Sarizotan

drug
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Also known as EMD-77697

Summary

Sarizotan (CHEMBL220808) is a phase-3 clinical-stage small molecule; indicated across 2 conditions including movement disorder and rett syndrome.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Indications: 2 conditions
  • Clinical trials: 3
  • Chemistry: 348.4 Da · C22H21FN2O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL220808
NameSarizotan
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID6918388
Molecular formulaC22H21FN2O
Molecular weight348.4
InChIKeyHKFMQJUJWSFOLY-OAQYLSRUSA-N

SMILES: C1CC2=CC=CC=C2O[C@H]1CNCC3=CC(=CN=C3)C4=CC=C(C=C4)F

IUPAC name: 1-[(2R)-3,4-dihydro-2H-chromen-2-yl]-N-[[5-(4-fluorophenyl)-3-pyridinyl]methyl]methanamine

Also known as: EMD-77697, Sarizotan, SARIZOTAN

Parent form; salt/anhydrous children: CHEMBL2146110

Patent coverage: 443 distinct patent families (1,853 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,846 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: 5-hydroxytryptamine receptor 1A, 5-hydroxytryptamine receptor 1A, 5-hydroxytryptamine receptor 2A, D(2) dopamine receptor.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 4 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
P193278.65Ki2.24nMCHEMBL_ACT_1818590
P611697.72Ki19.05nMCHEMBL_ACT_1818633
HTR1A7.11EC5077.62nMCHEMBL_ACT_1818655
P148425.67Ki2138nMCHEMBL_ACT_1818611

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

2 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)PhaseMONDOEFO
movement disorder3MONDO:0005395EFO:0004280
Rett syndrome2MONDO:0010726MONDO:0010726

Clinical trials

Total trials: 3.

Phase distribution

PhaseTrials
PHASE32
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00105508PHASE3COMPLETEDSarizotan HC1 in Patients With Parkinson’s Disease Suffering From Treatment-associated Dyskinesia
NCT00105521PHASE3COMPLETEDSarizotan in Participants With Parkinson’s Disease Suffering From Treatment Associated Dyskinesia
NCT00310661Not specifiedTERMINATEDSarizotan in the Treatment of Neuroleptic-induced Tardive Dyskinesia

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).