Tradipitant

Summary

Tradipitant (CHEMBL3544984) is a phase-3 clinical-stage small molecule targeting TACR1; indicated across 8 conditions including atopic eczema and gastroparesis.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (TACR1)
• Indications: 8 conditions
• Clinical trials: 22
• Chemistry: 587.9 Da · C28H16ClF6N5O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3544984
Name	Tradipitant
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	9916461
Molecular formula	C28H16ClF6N5O
Molecular weight	587.9
InChIKey	CAVRKWRKTNINFF-UHFFFAOYSA-N

SMILES: C1=CC=C(C(=C1)C(=O)C2=C(N=CC=C2)C3=C(N(N=N3)CC4=CC(=CC(=C4)C(F)(F)F)C(F)(F)F)C5=CC=NC=C5)Cl

IUPAC name: [2-[1-[[3,5-bis(trifluoromethyl)phenyl]methyl]-5-pyridin-4-yltriazol-4-yl]-3-pyridinyl]-(2-chlorophenyl)methanone

Also known as: LY-686017, Ly686017, LY686017, Tradipitant, VLY-686, TRADIPITANT

Patent coverage: 137 distinct patent families (396 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 380 (96%) 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
TACR1	NK1 receptor	Antagonist	7	0.7%	P25103

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 1 target gene(s): TACR1.

Top Reactome pathways

4 total, by targets touching each:

Pathway	Targets	Genes
Tachykinin receptors bind tachykinins	1	TACR1
G alpha (q) signalling events	1	TACR1
Cargo recognition for clathrin-mediated endocytosis	1	TACR1
Clathrin-mediated endocytosis	1	TACR1

Dominant GO biological processes

GO term	Targets
aggressive behavior	1
positive regulation of leukocyte migration	1
angiotensin-mediated drinking behavior	1
inflammatory response	1
adenylate cyclase-activating G protein-coupled receptor signaling pathway	1
phospholipase C-activating G protein-coupled receptor signaling pathway	1
positive regulation of cytosolic calcium ion concentration	1
phospholipase C-activating tachykinin receptor signaling pathway	1
tachykinin receptor signaling pathway	1
long-term memory	1
associative learning	1
detection of abiotic stimulus	1
response to ozone	1
positive regulation of epithelial cell migration	1
response to auditory stimulus	1

Indications & clinical

Indications

8 indications (0 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
atopic eczema	3	MONDO:0004980	EFO:0000274
gastroparesis	3	MONDO:0006769	EFO:1000948
motion sickness	3	MONDO:0008015	EFO:0006928
severe acute respiratory syndrome	3	MONDO:0005091	MONDO:0100096
social phobia	2	MONDO:0001247	EFO:1001917
alcohol abuse	2	MONDO:0002046	MONDO:0007079
dyspepsia	2	MONDO:0002268	EFO:0008533

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

Clinical trials

Total trials: 22.

Phase distribution

Phase	Trials
PHASE3	9
PHASE2	9
PHASE1	2
PHASE1/PHASE2	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04326426	PHASE3	ENROLLING_BY_INVITATION	ODYSSEY: A Study to Investigate the Efficacy of Tradipitant in Treating Severe or Critical COVID-19 Infection
NCT06138613	PHASE3	ACTIVE_NOT_RECRUITING	Motion Delos: An Open Label Safety and Efficacy of Tradipitant in Participants Affected by Motion Sickness
NCT06836557	PHASE3	RECRUITING	Open Label Safety Study of Tradipitant in Idiopathic and Diabetic Gastroparesis
NCT07446439	PHASE3	RECRUITING	A Study to Evaluate Tradipitant on Treating Nausea and Vomiting Induced by GLP-1R Agonist Use
NCT03568331	PHASE3	COMPLETED	Evaluating the Effects of Tradipitant vs. Placebo in Atopic Dermatitis (EPIONE)
NCT04028492	PHASE3	COMPLETED	Evaluating the Safety and Efficacy of Tradipitant vs. Placebo in Idiopathic and Diabetic Gastroparesis
NCT04140695	PHASE3	TERMINATED	Evaluating the Effects of Tradipitant vs. Placebo in Atopic Dermatitis (EPIONE2)
NCT04327661	PHASE3	COMPLETED	Motion Syros: A Study to Investigate the Efficacy of Tradipitant in Subjects Affected by Motion Sickness
NCT05903924	PHASE3	COMPLETED	Motion Serifos: A Study to Investigate the Efficacy of Tradipitant in Participants Affected by Motion Sickness
NCT05653310	PHASE2	ENROLLING_BY_INVITATION	Tradipitant for Functional Dyspepsia
NCT00191022	PHASE2	COMPLETED	Comparison of LY686017 With a Marketed Drug in the Treatment of Social Anxiety Disorder
NCT00310427	PHASE2	COMPLETED	Effect of LY686017 on Alcohol Craving
NCT00805441	PHASE2	COMPLETED	A Study in the Treatment of Alcohol Dependence.
NCT02004041	PHASE2	COMPLETED	Proof of Concept of VLY-686 in Subjects With Treatment-Resistant Pruritus Associated With Atopic Dermatitis
NCT02651714	PHASE2	COMPLETED	Tradipitant in Treatment-resistant Pruritus Associated With Atopic Dermatitis
NCT02970968	PHASE2	COMPLETED	Study to Assess the Efficacy of VLY-686 in Relieving Symptoms of Gastroparesis
NCT03772340	PHASE2	COMPLETED	Motion Sifnos: A Study to Investigate the Efficacy of Tradipitant in Subjects Affected by Motion Sickness
NCT04849559	PHASE1/PHASE2	COMPLETED	Effects of Tradipitant on Satiation, Gastric Volume, Gastric Accommodation, and Gastric Emptying in Healthy Volunteers
NCT06804603	PHASE2	COMPLETED	A Study to Measure the Effects of Using Tradipitant on Nausea and Vomiting After GLP-1R Agonist Use
NCT01919944	PHASE1	COMPLETED	Study of Itch Control by VLY-686 in Healthy Volunteers After Intradermal Injections of Substance P
NCT02621385	PHASE1	COMPLETED	Study to Assess the Effect of Multiple Doses of Tradipitant on CYP3A4 Using Midazolam as a Substrate in Healthy Subjects
NCT04474990	Not specified	AVAILABLE	Single-Patient Expanded Access Protocol for Tradipitant In A Single Patient With Gastroparesis

