The above article of ours on “PAK1-blockers: Potential
therapeutics against COVID-19” has been cited over 800 times during last 3 months
since its publication in mid-April 2020, this “working hypothesis” of ours appears to be
widely accepted or seriously considered among world medical/ scientific community.
Considering the current “gloomy” situation that the COVID-19 pandemic, costing nearly 600,000 deaths during last 6 months, is still actively hanging
around world-wide, in particular US, and it will take 6-12 more months till any
effective vaccine becomes available world-wide, we will try to contact a
pharma, asking for making 200 g of 15K, our potent PAK1-blocker, at GMP
facility for its clinical trials against COVID-19, with at least 100 patients
for 30 days, compared with Ivermectin (0.15 mg/kg once or twice) which has been
proven to be effective clinically. For detail of the Ivermectin clinical trials
against COVID-19, see below:
Once FDA approves 15K for marketing, we shall
try to organize its clinical trials against chemo-resistant pancreatic cancers and
many other PAK1-dependent diseases. Sometimes
we have to change a plan or strategy, depending on the given situation.
Flexibility is the key for a great success.
The “clinical” protocol:
According to our own in vivo (pancreatic cancer
xenografts in mice) test of 15K, its daily dose of 0.1 mg/kg is sufficient to
suppress almost completely the growth of these cancers at least, and even 5
mg/kg (50 times of the EC) causes no side effect:
Thus, the testing dose of 15K for COVID-19
patients treated at ICU (intensive care unit) would be around 0.1 mg/kg daily or
less (6 mg/60 kg, twice a week). Thus, for the first round of trials, we need at
least 20 g of 15K, around 6-7, 000 tablets of 3 mg, sufficient for treating at
least 100 patients over 30 days. Since 15K is expected to lower the blood
pressure to a certain extent, we shall monitor both their blood pressure and
COVID-19 symptom closely during 15K treatment (up to 30 days, dead or alive).
Of course, we shall ask more than a dozen
"healthy" volunteers including myself for taking the precisely same dose of 15K over
a month, making it sure that 15K causes no side effect on these "healthy" individuals in advance.
The Protocol for 15K synthesis
15K was synthesized from an old PAK1-blocking pain-killer
called “Ketorolac” (R-form) via Click Chemistry (CC), which catalyzes the
esterization of its COOH with 2-azido anisole in the presence of copper ion with
a high yield. For detail, see the following website:
This CC boosts the cell-permeability (and
thereby both anti-cancer and anti-PAK1 activities) of Ketorolac over 500 times,
but without any loss of its water-solubility.
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