Tavaborole

Summary

Tavaborole (CHEMBL443052) is an approved small-molecule antifungal agent (ATC D01AE24); indicated across 2 conditions including tinea infection and tinea unguium.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: D01AE24
• Indications: 2 conditions
• Clinical trials: 7
• Chemistry: 151.93 Da · C7H6BFO2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL443052
Name	Tavaborole
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	11499245
ChEBI	CHEBI:77942
ATC	D01AE24
Molecular formula	C7H6BFO2
Molecular weight	151.93
InChIKey	LFQDNHWZDQTITF-UHFFFAOYSA-N

SMILES: B1(C2=C(CO1)C=C(C=C2)F)O

IUPAC name: 5-fluoro-1-hydroxy-3H-2,1-benzoxaborole

ChEBI definition: A member of the class of benzoxaboroles that is 1,3-dihydro-1-hydroxy-2,1-benzoxaborole substituted at position 5 by a fluoro group. A topical antifungal agent used for the treatment of onychomycosis (fungal infection of the toenails and fingernails).

Pharmacological roles (ChEBI): antifungal agent, protein synthesis inhibitor, EC 6.1.1.4 (leucine—tRNA ligase) inhibitor.

Also known as: AN-2690, AN2690, Kerydin, SCH 900340, SCH-900340, Tavaborol, Tavaborole, SID174316125, TAVABOROLE, tavaborole, Tavaborole; Kerydin

Patent coverage: 264 distinct patent families (665 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 418 (63%) 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: 4 (assay-derived). Sample: Leucine–tRNA ligase, cytoplasmic, Carbonic anhydrase 2, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A, Carbonic anhydrase 1.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 8 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CA2	6.33	Ki	462	nM	CHEMBL_ACT_18331778
CA2	6.33	Ki	462	nM	CHEMBL_ACT_22900981
P26637	5.73	Ki	1850	nM	CHEMBL_ACT_1887714
CA1	5.7	Ki	2015	nM	CHEMBL_ACT_18331753
P26637	5.68	IC50	2100	nM	CHEMBL_ACT_1887715

Target pathways

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

Indications & clinical

Indications

2 indications (2 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
tinea infection	4	MONDO:0005982	EFO:0007510
tinea unguium	4	MONDO:0001628	MONDO:0001628

Clinical trials

Total trials: 7.

Phase distribution

Phase	Trials
PHASE2	5
PHASE4	1
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03405818	PHASE4	COMPLETED	An Evaluation of the Safety and Pharmacokinetics of Tavaborole Topical Solution for the Treatment of Fungal Disease of the Toenail in Children and Adolescents
NCT00679601	PHASE2	COMPLETED	Absorption and Systemic Study of AN2690 in Patients With Moderate to Severe Onychomycosis (ADME II)
NCT00679770	PHASE2	COMPLETED	Study of Different Doses of a Novel Treatment for Onychomycosis
NCT00679965	PHASE2	COMPLETED	Study of Different Doses of a Novel Treatment for Onychomycosis
NCT00680134	PHASE2	COMPLETED	Safety and Efficacy Evaluation of Topically Applied AN2690 Solutions for Subjects With Onychomycosis
NCT00680160	PHASE2	COMPLETED	Absorption and Systemic Study of AN2690 in Patients With Moderate to Severe Onychomycosis (ADME I)
NCT00680095	PHASE1	COMPLETED	Cumulative Irritation Test

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).