Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C28H32ClO5P |
| Molecular Weight | 514.977 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)C1=CC(CC2=C(C)C=C(OC[P@@]3(=O)OCC[C@H](O3)C4=CC=CC(Cl)=C4)C=C2C)=CC=C1O
InChI
InChIKey=LGGPZDRLTDGYSQ-JADSYQMUSA-N
InChI=1S/C28H32ClO5P/c1-18(2)25-14-21(8-9-27(25)30)15-26-19(3)12-24(13-20(26)4)32-17-35(31)33-11-10-28(34-35)22-6-5-7-23(29)16-22/h5-9,12-14,16,18,28,30H,10-11,15,17H2,1-4H3/t28-,35+/m0/s1
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 |
|
| Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs. | 2008 Nov 27 |
|
| 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
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
SUBSTANCE RECORD
