Reparixin

Summary

Reparixin (CHEMBL191413) is a phase-3 clinical-stage small molecule targeting CXCR2; indicated across 8 conditions including pneumonia and viral pneumonia.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (CXCR2)
• Indications: 8 conditions
• Clinical trials: 14
• Chemistry: 283.39 Da · C14H21NO3S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL191413
Name	Reparixin
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	9838712
Molecular formula	C14H21NO3S
Molecular weight	283.39
InChIKey	KQDRVXQXKZXMHP-LLVKDONJSA-N

SMILES: C[C@H](C1=CC=C(C=C1)CC(C)C)C(=O)NS(=O)(=O)C

IUPAC name: (2R)-2-[4-(2-methylpropyl)phenyl]-N-methylsulfonylpropanamide

Also known as: DF 1681Y, Df-1681y, DF-1681Y, DF1681Y, Reparixin, Reparixina, Reparixine, Repertaxin, REPARIXIN, SID144205825, ReparixinÊ, reparixin

Parent form; salt/anhydrous children: CHEMBL1527147

Patent coverage: 247 distinct patent families (653 SureChEMBL compound mentions), from 1 matched compound structure(s). 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
CXCR2	CXCR2	Negative	6.4	0.1%	P25025

Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Interleukin-8 receptors, CXCR1/CXCR2, C-X-C chemokine receptor type 2, C-X-C chemokine receptor type 1.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
CXCR2	9	IC50	1	nM	CHEMBL_ACT_12149707
CXCR1	9	IC50	1	nM	CHEMBL_ACT_12149709
CXCR1	9	IC50	1	nM	CHEMBL_ACT_25709893
CXCR1	8.28	IC50	5.3	nM	CHEMBL_ACT_1487835
CXCR2	7	IC50	100	nM	CHEMBL_ACT_12149708
CXCR2	7	IC50	100	nM	CHEMBL_ACT_25709892

Target pathways

Aggregated over 1 target gene(s): CXCR2.

Top Reactome pathways

3 total, by targets touching each:

Pathway	Targets	Genes
Chemokine receptors bind chemokines	1	CXCR2
G alpha (i) signalling events	1	CXCR2
Neutrophil degranulation	1	CXCR2

Dominant GO biological processes

GO term	Targets
dendritic cell chemotaxis	1
chemotaxis	1
inflammatory response	1
immune response	1
cellular defense response	1
signal transduction	1
cell surface receptor signaling pathway	1
phospholipase C-activating G protein-coupled receptor signaling pathway	1
positive regulation of cytosolic calcium ion concentration	1
positive regulation of cell population proliferation	1
calcium-mediated signaling	1
neutrophil chemotaxis	1
receptor internalization	1
interleukin-8-mediated signaling pathway	1
neutrophil activation	1

Indications & clinical

Indications

8 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)	Phase	MONDO	EFO
pneumonia	3	MONDO:0005249	EFO:0003106
viral pneumonia	3	MONDO:0006012	EFO:0007541
type 1 diabetes mellitus	3	MONDO:0005147	MONDO:0005147
severe acute respiratory syndrome	3	MONDO:0005091	MONDO:0100096
chronic pancreatitis	2	MONDO:0005003	EFO:0000342
ischemia reperfusion injury	2	MONDO:0005203	EFO:0002687
breast neoplasm	2	MONDO:0021100	MONDO:0007254
adult acute respiratory distress syndrome	2	MONDO:0100130	MONDO:0100130

Clinical trials

Total trials: 14.

Phase distribution

Phase	Trials
PHASE2	8
PHASE3	3
PHASE2/PHASE3	2
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01817959	PHASE3	COMPLETED	Study to Assess Efficacy & Safety of Reparixin in Pancreatic Islet Transplantation
NCT01967888	PHASE2/PHASE3	COMPLETED	Efficacy and Safety of Reparixin in Pancreatic Islet Auto-transplantation
NCT04794803	PHASE2/PHASE3	TERMINATED	Reparixin in COVID-19 Pneumonia - Efficacy and Safety
NCT04878055	PHASE3	COMPLETED	Study on Efficacy and Safety of Reparixin in the Treatment of Hospitalized Patients With Severe COVID-19 Pneumonia.
NCT05254990	PHASE3	TERMINATED	Reparixin add-on Therapy to Standard Care to Limit Progression in Pts With COVID19 & Other Community Acquired Pneumonia
NCT05835466	PHASE2	RECRUITING	Reparixin in Patients With Myelofibrosis Myeloproliferative Neoplasms Research Consortium (MPN-RC 120)
NCT00224406	PHASE2	COMPLETED	Repertaxin in Prevention of Primary Graft Dysfunction After Lung Transplantation
NCT01220856	PHASE2	COMPLETED	Reparixin in Pancreatic Islet Transplantation
NCT01861054	PHASE2	TERMINATED	Pilot Study to Evaluate Safety & Biological Effects of Orally Administered Reparixin in Early Breast Cancer
NCT02370238	PHASE2	COMPLETED	A Double-blind Study of Paclitaxel in Combination With Reparixin or Placebo for Metastatic Triple-Negative Breast Cancer
NCT03031470	PHASE2	TERMINATED	Pilot Study of Reparixin for Early Allograft Dysfunction Prevention in Liver Transplantation
NCT05212701	PHASE2	WITHDRAWN	To Assess Efficacy and Safety of Oral Reparixin in Patients With Fatigue and Locally Advanced / Metastatic Breast Cancer
NCT05496868	PHASE2	COMPLETED	Add-on Reparixin in Adult Patients With ARDS
NCT02001974	PHASE1	COMPLETED	Pilot Study to Evaluate Reparixin With Weekly Paclitaxel in Patients With HER 2 Negative Metastatic Breast Cancer (MBC)

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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.

13 molecules share ≥1 primary target. Top 13 by shared-target count:

Molecule	Source	Status	Shared targets
CISPLATIN	ChEMBL	Phase 4 (approved)	CXCR2
DEXIBUPROFEN	ChEMBL	Phase 4 (approved)	CXCR2
DEXKETOPROFEN	ChEMBL	Phase 4 (approved)	CXCR2
DISULFIRAM	ChEMBL	Phase 4 (approved)	CXCR2
LADARIXIN	ChEMBL	Phase 3	CXCR2
AZD-8797	ChEMBL	Phase 2	CXCR2
DANIRIXIN	ChEMBL	Phase 2	CXCR2
ELUBRIXIN	ChEMBL	Phase 2	CXCR2
NAVARIXIN	ChEMBL	Phase 2	CXCR2
SX-682	ChEMBL	Phase 2	CXCR2
VIMNERIXIN	ChEMBL	Phase 2	CXCR2
Mavorixafor	PubChem	Approved	CXCR2
Naproxen	PubChem	Approved	CXCR2