Molnupiravir

Molnupiravir 속성

Molnupiravir C화학적 특성, 용도, 생산

개요

EIDD-2801 is an orally bioavailable prodrug of the antiviral nucleoside derivative N4- hydroxycytidine (NHC, EIDD-1931). It is a nucleotide analog inhibitor of RNA-dependent RNA polymerases (RdRps). The compound interferes with the action of viral RNA polymerase. It exerts its antiviral action through introduction of copying errors during viral RNA replication. The active drug incorporates into the genome of RNA viruses, leading to an accumulation of mutations known as viral error catastrophe. The broadspectrum antiviral agent EIDD-2801 inhibits viral RNA replication in various unrelated RNA viruses including influenza, Ebola, Venezuelan equine encephalitis virus (VEEV) and coronaviruses, including SARS-CoV, MERS-CoV and SARS-CoV-2. EIDD-2801 has the potential for COVID-19, seasonal and pandemic influenza treatment.

역사

Molnupiravir (EIDD-2801/MK-4482) is an investigational, orally bioavailable form of a potent ribonucleoside analog that inhibits the replication of multiple RNA viruses including SARS-CoV-2, the causative agent of COVID-19. Molnupiravir has been shown to be active in several models of SARS-CoV-2, including for prophylaxis, treatment and prevention of transmission, as well as SARS-CoV-1 and MERS. EIDD-2801 was invented at Drug Innovations at Emory (DRIVE), LLC, a not-for-prot biotechnology company wholly owned by Emory University, and with partial funding support from the U.S. government. Since licensed by Ridgeback, all funds used for the development of EIDD-2801 by Ridgeback have been provided by Wayne and Wendy Holman and Merck.

용도

EIDD 2801 is an orally bioavailable broad-spectrum antiviral that inhibits SARS-CoV-2 and other multiple endemic, epidemic and bat coronavirus and has the potential for seasonal and pandemic influenza treatment. An isopropylester prodrug of the ribonucleoside analog of EIDD-1931 that exhibits anti-influenza virus and coronaviruses activities.

정의

Molnupiravir is a nucleoside analogue that is N(4)-hydroxycytidine in which the 5'-hydroxy group is replaced by a (2-methylpropanoyl)oxy group. It is the prodrug of the active antiviral ribonucleoside analog N(4)-hydroxycytidine (EIDD-1931), has activity against a number of RNA viruses including SARS-CoV-2, MERS-CoV, and seasonal and pandemic influenza viruses. It is currently in phase III trials for the treatment of patients with COVID-19. It has a role as a prodrug, an anticoronaviral agent and an antiviral drug. It is a nucleoside analogue, an isopropyl ester and a ketoxime. It derives from a N(4)-hydroxycytidine.
www.ebi.ac.uk

생물학적 활성

EIDD-2801 is an orally active, 5′-isopropylester prodrug form of the antiviral ribonucleoside analog N4-hydroxycytidine (NHC, EIDD-1931) with known anti-viral activity against SARS-CoV, SARS-CoV-2, RSV, influenza A & B (IAV & IBV), HCV, pestivirus, bovine viral diarrhoea virus (BVDV), Ebola (EBOV), Chikungunya (CHIKV), venezuelan equine encephalitis (VEEV). EIDD-2801 is efficiently hydrolyzed to NHC in vivo, being more orally bioavailable than NHC in nonhuman primates and ferrets, while maintaining similar oral bioavailability as NHC in mice. EIDD-2801 displays in vivo efficacy against pandemic and seasonal IAV strains in ferrets (lowest ED = 2.3 and 7 mg/kg b.i.d. p.o., respectively).

Regulatory Status

Molnupiravir (as EIDD-2801) was developed at Drug Innovation Ventures at Emory (DRIVE), a not-forprofit biotechnology company owned by Emory University, Atlanta. It was then licensed by Ridgeback Biotherapeutics, and is now developed further in cooperation with Merck & Co. (in Europe: Merck Sharp & Dohme/ MSD).
Molnupiravir is not approved by the European Medicines Agency (EMA) or the American Food and Drug Administration (FDA).

참고 문헌

[1] Toots M, Yoon J-J, Cox RM et al. Characterization of orally efficacious influenza drug with high resistance barrier in ferrets and human airway epithelia. Science Translational Medicine 2019;11(515). Epub 23 Oct 2019.
[2] Toots M, Yoon J-J, Hart M et al. . Quantitative Efficacy Paradigms of the Influenza Clinical Drug Candidate EIDD-2801 in the Ferret Model. Transl Res 2020. Epub 2019 Dec 25.
[3] Halford B. An emerging antiviral takes aim at COVID-19. American Chemical Society; 2020 [14.12.2020]; Available from: https://cen.acs.org/pharmaceuticals/drug-development/emergingantiviral-takes-aim-COVID-19/98/web/2020/05.
[4] Ridgeback Biotherapeutics. OVERVIEW OF EIDD-2801 (MK-4482). [Presentation]. provided via email 2020.

Molnupiravir 준비 용품 및 원자재

원자재

준비 용품

Molnupiravir 공급 업체

공급자	전화	이메일	국가	제품 수	이점
weifang runzhong fine chemical co., ltd	536-7868377 +8618653686003	sq@runzhongchem.com	China	187	58
Jinan Jianfeng Chemical Co., Ltd	0531-88110457; +8615562555968	info@pharmachemm.com	China	246	58
HangZhou RunYan Pharma Technology Co.,LTD.	+86-88660901 +86-18112526015	sales@runyanpharma.com	China	326	58
Hebei Yanxi Chemical Co., Ltd.	+8617531190177	peter@yan-xi.com	China	5993	58
Anhui Ruihan Technology Co., Ltd	+8617756083858	daisy@anhuiruihan.com	China	994	58
Shaanxi TNJONE Pharmaceutical Co., Ltd	+86-13474506593 +86-13474506593	sarah@tnjone.com	China	794	58
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32480	60
Shenzhen Nexconn Pharmatechs Ltd	+86-755-89396905 +86-15013857715	admin@nexconn.com	China	7838	58
Shaanxi Dideu Medichem Co. Ltd	18192627656	1012@dideu.com	China	3657	58
ENBRIDGE PHARMTECH CO., LTD.	+8613812269233	tinayang@enbridgepharm.com	China	303	58

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