OTESECONAZOLE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C23H16F7N5O2
Molecular Weight	527.3943
Optical Activity	( + )
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O[C@@](CN1C=NN=N1)(C2=CC=C(F)C=C2F)C(F)(F)C3=NC=C(C=C3)C4=CC=C(OCC(F)(F)F)C=C4

InChI

InChIKey=IDUYJRXRDSPPRC-NRFANRHFSA-N

InChI=1S/C23H16F7N5O2/c24-16-4-7-18(19(25)9-16)21(36,11-35-13-32-33-34-35)23(29,30)20-8-3-15(10-31-20)14-1-5-17(6-2-14)37-12-22(26,27)28/h1-10,13,36H,11-12H2/t21-/m0/s1

HIDE SMILES / InChI

Description
Sources: https://pubmed.ncbi.nlm.nih.gov/35713845|https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/215888s000lbl.pdf

Oteseconazole (VIVJOA™) is an orally administered azole antifungal agent developed by Mycovia Pharmaceuticals for the treatment of fungal infections. It inhibits cytochrome P450 (CYP) 51, thereby affecting the formation and integrity of the fungal cell membrane, but has a low affinity for human CYP enzymes due to its tetrazole metal-binding group. Oteseconazole is the first agent to be approved (in April 2022) for recurrent vulvovaginal candidiasis (RVVC) in the USA, where it is indicated to reduce the incidence of RVVC in females with a history of RVVC who are NOT of reproductive potential. Clinical development for the treatment of onychomycosis, and invasive and opportunistic infections is ongoing.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Lanosterol 14-alpha demethylase 15 Target ID: P10613 Gene ID: 3641571.0 Gene Symbol: ERG11 Target Organism: Candida albicans (strain SC5314 / ATCC MYA-2876) (Yeast) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/215888s000lbl.pdf\|https://adisinsight.springer.com/drugs/800034957	Inhibitor 8504		39.0 nM [Kd]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Vulvovaginal candidiasis 13 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/215888s000lbl.pdf	Curative		Approved 8583	VIVJOA Approved Use VIVJOA™ is an azole antifungal indicated to reduce the incidence of recurrent vulvovaginal candidiasis (RVVC) in females with a history of RVVC who are NOT of reproductive potential. Launch Date 2022

C_max

Value	Dose	Analyte	Population
44.7 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
79.7 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
165 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
180 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
338 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	320 mg single, oral dose: 320 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
988 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	320 mg single, oral dose: 320 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
531 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=175	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
1130 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=175	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
1920 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=175	160 mg 1 times / day multiple, oral dose: 160 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
3300 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=175	320 mg 1 times / day multiple, oral dose: 320 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
8680 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=177	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
6575 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=177	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
15000 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=177	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
12850 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=177	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
538 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=179	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
781.2 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=179	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: HIGH-FAT
629.3 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=179	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: LOW-FAT
793.7 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=179	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: HIGH-FAT
3507 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=183	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: HIGH-FAT
0.41 μg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=192	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
0.97 μg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=192	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
1.8 μg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=193	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
3.12 μg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=193	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
1.34 μg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=193	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
2.75 μg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=193	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
16145 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
35037 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
84635 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
108869 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
241971 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	320 mg single, oral dose: 320 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
953119 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	320 mg single, oral dose: 320 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
10202 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=175	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
23143 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=175	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
38661 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=175	160 mg 1 times / day multiple, oral dose: 160 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
67164 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=175	320 mg 1 times / day multiple, oral dose: 320 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
538229.5 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=177	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
422455.21 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=177	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
900275 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=177	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
852537.5 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=177	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
17110 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=179	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
23200 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=179	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: HIGH-FAT
17430 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=179	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: LOW-FAT
20600 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=179	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: HIGH-FAT
4301156.522 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=183	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: HIGH-FAT
1.87 μg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=192	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
4.23 μg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=192	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
12.3 μg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=193	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
21.6 μg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=193	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
9.12 μg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=193	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
20.5 μg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=193	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
393 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
548 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
536 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
618 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
873 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	320 mg single, oral dose: 320 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
1467 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=174	320 mg single, oral dose: 320 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
2103 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=175	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
2445 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=175	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
3227 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=175	160 mg 1 times / day multiple, oral dose: 160 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
5207 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=175	320 mg 1 times / day multiple, oral dose: 320 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
1514.47 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=177	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
2378.14 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=177	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
4390.84 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=177	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
2753.12 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=177	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
2114.012 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=183	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	OTESECONAZOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: HIGH-FAT

