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attilathehunt

07/27/20 4:09 PM

#315245 RE: petemantx #315244

not correct - Six are preclinical and Six Phase1..


Clofazimine Leprosy Approved (FDA)

Astemizole Allergies Approved (FDA) and withdrawn

Remdesivir Virus infection Emergency Use Authorization (EUA) (FDA)

Hanfangchin A (Tetrandrine) Cancer, Plasmodium infection Phase III

Apilimod Autoimmune disease, Cancer Phase II

MLN-3897 Bone disease, Inflammatory disease Phase II

ONO 5334 Osteoporosis Phase II

Elopiprazole Psychotic disorder Phase I

SDZ-62-434 Cancer Phase I

YH-1238 Stomach ulcer Phase I

DS-6930 Diabetes mellitus Phase I

N-tert-Butylisoquine (GSK369796) Plasmodium infection Phase I

R 82913 HIV infection Phase I

VBY-825 Bone cancer, NASH, PBC Phase 0

8-(3-Chlorostyryl)caffeine Psychotic disorder Preclinical

AMG-2674 Pain Preclinical

KW 8232 Osteoporosis Preclinical

MDL 28170 Alzheimers disease Preclinical

SB-616234-A Mood disorder Preclinical

SL-11128 Cancer Preclinical

Z LVG CHN2 Bacterial infection Preclinical
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attilathehunt

07/27/20 4:12 PM

#315246 RE: petemantx #315244

What we need is a bona fide partner with clout!

Tuesday's are days deals are normally announced so maybe tomorrow we hear something, otherwise we may fill the gap between .158 and .17

Speed is of the essence.
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KMBJN

07/27/20 4:18 PM

#315249 RE: petemantx #315244

No, they tested preclinical targets too, including brilacidin:

Towards this end, we profiled a library of known drugs encompassing approximately 12,000 clinical-stage or FDA-approved small molecules. We report the identification of 100 molecules that inhibit viral replication, including 21 known drugs that exhibit dose response relationships. Of these, thirteen were found to harbor effective concentrations likely commensurate with achievable therapeutic doses in patients ...

..

Here,
we describe a high-throughput reprofiling screen using the ReFRAME
(Repurposing, Focused Rescue, and Accelerated Medchem) drug
library, a comprehensive open-access library of ~12,000 that have been
either FDA-approved or registered outside the US, entered clinical trials,
or undergone significant pre-clinical characterization14, to identify
existing drugs that harbor antiviral activity against SARS-CoV-2 in a
cell-based assay14,15.



and it looks like brilacidin was in the database of 12,000 compounds:

https://reframedb.org/search?query=brilacidin&type=string

Maybe it was a difference in methods such as SARS2 isolate or MOI used or hours post infection?

Brilacidin in RBL hands inhibited SARS2 by ~50% at 5 uM in VERO cells 16 hours post infection:



From the Nature study:

Specifically, the potential antiviral activity of 11,987 compounds
against SARS-CoV-2 was assessed in Vero E6 cells. The assay,
conducted at a final compound concentration of 5 µM was designed to
capture multicycle replication, based upon low viral input (MOI = 0.01)
and an extended endpoint measurement (72 hours post-infection).


...

Approximately 300 compounds were identified for validation
studies based on criteria outlined in Materials & Methods (also see
supplementary Discussion). We assessed the activity of selected hits
at 2.5 and 1 µM, in contrast to the 5 µM concentrations employed in the
original screen, using an orthogonal assay readout. Specifically, Vero E6
cells treated with selected compounds were challenged with another
SARS-CoV-2 isolate (SARS-CoV-2 USA-WA1/2020), and viral infection
directly quantified through immunostaining