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Frovatriptan

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Also known as Allergo filmtablettenMigardMylatrip

Summary

Frovatriptan (CHEMBL1279) is an approved small molecule (ATC N02CC07) targeting HTR1A, HTR1B, and HTR1D; indicated across 2 conditions including migraine disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: N02CC07
  • Targets: 3 (HTR1A, HTR1B, HTR1D)
  • Indications: 2 conditions
  • Clinical trials: 8
  • Chemistry: 243.3 Da · C14H17N3O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1279
NameFrovatriptan
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID77992
ATCN02CC07
Molecular formulaC14H17N3O
Molecular weight243.3
InChIKeyXPSQPHWEGNHMSK-SECBINFHSA-N

SMILES: CN[C@@H]1CCC2=C(C1)C3=C(N2)C=CC(=C3)C(=O)N

IUPAC name: (6R)-6-(methylamino)-6,7,8,9-tetrahydro-5H-carbazole-3-carboxamide

Also known as: Allergo filmtabletten, Frovatriptan, Migard, Mylatrip, frovatriptan, FROVATRIPTAN

Parent form; salt/anhydrous children: CHEMBL1200371, CHEMBL2138684

Patent coverage: 1,894 distinct patent families (7,695 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 7,653 (99%) 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

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
HTR1A5-HT1A receptorAgonist7.220%P08908
HTR1B5-HT1B receptorAgonist7.990.2%P28222
HTR1D5-HT1D receptorAgonist8.360%P28221

Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: 5-hydroxytryptamine receptor 1B, 5-hydroxytryptamine receptor 1D, 5-hydroxytryptamine receptor 1A.

Bioactivity

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

TargetpChemblTypeValueUnitActivity ID
HTR1B8.36Ki4.4nMCHEMBL_ACT_25553870
HTR1D8.36Ki4.4nMCHEMBL_ACT_25553875
HTR1D8.36Ki4.4nMCHEMBL_ACT_784951
HTR1B7.99Ki10.3nMCHEMBL_ACT_784953
HTR1A7.21Ki62nMCHEMBL_ACT_784952

Target pathways

Aggregated over 3 target gene(s): HTR1A, HTR1B, HTR1D.

Top Reactome pathways

8 total, by targets touching each:

PathwayTargetsGenes
Signal Transduction3HTR1A, HTR1B, HTR1D
Signaling by GPCR3HTR1A, HTR1B, HTR1D
Class A/1 (Rhodopsin-like receptors)3HTR1A, HTR1B, HTR1D
Amine ligand-binding receptors3HTR1A, HTR1B, HTR1D
Serotonin receptors3HTR1A, HTR1B, HTR1D
GPCR ligand binding3HTR1A, HTR1B, HTR1D
GPCR downstream signalling2HTR1B, HTR1D
G alpha (i) signalling events2HTR1B, HTR1D

Dominant GO biological processes

GO termTargets
G protein-coupled receptor signaling pathway3
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger3
adenylate cyclase-inhibiting serotonin receptor signaling pathway3
chemical synaptic transmission3
regulation of behavior3
signal transduction3
adenylate cyclase-activating G protein-coupled receptor signaling pathway2
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway2
vasoconstriction2
behavioral fear response1
serotonin receptor signaling pathway1
gamma-aminobutyric acid signaling pathway1
positive regulation of cell population proliferation1
regulation of serotonin secretion1
regulation of vasoconstriction1

Indications & clinical

Indications

2 indications (1 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
migraine disorder4MONDO:0005277MONDO:0005277

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

Clinical trials

Total trials: 8.

Phase distribution

PhaseTrials
PHASE33
PHASE42
Not specified2
PHASE21

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00846495PHASE4COMPLETEDPilot Study to Compare Frovatriptan vs. Topiramate for Prevention of Migraine
NCT00904098PHASE4COMPLETEDEffectiveness And Safety Of Frovatriptan For The Management (Acute Treatment) Of Menstrual Migraine
NCT00644033PHASE3COMPLETEDA Randomized Trial of Frovatriptan for the Intermittent Prevention of Menstrual Migraine
NCT00821483PHASE3COMPLETEDA Double Blind Placebo-controlled, Parallel Group Study to Assess the Efficacy and Safety of Frovatriptan in the Acute Treatment of Migraine
NCT01035983PHASE3COMPLETEDSafety and Tolerability of Frovatriptan to Prevention of Menstrually Associated Migraine (MAM) Headaches
NCT01044251PHASE2COMPLETEDFrovatriptan as a Transitional Therapy in Medication Overuse Headache
NCT00440232Not specifiedCOMPLETEDA Research Study To Evaluate If Frovatriptan Is Safe And Effective In Preventing Migraine Headache After Fasting
NCT00700128Not specifiedCOMPLETEDPrevention of Menstrual Migraines: Using Frovatriptan or Placebo During Hormone Free Intervals

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 7 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

