Tariquidar

Summary

Tariquidar (CHEMBL348475) is a phase-3 clinical-stage small molecule targeting ABCB1; indicated across 6 conditions including non-small cell lung carcinoma and adrenal cortex carcinoma.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (ABCB1)
• Indications: 6 conditions
• Clinical trials: 8
• Chemistry: 646.7 Da · C38H38N4O6

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL348475
Name	Tariquidar
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	148201
Molecular formula	C38H38N4O6
Molecular weight	646.7
InChIKey	LGGHDPFKSSRQNS-UHFFFAOYSA-N

SMILES: COC1=C(C=C2CN(CCC2=C1)CCC3=CC=C(C=C3)NC(=O)C4=CC(=C(C=C4NC(=O)C5=CC6=CC=CC=C6N=C5)OC)OC)OC

IUPAC name: N-[2-[[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]carbamoyl]-4,5-dimethoxyphenyl]quinoline-3-carboxamide

Also known as: Tariquidar, XR-9576, XR9576, tariquidar, TARIQUIDAR, SID174006280, Tariguidar, (+)-Tariquidar

Parent form; salt/anhydrous children: CHEMBL1214643

Patent coverage: 1,079 distinct patent families (3,984 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 3,764 (94%) 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
ABCB1	ABCB1	Inhibition	7.42	0.4%	P08183

Broader ChEMBL bioactivity targets: 8 (assay-derived). Sample: Cytochrome P450 2D6, Multidrug resistance-associated protein 1, Cytochrome P450 1A2, Cytochrome P450 2C9, ATP-dependent translocase ABCB1, Cytochrome P450 2C8, ATP-dependent translocase ABCB1, Broad substrate specificity ATP-binding cassette transporter ABCG2.

Bioactivity

ChEMBL activities: 64 potent at pChembl ≥ 5 of 69 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ABCB1	9.59	IC50	0.26	nM	CHEMBL_ACT_23198006
ABCB1	9.18	IC50	0.66	nM	CHEMBL_ACT_16795966
ABCB1	9.15	IC50	0.71	nM	CHEMBL_ACT_23198010
ABCB1	8.69	IC50	2.05	nM	CHEMBL_ACT_23197998
ABCB1	8.49	IC50	3.26	nM	CHEMBL_ACT_23198002
ABCB1	8.48	IC50	3.34	nM	CHEMBL_ACT_23197994
ABCB1	8.12	IC50	7.57	nM	CHEMBL_ACT_23197986
ABCB1	8.04	IC50	9.05	nM	CHEMBL_ACT_16795956
ABCG2	8	EC50	10	nM	CHEMBL_ACT_12689985
ABCG2	8	EC50	10	nM	CHEMBL_ACT_26159512
ABCB1	7.8	EC50	16	nM	CHEMBL_ACT_23227965
ABCB1	7.73	IC50	18.51	nM	CHEMBL_ACT_16795996
ABCB1	7.61	IC50	24.77	nM	CHEMBL_ACT_16795915
ABCB1	7.6	IC50	24.97	nM	CHEMBL_ACT_16795986
ABCB1	7.49	IC50	32.7	nM	CHEMBL_ACT_23227954
ABCB1	7.48	IC50	33.11	nM	CHEMBL_ACT_10954675
ABCB1	7.46	EC50	35	nM	CHEMBL_ACT_25910544
ABCB1	7.46	IC50	35	nM	CHEMBL_ACT_25910772
ABCB1	7.42	IC50	38	nM	CHEMBL_ACT_2138038
ABCB1	7.42	IC50	38.02	nM	CHEMBL_ACT_2138039
ABCB1	7.36	EC50	44	nM	CHEMBL_ACT_12689995
ABCB1	7.36	EC50	44	nM	CHEMBL_ACT_14578006
ABCB1	7.36	EC50	44	nM	CHEMBL_ACT_26159464
ABCB1	7.28	IC50	53	nM	CHEMBL_ACT_25910751
P06795	7.19	IC50	64	nM	CHEMBL_ACT_2138040
P06795	7.19	IC50	64.57	nM	CHEMBL_ACT_2138041
ABCB1	7.17	EC50	68	nM	CHEMBL_ACT_1943300
ABCB1	7.16	IC50	70	nM	CHEMBL_ACT_16795946
ABCB1	7.14	IC50	72.44	nM	CHEMBL_ACT_2230278
ABCB1	7.11	IC50	78	nM	CHEMBL_ACT_2614753

Target pathways

Aggregated over 1 target gene(s): ABCB1.

