Lasmiditan

Summary

Lasmiditan (CHEMBL3039520) is an approved small molecule (ATC N02CC08) targeting HTR1F; indicated across 2 conditions including migraine disorder and drug dependence.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N02CC08
• Targets: 1 (HTR1F)
• Indications: 2 conditions
• Clinical trials: 32
• Chemistry: 377.4 Da · C19H18F3N3O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3039520
Name	Lasmiditan
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	11610526
ATC	N02CC08
Molecular formula	C19H18F3N3O2
Molecular weight	377.4
InChIKey	XEDHVZKDSYZQBF-UHFFFAOYSA-N

SMILES: CN1CCC(CC1)C(=O)C2=NC(=CC=C2)NC(=O)C3=C(C=C(C=C3F)F)F

IUPAC name: 2,4,6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-2-pyridinyl]benzamide

Also known as: COL-144, Lasmiditan, LY573144, LASMIDITAN, Lasmiditan (hydrochloride)

Parent form; salt/anhydrous children: CHEMBL3039526

Patent coverage: 218 distinct patent families (550 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 399 (73%) 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).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
HTR1F	5-HT1F receptor	Full agonist	8.7	0.1%	P30939

Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: 5-hydroxytryptamine receptor 1F, D(1B) dopamine receptor, 5-hydroxytryptamine receptor 1D, Muscarinic acetylcholine receptor M5, 5-hydroxytryptamine receptor 1E, Kappa-type opioid receptor, Sigma non-opioid intracellular receptor 1, 5-hydroxytryptamine receptor 7, Sigma intracellular receptor 2.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
HTR1F	8.66	Ki	2.21	nM	CHEMBL_ACT_24710356
HTR1F	7.06	IC50	87.84	nM	CHEMBL_ACT_23248392
HTR1E	6.9	Ki	126.9	nM	CHEMBL_ACT_25741610
TMEM97	6.74	Ki	184.1	nM	CHEMBL_ACT_25741614
DRD5	6.6	Ki	252.7	nM	CHEMBL_ACT_25741608
OPRK1	6.45	Ki	356.6	nM	CHEMBL_ACT_25741612
CHRM5	6.2	Ki	632	nM	CHEMBL_ACT_25741607
HTR1D	6.06	Ki	869.4	nM	CHEMBL_ACT_25741609
SIGMAR1	5.5	Ki	3133	nM	CHEMBL_ACT_25741613
HTR7	5.27	Ki	5407	nM	CHEMBL_ACT_25741611

Target pathways

Aggregated over 1 target gene(s): HTR1F.

Top Reactome pathways

8 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	1	HTR1F
Signaling by GPCR	1	HTR1F
Class A/1 (Rhodopsin-like receptors)	1	HTR1F
Amine ligand-binding receptors	1	HTR1F
GPCR downstream signalling	1	HTR1F
Serotonin receptors	1	HTR1F
G alpha (i) signalling events	1	HTR1F
GPCR ligand binding	1	HTR1F

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	1
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	1
adenylate cyclase-inhibiting serotonin receptor signaling pathway	1
chemical synaptic transmission	1
signal transduction	1
G protein-coupled receptor signaling pathway	1
adenylate cyclase-activating G protein-coupled receptor signaling pathway	1

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).

Indication	Trial phase	MONDO	EFO
migraine disorder	4	MONDO:0005277	MONDO:0005277
drug dependence	1	MONDO:0005303	EFO:0003890

Clinical trials

Total trials: 32.

