Radotinib

Summary

Radotinib (CHEMBL4297524) is a phase-3 clinical-stage small molecule; indicated across 2 conditions including chronic myeloid leukemia and parkinson disease.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 2 conditions
• Clinical trials: 8
• Chemistry: 530.5 Da · C27H21F3N8O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4297524
Name	Radotinib
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	16063245
Molecular formula	C27H21F3N8O
Molecular weight	530.5
InChIKey	DUPWHXBITIZIKZ-UHFFFAOYSA-N

SMILES: CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)N3C=C(N=C3)C)NC4=NC=CC(=N4)C5=NC=CN=C5

IUPAC name: 4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyrazin-2-ylpyrimidin-2-yl)amino]benzamide

Also known as: IY5511, Radotinib, RADOTINIB, radotinib

Patent coverage: 748 distinct patent families (1,987 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 1,640 (83%) 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

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Neuronal acetylcholine receptor subunit alpha-4, Bcr/Abl fusion protein, Prostaglandin G/H synthase 1, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A, Adenosine receptor A3, Vascular endothelial growth factor receptor 2, Nuclear receptor subfamily 1 group I member 2.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 9 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ABL1	8.92	IC50	1.2	nM	CHEMBL_ACT_24707070
ADORA3	6.53	AC50	297.8	nM	CHEMBL_ACT_25198695
KDR	5.81	AC50	1538	nM	CHEMBL_ACT_25168207
ADORA3	5.48	AC50	3300	nM	CHEMBL_ACT_25134005
NR1I2	5.22	AC50	6000	nM	CHEMBL_ACT_25188038

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

2 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
chronic myeloid leukemia	3	MONDO:0011996	EFO:0000339
Parkinson disease	2	MONDO:0005180	MONDO:0005180

Clinical trials

Total trials: 8.

Phase distribution

Phase	Trials
PHASE3	3
PHASE2	2
PHASE1/PHASE2	1
PHASE1	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03459534	PHASE3	RECRUITING	A Phase 3 Study for the Efficacy and Safety of Radotinib in CP-CML Patients With Failure or Intolerance to Previous TKIs
NCT03722420	PHASE3	ACTIVE_NOT_RECRUITING	Randomized Evaluation of Radotinib Versus Imatinib in Phase III Study for Efficacy With Chinese Patients (RERISE China)
NCT01511289	PHASE3	COMPLETED	Radotinib Versus Imatinib in Newly Diagnosed Philadelphia Chromosome and Chronic Myeloid Leukemia Chronic Phase Patients
NCT04691661	PHASE2	RECRUITING	Safety, Tolerability, Pharmacokinetics and Efficacy Study of Radotinib in Parkinson’s Disease
NCT01602952	PHASE1/PHASE2	COMPLETED	Philadelphia Chromosome Positive CML Patients Without Optimal Response or Tolerance to Bcr-Abl TKI
NCT02422719	PHASE2	UNKNOWN	Radotinib as 3rd or Later Line Therapy in CP-CML
NCT06461078	PHASE1	COMPLETED	Clinical Trial to Investigate the Effects of Food on the Pharmacokinetics and Safety of Orally Administered Radotinib
NCT06665412	Not specified	RECRUITING	Efficacy and Safety of Dose Redution of Radotinib as a First Line Treament in Ph+ CML

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

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).