Letermovir | MK-8828 | CAS#917389-32-3 | antiviral

Letermovir
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 319765

CAS#: 917389-32-3

Description: Letermovir, also known as MK-8828 and AIC-246, is an antiviral drug that is being developed for the treatment of cytomegalovirus (CVM) infections. Letermovir has been tested in CMV infected patients with allogeneic stem cell transplants and may also be useful for other patients with a compromised immune system such as those with organ transplants or HIV infections.

Chemical Structure

Letermovir

CAS# 917389-32-3

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 319765
Name: Letermovir
CAS#: 917389-32-3
Chemical Formula: C29H28F4N4O4
Exact Mass: 572.20
Molecular Weight: 572.561
Elemental Analysis: C, 60.84; H, 4.93; F, 13.27; N, 9.79; O, 11.18

Price and Availability

Size	Price	Availability
10mg	USD 250	2 Weeks
50mg	USD 550	2 Weeks
100mg	USD 850	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: MK-8828; MK 8828; MK8828; AIC-246; AIC 246; AIC246; Letermovir; Prevymis

IUPAC/Chemical Name: (S)-2-(8-fluoro-3-(2-methoxy-5-(trifluoromethyl)phenyl)-2-(4-(3-methoxyphenyl)piperazin-1-yl)-3,4-dihydroquinazolin-4-yl)acetic acid

InChi Key: FWYSMLBETOMXAG-QHCPKHFHSA-N

InChi Code: InChI=1S/C29H28F4N4O4/c1-40-20-6-3-5-19(16-20)35-11-13-36(14-12-35)28-34-27-21(7-4-8-22(27)30)23(17-26(38)39)37(28)24-15-18(29(31,32)33)9-10-25(24)41-2/h3-10,15-16,23H,11-14,17H2,1-2H3,(H,38,39)/t23-/m0/s1

SMILES Code: O=C(O)C[C@@H]1N(C2=CC(C(F)(F)F)=CC=C2OC)C(N3CCN(C4=CC=CC(OC)=C4)CC3)=NC5=C1C=CC=C5F

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Instruction:

View handling instruction

Biological target:	Letermovir (AIC246) is a potent inhibitor of CMV.
In vitro activity:	AIC246 (letermovir) is a potent anticytomegalovirus drug in clinical development. This study reports a consistent antiviral efficacy of AIC246 against human cytomegalovirus laboratory strains, clinical isolates, and virus variants resistant to approved drugs. Reference: Antimicrob Agents Chemother. 2012 Feb;56(2):1135-7. https://pubmed.ncbi.nlm.nih.gov/22106211/
In vivo activity:	This study demonstrates that AIC246 exhibits excellent in vitro inhibitory activity against HCMV laboratory strains and clinical isolates, retains activity against ganciclovir-resistant viruses, is well tolerated in different cell types (median selectivity index, 18,000), and exerts a potent in vivo efficacy in a mouse xenograft model. Reference: Antimicrob Agents Chemother. 2010 Mar;54(3):1290-7. https://pubmed.ncbi.nlm.nih.gov/20047911/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	Ethanol	60.0	104.79
	Ethanol:PBS (pH 7.2) (1:1)	0.5	0.87

Preparing Stock Solutions

The following data is based on the product molecular weight 572.56 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Goldner T, Hempel C, Ruebsamen-Schaeff H, Zimmermann H, Lischka P. Geno- and phenotypic characterization of human cytomegalovirus mutants selected in vitro after letermovir (AIC246) exposure. Antimicrob Agents Chemother. 2014;58(1):610-3. doi: 10.1128/AAC.01794-13. Epub 2013 Nov 4. PMID: 24189264; PMCID: PMC3910730. 2. Marschall M, Stamminger T, Urban A, Wildum S, Ruebsamen-Schaeff H, Zimmermann H, Lischka P. 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. doi: 10.1128/AAC.05908-11. Epub 2011 Nov 21. PMID: 22106211; PMCID: PMC3264222. 3. Lischka P, Hewlett G, Wunberg T, Baumeister J, Paulsen D, Goldner T, Ruebsamen-Schaeff H, Zimmermann H. In vitro and in vivo activities of the novel anticytomegalovirus compound AIC246. Antimicrob Agents Chemother. 2010 Mar;54(3):1290-7. doi: 10.1128/AAC.01596-09. Epub 2010 Jan 4. PMID: 20047911; PMCID: PMC2826024.
In vitro protocol:	1. Goldner T, Hempel C, Ruebsamen-Schaeff H, Zimmermann H, Lischka P. Geno- and phenotypic characterization of human cytomegalovirus mutants selected in vitro after letermovir (AIC246) exposure. Antimicrob Agents Chemother. 2014;58(1):610-3. doi: 10.1128/AAC.01794-13. Epub 2013 Nov 4. PMID: 24189264; PMCID: PMC3910730. 2. Marschall M, Stamminger T, Urban A, Wildum S, Ruebsamen-Schaeff H, Zimmermann H, Lischka P. 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. doi: 10.1128/AAC.05908-11. Epub 2011 Nov 21. PMID: 22106211; PMCID: PMC3264222.
In vivo protocol:	1. Lischka P, Hewlett G, Wunberg T, Baumeister J, Paulsen D, Goldner T, Ruebsamen-Schaeff H, Zimmermann H. In vitro and in vivo activities of the novel anticytomegalovirus compound AIC246. Antimicrob Agents Chemother. 2010 Mar;54(3):1290-7. doi: 10.1128/AAC.01596-09. Epub 2010 Jan 4. PMID: 20047911; PMCID: PMC2826024.

