Once again, nothing better than knowing what you are investing in.
Here is a recent research paper dealing with treating C19 with Amantadine and HMA, of which BIT225 is related. The paper sites Biotron's previous SARS-COV-1 research many times, in fact, they are repeating Biotrons earlier SARS1 work on SARS2, using the same compounds that Biotron did back in 2003, and suggesting their use for treating C19 now. Fancy that.
Biotron of course know all this and are one step ahead with BIT225.
Amantadine C10H17N
HMA C12H18CIN7OBIT225 C
16H
15N
5O (original version)
Amantadine has potential for the treatment of COVID-19 because it inhibits known and novel ion channels encoded by SARS-CoV-2I've copied some BITS from the paper - pardon the pun. In case you need to fact check the Biotron connection, start with reference 12. It is the one cited most. But nothing better than reading the original. This paper is in fact somewhat simpler.
Extracts
- We demonstrate that amantadine and hexamethylene-amiloride (HMA)......block the ion channel activity of Protein E from SARS-CoV-2, a conserved viroporin among coronaviruses.
- marketed drugs, such as amantadine as well as rimantadine, which both target the M2 viroporin in influenza A virus9,10,11 and hexamethylene-amiloride (HMA) that blocks influenza A M2 and SARS-CoV-1 Protein E12,13. Amantadine has been observed to also block the SARS-CoV-1 Protein E viroporin14.
- SARS-CoV-2 is the cause of the ongoing pandemic of COVID-19. It is highly homologous to the deadly SARS-CoV-1 (also known as SARS-CoV), giving rise to the “SARS” epidemic in 2002, and to the Middle East respiratory syndrome coronavirus giving rise to MERS in 201215. One conserved viroporin has been identified in all of these three coronaviruses, the homo-pentameric cation-conducting Protein E16.
- Protein E ion channel activity represents a determinant for SARS-CoV-1 virulence, which mirrors the pathology associated with the severe cases of SARS-CoV-2 infection. This suggests that inhibition of the SARS-CoV-2 Protein E viroporin might likewise limit pathogenicity and thus be of therapeutic value in SARS-CoV-2 infections.
- Amantadine has previously been shown by surface plasmon resonance to bind to the native transmembrane α-helical region of the SARS-CoV-1 Protein E (ETM) and by electrophysiology to block full-length Protein E (aa 1–75)-mediated conductance at low mM concentration12,14- Amantadine efficiently blocked the activity of SARS-CoV-2 Protein E (77%;
p = 0.006, Fig.
1b), and consistent with previous data
14, also blocked that of SARS-CoV-1 Protein E (66%,
p = 0.005, Supplementary Fig.
1b)
12,14.
- Taken together, amantadine blocked two of the four ion channels in SARS-CoV-2 (Protein E and ORF10) and the activity of all four ion channels in SARS-CoV-2 was significantly inhibited by at least one of the eight applied drugs.
- The use of amantadine rests on several decades of clinical experience, facilitating a potential repurposing for the prevention and treatment of SARS-CoV-2 infection and pathogenesis.
To this last point, may I add my own contribution.
Biotron researchers were the first - 2003 - to use Amatadine on SARS-COV-1, and demonstrated the prevention of ion channel activity of the E protein viroporin. Since then they have continued this technology on the corresponding viroporins of HIV and Hepatitis B with excellent results. They have now turned their attention to SARS-COV-2, with early, but oustanding results to date..........
I think I'm going to fall from my stalactite.
If you havn't yet read any of Biotron's early research, here is a paper of relevance, or see the first post of this thread for furtther references.
Amiloride derivatives block ion channel activity and enhancement of virus-like particle budding caused by HIV-1 protein Vpu