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.

45 molecules share ≥1 primary target. Top 45 by shared-target count:

Molecule	Source	Status	Shared targets
ACLIDINIUM BROMIDE	ChEMBL + PubChem	Phase 4 (approved)	TACR1
FIDAXOMICIN	ChEMBL + PubChem	Phase 4 (approved)	TACR1
ROLAPITANT	ChEMBL + PubChem	Phase 4 (approved)	TACR1
AMOXAPINE	ChEMBL	Phase 4 (approved)	TACR1
APREPITANT	ChEMBL	Phase 4 (approved)	TACR1
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	TACR1
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	TACR1
BOSUTINIB	ChEMBL	Phase 4 (approved)	TACR1
CARVEDILOL	ChEMBL	Phase 4 (approved)	TACR1
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	TACR1
CYCLOSPORINE	ChEMBL	Phase 4 (approved)	TACR1
DEXTROMETHORPHAN	ChEMBL	Phase 4 (approved)	TACR1
DOXAZOSIN	ChEMBL	Phase 4 (approved)	TACR1
ECONAZOLE	ChEMBL	Phase 4 (approved)	TACR1
HALOPERIDOL	ChEMBL	Phase 4 (approved)	TACR1
ITRACONAZOLE	ChEMBL	Phase 4 (approved)	TACR1
LANSOPRAZOLE	ChEMBL	Phase 4 (approved)	TACR1
MICONAZOLE	ChEMBL	Phase 4 (approved)	TACR1
NEFAZODONE	ChEMBL	Phase 4 (approved)	TACR1
NETUPITANT	ChEMBL	Phase 4 (approved)	TACR1
NILOTINIB	ChEMBL	Phase 4 (approved)	TACR1
PAROXETINE	ChEMBL	Phase 4 (approved)	TACR1
RITONAVIR	ChEMBL	Phase 4 (approved)	TACR1
TAMOXIFEN	ChEMBL	Phase 4 (approved)	TACR1
TERFENADINE	ChEMBL	Phase 4 (approved)	TACR1
THIOTHIXENE	ChEMBL	Phase 4 (approved)	TACR1
TRAZODONE	ChEMBL	Phase 4 (approved)	TACR1
CASOPITANT	ChEMBL	Phase 3	TACR1
SAREDUTANT	ChEMBL	Phase 3	TACR1
SERLOPITANT	ChEMBL	Phase 3	TACR1
BEFETUPITANT	ChEMBL	Phase 2	TACR1
DAPITANT	ChEMBL	Phase 2	TACR1
DNK333	ChEMBL	Phase 2	TACR1
LANEPITANT	ChEMBL	Phase 2	TACR1
ORVEPITANT	ChEMBL	Phase 2	TACR1
OSANETANT	ChEMBL	Phase 2	TACR1
SPERGUALIN	ChEMBL	Phase 2	TACR1
TALNETANT	ChEMBL	Phase 2	TACR1
TELMAPITANT	ChEMBL	Phase 2	TACR1
VESTIPITANT	ChEMBL	Phase 2	TACR1
VOFOPITANT	ChEMBL	Phase 2	TACR1
Alogliptin	PubChem	Approved	TACR1
Belzutifan	PubChem	Approved	TACR1
Propoxyphene	PubChem	Approved	TACR1
Tiotropium Bromide Monohydrate	PubChem	Approved	TACR1