Letermovir  (Synonyms: AIC246; MK-8228)

Letermovir (GMP) is the GMP grade of Letermovir (HY-15233). GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Letermovir (GMP) is an orally active CMV inhibitor. Letermovir (GMP) targets the CMV terminase complex rather than CMV DNA polymerase and exerts its antiviral activity. Letermovir (GMP) can be used in the study of CMV infection^[1].

AIC246 has consistent antiviral efficacy, and there is remarkable selectivity of AIC246 for human cytomegaloviruses^[1]. AD169 mutant strains and designated rAIC246-1 and rAIC246-2 are highly resistant to Letermovir (AIC246), with EC₅₀s of 5.6 nM, 1.24 μM, 0.37 μM, respectively. Letermovir inhibits HCMV replication through a specific antiviral mechanism that involves the viral gene product UL56. Letermovir inhibits HCMV replication in cell culture by interfering with the proper cleavage/packaging of HCMV progeny DNA^[2]. Letermovir inhibits the current gold standard GCV by more than 400-fold with respect to EC₅₀s (mean, 4.5 nM versus 2 μM) and by more than 2,000-fold with respect to EC₉₀ values (mean, 6.1 nM versus 14.5 μM)^[3]. Letermovir in conbination with anti-HCMV drugs causes additive antiviral effects, but there is no interaction between letermovir and anti-HIV drugs^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Letermovir (10-100 mg/kg/day, p.o.) leads to a dose-dependent reduction of the HCMV titer in transplanted cells compared to that of the placebo-treated control group using the mouse xenograft model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

572.55

C₂₉H₂₈F₄N₄O₄

917389-32-3

FC1=C(N=C(N2CCN(C3=CC=CC(OC)=C3)CC2)N(C4=CC(C(F)(F)F)=CC=C4OC)[C@H]5CC(O)=O)C5=CC=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Lischka P, et al. In vitro and in vivo activities of the novel anticytomegalovirus compound AIC246. Antimicrob Agents Chemother. 2010 Mar;54(3):1290-7.  [Content Brief]

  [2]. Wildum S, et al. In vitro drug combination studies of Letermovir (AIC246, MK-8228) with approved anti-human cytomegalovirus (HCMV) and anti-HIV compounds in inhibition of HCMV and HIV replication. Antimicrob Agents Chemother. 2015;59(6):3140-8.  [Content Brief]

  [3]. Marschall M, et al. In vitro evaluation of the activities of the novel anticytomegalovirus compound AIC246 (letermovir) against herpesviruses and other human pathogenic viruses. Antimicrob Agents Chemother. 2012 Feb;56(2):1135-7.  [Content Brief]

  [4]. Goldner T, et al. The novel anticytomegalovirus compound AIC246 (Letermovir) inhibits human cytomegalovirus replication through a specific antiviral mechanism that involves the viral terminase. J Virol. 2011 Oct;85(20):10884-93.  [Content Brief]