VILOXAZINE

Details

Stereochemistry	RACEMIC
Molecular Formula	C13H19NO3
Molecular Weight	237.2949
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCOC1=CC=CC=C1OCC2CNCCO2

InChI

InChIKey=YWPHCCPCQOJSGZ-UHFFFAOYSA-N

InChI=1S/C13H19NO3/c1-2-15-12-5-3-4-6-13(12)17-10-11-9-14-7-8-16-11/h3-6,11,14H,2,7-10H2,1H3

HIDE SMILES / InChI

Molecular Formula	C13H19NO3
Molecular Weight	237.2949
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/211964s003lbl.pdf | https://pubmed.ncbi.nlm.nih.gov/34003459 | https://pubmed.ncbi.nlm.nih.gov/35015448 | https://pubmed.ncbi.nlm.nih.gov/34036533 |

Viloxazine is a selective norepinephrine reuptake inhibitor that has a long history of clinical use in Europe as an antidepressant. An immediate-release formulation was approved for the treatment of depression in the UK in 1974, and was subsequently marketed there and in several European countries for 30 years with no major safety concerns. In April of 2021, the United States Food and Drug Administration (FDA) approved the use of viloxazine (QELBREE), developed by Supernus Pharmaceuticals, for the treatment of attention-deficit/hyperactivity disorder (ADHD) in pediatric and adult patients. Approval was based on positive results from a series of short-term phase III clinical trials in which viloxazine improved the severity of ADHD symptoms in children and adolescents with diagnosed ADHD. Viloxazine is available as extended-release capsules for once-daily oral administration.

CNS Activity

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Sodium-dependent noradrenaline transporter 39 Target ID: P23975 Gene ID: 6530.0 Gene Symbol: SLC6A2 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/27230580	Inhibitor 8504
Sodium-dependent noradrenaline transporter 39 Target ID: P23975 Gene ID: 6530.0 Gene Symbol: SLC6A2 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/27230580	Inhibitor 8504		2300.0 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Attention Deficit Hyperactivity Disorder 2 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/211964s003lbl.pdf	Primary		Approved 8583	QELBREE Approved Use Treatment of Attention Deficit Hyperactivity Disorder in adults and pediatric patients 6 years and older Launch Date 2021

C_max

Value	Dose	Analyte	Population
1.33 μg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=214	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VILOXAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1.66 μg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=215	200 mg 1 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VILOXAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1.34 μg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=216	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VILOXAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
1.21 μg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=216	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VILOXAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
1.22 μg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=216	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VILOXAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
2.83 μg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=222	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	VILOXAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
3.06 μg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=222	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	VILOXAZINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
3.25 μg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=222	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	VILOXAZINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
4.65 μg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=222	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	VILOXAZINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
8 μg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=223	900 mg 1 times / day steady-state, oral dose: 900 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VILOXAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
6.59 μg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=223	900 mg 1 times / day steady-state, oral dose: 900 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VILOXAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
27.3 μg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=214	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VILOXAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
24.7 μg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=215	200 mg 1 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VILOXAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
25.64 μg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=216	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VILOXAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
24.45 μg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=216	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VILOXAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
23.68 μg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=216	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VILOXAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
61.84 μg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=222	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	VILOXAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
67.59 μg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=222	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	VILOXAZINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
80.38 μg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=222	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	VILOXAZINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
117.5 μg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=222	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	VILOXAZINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
134.32 μg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=223	900 mg 1 times / day steady-state, oral dose: 900 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VILOXAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
106.89 μg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=223	900 mg 1 times / day steady-state, oral dose: 900 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VILOXAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
7.02 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=214	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:		VILOXAZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
24.3% OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=140			VILOXAZINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
400 mg 1 times / day steady, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf	unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf	Other AEs: somnolence... Other AEs: somnolence (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf
600 mg 1 times / day steady, oral Highest studied dose Dose: 600 mg, 1 times / day Route: oral Route: steady Dose: 600 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf	unhealthy Health Status: unhealthy Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf	Disc. AE: Somnolence, Fatigue... AEs leading to discontinuation/dose reduction: Somnolence (2%) Fatigue (1%) Tachycardia (1%) Dizziness (1%) Depression (1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf
100 mg 1 times / day steady-state, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: steady-state Dose: 100 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf	unhealthy Health Status: unhealthy Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf	Disc. AE: Fatigue, Tachycardia... AEs leading to discontinuation/dose reduction: Fatigue (1%) Tachycardia (1%) Dizziness (1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf
200 mg 1 times / day steady, oral Studied dose Dose: 200 mg, 1 times / day Route: oral Route: steady Dose: 200 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf	unhealthy Health Status: unhealthy Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf	Disc. AE: Somnolence, Abdominal pain... AEs leading to discontinuation/dose reduction: Somnolence (2 patients) Abdominal pain (1 patient) Fatigue (1 patient) Nausea (2 patients) Tachycardia (1 patient) Decreased appetite (2 patients) Headache (1 patient) Insomnia (1 patient) Irritability (2 patients) Suicidal ideation (serious, 1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf
200 mg 1 times / day steady-state, oral Studied dose Dose: 200 mg, 1 times / day Route: oral Route: steady-state Dose: 200 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf	unhealthy Health Status: unhealthy Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf	Disc. AE: Somnolence, Abdominal pain... AEs leading to discontinuation/dose reduction: Somnolence (1%) Abdominal pain (1%) Anxiety (1%) Diarrhea (1%) Syncope (1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf
400 mg 1 times / day steady, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf	unhealthy Health Status: unhealthy Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf	Disc. AE: Somnolence, Abdominal pain... AEs leading to discontinuation/dose reduction: Somnolence (0.2%) Abdominal pain (1 patient) Nausea (1 patient) Headache (1 patient) Insomnia (1 patient) Dyspepsia (1 patient) Self-harm (1 patient) Vomiting (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf

