MDL | MFCD00945570 |
---|---|
Molecular Weight | 376.24 |
Molecular Formula | C15H19Cl2N3O4 |
SMILES | ClC1=C(Cl)C=C2C(N=C(NC(C)C)N2[C@@H]3[C@@H](O)[C@@H](O)[C@H](CO)O3)=C1 |
Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC 50 of 3 nM. Maribavir has potent antiviral activity against HCMV and Epstein-Barr virus ( EBV ).
HCMV [1]
Maribavir is a potent inhibitor of the autophosporylation of the wild type and all the major Ganciclovir (GCV) resistant UL97 mutants analysed with a mean IC 50 of 35 nM. The M460I mutation results in hypersensitivity to Maribavir with an IC 50 of 4.8 nM. A Maribavir resistant mutant of UL97 (L397R) is functionally compromised as both a Ganciclovir kinase and a protein kinase (~ 10% of wild type levels). Enzyme kinetic experiments demonstrate that Maribavir is a competitive inhibitor of ATP with a K i of 10 nM [1] . Maribavir (1263W94) inhibits viral replication in a dose-dependent manner, with IC 50 of 0.12±0.01 μM as measured by a multicycle DNA hybridization assay. The pUL97 protein kinase is strongly inhibited by Maribavir, with 50% inhibition occurring at 3 nM [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT04131556 | Shire|Takeda |
Healthy Volunteers
|
October 25, 2019 | Phase 1 |
NCT04497883 | Shire|Takeda |
Healthy Volunteers
|
August 7, 2020 | Phase 1 |
NCT01611974 | Shire|Takeda |
Cytomegalovirus (CMV)
|
July 17, 2012 | Phase 2 |
NCT05319353 | Takeda|Takeda Development Center Americas, Inc. |
Cytomegalovirus (CMV)
|
March 31, 2023 | Phase 3 |
NCT00223925 | Shire|Takeda |
Cytomegalovirus Infection
|
October 28, 2004 | Phase 2 |
NCT02927067 | Shire|Takeda Development Center Americas, Inc.|Takeda |
Cytomegalovirus (CMV)
|
April 14, 2017 | Phase 3 |
NCT05382104 | Takeda|Takeda Development Center Americas, Inc. |
Healthy Volunteers
|
June 1, 2022 | Phase 1 |
NCT02775240 | Shire|Takeda |
Cytomegalovirus (CMV)
|
July 21, 2016 | Phase 1 |
NCT02931539 | Shire|Takeda |
Cytomegalovirus (CMV)
|
December 22, 2016 | Phase 3 |
NCT00002373 | Glaxo Wellcome|NIH AIDS Clinical Trials Information Service |
Cytomegalovirus Infections|HIV Infections
|
Phase 1 | |
NCT05137717 | Takeda |
Cytomegalovirus (CMV)
|
December 23, 2021 | Phase 3 |
NCT00497796 | Shire|Takeda |
Cytomegalovirus Infections
|
July 23, 2007 | Phase 3 |
NCT00411645 | Shire|Takeda |
Cytomegalovirus Infections
|
December 13, 2006 | Phase 3 |
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 200 mg/mL ( 531.58 mM ; Need ultrasonic)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.6579 mL | 13.2894 mL | 26.5788 mL |
5 mM | 0.5316 mL | 2.6579 mL | 5.3158 mL |
10 mM | 0.2658 mL | 1.3289 mL | 2.6579 mL |
Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.87 mg/mL (7.63 mM); Clear solution
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.64 mM); Clear solution
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.64 mM); Clear solution