Mitoglitazone

pharmacological · endocrine · nervous · Oral

Mitoglitazone. A thiazolidinedione-derived insulin sensitiser that acts on the mitochondrial pyruvate carrier — the "mitochondrial target of thiazolidinediones"…

A thiazolidinedione-derived insulin sensitiser that acts on the mitochondrial pyruvate carrier — the "mitochondrial target of thiazolidinediones" (mTOT) — rather than by activating PPAR-gamma, which is the stated basis for lowering glucose comparably to pioglitazone with less fluid retention. PMID:27928028 used it as the tool compound for that target: verbatim, "To test this, we used MSDC-0160, a compound that specifically targets MPC, to reduce its activity", and "Targeting MPC in multiple models resulted in modulation of mitochondrial function and mTOR signaling, with normalization of autophagy and a reduction in glial cell activation." Its own trial describes it as "an mTOT modulator" (PMID:23462886). NO RECEPTOR-OCCUPANCY MECHANISM AND NO BINDING CONSTANT IS PUBLISHED.

PubChem CID 10429242 under both `mitoglitazone` and `MSDC-0160` (C19H18N2O4S, 370.4), re-queried 2026-09-26. DOSES are verbatim from the two human trials, in both of which the compound is the subject. Type 2 diabetes, phase IIb, 12 weeks, steady state (PMID:23462886): "258 patients with type 2 diabetes completed a 12-week protocol with 50, 100, or 150 mg of MSDC-0160 (an mTOT modulator), 45 mg pioglitazone HCl (a PPAR-gamma agonist), or a placebo." Mild Alzheimer's disease, 12 weeks (PMID:24931567): "MSDC-0160 (150 mg once daily; N=16) compared to placebo (N=13) for 12 weeks did not result in a significant difference in glucose metabolism in pre-defined regions when referenced to the pons or whole brain." THE ROUTE IS AN INFERENCE, NOT A CITATION, and is flagged as such: neither abstract writes "oral" or "PO" anywhere. The dose form, the once-daily outpatient schedule over 12 weeks and the oral pioglitazone comparator all imply it, but PO here is this record's reasoning and not something either paper states. A CITATION DELIBERATELY NOT MADE: PMID:23690925 is the paper that identifies mTOT as Mpc1/Mpc2, but it never mentions MSDC-0160 — the agent it names is MSDC-0602. Citing it for THIS compound would be a textbook R2 secondary citation, so the mTOT claim here is taken from the compound's own trial and from PMID:27928028 instead. Also checked and rejected for numbers: PMID:41519796 (mouse/in-vitro osteoclast), PMID:35895232 (rat PD model), PMID:37755339 (review).

Sources: PMID:23462886, PMID:24931567, PMID:27928028