| Bioactivity | Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively[1]. | ||||||||||||
| Target | IC50: 4.5 nM (wild type reverse transcriptase); 5.5 nM ( K103N reverse transcriptase); 6.1 nM (Y181C reverse transcriptase) | ||||||||||||
| Invitro | Selectivity and cytotoxicity studies confirmed that Doravirine is a highly specific nonnucleoside reverse transcriptase inhibitors with minimum off-target activities. In the presence of 50% normal human serum (NHS), Doravirine shows excellent potency in suppressing the replication of WT virus, with a 95% effective concentration (EC95) of 20 nM, as well as K103N, Y181C, and K103N/Y181C mutant viruses with EC9595 of 43, 27, and 55 nM, respectively. Doravirine exhibits similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses)[1]. | ||||||||||||
| In Vivo | Administration of 50 mg Doravirine with a high-fat meal is associated with slight elevations in AUC time zero to infinity and C24 h with no change in Cmax[2]. | ||||||||||||
| Name | Doravirine | ||||||||||||
| CAS | 1338225-97-0 | ||||||||||||
| Formula | C17H11ClF3N5O3 | ||||||||||||
| Molar Mass | 425.75 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Lai MT et al. In vitro characterization of MK-1439, a novel HIV-1 nonnucleoside reverse transcriptase inhibitor. Antimicrob Agents Chemother. 2014;58(3):1652-63. [2]. Anderson MS et al. Safety, tolerability and pharmacokinetics of doravirine, a novel HIV non-nucleoside reverse transcriptase inhibitor, after single and multiple doses in healthy subjects. Antivir Ther. 2015;20(4):397-405. |
Doravirine
CAS: 1338225-97-0 F: C17H11ClF3N5O3 W: 425.75
Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of4.5 nM, 5.5 n
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