Raltegravir

The to raltegravir is the name international non-proprietary of Isentress©, an inhibiting of the intégrase of HIV, currently in the course of experimentation (clinical trials of phase III). This molecule, patented by the laboratories Merck & Co., is also known under the name of code MK-0518.

Posology and side effects

Usual posology is of 400 Mg, twice a day. The tablets should not necessarily be introduced with food, contrary to others antirétroviraux.

A test of phase I showed that amounts of 200,400 or 600 Mg gave a priori the same result in term of reduction of Viral load.

The side effects at least seem non-existent, or comparable with those met at the time of the administration of a Placebo: nauseas, giddinesses, diarrheas. Among certain patients, one however could observe an increase in the rate of Créatine kinase, without being able to establish that this problem was due to the drug.

On this last point, it is advisable however to apply the precaution principle, to raltegravir it at present being one of the only molecules acting on the Intégrase of the viruses available; one does not know possible long-term side effects. Moreover, it should be stressed that the inhibiting intégrase act directly on DNA proviral, and thus near the DNA of the cells concerned, which could represent a danger of which one knows nothing yet. It also should be noticed that the tests on the animals showed a noxious activity on the Fœtus.

Effectiveness and accessibility

The molecule seems very powerful, in spite of the little of retreat which one has on his use. It in particular makes it possible to reach a undetectable viral load good more quickly than with a trithérapie including/understanding Efavirenz. It is accessible to the patients in exhaust thanks to a ATU and could in the long term replace the Enfuvirtide, because to raltegravir it is much simpler to manage, and should be effective on the resistant viruses. The drug obtained the agreement of FDA for a marketing in the in October 2007 United States. Its price should be 27$ per day, which represents a very important sum for a antirétroviral.

Two other molecules of the class of the anti-intégrase: the Elvitegravir of Gilead Sciences and MK-2048, it also developed by Merck & Co.

Liens externes

a card in connection with raltegravir it on HIV Medication Guides (in French)
: code name MK-0518, a file on Internet site of the gay magazine Obstinate
short, HIV: good performances of an inhibiter of the intégrase on Caducee.net
Note of Isentress on the site of AFSSAPS
a '' complete memorandum '' on aidsmeds.com
the official site, www.isentress.com

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