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ezetimibe first results on hbsag quant

i just received hbsag quantity now and it lowered for the first time to less than 4000iu/ml in 3 years (all tests in same lab with authomated diluition)

hbsag baseline before ezetimibe 4207iu/ml
(stable around this value in 2012, in previous years up and down from 7300 to 4200iu/ml, never reached less)
hbsag after 9weeks of ezetimibe 3644iu/ml

i have used 10mg dose for about 4weeks and then increased to 50mg daily, no sides, all blood tests normal (alt lowered from 45-50 to 31)

the therapy used is entecavir plus tenofovir and ezetimibe add on

not correlated with therapy or response:
tot cholesterol from 164 to 131-139
ldl from 92 to 71-79
hdl from 61 to 44-39
trigl from 57 to 40

ast-alt lowered from 27-37 to 28-31 one month ago, will recheck this month
34 Responses
Avatar universal

please comment on these results, i think that monthly hbsag quant may confirm if we are having a good result from ezetimibe, we have only one thing certain from 2009 to 2012 hbsag stable from 4200 to 7300 no matter what we tried (alinia or imiquimod)

would you also add intf to this combo tdf+etv+ezetimibe since imiquimod too failed?liver specialists scheduled intf add on for this year
Avatar universal
ezetimibe is a drug that lowers cholesterol level, isn't it?

I also noticed that decrease in cholesterol affects hbsAg quantity. Since Oct'12 to Dec'12 I lost 3 kilos and
cholesterol went down from 5.6 to 4.95.
HDL was stable around 1.4 but
LDL went down from 4.1 to 3.0
HbsAg went down from 1795 iU/ml to 1447 iU/ml

I did not take any drugs except for the supplements VitD3 1k a day, LivOn GSH+VITC+AntiAge, changed diet a bit.
Avatar universal

it may be just a coincidence or improved immune response by those supplements because me and some other members tried simvastatin or red yeast rice supplements in the past and it did lowered chol but no effect on hbsag at all

ezetimibe doesn t work on cholesterol to interfere with hbv but it is thought to interfere with some steps after hbv entry, something before cccdna and hbsag formation.in vitro it did lower cccdna and hbsag but as regards vivo no data yet
Avatar universal

as regards hcv ezetimibe blocks cellular entry receptors
Avatar universal
I wonder if HbsAg level will stay if you stop ezetimibe...
Avatar universal
This looks like a real response that has shifted the daily kinetics of reinfection so that the total cccDNA might be reduced. You took a very high dose, i suspect the regular low dose of 10mg would not have shown much effect.

Since ezetimibe is reported to block virion uptake at a later step it might work synergistic with Myrcludex in reducing the reinfection rate.

The key question is now if a further reduction of surface antigen can be expected, or if this is new setpoint reached with no more progress in infected cell reduction. I think there is a chance that the reduction might continue, similar to what we expect from a properly dosed Myrcludex treatment.

If you see a further drop in upcoming tests, I would definitely recommend to have it as a component add on to the planned IFN therapy. If there is a continuing drop i would not start the IFN as long as the effect shows true progression.

When is your next hbsag quant scheduled?
Avatar universal

i can do it whatever timepoint now even with no prescription, it is just 7-10€ cost test and can also try higher dosages since no sides in case of furthur decline

what would you suggest monthly test or every 15 days?


Avatar universal
I think we need more time points to make a scientific decision but the result is promising.
I can't find any data on toxicology or dosage escalation studies on Ezitimibe, therefore, I will advice not to exceed 50 mg daily dosage  because all the trial with Ezitimibe was 10 mg daily .. This is just my opinion and our great asset Studyforhope can contribute.

Avatar universal
Once monthly testing should give meaningful results. However right mow a retesting in two weeks would be useful to confirm that it was not just a temporary fluctuation in surface antigen expression activity without a true reduction in cccDNA content.
Avatar universal
I agree that dose increases have to be handled very carefully. Stefano already jumped into uncharted lands with the 50mg dose. I would recommend a test of pancreatic Lipase.

On the other hand, he might not have seen an effect with the standard 10mg dose. It is further possible that he is still in the middle of the dose response curve.
What has to be kept in mind is that this secondary entry inhibitor effect cannot lead directly to an elimination of infected cells. The elimination is depending on ongoing immune mediated infected cell removal or noncytolytic clearance. Once entry blocking is complete, any further dose escalation will achieve nothing but trouble.
But we dont know if the 50mg dose is already causing a near max effect.

Avatar universal

is pancreatic lipase urgent?if not i ll test in 2 weeks with hbsag quant
Avatar universal
I have seen article on Ezitimibe viral activities and there is a patent in the USA blocking the use of it and the like group  on treatment of HBV.
There's possibility that 50mg is still ok but it has to be monitored.
Although this drug is designed for liver metabolism, i ll suggest that due to massive increase in the usual recommended daily dosage to do a Kidney function test if its available.
A daily dosage of 50 mg might well be within the tolerable range and the decision to use 10mg for therapeutic effect is design  for long term use.
I am watching closely.
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