F_unbound

Value	Dose	Co-administered	Analyte	Population
0.3% OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=35 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=165			OTESECONAZOLE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf	unhealthy, ADOLESCENT\|ADULT Health Status: unhealthy Age Group: ADOLESCENT\|ADULT Sex: F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf	Disc. AE: Vaginal in, Adverse event... Other AEs: Adverse event... AEs leading to discontinuation/dose reduction: Vaginal in (0.5%) Adverse event (0.5%) Other AEs: Adverse event (0.5%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf
150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf	Disc. AE: Adverse event... AEs leading to discontinuation/dose reduction: Adverse event (0.9%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf
150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf	Disc. AE: Pancreatitis, Adverse event... AEs leading to discontinuation/dose reduction: Pancreatitis (1 or 2, 2.4%) Adverse event (1 or 2, 4.9%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf
300 mg 1 times / day multiple, oral Studied dose Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf	Disc. AE: Dermatitis allergic... AEs leading to discontinuation/dose reduction: Dermatitis allergic (2.4%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf

AEs

AE	Significance	Dose	Population
Adverse event	0.5%	150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf	unhealthy, ADOLESCENT\|ADULT Health Status: unhealthy Age Group: ADOLESCENT\|ADULT Sex: F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf
Adverse event	0.5% Disc. AE	150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf	unhealthy, ADOLESCENT\|ADULT Health Status: unhealthy Age Group: ADOLESCENT\|ADULT Sex: F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf
Vaginal in	0.5% Disc. AE	150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf	unhealthy, ADOLESCENT\|ADULT Health Status: unhealthy Age Group: ADOLESCENT\|ADULT Sex: F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf
Adverse event	0.9% Disc. AE	150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf
Pancreatitis	1 or 2, 2.4% Disc. AE	150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf
Adverse event	1 or 2, 4.9% Disc. AE	150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf
Dermatitis allergic	2.4% Disc. AE	300 mg 1 times / day multiple, oral Studied dose Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inducer 1087 inhibitor 2252	inhibitor 2438 substrate 1193 inducer 440	inhibitor 2507 substrate 1388	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP3A5 136 CYP2B6 926 CYP2C19 2057 BCRP 910 CYP1A2 2153 CYP2C8 1057 OATP1B3 961 P-gp 1741 OATP1B1 1079 OAT1 725 OAT3 747 OCT2 779	OATP1B3 435 OATP1B1 503 BCRP 697 P-gp 2052 CYP3A5 446 CYP2C19 1119 CYP2E1 729 CYP1A2 1197 CYP2C8 810 CYP2A6 626 OAT1 395 OAT3 391 CYP2B6 776 OCT2 434	CYP3A5 92 CYP2B6 669 CYP2C19 329 CYP2C8 198 CYP1A2 832

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=166 Page: 166.0	no
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=169 Page: 169.0	no
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=169 Page: 169.0	no
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=169 Page: 169.0	no
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=36 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=169 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=188 Page: 36 \| 120 \| 169 \| 188	yes [IC50 0.415 uM]	yes (co-administration study) Comment: Oteseconazole resulted in a clinically significant increase in rosuvastatin exposure (increased AUC and Cmax approximately 94% to 118%) . Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=36 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=169 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=188 Page: 36 \| 120 \| 169 \| 188
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=166 Page: 166.0	yes [IC50 1.4 uM]
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=169 Page: 169.0	yes [IC50 2.57 uM]
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=36 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=169 Page: 36 \| 169	yes [IC50 2.88 uM]	no (co-administration study) Comment: Oteseconazole had no clinically meaningful effect on the PK of digoxin (P-gp substrate). Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=36 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=169 Page: 36 \| 169
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=169 Page: 169.0	yes [IC50 2.97 uM]
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=166 Page: 166.0	yes [IC50 4 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=166 Page: 166.0	yes [IC50 9.4 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=36 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=166 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=185 Page: 36 \| 166 \| 185	yes [IC50 9.6 uM]	no (co-administration study) Comment: No clinically significant inhibition of midazolam metabolism Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=36 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=166 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=185 Page: 36 \| 166 \| 185
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=166 Page: 166.0	yes [IC50 9.7 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=166 Page: 166.0	yes [IC50 >10 uM]
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf3page=166 Page: 166.0	yes
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf3page=166 Page: 166.0	yes
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf3page=166 Page: 166.0	yes
CYP2C8 1117	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf3page=166 Page: 166.0	yes
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf3page=166 Page: 166.0	yes
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf3page=166 Page: 166.0	yes
CYP3A5 201	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=36 Page: 36.0	yes
CYP3A5 201	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf3page=166 Page: 166.0	yes
CYP3A5 201	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=36 Page: 36.0	yes
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=36 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=119 Page: 36 \| 119	yes	unlikely (co-administration study) Comment: Oteseconazole (600mg QD (maintenance dose is 150mg QW) caused weak induction of CYP3A4 based on around 36% decrease in AUC of midazolam Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=36 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=119 Page: 36 \| 119