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1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548861/ PubMed PMID: 31644168.

2: Letermovir for cytomegalovirus prophylaxis. Aust Prescr. 2019 Jun;42(3):107. doi: 10.18773/austprescr.2019.032. Epub 2019 Apr 24. Review. PubMed PMID: 31363312; PubMed Central PMCID: PMC6594842.

3: Gerna G, Lilleri D, Baldanti F. An overview of letermovir: a cytomegalovirus prophylactic option. Expert Opin Pharmacother. 2019 Aug;20(12):1429-1438. doi: 10.1080/14656566.2019.1637418. Epub 2019 Jul 8. Review. PubMed PMID: 31282759.

4: El Helou G, Razonable RR. Letermovir for the prevention of cytomegalovirus infection and disease in transplant recipients: an evidence-based review. Infect Drug Resist. 2019 Jun 4;12:1481-1491. doi: 10.2147/IDR.S180908. eCollection 2019. Review. PubMed PMID: 31239725; PubMed Central PMCID: PMC6556539.

5: Clinical Review Report: Letermovir (Prevymis): (Merck Canada Inc.): Indication: For the prophylaxis of cytomegalovirus (CMV) infection in adult CMV-seropositive recipients (R+) of an allogeneic hematopoietic stem cell transplant [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2018 Jul. Available from http://www.ncbi.nlm.nih.gov/books/NBK539334/ PubMed PMID: 30942986.

6: Pharmacoeconomic Review Report: Letermovir (Prevymis): (Merck Canada Inc.): Indication: For the prophylaxis of cytomegalovirus (CMV) infection in adult CMV-seropositive recipients (R+) of an allogeneic hematopoietic stem cell transplant [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2018 Jul. Available from http://www.ncbi.nlm.nih.gov/books/NBK539213/ PubMed PMID: 30933449.

7: CADTH Canadian Drug Expert Committee Recommendation: Letermovir (Prevymis — Merck Canada Inc.): Indication: Cytomegalovirus infection, prophylaxis [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2018 Jun. No abstract available. Available from http://www.ncbi.nlm.nih.gov/books/NBK538995/ PubMed PMID: 30912896.

8: Piret J, Boivin G. Clinical development of letermovir and maribavir: Overview of human cytomegalovirus drug resistance. Antiviral Res. 2019 Mar;163:91-105. doi: 10.1016/j.antiviral.2019.01.011. Epub 2019 Jan 25. Review. PubMed PMID: 30690043.

9: Deleenheer B, Spriet I, Maertens J. Pharmacokinetic drug evaluation of letermovir prophylaxis for cytomegalovirus in hematopoietic stem cell transplantation. Expert Opin Drug Metab Toxicol. 2018 Dec;14(12):1197-1207. doi: 10.1080/17425255.2018.1550485. Epub 2018 Dec 4. Review. PubMed PMID: 30479172.

10: Foolad F, Aitken SL, Chemaly RF. Letermovir for the prevention of cytomegalovirus infection in adult cytomegalovirus-seropositive hematopoietic stem cell transplant recipients. Expert Rev Clin Pharmacol. 2018 Oct;11(10):931-941. doi: 10.1080/17512433.2018.1500897. Epub 2018 Sep 18. Review. PubMed PMID: 30004790.

11: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK500949/ PubMed PMID: 30000008.

12: Cho JC, Le AD, Locke SC. Letermovir for prophylaxis of cytomegalovirus in allogeneic hematopoietic stem cell recipients. Drugs Today (Barc). 2018 Jun;54(6):361-368. doi: 10.1358/dot.2018.54.6.2833982. Review. PubMed PMID: 29998227.

13: Razonable RR. Role of letermovir for prevention of cytomegalovirus infection after allogeneic haematopoietic stem cell transplantation. Curr Opin Infect Dis. 2018 Aug;31(4):286-291. doi: 10.1097/QCO.0000000000000459. Review. PubMed PMID: 29746444.

14: Frange P, Leruez-Ville M. Maribavir, brincidofovir and letermovir: Efficacy and safety of new antiviral drugs for treating cytomegalovirus infections. Med Mal Infect. 2018 Dec;48(8):495-502. doi: 10.1016/j.medmal.2018.03.006. Epub 2018 Apr 9. Review. PubMed PMID: 29650261.

15: Kim ES. Letermovir: First Global Approval. Drugs. 2018 Jan;78(1):147-152. doi: 10.1007/s40265-017-0860-8. Review. PubMed PMID: 29288370.

16: Bowman LJ, Melaragno JI, Brennan DC. Letermovir for the management of cytomegalovirus infection. Expert Opin Investig Drugs. 2017 Feb;26(2):235-241. doi: 10.1080/13543784.2017.1274733. Epub 2016 Dec 28. Review. PubMed PMID: 27998189.

17: Melendez DP, Razonable RR. Letermovir and inhibitors of the terminase complex: a promising new class of investigational antiviral drugs against human cytomegalovirus. Infect Drug Resist. 2015 Aug 5;8:269-77. doi: 10.2147/IDR.S79131. eCollection 2015. Review. PubMed PMID: 26345608; PubMed Central PMCID: PMC4531042.

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