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Thursday, June 22, 2017

Absolutegravir

Absolutegravir

Our readership explodes: we have new projects, we need help! we are looking for translators and also voices for podcasts. Someone to animate via social networks would also be of great help! You like this blog, so, please help!


This was originally published here, in French. We provide this translation for your convenience, practical aspects may differ where you live.

Absolutégravir

By Charles-Edouard!

Not seen on TV, drug-induced Suicides and Insomnia ...

Déjà Vu ... Time and time again! First, beware of depression and the suicidal ideations induced by bad medication: it does not warn you and it is serious, even mortal. Of course you know where it comes from. Beware of Russian medical roulette: we try a combo, then another, then another: it is a trick of Septits doctors. Beware of drug overload: antidepressant, anxiolytic, sleeping pill, when you already take massive doses of 3 molecules... A priori, without this being a medical advice, you could begin to consider the Short Cycle (you are already eligible for the FOTO mode) ... Well ... Let's see what the future holds:

Absolutegravir: a new kid on the block


First, it's a ... -gravir. According to the naming rule that identifies molecules, it is a (preferential) integrase inhibitor. Here is one list. -gravir is one of the newest.

Same as for horses, there is a first-letter rule, in the order of appearance. We have: Elvitegravir (Gilead); Dolutegravir (ViiV); Cabotegravir (ViiV); Bictegravir (Gilead).

And to all honorable lords, I take, in order, the letter A, which I make follow with a consonant. So, gentlemen of Pharmaceutical Marketing, take note: the letter A is reserved for Charles-Edouard!

Why 'Absolut'? Certainly, I like vodka ... And as Absolutegravir is a dream by fellows of good company, a little crazy, so, it falls very well.

Absolutegravir: born in a flash of lucidity by Wainberg / Raffi


Wainberg / Mesplède and Raffi have published a prospective opinion: What if HIV were unable to develop resistance against a new therapeutic agent?.

Wainberg and Raffi are accustomed to the manger ... We may expect a panegyric in favor of DTG. However, this opinion dates back from 2013, and foresees everything that the clinic will subsequently observe (Achille's Heel (2015), success in naïve patients (2016), etc.).

No resistance? Yes! There is a heavy gun fire by BigPharma, whose evergreening policy (drug market deployment at a good timing) is based on the concept of multi-therapy. Monotherapy is the programmed end of the goose that lays the golden egg!...

Absolutegravir = zero resistance, zero, zero, zero


Obviously, any resemblance to existing or past molecules is purely coincidental. We put this at the end of scenarios inspired by actual facts, so as not to be bothered.

So, Absolutegravir, is not DTG. We're clear on that.

Unlike other ARVs, discovered by trial / error, it is computer-generated: Integrase has been digitized (see this 3D animation), and a docking software tests millions of configurations, sticking as efficiently as possible to the integrase, occupying a spot that the virus so badly needs. Sorry My Lord, this seat is not available...

A first pass is made with a non-mutated 'wild-type' Integrase and then re-done on mutated integrases until the ultimate molecule (s) is found.

A further screening is then carried out to ensure that the molecule does not (or little) stick to common enzymes, to be more specific, and to avoid side effects. This is made possible because many proteins / enzymes have also been digitized. It costs a lot, but we have plenty of cash, because our previous baby was the blockbuster of the last century.

As usual, we add a molecule (eg a fluorinated bridge) that the liver has a hard time to break, resulting in a very long plasma half-life ... It is useless except to generate billions of profit. Go ask Gilead, these are the Kings of the Fluor Trick and the Kings of Oil!

Absolutegravir: how many milligrams?


Because there are no side effect, and you will want to be successful in commercialization, you dose it to the max, but less than older molecules. Say, 50 or 75 mg should do it ... In Phase II, 2 or 10 mg it's quite enough, but we do not care about Phase II trials! In 20 years, we can release a cousin, 30 mg, and extend our profits for another 20 years!

Afterall, the dosage is, ultimately, the responsibility of doctors, not pharmacists.

There is no resistance: non-compliance, fortuitous or planned, has no consequence: too few, then VL goes up, and we crank up the dose a little. In short, we manage the way diabetics do: a drop of blood and we manage; In the end, we find the optimal and there you go: we have an optimized treatment, personalized, insensitive to non-observance.

Absolutegravir and the Darwinian black hole


Absolutegravir does not select any resistance. The Darwinian black hole, which appears when a main mutation leads the virus to a replicative dead-end, is irrelevant here. It is a concept of the era before, the world of yesterday, DTG and its R263K.

As it is personalized, by the doctor (useful maybe, but not indispensable), we come from all Europe to see these miraculous doctors, who make the big bucks!

Absolutegravir: when should we expect it?


Absolutegravir is the atomic bomb on the market: the day it comes out, we earn royalties for 20 years, but after these, it is over, finished. The epidemic is over, the drama is finished, and the goose that lays the golden eggs is dead.

Absolutegravir will be the last molecule to appear on the market, because it will kill the market, and we, as the owner of the perfect molecule, will only put it on the market when we have exhausted all the tricks to extend our huge profits.

Life is beautiful

Good Weekend, good fuck, and not too many drugs (licit or not ...)



Our readership explodes: we have new projects, we need help! we are looking for translators and also voices for podcasts. Someone to animate via social networks would also be of great help! You like this blog, so, please help!


This was originally published here, in French. We provide this translation for your convenience, practical aspects may differ where you live.

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