Newinvestor68, losingmyshirt you should find another hobbyInvesting is not for you two geniuses or is this just Penny another loser, your probably the same person is my guess, a SHORTER. Going to suck going forward for you dipshitt.
This is what Salzman is bring to the aquistion, read slooow, try to comprehend, lloosseerrss.
R-107 is a nitric oxide pro-drug
R-107 is a liquid pro-drug of nitric oxide that can be administered by injection, unlike nitric oxide gas, which requires a special type of delivery device, and complex administration by trained respiratory therapists. When administered by injection, R-107 is slowly hydrolyzed, releasing its active moiety, R-100, which in turn steadily and slowly releases nitric oxide into the lung tissue.
Put simply, following injection, R-107 is metabolized and releases R-100, which in turn releases nitric oxide into the tissues of the lung. R-100 is the pharmaceutically active payload of R-107.
Pharmacokinetic data are indicative of rapid conversion of R-107 to active therapeutic payload
Salzman Group studied the pharmacokinetic characteristics of R-107 when administered at a dose of 10 milligrams per kilogram to rats via an intravenous injection. The purpose of this study was to measure the levels of R-107, and its payload R-100 and the metabolite HMP (generated after release of nitric oxide from R-100), in the plasma of rats following injection. This study is a requirement for an investigational new drug (IND) application that the company intends to submit in the second quarter of 2020 to the U.S. Food and Drug Administration (FDA) in support of a first-in-human phase 1a clinical trial. The company is planning to carry out a phase 1a safety and pharmacokinetic study of intramuscular R-107 using a single dose escalation design in healthy middle-aged volunteers at CMAX, a clinical contract research organization located at Royal Adelaide Hospital in Australia.
Results from this rat pharmacokinetic study, carried out at Envigo Labs in the United Kingdom, demonstrated a rapid buildup of the pro-drug R-107, with peak plasma concentrations (Cmax) reached after five and eight minutes (Tmax) in male and female rats, respectively. Conversion of R-107 to its active payload R-100 was extremely rapid, with R-100 attaining its peak plasma concentration (Cmax) only 15 minutes after the dosing of R-107. Thereafter, R-100 was cleared from the plasma with half-lives (t one-half) of 2.7 and 7.7 hours in male and female rats, respectively. Given that R-107 and its payload, R-100, are hydrophobic, it was not unexpected to observe a large volume of distribution (Vd), indicative that they had partitioned into fat stores forming a functional drug depot. These findings predict that a single dose of the R-107 pro-drug in humans will produce sustained plasma levels of the active payload R-100, which would then release nitric oxide into the lung over many hours.
Pharmacokinetic data are indicative of sustained release of nitric oxide from active payload R-100
In a follow-on pharmacokinetic study also carried out at Envigo Labs, the active payload R-100 was administered at a dose of 10 milligrams per kilogram to rats via an intravenous injection. The purpose of this investigation was to measure the levels of the metabolite HMP, which is formed when R-100 discharges nitric oxide. This study is also an obligatory component of the IND to be submitted to the FDA. Results from this study showed a total exposure to HMP of less than 30 per cent of the total R-100 administered, indicating that the release of nitric oxide from HMP is relatively slow. Accordingly, R-100 functions as a depot of nitric oxide, providing for sustained exposure to nitric oxide in tissues.
Taken together, the interpretation of the findings from the above two studies is that R-107 is readily converted in vivo into its active payload R-100, which accumulates in a tissue depot and provides for a sustained release of nitric oxide into tissues. Pharmacokinetic studies taking place now in large animals will offer additional insight into the predicted exposure levels in humans dosed with R-107.
GLTA