Drug as victim

Target	Modality	Activity
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=35 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=169 Page: 35 \| 118 \| 169	no
CYP1A2 1197	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=35 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=165 Page: 35 \| 165	no
CYP2A6 626	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=35 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=165 Page: 35 \| 165	no
CYP2B6 776	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=35 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=165 Page: 35 \| 165	no
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=35 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=165 Page: 35 \| 165	no
CYP2C8 810	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=35 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=165 Page: 35 \| 165	no
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=35 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=165 Page: 35 \| 165	no
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=35 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=165 Page: 35 \| 165	no
CYP2E1 729	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=35 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=165 Page: 35 \| 165	no
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=35 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=165 Page: 35 \| 165	no
CYP3A5 446	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=35 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=165 Page: 35 \| 165	no
OAT1 395	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=118 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=169 Page: 118 \| 169	no
OAT3 391	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=118 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=169 Page: 118 \| 169	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=35 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=169 Page: 35 \| 118 \| 169	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=35 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=169 Page: 35 \| 118 \| 169	no
OCT2 434	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=35 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=169 Page: 35 \| 118 \| 169	no
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=35 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=169 Page: 35 \| 118 \| 169	no

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215888Orig1s000IntegratedR.pdf#page=132 Page: 132.0

PubMed

Title	Date	PubMed
Interscience Conference on Antimicrobial Agents and Chemotherapy - 50th Annual Meeting - Research on Promising New Agents: Part 2.	2010 Nov	21046516
The clinical candidate VT-1161 is a highly potent inhibitor of Candida albicans CYP51 but fails to bind the human enzyme.	2014 Dec	25224009
Structural analyses of Candida albicans sterol 14α-demethylase complexed with azole drugs address the molecular basis of azole-mediated inhibition of fungal sterol biosynthesis.	2017 Apr 21	28258218

Patents

Sample Use Guides

In Vivo Use Guide

There are two recommended VIVJOA dosage regimens: a VIVJOAonly regimen and a Fluconazole/VIVJOA regimen. Use one of these two dosage regimens. (2.1) o Administer VIVJOA orally with food. (2.1) • For the VIVJOA-only Dosage Regimen: (2.2) o On Day 1: Administer VIVJOA 600 mg (as a single dose), then o On Day 2: Administer VIVJOA 450 mg (as a single dose), then o Beginning on Day 14: Administer VIVJOA 150 mg once a week (every 7 days) for 11 weeks (Weeks 2 through 12). • For the Fluconazole/VIVJOA Dosage Regimen, prescribe fluconazole and: (2.3) o On Day 1, Day 4, and Day 7: Administer fluconazole 150 mg orally, then o On Days 14 through 20: Administer VIVJOA 150 mg once daily for 7 days, then o Beginning on Day 28: Administer VIVJOA 150 mg once a week (every 7 days) for 11 weeks (Weeks 4 through 14).

Route of Administration: Oral

In Vitro Use Guide

The binding affinity of VT-1161 for Candida albicans CYP51 was high (dissociation constant [Kd], ≤ 39 nM). VT-1161 at concentrations up to 86 μM did not perturb the spectrum of recombinant human CYP51 VT-1161 (MIC = 0.002 μg ml(-1)) had a more pronounced fungal sterol disruption profile (increased levels of methylated sterols and decreased levels of ergosterol) than the known CYP51 inhibitor voriconazole..

Name

Type

Language

OTESECONAZOLE

Official Name

English

oteseconazole [INN]

Preferred Name

English

(R)-2-(2,4-difluorophenyl)-1,1-difluoro-3-(1H-tetrazol-1-yl)-1-(5-(4-(2,2,2-trifluoroethoxy)phenyl)pyridin-2-yl)propan-2-ol

Systematic Name

English

VT-1161

Code

English

OTESECONAZOLE, (+)-

Common Name

English

2-Pyridineethanol, ?-(2,4-difluorophenyl)-?,?-difluoro-?-(1H-tetrazol-1-ylmethyl)-5-[4-(2,2,2-trifluoroethoxy)phenyl]-, (?R)-

Systematic Name

English

(?R)-?-(2,4-Difluorophenyl)-?,?-difluoro-?-(1H-tetrazol-1-ylmethyl)-5-[4-(2,2,2-trifluoroethoxy)phenyl]-2-pyridineethanol

Systematic Name

English

OTESECONAZOLE [USAN]

Common Name

English

Oteseconazole [WHO-DD]

Common Name

English

VIVJOA

Brand Name

English

Code System Code Type Description

USAN

HI-55