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

MoleculeSourceStatusShared targets
DIHYDROERGOTAMINEChEMBL + PubChemPhase 4 (approved)HTR1A, HTR1B, HTR1D
ARIPIPRAZOLEChEMBLPhase 4 (approved)HTR1A, HTR1B, HTR1D
BREXPIPRAZOLEChEMBLPhase 4 (approved)HTR1A, HTR1B, HTR1D
CARIPRAZINEChEMBLPhase 4 (approved)HTR1A, HTR1B, HTR1D
ERGOTAMINEChEMBLPhase 4 (approved)HTR1A, HTR1B, HTR1D
IMIPRAMINEChEMBLPhase 4 (approved)HTR1A, HTR1B, HTR1D
KETANSERINChEMBLPhase 4 (approved)HTR1A, HTR1B, HTR1D
NARATRIPTANChEMBLPhase 4 (approved)HTR1A, HTR1B, HTR1D
NEFAZODONEChEMBLPhase 4 (approved)HTR1A, HTR1B, HTR1D
OXYMETAZOLINEChEMBLPhase 4 (approved)HTR1A, HTR1B, HTR1D
RISPERIDONEChEMBLPhase 4 (approved)HTR1A, HTR1B, HTR1D
RIZATRIPTANChEMBLPhase 4 (approved)HTR1A, HTR1B, HTR1D
SALMETEROLChEMBLPhase 4 (approved)HTR1A, HTR1B, HTR1D
SILODOSINChEMBLPhase 4 (approved)HTR1A, HTR1B, HTR1D
SUMATRIPTANChEMBLPhase 4 (approved)HTR1A, HTR1B, HTR1D
VILAZODONEChEMBLPhase 4 (approved)HTR1A, HTR1B, HTR1D
XYLOMETAZOLINEChEMBLPhase 4 (approved)HTR1A, HTR1B, HTR1D
ZOLMITRIPTANChEMBLPhase 4 (approved)HTR1A, HTR1B, HTR1D
SEROTONINChEMBLPhase 3HTR1A, HTR1B, HTR1D
YOHIMBINEChEMBLPhase 3HTR1A, HTR1B, HTR1D
ACETRYPTINEChEMBLPhase 2HTR1A, HTR1B, HTR1D
GSK163090ChEMBLPhase 2HTR1A, HTR1B, HTR1D
MEBUFOTENINChEMBLPhase 2HTR1A, HTR1B, HTR1D
PSILOCINChEMBLPhase 2HTR1A, HTR1B, HTR1D
PALIPERIDONEChEMBL + PubChemPhase 4 (approved)HTR1B, HTR1D
AZELASTINEChEMBLPhase 4 (approved)HTR1B, HTR1D
CINACALCETChEMBLPhase 4 (approved)HTR1A, HTR1D
CLOZAPINEChEMBLPhase 4 (approved)HTR1A, HTR1B
ELETRIPTANChEMBLPhase 4 (approved)HTR1A, HTR1B
LOPERAMIDEChEMBLPhase 4 (approved)HTR1A, HTR1D
MIANSERINChEMBLPhase 4 (approved)HTR1A, HTR1D
OLANZAPINEChEMBLPhase 4 (approved)HTR1A, HTR1B
PINDOLOLChEMBLPhase 4 (approved)HTR1A, HTR1B
PRAMIPEXOLEChEMBLPhase 4 (approved)HTR1A, HTR1B
PRAZOSINChEMBLPhase 4 (approved)HTR1A, HTR1D
SERTINDOLEChEMBLPhase 4 (approved)HTR1A, HTR1B
TEGASERODChEMBLPhase 4 (approved)HTR1A, HTR1D
ALNIDITANChEMBLPhase 2HTR1A, HTR1D
LYSERGIDEChEMBLPhase 2HTR1A, HTR1D
MAZAPERTINEChEMBLPhase 2HTR1A, HTR1B
NIGULDIPINEChEMBLPhase 2HTR1A, HTR1B
PENFLURIDOLChEMBLPhase 2HTR1A, HTR1D
RITANSERINChEMBLPhase 2HTR1A, HTR1B
SPIRAMIDEChEMBLPhase 2HTR1A, HTR1D
LASMIDITANChEMBL + PubChemPhase 4 (approved)HTR1D
ACEMETACINChEMBLPhase 4 (approved)HTR1A
ACETOPHENAZINEChEMBLPhase 4 (approved)HTR1A
ACETYLCHOLINEChEMBLPhase 4 (approved)HTR1A
ALMOTRIPTANChEMBLPhase 4 (approved)HTR1A
AMILORIDEChEMBLPhase 4 (approved)HTR1A
AMITRIPTYLINEChEMBLPhase 4 (approved)HTR1A
AMLODIPINEChEMBLPhase 4 (approved)HTR1A
AMODIAQUINEChEMBLPhase 4 (approved)HTR1A
AMOXAPINEChEMBLPhase 4 (approved)HTR1A
ANTAZOLINEChEMBLPhase 4 (approved)HTR1A
APOMORPHINEChEMBLPhase 4 (approved)HTR1A
ARTICAINEChEMBLPhase 4 (approved)HTR1A
ASENAPINEChEMBLPhase 4 (approved)HTR1A
ASTEMIZOLEChEMBLPhase 4 (approved)HTR1A
AZATADINEChEMBLPhase 4 (approved)HTR1A

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