MK-2048

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 infection.[1] It is a second generation integrase design thought to be superior to the first available integrase inhibitor, raltegravir, in that "MK-2048 has a dissociation half-life of 32 hours on wild-type integrase—more than four times that of raltegravir",[1][2] 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.[1] MK-2048 is being investigated for use as part of a pre-exposure prophylaxis (PrEP) approach to the treatment of HIV infection.[3] At the time of these reports, there was no indication of the time by which "MK-2048, or related compounds, [would] be ready for clinical trials".[1]

MK-2048
MK-2048
Clinical data
ATC code
  • none
Legal status
Legal status
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.233.568
Chemical and physical data
FormulaC21H21ClFN5O4
Molar mass461.87 g/mol g·mol−1
3D model (JSmol)

Further reading
  • Wenning L, Nguyen B, Teppler H, et al. Pharmacokinetic/Pharmacodynamic Analyses for Raltegravir in Phase II and III studies in Treatment Experienced HIV-Infected Patients. 9th International Workshop on Clinical Pharmacology of HIV Therapy. April 7-9, 2008. New Orleans. Abstract O_21.


References
  1. Mascolini, M. (April 17, 2009). "Conference Reports for NATAP: Merck Offers Unique Perspective on Second-Generation Integrase Inhibitor [10th International Workshop on Clinical Pharmacology of HIV Therapy, April 15–17, 2009, Amsterdam]". NATAP.org. Retrieved November 8, 2009.
  2. Grobler, J.A., McKenna, P.M., Ly, S.; et al. (April 17, 2009). "Presentation, Abstract O-10: Functionally Irreversible Inhibition of Integration by Slowly Dissociating Strand Transfer Inhibitors. [10th International Workshop on Clinical Pharmacology of HIV Therapy, April 15–17, 2009, Amsterdam]". NATAP.org. Explicit use of et al. in: |author= (help); Missing or empty |url= (help)CS1 maint: multiple names: authors list (link)
  3. Alcorn, K. (April 28, 2009). "Ralvetgravir Shows Potential for use as PrEP Drug". AIDSmap.com. Retrieved November 8, 2009.
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