[CAS NO. 917389-32-3] Letermovir

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PRODUCTS SPECIFICATIONS [917389-32-3]

Catalog

HY-15233

Brand

MCE

CAS

917389-32-3

DESCRIPTION [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

For research use only. We do not sell to patients.

15 Publications Citing Use of MCE

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

In Vitro:

DMSO : ≥ 100 mg/mL ( 174.66 mM )

* "≥" means soluble, but saturation unknown.

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

4-Quinazolineacetic acid, 8-fluoro-3,4-dihydro-2-[4-(3-methoxyphenyl)-1-piperazinyl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-, (4S)-

(4S)-8-Fluoro-3,4-dihydro-2-[4-(3-methoxyphenyl)-1-piperazinyl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-4-quinazolineacetic acid

AIC 246

Letermovir

Prevymis

(S)-2-(8-Fluoro-3-(2-methoxy-5-(trifluoromethyl)phenyl)-2-(4-(3-methoxyphenyl)piperazin-1-yl)-3,4-dihydroquinazolin-4-yl)acetic acid