MK-2048
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MK-2048 is the Merck & Co. designation for a molecule in its pre-clinical drug discovery that is an integrase inhibitor-class of agent intended to be used against
HIV The human immunodeficiency viruses (HIV) are two species of ''Lentivirus'' (a subgroup of retrovirus) that infect humans. Over time, they cause acquired immunodeficiency syndrome (AIDS), a condition in which progressive failure of the immune ...
infection. It is a second generation integrase design thought to be superior to the first available integrase inhibitor,
raltegravir Raltegravir, sold under the brand name Isentress, is an antiretroviral medication used, together with other medication, to treat HIV/AIDS. It may also be used, as part of post exposure prophylaxis, to prevent HIV infection following potential ex ...
, in that "MK-2048 has a dissociation half-life of 32 hours on wild-type integrase—more than four times that of raltegravir", and its dissociation half-life against the important HIV integrase mutant N155H was on the same order of magnitude as that of raltegravir against wild-type virus, leading the Merck presenter to suggest the possibility of "reduced susceptibility to resistance mutations" for the second generation drug. MK-2048 is being investigated for use as part of a
pre-exposure prophylaxis Pre-exposure prophylaxis (PrEP) is the use of medications to prevent the spread of disease in people who have not yet been exposed to a disease-causing agent, usually a virus. The term typically refers to the use of antiviral drugs as a strate ...
(PrEP) approach to the treatment of HIV infection. At the time of these reports, there was no indication of the time by which "MK-2048, or related compounds,
ould Ould is an English surname and an Arabic name ( ar, ولد). In some Arabic dialects, particularly Hassaniya Arabic, ولد‎ (the patronymic, meaning "son of") is transliterated as Ould. Most Mauritanians have patronymic surnames. Notable p ...
be ready for clinical trials".


References

{{Antiretroviral drug Integrase inhibitors Experimental drugs