Top Reactome pathways

7 total, by targets touching each:

Pathway	Targets	Genes
Abacavir transmembrane transport	1	ABCB1
Abacavir ADME	1	ABCB1
Transport of small molecules	1	ABCB1
ABC-family protein mediated transport	1	ABCB1
Drug ADME	1	ABCB1
Atorvastatin ADME	1	ABCB1
Prednisone ADME	1	ABCB1

Dominant GO biological processes

GO term	Targets
G2/M transition of mitotic cell cycle	1
response to hypoxia	1
placenta development	1
xenobiotic metabolic process	1
female pregnancy	1
lactation	1
circadian rhythm	1
response to xenobiotic stimulus	1
hormone transport	1
response to progesterone	1
response to vitamin A	1
response to vitamin D	1
response to glucagon	1
maintenance of blood-brain barrier	1
cellular response to mycotoxin	1

Indications & clinical

Indications

6 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
non-small cell lung carcinoma	3	MONDO:0005233	EFO:0003060
adrenal cortex carcinoma	2	MONDO:0006639	EFO:1000796
neuralgia	1	MONDO:0021667	EFO:0005762
breast neoplasm	1	MONDO:0021100	MONDO:0007254
ovarian cancer	1	MONDO:0008170	MONDO:0008170
lung neoplasm	1	MONDO:0021117	MONDO:0008903

Clinical trials

Total trials: 8.

Phase distribution

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

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00042315	PHASE3	TERMINATED	A Double-Blind, Randomized, Placebo-Controlled, Multicenter, Phase III Study of Tariquidar + Vinorelbine as First-Line Therapy in Non-Small Cell Lung Cancer (NSCLC)
NCT00069160	PHASE2	COMPLETED	Tariquidar and Docetaxel to Treat Patients With Lung, Ovarian, Renal and Cervical Cancer
NCT00071058	PHASE2	COMPLETED	Surgery Plus Chemotherapy (Doxorubicin, Vincristine and Etoposide), Mitotane, and Tariquidar to Treat Adrenocortical Cancer
NCT00082368	PHASE2	COMPLETED	PET Imaging With Tc-94m Sestamibi to Assess Resistance to Chemotherapy
NCT04603066	PHASE1/PHASE2	COMPLETED	Tariquidar-ondansetron Combination in Neuropathic Pain
NCT00001944	PHASE1	COMPLETED	Vinorelbine and XR9576 to Treat Cancer
NCT00011414	PHASE1	COMPLETED	Phase I Trial of Tariquidar (XR9576) in Combination With Doxorubicin, Vinorelbine, or Docetaxel in Pediatric Patients With Solid Tumors
NCT03809234	PHASE1	TERMINATED	Pgp Transporter and CNS Biodistribution of Ondansetron in Healthy Volunteers

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.

