Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H30N5O10P |
Molecular Weight | 519.4435 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)OC(=O)OCOP(=O)(CO[C@]([H])(C)Cn1cnc2c(N)ncnc21)OCOC(=O)OC(C)C
InChI
InChIKey=JFVZFKDSXNQEJW-CQSZACIVSA-N
InChI=1S/C19H30N5O10P/c1-12(2)33-18(25)28-9-31-35(27,32-10-29-19(26)34-13(3)4)11-30-14(5)6-24-8-23-15-16(20)21-7-22-17(15)24/h7-8,12-14H,6,9-11H2,1-5H3,(H2,20,21,22)/t14-/m1/s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/20439609Curator's Comment:: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/20439609 and http://ir.chimerix.com/releasedetail.cfm?releaseid=752310
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20439609
Curator's Comment:: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/20439609 and http://ir.chimerix.com/releasedetail.cfm?releaseid=752310
CMX157 is a lipid (1-0-hexadecyloxypropyl) conjugate of the acyclic nucleotide analog tenofovir (TFV) with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. CMX157 was designed to mimic lysophosphatidylcholine to take advantage of natural lipid uptake pathways and to achieve high intracellular concentrations of the active antiviral, with the aim of increasing the effectiveness of TFV against wild-type and mutant HIV. CMX157 demonstrated potential to effectively suppress replication of multiNRTI-resistant (MNR) HIV that cannot be treated with any currently available NRTIs, including TDF. It is in phase II clinical trial for HIV infections in USA and phase Ib portion of the phase I/II trial for Hepatitis B in Thailand (PO).
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: HIV-1, subtype A 92RW009 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20439609 |
3.3 nM [EC50] | ||
Target ID: HIV-2 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20439609 |
3.5 nM [EC50] | ||
Target ID: HBV replication Sources: https://www.ncbi.nlm.nih.gov/pubmed/17646420 |
0.49 µM [EC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02710604
For hepatitis B - 5-100mg tablet
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20439609
CMX-157 was active against all major subtypes of HIV-1 and HIV-2 in fresh human peripheral blood mononuclear cells (PBMCs) and against all HIV-1 strains evaluated in monocyte-derived macrophages, with 50% effective concentrations (EC(50)s) ranging between 0.20 and 7.2 nM.
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WHO-VATC |
QJ05AR09
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EMA ASSESSMENT REPORTS |
STRIBILD (AUTHORIZED: HIV INFECTIONS)
Created by
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WHO-ATC |
J05AR24
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admin on Sat Jun 26 10:30:15 UTC 2021 , Edited by admin on Sat Jun 26 10:30:15 UTC 2021
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WHO-ATC |
J05AR09
Created by
admin on Sat Jun 26 10:30:15 UTC 2021 , Edited by admin on Sat Jun 26 10:30:15 UTC 2021
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WHO-ATC |
J05AR12
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admin on Sat Jun 26 10:30:15 UTC 2021 , Edited by admin on Sat Jun 26 10:30:15 UTC 2021
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WHO-ATC |
J05AF07
Created by
admin on Sat Jun 26 10:30:15 UTC 2021 , Edited by admin on Sat Jun 26 10:30:15 UTC 2021
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WHO-VATC |
QJ05AR11
Created by
admin on Sat Jun 26 10:30:15 UTC 2021 , Edited by admin on Sat Jun 26 10:30:15 UTC 2021
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WHO-ATC |
J05AR11
Created by
admin on Sat Jun 26 10:30:15 UTC 2021 , Edited by admin on Sat Jun 26 10:30:15 UTC 2021
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WHO-VATC |
QJ05AR06
Created by
admin on Sat Jun 26 10:30:15 UTC 2021 , Edited by admin on Sat Jun 26 10:30:15 UTC 2021
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WHO-ATC |
J05AR06
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admin on Sat Jun 26 10:30:15 UTC 2021 , Edited by admin on Sat Jun 26 10:30:15 UTC 2021
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WHO-ATC |
J05AR08
Created by
admin on Sat Jun 26 10:30:15 UTC 2021 , Edited by admin on Sat Jun 26 10:30:15 UTC 2021
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WHO-VATC |
QJ05AR03
Created by
admin on Sat Jun 26 10:30:15 UTC 2021 , Edited by admin on Sat Jun 26 10:30:15 UTC 2021
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WHO-ATC |
J05AR03
Created by
admin on Sat Jun 26 10:30:15 UTC 2021 , Edited by admin on Sat Jun 26 10:30:15 UTC 2021
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WHO-VATC |
QJ05AF07
Created by
admin on Sat Jun 26 10:30:15 UTC 2021 , Edited by admin on Sat Jun 26 10:30:15 UTC 2021
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WHO-VATC |
QJ05AR08
Created by
admin on Sat Jun 26 10:30:15 UTC 2021 , Edited by admin on Sat Jun 26 10:30:15 UTC 2021
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DB00300
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2593
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C418563
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SUB20643
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PRIMARY | |||
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Tenofovir disoproxil
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PRIMARY | |||
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5481350
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PRIMARY | |||
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201341-05-1
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201341-05-1
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PRIMARY | |||
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M10559
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PRIMARY | Merck Index | ||
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F4YU4LON7I
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300195
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PRIMARY | RxNorm |
ACTIVE MOIETY
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SUBSTANCE RECORD