Phase distribution

Phase	Trials
PHASE1	21
PHASE3	7
PHASE2	3
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02439320	PHASE3	COMPLETED	Lasmiditan Compared to Placebo in the Acute Treatment of Migraine:
NCT02565186	PHASE3	COMPLETED	An Open-label, Long-term, Safety Study of Lasmiditan for the Acute Treatment of Migraine
NCT02605174	PHASE3	COMPLETED	Three Doses of Lasmiditan (50 mg, 100 mg and 200 mg) Compared to Placebo in the Acute Treatment of Migraine
NCT03670810	PHASE3	COMPLETED	A Study of Lasmiditan (LY573144) Over Four Migraine Attacks
NCT04218162	PHASE3	COMPLETED	Lasmiditan Compared to Placebo in the Acute Treatment of Migraine in Korean
NCT04396236	PHASE3	TERMINATED	A Study of Lasmiditan (LY573144) Treatment in Children Aged 6 to 17 With Migraine
NCT04396574	PHASE3	TERMINATED	A 12-Month Study of Lasmiditan (LY573144) Treatment in Children Aged 6 to 17 With Migraine
NCT00384774	PHASE2	COMPLETED	A Placebo-Controlled Adaptive Treatment Assignment Study of Intravenous COL-144 in the Acute Treatment of Migraine
NCT00883051	PHASE2	COMPLETED	Dose-ranging Study of Oral COL-144 in Acute Migraine Treatment
NCT03962738	PHASE2	COMPLETED	A Study Lasmiditan (LY573144) in a Single Migraine Attack in Japanese Participants With Migraine
NCT02233296	PHASE1	COMPLETED	Food-Effect Study in Healthy Participants
NCT03009162	PHASE1	COMPLETED	Study of Oral Lasmiditan in Participants With Normal and Impaired Renal Function
NCT03012334	PHASE1	COMPLETED	The Effects of Lasmiditan on Simulated Driving Performance - Healthy Participants
NCT03040479	PHASE1	COMPLETED	Pharmacokinetic Single Dose Study of Oral Lasmiditan in Participants With Normal and Impaired Hepatic Function
NCT03076970	PHASE1	COMPLETED	Effect of Single Oral Doses of Lasmiditan When Coadministered With Single Oral Doses of Sumatriptan in Healthy Participants
NCT03182920	PHASE1	COMPLETED	A Study of Lasmiditan in Healthy Participants
NCT03247790	PHASE1	COMPLETED	A Study of Lasmiditan in Participants With Migraine
NCT03252015	PHASE1	COMPLETED	A Study of Multiple Doses of Lasmiditan in Healthy Participants
NCT03270644	PHASE1	COMPLETED	A Study of Lasmiditan and Propranolol in Healthy Participants
NCT03286218	PHASE1	COMPLETED	A Study of the Abuse Potential of Lasmiditan in Participants Who Are Recreational Drug Users
NCT03308669	PHASE1	COMPLETED	A Study of Lasmiditan in Healthy Participants When Co-administered With Topiramate
NCT03310411	PHASE1	COMPLETED	A Study of Lasmiditan When Given With Sumatriptan in Healthy Participants
NCT03406260	PHASE1	COMPLETED	A Study of Lasmiditan in Healthy Elderly Participants
NCT03459612	PHASE1	COMPLETED	A Study of Lasmiditan on Simulated Driving Performance in Healthy Participants
NCT03465436	PHASE1	COMPLETED	A Study of Lasmiditan on the Heart in Healthy Participants
NCT03579940	PHASE1	COMPLETED	A Study of Lasmiditan in Healthy Japanese and Caucasian Participants
NCT03937648	PHASE1	UNKNOWN	Study to Evaluate Pharmacokinetics, Safety, and Tolerability Ildong COL-144 Tablet in Korean Healthy Volunteers
NCT03988088	PHASE1	COMPLETED	A Study of Lasmiditan (LY573144) in Children Aged 6 to 17 With Migraine
NCT04081324	PHASE1	COMPLETED	A Study of Lasmiditan in Healthy Chinese Participants
NCT04749914	PHASE1	COMPLETED	A Study of Lasmiditan in Healthy Volunteers
NCT04881747	PHASE1	COMPLETED	A Study to Compare Two Different Formulations of Lasmiditan in Healthy Participants
NCT05903040	Not specified	COMPLETED	Ditan Acute tReatments: Effectiveness and Tolerability (DART)

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.

Related molecules

Related molecules

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.

18 molecules share ≥1 primary target. Top 18 by shared-target count:

Molecule	Source	Status	Shared targets
IMIPRAMINE	ChEMBL + PubChem	Phase 4 (approved)	HTR1F
SUMATRIPTAN	ChEMBL + PubChem	Phase 4 (approved)	HTR1F
SEROTONIN	ChEMBL + PubChem	Phase 3 (approved)	HTR1F
MEBUFOTENIN	ChEMBL	Phase 2	HTR1F
Clozapine	PubChem	Approved	HTR1F
Cyproheptadine	PubChem	Approved	HTR1F
Dihydroergotamine	PubChem	Approved	HTR1F
Eletriptan	PubChem	Approved	HTR1F
Ergotamine	PubChem	Approved	HTR1F
methylergonovine	PubChem	Approved	HTR1F
Naratriptan	PubChem	Approved	HTR1F
Olanzapine	PubChem	Approved	HTR1F
Quetiapine	PubChem	Approved	HTR1F
Risperidone	PubChem	Approved	HTR1F
Rizatriptan	PubChem	Approved	HTR1F
Sorafenib	PubChem	Approved	HTR1F
Yohimbine	PubChem	Approved	HTR1F
Zolmitriptan	PubChem	Approved	HTR1F