Details
Stereochemistry | ACHIRAL |
Molecular Formula | C19H25O5P |
Molecular Weight | 364.3726 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)C1=CC(CC2=C(C)C=C(OCP(O)(O)=O)C=C2C)=CC=C1O
InChI
InChIKey=SVXLLCKJKRYATC-UHFFFAOYSA-N
InChI=1S/C19H25O5P/c1-12(2)17-9-15(5-6-19(17)20)10-18-13(3)7-16(8-14(18)4)24-11-25(21,22)23/h5-9,12,20H,10-11H2,1-4H3,(H2,21,22,23)
MB-07811 (VK-2809) is the liver-activated prodrug of a phosphonate-containing thyroid hormone receptor beta agonist MB-07344. In animal studies, it showed potent lipid and cholesterol lowering activity. Viking Therapeutics is developing MB-07811 hypercholesterolaemia and non-alcoholic fatty liver disease.
Originator
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
Preclinical pharmacokinetics of a HepDirect prodrug of a novel phosphonate-containing thyroid hormone receptor agonist. | 2008 Nov |
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Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs. | 2008 Nov 27 |
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Thyroid hormone beta receptor activation has additive cholesterol lowering activity in combination with atorvastatin in rabbits, dogs and monkeys. | 2009 Feb |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02927184 http://ir.vikingtherapeutics.com/2019-04-11-Viking-Therapeutics-Presents-New-Data-from-Phase-2-Study-of-VK2809-in-Patients-with-Non-Alcoholic-Fatty-Liver-Disease-NAFLD-and-Elevated-LDL-Cholesterol-at-The-International-Liver-Congress-TM-2019
The Phase 2 study was a randomized, double-blind, placebo-controlled, parallel-group study designed to evaluate the efficacy, safety and tolerability of MB-07811 (VK-2809) in patients with elevated LDL-C and NAFLD. Patients were randomized to receive placebo, 5 mg VK2809 dosed daily, 10 mg VK2809 dosed every other day, or 10 mg VK2809 dosed daily for 12 weeks.
Route of Administration:
Oral
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ACTIVE MOIETY
PRODRUG (METABOLITE ACTIVE)