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Resmetirom

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Also known as Mgl-3196RezdiffraVIA-3196Resmetriom

Summary

Resmetirom (CHEMBL3261331) is an approved small molecule targeting THRA and THRB; indicated across 6 conditions including metabolic dysfunction-associated steatotic liver disease and metabolic dysfunction-associated steatohepatitis.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • Targets: 2 (THRA, THRB)
  • Indications: 6 conditions
  • Clinical trials: 21
  • Chemistry: 435.2 Da · C17H12Cl2N6O4

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL3261331
NameResmetirom
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID15981237
Molecular formulaC17H12Cl2N6O4
Molecular weight435.2
InChIKeyFDBYIYFVSAHJLY-UHFFFAOYSA-N

SMILES: CC(C)C1=CC(=NNC1=O)OC2=C(C=C(C=C2Cl)N3C(=O)NC(=O)C(=N3)C#N)Cl

IUPAC name: 2-[3,5-dichloro-4-[(6-oxo-5-propan-2-yl-1H-pyridazin-3-yl)oxy]phenyl]-3,5-dioxo-1,2,4-triazine-6-carbonitrile

Also known as: Mgl-3196, MGL-3196, Resmetirom, Rezdiffra, VIA-3196, RESMETIROM, resmetirom, Resmetriom

Patent coverage: 497 distinct patent families (1,315 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
THRAThyroid hormone receptor-αAgonist5.431.7%P10827
THRBThyroid hormone receptor-βAgonist6.680%P10828

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Thyroid hormone receptor alpha, Thyroid hormone receptor beta, Cytochrome P450 2C9, Cytochrome P450 2C8.

Bioactivity

ChEMBL activities: 13 potent at pChembl ≥ 5 of 14 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
THRB7.14EC5073nMCHEMBL_ACT_26051822
THRB6.78EC50167.1nMCHEMBL_ACT_24922608
THRB6.7EC50200nMCHEMBL_ACT_26335907
THRB6.68EC50210nMCHEMBL_ACT_14658935
THRB6.68EC50210nMCHEMBL_ACT_29165391
CYP2C86.05IC50900nMCHEMBL_ACT_26051912
THRA6.03EC50934nMCHEMBL_ACT_26051796
THRB6EC50990nMCHEMBL_ACT_25062823
THRB5.62EC502370nMCHEMBL_ACT_26051864
THRA5.56EC502735nMCHEMBL_ACT_24922573
THRA5.54EC502850nMCHEMBL_ACT_25062803
THRA5.43EC503740nMCHEMBL_ACT_14658969
THRA5.23EC505930nMCHEMBL_ACT_26051858

Target pathways

Aggregated over 2 target gene(s): THRA, THRB.

Top Reactome pathways

9 total, by targets touching each:

PathwayTargetsGenes
Generic Transcription Pathway2THRA, THRB
Nuclear Receptor transcription pathway2THRA, THRB
SUMOylation of intracellular receptors2THRA, THRB
RNA Polymerase II Transcription2THRA, THRB
Gene expression (Transcription)2THRA, THRB
SUMOylation1THRB
SUMO E3 ligases SUMOylate target proteins1THRB
Metabolism of proteins1THRB
Post-translational protein modification1THRB

Dominant GO biological processes

GO termTargets
negative regulation of transcription by RNA polymerase II2
thyroid hormone receptor signaling pathway2
positive regulation of thyroid hormone receptor signaling pathway2
regulation of transcription by RNA polymerase II2
regulation of heart contraction2
female courtship behavior2
cell differentiation2
mRNA transcription by RNA polymerase II2
negative regulation of DNA-templated transcription2
positive regulation of transcription by RNA polymerase II2
retinoic acid receptor signaling pathway2
type I pneumocyte differentiation2
regulation of DNA-templated transcription2
animal organ morphogenesis2
intracellular receptor signaling pathway2

Indications & clinical

Indications

6 indications (3 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
metabolic dysfunction-associated steatotic liver disease4MONDO:0013209EFO:0003095
metabolic dysfunction-associated steatohepatitis4MONDO:0007027EFO:1001249
familial hypercholesterolemia2MONDO:0005439EFO:0004911

3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 21.