123 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
TRAMETINIB	ChEMBL + PubChem	Phase 4 (approved)	ABCB1
AMIODARONE	ChEMBL	Phase 4 (approved)	ABCB1
AMLODIPINE	ChEMBL	Phase 4 (approved)	ABCB1
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	ABCB1
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	ABCB1
ATAZANAVIR	ChEMBL	Phase 4 (approved)	ABCB1
AZELASTINE	ChEMBL	Phase 4 (approved)	ABCB1
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	ABCB1
CARVEDILOL	ChEMBL	Phase 4 (approved)	ABCB1
CERITINIB	ChEMBL	Phase 4 (approved)	ABCB1
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	ABCB1
CLARITHROMYCIN	ChEMBL	Phase 4 (approved)	ABCB1
CLOFAZIMINE	ChEMBL	Phase 4 (approved)	ABCB1
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	ABCB1
CYCLOSPORINE	ChEMBL	Phase 4 (approved)	ABCB1
DARUNAVIR	ChEMBL	Phase 4 (approved)	ABCB1
DAUNORUBICIN	ChEMBL	Phase 4 (approved)	ABCB1
DESLORATADINE	ChEMBL	Phase 4 (approved)	ABCB1
DILTIAZEM	ChEMBL	Phase 4 (approved)	ABCB1
DIPYRIDAMOLE	ChEMBL	Phase 4 (approved)	ABCB1
DONEPEZIL	ChEMBL	Phase 4 (approved)	ABCB1
DOXORUBICIN	ChEMBL	Phase 4 (approved)	ABCB1
EBASTINE	ChEMBL	Phase 4 (approved)	ABCB1
EMETINE	ChEMBL	Phase 4 (approved)	ABCB1
ERGOTAMINE	ChEMBL	Phase 4 (approved)	ABCB1
ERLOTINIB	ChEMBL	Phase 4 (approved)	ABCB1
ERYTHROMYCIN	ChEMBL	Phase 4 (approved)	ABCB1
ETRAVIRINE	ChEMBL	Phase 4 (approved)	ABCB1
FELODIPINE	ChEMBL	Phase 4 (approved)	ABCB1
FENTANYL	ChEMBL	Phase 4 (approved)	ABCB1
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	ABCB1
GEFITINIB	ChEMBL	Phase 4 (approved)	ABCB1
HALOPERIDOL	ChEMBL	Phase 4 (approved)	ABCB1
IMATINIB	ChEMBL	Phase 4 (approved)	ABCB1
INDOMETHACIN	ChEMBL	Phase 4 (approved)	ABCB1
ITRACONAZOLE	ChEMBL	Phase 4 (approved)	ABCB1
IVERMECTIN	ChEMBL	Phase 4 (approved)	ABCB1
KETOCONAZOLE	ChEMBL	Phase 4 (approved)	ABCB1
LANSOPRAZOLE	ChEMBL	Phase 4 (approved)	ABCB1
LEFAMULIN	ChEMBL	Phase 4 (approved)	ABCB1
LONAFARNIB	ChEMBL	Phase 4 (approved)	ABCB1
LOPERAMIDE	ChEMBL	Phase 4 (approved)	ABCB1
LOPINAVIR	ChEMBL	Phase 4 (approved)	ABCB1
LORATADINE	ChEMBL	Phase 4 (approved)	ABCB1
LOVASTATIN	ChEMBL	Phase 4 (approved)	ABCB1
METHADONE	ChEMBL	Phase 4 (approved)	ABCB1
MIBEFRADIL	ChEMBL	Phase 4 (approved)	ABCB1
MICONAZOLE	ChEMBL	Phase 4 (approved)	ABCB1
MIDOSTAURIN	ChEMBL	Phase 4 (approved)	ABCB1
MITOXANTRONE	ChEMBL	Phase 4 (approved)	ABCB1
NEFAZODONE	ChEMBL	Phase 4 (approved)	ABCB1
NELFINAVIR	ChEMBL	Phase 4 (approved)	ABCB1
NICARDIPINE	ChEMBL	Phase 4 (approved)	ABCB1
NINTEDANIB	ChEMBL	Phase 4 (approved)	ABCB1
NISOLDIPINE	ChEMBL	Phase 4 (approved)	ABCB1
OMEPRAZOLE	ChEMBL	Phase 4 (approved)	ABCB1
PACLITAXEL	ChEMBL	Phase 4 (approved)	ABCB1
PANTOPRAZOLE	ChEMBL	Phase 4 (approved)	ABCB1
PAROXETINE	ChEMBL	Phase 4 (approved)	ABCB1
PIMOZIDE	ChEMBL	Phase 4 (approved)	ABCB1