagonist, is designed to inhibit adenosine’s role in preventing lympocytes like CD8+ effector T cells and NK cells from infiltrating the tumor microenvironment, the company said. A combination of etrumadenant and chemotherapy regimen FOLFOX-6 posted a median PFS of 4.2 months, a median OS of 13.6 months and an objective response rate of 9.1%. The drug showed consistent benefits in BRAF/RAS mutated cancer cells, the company said.

The ARC-3 study wasn’t powered to compare that combination against placebo so it’s hard to know exactly what significance these results hold. But Arcus did highlight that patients on two established standards of care in that late-line setting reported a median PFS of 2 and 1 months, a median OS of 7.1 and 6.4 months and ORR of 1.6% and 1%, respectively. The study also showed that patients with high tumoral mutation burden and expression of CD73 within the tumor posted improved outcomes.

The results are promising enough that Arcus plans to advance etrumadenant into a Phase II/IIb study dubbed ARC-9 that will evaluate the drug in combination with the biotech’s anti-PD-1 antibody zimberelimab and FOLFOX with or without bevacizumab in second- and third-line metastatic colorectal cancer.

original content ©2020 to 2021 by Alan Robert Ross
Founder, Trust Intelligence
The foregoing is not investment advice.

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Re: GPR174 Omeros' start into cancer treatment

FYI from STAT
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One biotech's long road to relevance

After burning through more than $1 billion over the course of three decades without actually developing a drug, Agenus’s fortunes appear to be improving.

Yesterday, Bristol Myers Squibb agreed to pay $200 million in cash for a license to AGEN1777, an Agenus-invented cancer treatment aimed at a promising molecular target called TIGIT. In biotech terms, it’s not a particularly notable amount of money, and AGEN1777 has yet to be tested in a clinical trial and is years away from proving to be effective. But as Jacob Plieth points out in Evaluate Vantage, when you consider Agenus’s history, it’s recent run of form is incredible.

Pivot after pivot, Agenus has consistently struggled to stay solvent, mortgaging future royalty streams for cash and once trying to sell a cryptocurrency tied to a cancer drug. The company’s market value is still below $1 billion, but the Bristol deal combined with some promising late-stage data suggest Agenus’s fourth decade might be the one that brings success.

original content ©2020 to 2021 by Alan Robert Ross
Founder, Trust Intelligence
The foregoing is not investment advice.