Phase distribution

PhaseTrials
PHASE111
PHASE34
PHASE24
PHASE41
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT07249788PHASE4RECRUITINGResmiterom Efficacy & Safety in Patients With MASH
NCT03900429PHASE3ACTIVE_NOT_RECRUITINGA Phase 3 Study to Evaluate the Efficacy and Safety of MGL-3196 (Resmetirom) in Patients With NASH and Fibrosis
NCT04951219PHASE3ACTIVE_NOT_RECRUITINGA Phase 3 Study to Evaluate Safety and Biomarkers of Resmetirom (MGL-3196) in Patients With Non-alcoholic Fatty Liver Disease (NAFLD), MAESTRO-NAFLD-Open-Label-Extension (MAESTRO-NAFLD-OLE)
NCT05500222PHASE3ACTIVE_NOT_RECRUITINGA Phase 3 Study to Evaluate the Effect of Resmetirom on Clinical Outcomes in Patients With Well-compensated NASH Cirrhosis (MAESTRO-NASH-OUTCOMES)
NCT04197479PHASE3COMPLETEDA Phase 3 Study to Evaluate Safety and Biomarkers of Resmetirom (MGL-3196) in Non Alcoholic Fatty Liver Disease Patients
NCT07143968PHASE2RECRUITINGA Study to Evaluate the Use of Resmetirom in Participants With MASLD and HIV
NCT07335601PHASE2RECRUITINGStudy to Evaluate Resmetirom in Post-Liver Transplant Patients With MASH
NCT02912260PHASE2COMPLETEDPhase 2 Study of MGL-3196 in Patients With Non-Alcoholic Steatohepatitis (NASH)
NCT03038022PHASE2COMPLETEDStudy of MGL-3196 in Patients With Heterozygous Familial Hypercholesterolemia (HeFH)
NCT01367873PHASE1COMPLETEDAscending Single-Dose Study to Evaluate VIA-3196 in Healthy Subjects
NCT01519531PHASE1COMPLETEDAscending Multiple-Dose Study to Evaluate VIA-3196 in Healthy Subjects
NCT02542969PHASE1COMPLETEDDrug Interaction Study of MGL-3196 With Rosuvastatin and Simvastatin
NCT02749578PHASE1COMPLETEDDrug Interaction Study of MGL-3196 With Atorvastatin
NCT03220165PHASE1COMPLETEDRadiolabeled Study to Determine the Mass Balance of [14C] MGL-3196
NCT03413124PHASE1COMPLETEDBioavailability Study of MGL-3196 Tablets Compared to Capsules
NCT04643795PHASE1COMPLETEDPhase 1 Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of Multiple Oral Doses of MGL-3196 in Subjects With Varying Degrees of Hepatic Impairment and Healthy Matched Control Subjects
NCT04671056PHASE1COMPLETEDDrug Interaction Study of MGL-3196 With Pioglitazone
NCT04671069PHASE1COMPLETEDDrug Interaction Study of MGL-3196 With Clopidogrel
NCT06397872PHASE1COMPLETEDA Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of Multiple Oral Doses (6 Days) of 100 mg Resmetirom in Subjects With Severe Renal Impairment and in Matched Healthy Control Subjects With Normal Renal Function
NCT07216313PHASE1COMPLETEDA Drug-Drug Interaction Study of Denifanstat and Resmetirom in Healthy Adult Participants
NCT07541469Not specifiedRECRUITINGRezdiffra Pregnancy and Lactation Registry

