lasmiditan Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antimigraine (5-HT1 receptor agonists) 5351 439239-90-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lasmiditan
  • lasmiditan succinate
  • COL-144
  • LY-573144
  • reyvow
Reyvow (lasmiditan) is a serotonin (5-HT) 1F receptor agonist for oral administration, bindinding with high affinity to the 5-HT1F receptor. Lasmiditan presumably exerts its therapeutic effects in the treatment of migraine through agonist effects at the 5-HT1F receptor; however, the precise mechanism is unknown.
  • Molecular weight: 377.37
  • Formula: C19H18F3N3O2
  • CLOGP: 1.98
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 62.30
  • ALOGS: -4.33
  • ROTB: 4

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Nov. 10, 2019 FDA ELI LILLY AND CO

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Dizziness 230.04 110.34 99 480 372160 52976327
Sedation 154.59 110.34 40 539 29635 53318852
Feeling abnormal 152.03 110.34 56 523 135245 53213242

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event

Pharmacologic Action:

SourceCodeDescription
ATC N02CC08 NERVOUS SYSTEM
ANALGESICS
ANTIMIGRAINE PREPARATIONS
Selective serotonin (5HT1) agonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018490 Serotonin Agents
MeSH PA D017366 Serotonin Receptor Agonists

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Migraine indication 37796009 DOID:6364

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.03 acidic
pKa2 9.43 Basic
pKa3 0.49 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 100MG BASE REYVOW ELI LILLY AND CO N211280 Jan. 31, 2020 RX TABLET ORAL 8748459 March 27, 2023 ACUTE TREATMENT OF MIGRAINE
EQ 200MG BASE REYVOW ELI LILLY AND CO N211280 Dec. 18, 2020 DISCN TABLET ORAL 8748459 March 27, 2023 ACUTE TREATMENT OF MIGRAINE
EQ 50MG BASE REYVOW ELI LILLY AND CO N211280 Jan. 31, 2020 RX TABLET ORAL 8748459 March 27, 2023 ACUTE TREATMENT OF MIGRAINE
EQ 100MG BASE REYVOW ELI LILLY AND CO N211280 Jan. 31, 2020 RX TABLET ORAL 7423050 April 6, 2025 ACUTE TREATMENT OF MIGRAINE
EQ 200MG BASE REYVOW ELI LILLY AND CO N211280 Dec. 18, 2020 DISCN TABLET ORAL 7423050 April 6, 2025 ACUTE TREATMENT OF MIGRAINE
EQ 50MG BASE REYVOW ELI LILLY AND CO N211280 Jan. 31, 2020 RX TABLET ORAL 7423050 April 6, 2025 ACUTE TREATMENT OF MIGRAINE
EQ 100MG BASE REYVOW ELI LILLY AND CO N211280 Jan. 31, 2020 RX TABLET ORAL 11053214 Dec. 5, 2037 ACUTE TREATMENT OF MIGRAINE
EQ 200MG BASE REYVOW ELI LILLY AND CO N211280 Dec. 18, 2020 DISCN TABLET ORAL 11053214 Dec. 5, 2037 ACUTE TREATMENT OF MIGRAINE
EQ 50MG BASE REYVOW ELI LILLY AND CO N211280 Jan. 31, 2020 RX TABLET ORAL 11053214 Dec. 5, 2037 ACUTE TREATMENT OF MIGRAINE

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 100MG BASE REYVOW ELI LILLY AND CO N211280 Jan. 31, 2020 RX TABLET ORAL Jan. 31, 2025 NEW CHEMICAL ENTITY
EQ 200MG BASE REYVOW ELI LILLY AND CO N211280 Dec. 18, 2020 DISCN TABLET ORAL Jan. 31, 2025 NEW CHEMICAL ENTITY
EQ 50MG BASE REYVOW ELI LILLY AND CO N211280 Jan. 31, 2020 RX TABLET ORAL Jan. 31, 2025 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
5-hydroxytryptamine receptor 1F GPCR AGONIST Ki 8.65 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
760I9WM792 UNII
439239-92-6 SECONDARY_CAS_RN
4039151 VANDF
C4519199 UMLSCUI
05X PDB_CHEM_ID
CHEMBL3039520 ChEMBL_ID
11610526 PUBCHEM_CID
DB11732 DRUGBANK_ID
CHEMBL3039526 ChEMBL_ID
D10338 KEGG_DRUG
C554777 MESH_SUPPLEMENTAL_RECORD_UI
3928 IUPHAR_LIGAND_ID
9176 INN_ID
2256930 RXNORM
823027003 SNOMEDCT_US
823028008 SNOMEDCT_US
325205 MMSL
d09395 MMSL
018168 NDDF
018169 NDDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Reyvow HUMAN PRESCRIPTION DRUG LABEL 1 0002-0265 TABLET 50 mg ORAL Export only 1 sections
Reyvow HUMAN PRESCRIPTION DRUG LABEL 1 0002-0632 TABLET 100 mg ORAL Export only 1 sections
Reyvow HUMAN PRESCRIPTION DRUG LABEL 1 0002-4312 TABLET 50 mg ORAL NDA 32 sections
Reyvow HUMAN PRESCRIPTION DRUG LABEL 1 0002-4491 TABLET 100 mg ORAL NDA 32 sections