Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C18H26FN3O6 |
Molecular Weight | 399.4139 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)C(=O)OC[C@H]1O[C@@H](N2C=CC(N)=NC2=O)[C@](C)(F)[C@@H]1OC(=O)C(C)C
InChI
InChIKey=MLESJYFEMSJZLZ-MAAOGQSESA-N
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
Mericitabine is a specific inhibitor of hepatitis C virus (HCV) replication that target NS5B polymerase. Mericitabine, a prodrug, is hydrolyzed in vivo to produce PSI-6130. It had been studied in phase II clinical trials for the treatment of chronic hepatitis C. However, while it showed a good safety profile in clinical trials, it was not sufficiently effective to be used as a standalone agent.
Originator
Approval Year
Cmax
Value | Dose | Co-administered | Analyte | Population |
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0.557 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24025983 |
1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered: |
RO5012433 plasma | Homo sapiens population: HEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: FASTED |
|
0.854 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24025983 |
2000 mg single, oral dose: 2000 mg route of administration: Oral experiment type: SINGLE co-administered: |
RO5012433 plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
0.361 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24025983 |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
RO5012433 plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
10.2 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24025983 |
2000 mg single, oral dose: 2000 mg route of administration: Oral experiment type: SINGLE co-administered: |
RO4995855 plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
4.23 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24025983 |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
RO4995855 plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
11.2 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24025983 |
1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered: |
RO5012433 plasma | Homo sapiens population: HEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: FASTED |
|
20.5 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24025983 |
2000 mg single, oral dose: 2000 mg route of administration: Oral experiment type: SINGLE co-administered: |
RO5012433 plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
6.35 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24025983 |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
RO5012433 plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
113 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24025983 |
2000 mg single, oral dose: 2000 mg route of administration: Oral experiment type: SINGLE co-administered: |
RO4995855 plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
28.8 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24025983 |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
RO4995855 plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
22.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24025983 |
1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered: |
RO5012433 plasma | Homo sapiens population: HEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: FASTED |
|
21.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24025983 |
2000 mg single, oral dose: 2000 mg route of administration: Oral experiment type: SINGLE co-administered: |
RO5012433 plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
19 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24025983 |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
RO5012433 plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
5.54 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24025983 |
2000 mg single, oral dose: 2000 mg route of administration: Oral experiment type: SINGLE co-administered: |
RO4995855 plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
4.96 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24025983 |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
RO4995855 plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
PubMed
Title | Date | PubMed |
---|---|---|
Tetrazole and triazole as bioisosteres of carboxylic acid: discovery of diketo tetrazoles and diketo triazoles as anti-HCV agents. | 2013 Aug 15 |
|
Highly efficient infectious cell culture of three hepatitis C virus genotype 2b strains and sensitivity to lead protease, nonstructural protein 5A, and polymerase inhibitors. | 2014 Feb |
|
The combination of alisporivir plus an NS5A inhibitor provides additive to synergistic anti-hepatitis C virus activity without detectable cross-resistance. | 2014 Jun |
|
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. | 2016 |
|
Modelling the interaction between danoprevir and mericitabine in the treatment of chronic HCV infection. | 2016 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20942646
1500 mg doses twice daily for 2 weeks
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18285474
A stable HCV 1b replicon cell (Gt 1b Con1) line was treated with the NS5B nucleoside inhibitor R7128 (prodrug PSI-6130). Inhibition of HCV replicon-encoded Renilla luciferase reporter activity after 3 days of incubation was calculated - EC50 = 0.61 uM.
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C281
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NCI_THESAURUS |
C1557
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SUB89593
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16122663
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DTXSID201025655
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TA63JX8X52
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DB12045
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ZZ-121
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100000140218
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C98959
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940908-79-2
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CHEMBL562967
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9293
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Mericitabine
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ACTIVE MOIETY
SUBSTANCE RECORD