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

112 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
AMIODARONEChEMBL + PubChemPhase 4 (approved)THRA, THRB
LIOTHYRONINEChEMBL + PubChemPhase 4 (approved)THRA, THRB
LEVOTHYROXINEChEMBLPhase 4 (approved)THRA, THRB
ROXADUSTATChEMBLPhase 4 (approved)THRA, THRB
EPROTIROMEChEMBLPhase 3THRA, THRB
TIRATRICOLChEMBLPhase 3THRA, THRB
AXITIROMEChEMBLPhase 2THRA, THRB
DETROTHYRONINEChEMBLPhase 2THRA, THRB
MB07811ChEMBLPhase 2THRA, THRB
SOBETIROMEChEMBLPhase 2THRA, THRB
THYROPROPIC ACIDChEMBLPhase 2THRA, THRB
ACETAZOLAMIDEChEMBLPhase 4 (approved)THRB
ACETOHEXAMIDEChEMBLPhase 4 (approved)THRB
ACETYLCYSTEINEChEMBLPhase 4 (approved)THRB
ALTRETAMINEChEMBLPhase 4 (approved)THRB
AMANTADINEChEMBLPhase 4 (approved)THRB
AMILORIDEChEMBLPhase 4 (approved)THRB
AMINOCAPROIC ACIDChEMBLPhase 4 (approved)THRB
AMINOPYRINEChEMBLPhase 4 (approved)THRB
AMOXAPINEChEMBLPhase 4 (approved)THRB
ATORVASTATINChEMBLPhase 4 (approved)THRB
AZARIBINEChEMBLPhase 4 (approved)THRB
BENZBROMARONEChEMBLPhase 4 (approved)THRB
BISOPROLOLChEMBLPhase 4 (approved)THRB
BITHIONOLChEMBLPhase 4 (approved)THRB
CARBETAPENTANEChEMBLPhase 4 (approved)THRB
CHLORMADINONEChEMBLPhase 4 (approved)THRB
CHLORMEZANONEChEMBLPhase 4 (approved)THRB
CHLORPROPAMIDEChEMBLPhase 4 (approved)THRB
CLOMIPRAMINEChEMBLPhase 4 (approved)THRB
CYCLOTHIAZIDEChEMBLPhase 4 (approved)THRB
CYTARABINEChEMBLPhase 4 (approved)THRB
DAUNORUBICINChEMBLPhase 4 (approved)THRB
DEBRISOQUINChEMBLPhase 4 (approved)THRB
DEXTROTHYROXINEChEMBLPhase 4 (approved)THRB
DIAZOXIDEChEMBLPhase 4 (approved)THRB
DILTIAZEMChEMBLPhase 4 (approved)THRB
DIPYRIDAMOLEChEMBLPhase 4 (approved)THRB
DISOPYRAMIDEChEMBLPhase 4 (approved)THRB
DITHIAZANINE IODIDEChEMBLPhase 4 (approved)THRB
DOXORUBICINChEMBLPhase 4 (approved)THRB
DYCLONINEChEMBLPhase 4 (approved)THRB
GENTIAN VIOLETChEMBLPhase 4 (approved)THRB
HEXACHLOROPHENEChEMBLPhase 4 (approved)THRB
HYDROCHLOROTHIAZIDEChEMBLPhase 4 (approved)THRB
IDARUBICINChEMBLPhase 4 (approved)THRB
INAMRINONEChEMBLPhase 4 (approved)THRB
INDIGOTINDISULFONATEChEMBLPhase 4 (approved)THRB
ISOSORBIDEChEMBLPhase 4 (approved)THRB
ISOTRETINOINChEMBLPhase 4 (approved)THRB
LEFLUNOMIDEChEMBLPhase 4 (approved)THRB
MECLOFENAMATEChEMBLPhase 4 (approved)THRB
MESALAMINEChEMBLPhase 4 (approved)THRB
METHACYCLINEChEMBLPhase 4 (approved)THRB
METHYLENE BLUEChEMBLPhase 4 (approved)THRB
METHYLENE BLUE CATIONChEMBLPhase 4 (approved)THRB
METHYSERGIDEChEMBLPhase 4 (approved)THRB
METRONIDAZOLEChEMBLPhase 4 (approved)THRB
MOLSIDOMINEChEMBLPhase 4 (approved)THRB
OXYTETRACYCLINEChEMBLPhase 4 (approved)THRB

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot