Details
Stereochemistry | ACHIRAL |
Molecular Formula | C7H6BFO2 |
Molecular Weight | 151.931 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OB1OCC2=CC(F)=CC=C12
InChI
InChIKey=LFQDNHWZDQTITF-UHFFFAOYSA-N
InChI=1S/C7H6BFO2/c9-6-1-2-7-5(3-6)4-11-8(7)10/h1-3,10H,4H2
Molecular Formula | C7H6BFO2 |
Molecular Weight | 151.931 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4662369/
Curator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4662369/
Tavaborole is a boron-based pharmaceutical agent indicated for the topical treatment of toenail onychomycosis, a fungal infection of the nail and nail bed due to Trichophyton rubrum or Trichophyton mentagrophytes infection. Tavaborole acts by inhibiting an aminoacyl-transfer ribonucleic acid (tRNA) synthetase (AARS) - Leucyl-tRNA synthetase. Leucyl-tRNA synthetase is an essential fungal enzyme required for protein synthesis and for the catalysis of ATP-dependent ligation of L-leucine to tRNA(Leu). Tavaborole’s low molecular weight (approximately half of most antifungals, such as terbinafine and efinaconazole) permits optimal nail plate penetration, superior to that of existing topical antifungal medications.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: ENTREZ Gene ID: 10373871 (leucyl-tRNA synthetase) Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=26640371 |
|||
Target ID: ENTREZ Gene ID: 10373705 (leucyl-tRNA synthetase) Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=26640371 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Curative | KERYDIN Approved UseKERYDIN (tavaborole) topical solution, 5% is an oxaborole antifungal indicated for the treatment of onychomycosis of the toenails due to Trichophyton rubrum or Trichophyton mentagrophytes. Launch Date2014 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5.9 ng/mL |
5 % 1 times / day multiple, topical dose: 5 % route of administration: Topical experiment type: MULTIPLE co-administered: |
TAVABOROLE blood | Homo sapiens population: UNHEALTHY age: ADOLESCENT sex: UNKNOWN food status: UNKNOWN |
|
5.2 ng/mL |
5 % 1 times / day multiple, topical dose: 5 % route of administration: Topical experiment type: MULTIPLE co-administered: |
TAVABOROLE blood | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
76 ng × h/mL |
5 % 1 times / day multiple, topical dose: 5 % route of administration: Topical experiment type: MULTIPLE co-administered: |
TAVABOROLE blood | Homo sapiens population: UNHEALTHY age: ADOLESCENT sex: UNKNOWN food status: UNKNOWN |
|
75.8 ng × h/mL |
5 % 1 times / day multiple, topical dose: 5 % route of administration: Topical experiment type: MULTIPLE co-administered: |
TAVABOROLE blood | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
28.5 h |
5 % 1 times / day multiple, topical dose: 5 % route of administration: Topical experiment type: MULTIPLE co-administered: |
TAVABOROLE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
7.5 % 1 times / day multiple, topical Highest studied dose Dose: 7.5 %, 1 times / day Route: topical Route: multiple Dose: 7.5 %, 1 times / day Sources: |
unhealthy, 18-65 years n = 15 Health Status: unhealthy Condition: onychomycosis Age Group: 18-65 years Sex: M+F Population Size: 15 Sources: |
Disc. AE: Application site stinging, Pruritus... Other AEs: Application site irritation, Application site erythema... AEs leading to discontinuation/dose reduction: Application site stinging (grade 2) Other AEs:Pruritus (grade 2) Irritation skin (grade 3) Application site irritation Sources: Application site erythema Application site reaction |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.78 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.78 |
Disc. AE: Application site erythema, Application site exfoliation... AEs leading to discontinuation/dose reduction: Application site erythema (grade 2, 0.5%) Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.78Application site exfoliation (grade 2, 0.5%) |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
Disc. AE: Ingrowing nail, Application site pain... Other AEs: Skin induration... AEs leading to discontinuation/dose reduction: Ingrowing nail (0.5%) Other AEs:Application site pain (0.5%) Application site discharge (0.5%) Application site exfoliation (0.5%) Application site edema (0.5%) Edema peripheral (0.5%) Application site erythema (0.5%) Erythema (0.5%) Application site induration (0.5%) Application site reaction (0.5%) Skin maceration (0.5%) Application site pruritus (0.5%) Pruritus (0.5%) Skin induration (0.5%) Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
unhealthy, mean age 55 years n = 205 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 205 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
Other AEs: Dermatitis contact... Other AEs: Dermatitis contact (0.5%) Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.83 |
unhealthy, mean age 55 years n = 791 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 791 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.83 |
Other AEs: Upper respiratory tract infection, Back pain... Other AEs: Upper respiratory tract infection (5.44%) Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.83Back pain (3.29%) Application site exfoliation (2.65%) Ingrowing nail (2.53%) Procedural pain (2.53%) Muscle strain (2.4%) Arthralgia (2.15%) |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.85 |
unhealthy, mean age 55 years n = 791 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 791 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.85 |
Other AEs: Hypercholesterolaemia, Blood creatinine increased... Other AEs: Hypercholesterolaemia (1.01%) Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.85Blood creatinine increased (0.51%) Blood glucose increased (0.38%) Blood urea increased (0.38%) Hyperglycaemia (0.38%) Hyperlipidaemia (0.38%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Application site erythema | 7.5 % 1 times / day multiple, topical Highest studied dose Dose: 7.5 %, 1 times / day Route: topical Route: multiple Dose: 7.5 %, 1 times / day Sources: |
unhealthy, 18-65 years n = 15 Health Status: unhealthy Condition: onychomycosis Age Group: 18-65 years Sex: M+F Population Size: 15 Sources: |
|
Application site irritation | 7.5 % 1 times / day multiple, topical Highest studied dose Dose: 7.5 %, 1 times / day Route: topical Route: multiple Dose: 7.5 %, 1 times / day Sources: |
unhealthy, 18-65 years n = 15 Health Status: unhealthy Condition: onychomycosis Age Group: 18-65 years Sex: M+F Population Size: 15 Sources: |
|
Application site reaction | 7.5 % 1 times / day multiple, topical Highest studied dose Dose: 7.5 %, 1 times / day Route: topical Route: multiple Dose: 7.5 %, 1 times / day Sources: |
unhealthy, 18-65 years n = 15 Health Status: unhealthy Condition: onychomycosis Age Group: 18-65 years Sex: M+F Population Size: 15 Sources: |
|
Application site stinging | grade 2 Disc. AE |
7.5 % 1 times / day multiple, topical Highest studied dose Dose: 7.5 %, 1 times / day Route: topical Route: multiple Dose: 7.5 %, 1 times / day Sources: |
unhealthy, 18-65 years n = 15 Health Status: unhealthy Condition: onychomycosis Age Group: 18-65 years Sex: M+F Population Size: 15 Sources: |
Pruritus | grade 2 Disc. AE |
7.5 % 1 times / day multiple, topical Highest studied dose Dose: 7.5 %, 1 times / day Route: topical Route: multiple Dose: 7.5 %, 1 times / day Sources: |
unhealthy, 18-65 years n = 15 Health Status: unhealthy Condition: onychomycosis Age Group: 18-65 years Sex: M+F Population Size: 15 Sources: |
Irritation skin | grade 3 Disc. AE |
7.5 % 1 times / day multiple, topical Highest studied dose Dose: 7.5 %, 1 times / day Route: topical Route: multiple Dose: 7.5 %, 1 times / day Sources: |
unhealthy, 18-65 years n = 15 Health Status: unhealthy Condition: onychomycosis Age Group: 18-65 years Sex: M+F Population Size: 15 Sources: |
Application site erythema | grade 2, 0.5% Disc. AE |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.78 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.78 |
Application site exfoliation | grade 2, 0.5% Disc. AE |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.78 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.78 |
Skin induration | 0.5% | 5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
Application site discharge | 0.5% Disc. AE |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
Application site edema | 0.5% Disc. AE |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
Application site erythema | 0.5% Disc. AE |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
Application site exfoliation | 0.5% Disc. AE |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
Application site induration | 0.5% Disc. AE |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
Application site pain | 0.5% Disc. AE |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
Application site pruritus | 0.5% Disc. AE |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
Application site reaction | 0.5% Disc. AE |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
Edema peripheral | 0.5% Disc. AE |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
Erythema | 0.5% Disc. AE |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
Ingrowing nail | 0.5% Disc. AE |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
Pruritus | 0.5% Disc. AE |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
Skin maceration | 0.5% Disc. AE |
5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
unhealthy, mean age 55 years n = 194 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 194 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
Dermatitis contact | 0.5% | 5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
unhealthy, mean age 55 years n = 205 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 205 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.79 |
Arthralgia | 2.15% | 5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.83 |
unhealthy, mean age 55 years n = 791 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 791 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.83 |
Muscle strain | 2.4% | 5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.83 |
unhealthy, mean age 55 years n = 791 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 791 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.83 |
Ingrowing nail | 2.53% | 5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.83 |
unhealthy, mean age 55 years n = 791 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 791 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.83 |
Procedural pain | 2.53% | 5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.83 |
unhealthy, mean age 55 years n = 791 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 791 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.83 |
Application site exfoliation | 2.65% | 5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.83 |
unhealthy, mean age 55 years n = 791 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 791 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.83 |
Back pain | 3.29% | 5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.83 |
unhealthy, mean age 55 years n = 791 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 791 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.83 |
Upper respiratory tract infection | 5.44% | 5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.83 |
unhealthy, mean age 55 years n = 791 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 791 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.83 |
Blood glucose increased | 0.38% | 5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.85 |
unhealthy, mean age 55 years n = 791 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 791 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.85 |
Blood urea increased | 0.38% | 5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.85 |
unhealthy, mean age 55 years n = 791 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 791 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.85 |
Hyperglycaemia | 0.38% | 5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.85 |
unhealthy, mean age 55 years n = 791 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 791 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.85 |
Hyperlipidaemia | 0.38% | 5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.85 |
unhealthy, mean age 55 years n = 791 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 791 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.85 |
Blood creatinine increased | 0.51% | 5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.85 |
unhealthy, mean age 55 years n = 791 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 791 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.85 |
Hypercholesterolaemia | 1.01% | 5 % 1 times / day multiple, topical Recommended Dose: 5 %, 1 times / day Route: topical Route: multiple Dose: 5 %, 1 times / day Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.85 |
unhealthy, mean age 55 years n = 791 Health Status: unhealthy Condition: onychomycosis Age Group: mean age 55 years Sex: M+F Population Size: 791 Sources: Page: nda/2014/204427Orig1s000MedR.pdf - p.85 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000PharmR.pdf#page=18 Page: 18.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000PharmR.pdf#page=18 Page: 18.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000PharmR.pdf#page=18 Page: 18.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000PharmR.pdf#page=18 Page: 18.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000PharmR.pdf#page=18 Page: 18.0 |
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204427Orig1s000PharmR.pdf#page=16 Page: 16.0 |
PubMed
Title | Date | PubMed |
---|---|---|
Discovery of a new boron-containing antifungal agent, 5-fluoro-1,3-dihydro-1-hydroxy-2,1- benzoxaborole (AN2690), for the potential treatment of onychomycosis. | 2006 Jul 27 |
|
Spotlight on targeting aminoacyl-tRNA synthetases for the treatment of fungal infections. | 2006 Jul-Aug |
|
AN-2690, a novel antifungal for the topical treatment of onychomycosis. | 2007 Aug |
|
A genomic glimpse of aminoacyl-tRNA synthetases in malaria parasite Plasmodium falciparum. | 2009 Dec 31 |
|
Post-transfer editing by a eukaryotic leucyl-tRNA synthetase resistant to the broad-spectrum drug AN2690. | 2010 Sep 1 |
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The efficacy and safety of tavaborole, a novel, boron-based pharmaceutical agent: phase 2 studies conducted for the topical treatment of toenail onychomycosis. | 2014 Sep |
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Tavaborole: first global approval. | 2014 Sep |
Sample Use Guides
Tavaborole 5% topical solution (each milliliter of solution contains 43.5 mg of tavaborole) should be applyed to affected toenails once daily for 48 weeks. It should be applied to the entire toenail surface and under the tip of each toenail being treated (for topical use only and not for oral, ophthalmic, or intravaginal use).
Route of Administration:
Topical
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/26091387
Tavaborole demonstrated minimum inhibitory concentration (MIC) values ranging from 0.25–2 μg/mL against all fungi tested; addition of 5% keratin powder did not affect the MIC against T rubrum. The minimum fungicidal concentration (MFC) values for tavaborole against T rubrum and T mentagrophytes were 8 and 16 μg/mL, respectively.
Substance Class |
Chemical
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METABOLITE -> PARENT |
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PLASMA
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Tmax | PHARMACOKINETIC |
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SINGLE TOPICAL APPLICATION ON DAY 1 |
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