Aa
Irbesartan, might be 60 times more powerful to supress HBV entry than ezetimibe
A recent paper studied the effect of most FDA approved drugs on the inhibition of NTCP, the now known entry receptor for HBV. Ezetimibe was found to have a 50%inhibition conc of 25micromolar, while irbesartan, a commonly used angiotensin inhibitor to reduce blood pressure, was found to inhibit at 11.9 micromolar. Both compounds have similar MW, but irbesartan is given at up to 300mg per day, while exetimibe is dosed at 10mg. Thus the combination of 30fold higher approved dose and the double micromolar inhibition potency makes, in theory, irbesartan 60 fold more potent to inhibit Hbv entry. Of course, binding of these drugs to plasma proteins could cause substsntial differences in the available concentration on the hepatocyte membrane receptor, and the pharmacokinetics could further influence the in vivo efficscy. Tests in chimeric mice are urgently needed to determine the in vivo efficacy of this common, mostly beneficial medication on HBV reinfection inhibition.
can i stop both drugs and take them again only the day for the test of bile acids 2 hrs after?
yes, this is bad news, if the bile acids are not up, then the ntcp is not blocked. It might well be that the blood concentration of irbesartan falls to rapidly, then the blockage will disappear. Unfortunately, unless the blockage is consistent all 24 hours, it will allow reinfection. You could measure the bile acids 2 hours after drug intake, but even if it will increase it does not matter unless the effect lasts. The blockage of ntcp by myrcludex works so efficiently, that the bile acids are between 50 and 100 micromolar all the time, sometimes even higher after meals.
A combo with ifn is not going to increase the entry blocking effect, except of course that the further drop in produced virions will reduce the amount of visions seeking entry, but those will still be plenty enough. IFN will have another effect, however also limited, it will lead to destruction of a good percentage of virions whose core has entered the cytoplasm and prevent establishment of cccDNA in these cells, reducing the overall infection rate. But again, it will not be enough.
A combo with ifn is not going to increase the entry blocking effect, except of course that the further drop in produced virions will reduce the amount of visions seeking entry, but those will still be plenty enough. IFN will have another effect, however also limited, it will lead to destruction of a good percentage of virions whose core has entered the cytoplasm and prevent establishment of cccDNA in these cells, reducing the overall infection rate. But again, it will not be enough.
bad news from bile acids test:
25 mar 2013 zetia 50mg bile acids 1.2 micromol/l
11 apr 2013 zetia 50m plus irbersatan 300mg bile acids 1.0 micromol/l
normal range less than 6 micromol/l.drugs taken about 20hrs before test
i havent tested bile acids 2hrs after taking the pills, do you think it worths testing since it seems no ntcp block has happened?does it worth to try these drugs with peginterferon from other members to see if any boosting effect happens under that combo?
irbersatan is starting to be too heavy, extreme tireness especially at wake up has become not tollerable now, i can t get up before 10-11am
25 mar 2013 zetia 50mg bile acids 1.2 micromol/l
11 apr 2013 zetia 50m plus irbersatan 300mg bile acids 1.0 micromol/l
normal range less than 6 micromol/l.drugs taken about 20hrs before test
i havent tested bile acids 2hrs after taking the pills, do you think it worths testing since it seems no ntcp block has happened?does it worth to try these drugs with peginterferon from other members to see if any boosting effect happens under that combo?
irbersatan is starting to be too heavy, extreme tireness especially at wake up has become not tollerable now, i can t get up before 10-11am
people, we should be more focused where do they apply all this to real life cases.
For those of you that are doing research all this is very interesting sit and discuss things.. But we actually live with this nightmare. I am more interested in access to clinics where they apply all this. I will be the mice if it has to be.
The way I see things if things are known to work and not kill right away lets try it. That is what they should be doing.
For those of you that are doing research all this is very interesting sit and discuss things.. But we actually live with this nightmare. I am more interested in access to clinics where they apply all this. I will be the mice if it has to be.
The way I see things if things are known to work and not kill right away lets try it. That is what they should be doing.
As long as you have your own liver cells regenerating themselves there is no need or use for stem cells. Once the majority of these will have died and somehow their capacity to regenerate is exhausted , this type of treatment will make more sense, like in ESLD.
But the problem remains, that in the severely fibrotic and cirrhotic liver, there is also so much collagen, that the establishment of a meaningful liver micro-architecture is exceedingly difficult.
But the problem remains, that in the severely fibrotic and cirrhotic liver, there is also so much collagen, that the establishment of a meaningful liver micro-architecture is exceedingly difficult.
Can you please share your opinion regarding stem cell treatment for chronic liver diseases? I have read a lot regarding this type of treatment and a lot emphasize that it will become the mainstream in the near future for liver disease mainly for ESLD which is curable only by liver transplant. Thank you in advance.
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