Molecular Weight(MW): 425.75
Doravirine is a novel HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50 values of 12, 9.7, and 9.7 nM against the wild type (WT) and K103N and Y181C reverse transcriptase (RT) mutants, respectively, in a biochemical assay. It is highly specific with minimum off-target activities.
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Choose Selective Reverse Transcriptase Inhibitors
|Description||Doravirine is a novel HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50 values of 12, 9.7, and 9.7 nM against the wild type (WT) and K103N and Y181C reverse transcriptase (RT) mutants, respectively, in a biochemical assay. It is highly specific with minimum off-target activities.|
MK-1439 exhibits greater than 10,000-fold selectivity with respect to the cellular DNA polymerases α, ß, and γ with IC50s of >100 μM. In the screen with more than 110 protein targets including enzymes, transporters, ion channels, and receptor, MK-1439 shows an IC50 of greater than 10 μM against all targets except 5-HT2ß, where an IC50 of 2.5 μM is noted in a ligand binding assay. However, the 5-HT2ß activity is not observed in a functional cell-based assay monitoring the accumulation of inositol-1-phosphate. Therefore, the binding activity does not appear to translate into a 5-HT2ß functional response. MK-1439 does not display cytotoxicity in activated CD4+ T cells, PBMCs, monocytes, macrophages proliferating transformed cell lines, such as MT4, SupT1, and HL60 cell lines at concentrations of up to 100 μM.
In rats dosed IV at 1 mpk (60%PEG200), the clearance (CL) of MK-1439 is 5.4 mL/min/kg and the half time is 4.4 hr. Its volume of distribution (Vd) is 2.3 L/kg. The oral bioavailability of MK-1439 is 57% (doesed PO at 5 mpk). In dogs dosed IV at 0.5 mpk, the CL of MK-1439 is 0.36 mL/min/kg and half-time is 37 hr. The oral bioavailability of MK-1439 is 52% (doesed PO at 1 mpk). Overall, The pharmacokinetic profile of MK-1439 in preclinical species is favorable.
|In vitro||DMSO||85 mg/mL (199.64 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04097925||Not yet recruiting||Drug: Doravirine|Drug: Descovy||HIV-1-infection||Fundacio Lluita Contra la SIDA|Institut d''Investigació Biomèdica de Bellvitge|Hospital Universitari de Bellvitge||September 2019||Phase 2|
|NCT04079452||Not yet recruiting||Drug: Doravirine|Drug: Descovy||HIV-1-infection||Fundacio Lluita Contra la SIDA|Institut d''Investigació Biomèdica de Bellvitge|Hospital Universitari de Bellvitge||September 2019||Phase 3|
|NCT03894124||Completed||Drug: Doravirine||Human Immunodeficiency Virus||Chelsea and Westminster NHS Foundation Trust|Merck Sharp & Dohme Corp.|Imperial College London|University of Liverpool||June 12 2019||Phase 1|
|NCT02641067||Completed||Drug: Doravirine||Renal Impairment||Merck Sharp & Dohme Corp.||January 26 2016||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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