WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H319765
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.
Hodoodo Cat#: H319765
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
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:
Biological target: | |
In vitro activity: | |
In vivo activity: |
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: | |
In vitro protocol: | |
In vivo protocol: |
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.