Mericitabine

Mericitabine
Clinical data

Trade names	Mericitabine
Legal status
Legal status	Investigational New Drug
Identifiers
IUPAC name [(2R,3R,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-fluoro-4-methyl-3-(2-methylpropanoyloxy)oxolan-2-yl]methyl 2-methylpropanoate
CAS Number	940908-79-2^Y
PubChem (CID)	16122663
ChemSpider	17279576
UNII	TA63JX8X52^Y
KEGG	D10477
Chemical and physical data
Formula	C₁₈H₂₆FN₃O₆
Molar mass	399.419
3D model (Jmol)	Interactive image
SMILES CC(C)C(=O)OC[C@@H]1[C@H]([C@@]([C@@H](O1)N2C=CC(=NC2=O)N)(C)F)OC(=O)C(C)C
InChI InChI=1S/C18H26FN3O6/c1-9(2)14(23)26-8-11-13(28-15(24)10(3)4)18(5,19)16(27-11)22-7-6-12(20)21-17(22)25/h6-7,9-11,13,16H,8H2,1-5H3,(H2,20,21,25)/t11-,13-,16-,18-/m1/s1 Key:MLESJYFEMSJZLZ-MAAOGQSESA-N

Mericitabine (RG-7128) is an antiviral drug, a deoxycytidine analog (a type of nucleoside analog). It was developed as a treatment for hepatitis C, acting as a NS5B RNA polymerase inhibitor, but while it showed a good safety profile in clinical trials, it was not sufficiently effective to be used as a stand alone agent. However mericitabine has been shown to boost the efficacy of other antiviral drugs when used alongside them, and as most modern treatment regimens for hepatitis C use a combination therapy of several antiviral drugs, clinical trials have continued to see if it can form a part of a clinically useful drug treatment program.^[1]^[2]

References

↑ Gentile, I; Coppola, N; Buonomo, A. R.; Zappulo, E; Borgia, G (2014). "Investigational nucleoside and nucleotide polymerase inhibitors and their use in treating hepatitis C virus". Expert Opin Investig Drugs. 23 (9): 1211–23. doi:10.1517/13543784.2014.921680. PMID 24848437.
↑ Wedemeyer, H; Forns, X; Hézode, C; Lee, S. S.; Scalori, A; Voulgari, A; Le Pogam, S; Nájera, I; Thommes, J. A. (2016). "Mericitabine and Either Boceprevir or Telaprevir in Combination with Peginterferon Alfa-2a plus Ribavirin for Patients with Chronic Hepatitis C Genotype 1 Infection and Prior Null Response: The Randomized DYNAMO 1 and DYNAMO 2 Studies". PLoS One. 11 (1): e0145409. Bibcode:2016PLoSO..1145409W. doi:10.1371/journal.pone.0145409. PMC 4713467. PMID 26752189.

RNA virus antivirals (primarily J05, also S01AD and D06BB)

Hepatitis C

NS3/4A protease inhibitors (–previr)	Asunaprevir Boceprevir Faldaprevir^‡ Grazoprevir Paritaprevir Simeprevir Telaprevir

NS5A inhibitors (–asvir)	Daclatasvir Elbasvir Ledipasvir MK-3682 MK-8408 Odalasvir^† Ombitasvir Ravidasvir^† Samatasvir^† Velpatasvir

NS5B RNA polymerase inhibitors (–buvir)	Beclabuvir^† Dasabuvir Deleobuvir^§ Filibuvir^§ Setrobuvir^§ Sofosbuvir Radalbuvir^†

Combination drugs	Elbasvir/grazoprevir Ledipasvir/sofosbuvir Ombitasvir/paritaprevir/ritonavir Sofosbuvir/daclatasvir Velpatasvir/sofosbuvir

Picornavirus

viral entry: Pleconaril^†

Anti-influenza agents

Umifenovir

neuraminidase inhibitors/release phase (Oseltamivir
Zanamivir
Peramivir, Laninamivir^†)

Multiple/general

Interferon	Interferon alfa 2b Peginterferon alfa-2a^#

Multiple/unknown	BCX4430^† Favipiravir GS-5734^† Mericitabine^† MK-608^§ NITD008^§ Moroxydine Ribavirin^#/Taribavirin^† Triazavirin

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

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Mericitabine

See also

References