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[CAS NO. 917389-32-3] Letermovir
| Ships within | Stock | Price | Qty | Total |
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| Catalog: | HY-15233 |
| Brand: | MCE |
| CAS: | 917389-32-3 |
Overview
| MDL | MFCD22572725 |
|---|---|
| Molecular Weight | 572.55 |
| Molecular Formula | C29H28F4N4O4 |
| SMILES | 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 |
15 Publications Citing Use of MCE
- [1]PLoS Pathog. 2017 Feb 27;13(2):e1006202.
- [2]Antimicrob Agents Chemother. 2020 Dec 16;65(1):e01627-20.
- [3]Antimicrob Agents Chemother. 2018 Aug 27;62(9). pii: e00922-18.
- [4]Antimicrob Agents Chemother. 2015 Oct;59(10):6588-93.
- [5]J Virol. 2017 Jan 18;91(3). pii: e02152-16.
- [6]Antiviral Res. 2022 Jun 8;105361.
- [7]Antivir Res. 2019 Dec;172:104639.
- [8]Antiviral Res. 2018 Oct;158:255-263.
- [9]Antiviral Res. 2018 Sep;157:128-133.
- [10]Antiviral Res. 2017 Dec;148:1-4.
- [11]Eur J Pharm Sci. 2019 Jan 15;127:29-37.
- [12]PLoS One. 2020 Apr 30;15(4):e0232140.
- [13]Microbiol Immunol. 2018 Oct;62(10):651-658.
- [14]Patent. US20210228711A1.
- [15]Johannes Gutenberg-Universität Mainz. 17-Aug-2021.
Summary
Letermovir (AIC246) is a potent inhibitor of CMV , which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.
In Vitro
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 EC 50 s 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 EC 50 s (mean, 4.5 nM versus 2 μM) and by more than 2,000-fold with respect to EC 90 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04129398 | Merck Sharp & Dohme LLC |
Cytomegalovirus Infection|Cytomegalovirus Disease
|
December 27, 2019 | Phase 3 |
| NCT03930615 | Merck Sharp & Dohme LLC |
Cytomegalovirus Infection
|
June 21, 2019 | Phase 3 |
| NCT04840199 | National Institute of Allergy and Infectious Diseases (NIAID)|Merck Sharp & Dohme LLC |
HIV Infections|Cytomegalovirus|CMV
|
November 2, 2022 | Phase 2 |
| NCT04732260 | Assistance Publique - Hôpitaux de Paris |
Pregnant Women Undergoing TOP|TOP - Failed Attempted Termination of Pregnancy
|
June 11, 2021 | Not Applicable |
| NCT05041426 | Fernanda P Silveira, MD, MS|Merck Sharp & Dohme LLC|University of Pittsburgh |
Lung Transplant|CMV
|
December 6, 2021 | Phase 2 |
| NCT05626530 | Tufts Medical Center |
Cytomegalovirus Infections|Infection in Solid Organ Transplant Recipients|Neutropenia|Antiviral Toxicity
|
December 15, 2022 | Phase 4 |
| NCT02137772 | Merck Sharp & Dohme LLC |
Prevention of CMV Infection or Disease
|
June 6, 2014 | Phase 3 |
| NCT03728426 | Amy C. Sherman, MD|Merck Sharp & Dohme LLC|Dana-Farber Cancer Institute |
Cytomegalovirus Infections
|
January 11, 2019 | Phase 2 |
| NCT05446571 | Assistance Publique - Hôpitaux de Paris |
Pregnant Women|CMV Infected Fetuses
|
December 2022 | Phase 3 |
| NCT04904614 | Tufts Medical Center|Merck Sharp & Dohme LLC |
Cytomegalovirus Disease|Cytomegalovirus Infections|Heart Transplant Infection|Antiviral Toxicity|Neutropenia
|
October 1, 2021 | Phase 4 |
| NCT01063829 | AiCuris Anti-infective Cures AG|Quintiles, Inc. |
HCMV Reactivation or HCMV End-Organ Disease
|
March 2010 | Phase 2 |
| NCT04017962 | Memorial Sloan Kettering Cancer Center|Merck Sharp & Dohme LLC |
CMV|CMV Infection|Hematopoietic Cell Transplant
|
July 19, 2019 | Phase 2 |
| NCT05362916 | Jean-Pierre Routy|McGill University Health Centre+Research Institute of the McGill University Health Centre |
People Living With HIV
|
September 26, 2022 | Not Applicable |
| NCT04312841 | Ohio State University Comprehensive Cancer Center|Merck Sharp & Dohme LLC |
B-Cell Prolymphocytic Leukemia|Chronic Lymphocytic Leukemia|Peripheral T-Cell Lymphoma|Primary Cutaneous T-Cell Non-Hodgkin Lymphoma|Sezary Syndrome|T-Cell Prolymphocytic Leukemia
|
September 15, 2020 | Phase 2 |
| NCT03443869 | Merck Sharp & Dohme LLC |
CMV Disease
|
May 3, 2018 | Phase 3 |
| NCT05432778 | University Medical Centre Ljubljana |
CMV Viremia
|
August 1, 2022 | Phase 2 |
| NCT03940586 | Merck Sharp & Dohme LLC |
Cytomegalovirus (CMV) Infection
|
August 8, 2019 | Phase 2 |
| NCT04060277 | City of Hope Medical Center|National Cancer Institute (NCI) |
Accelerated Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Acute Lymphoblastic Leukemia|Acute Myeloid Leukemia|Chronic Lymphocytic Leukemia|Chronic Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Hematopoietic and Lymphoid Cell Neoplasm|Hodgkin Lymphoma|Lymphoblastic Lymphoma|Myelodysplastic Syndrome|Myelofibrosis|Myeloproliferative Neoplasm|Non-Hodgkin Lymphoma
|
October 7, 2019 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 174.66 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7466 mL | 8.7329 mL | 17.4657 mL |
| 5 mM | 0.3493 mL | 1.7466 mL | 3.4931 mL |
| 10 mM | 0.1747 mL | 0.8733 mL | 1.7466 mL |
References
- [1] 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.
- [2] 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.
- [3] 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.
- [4] 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.
Synonyms
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