AEs

Overview

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

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2C8 1057 OAT1 725 OATP1B1 1079 OAT3 747 OATP1B3 961 CYP2B6 926 CYP1A2 2153 MATE2-K 77 OCT2 779 BCRP 910 P-gp 1741 CYP2C19 2057 MATE1 415	OCT 4 OAT 5 OATP1B3 435 BCRP 697 MATE 2 P-gp 2052 UGT1A9 423 CYP2B6 776 UGT2B15 236 UGT1A1 479 OATP1B1 503 UGT1A3 470 CYP1A2 1197 UGT1A6 343 UGT1A4 399 UGT2B7 456	CYP1A2 832 CYP2B6 669 CYP3A4/5 133 CYP1A1 151

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
MATE2-K 77	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144.0	no [IC50 3300 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144 \| 210	no [IC50 >1010 uM]
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144 \| 210	no [IC50 >1010 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144 \| 210	no [IC50 >1010 uM]
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144 \| 212	no [IC50 >150 uM]
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144.0	no [IC50 >150 uM]
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144.0	no [IC50 >150 uM]
CYP3A4/5 357	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144 \| 210	no
MATE1 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144.0	weak [IC50 140 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=41 Page: 41 \| 144 \| 210 \| 217	weak [IC50 141 uM]	yes (co-administration study) Comment: Increased dextromethorphan Cmax by 150.76% and AUCinf by 189.71% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=41 Page: 41 \| 144 \| 210 \| 217
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144 \| 210	weak [IC50 184 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=41 Page: 41 \| 144 \| 210 \| 218	weak [IC50 221 uM]	yes (co-administration study) Comment: Increased midazolam Cmax by 112.81% and AUCinf by 168.91% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=41 Page: 41 \| 144 \| 210 \| 218
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144 \| 212	weak [Inhibition 150 uM]
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144 \| 212	weak [Inhibition 150 uM]
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144 \| 212	weak [Inhibition 150 uM]
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144 \| 212	weak [Inhibition 150 uM]
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=41 Page: 41 \| 144 \| 210 \| 217	yes [IC50 0.269 uM]	yes (co-administration study) Comment: Increased caffeine AUCinf by 583.35% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=41 Page: 41 \| 144 \| 210 \| 217
CYP1A1 272	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144.0	yes
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144 \| 210	yes
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144 \| 210	yes
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=144 Page: 144.0	yes

Drug as victim

Target	Modality	Activity	Metabolite
UGT1A4 399	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=141 Page: 141.0		5-hydroxyviloxazine 2
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=40 Page: 40.0	no
MATE 2	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=40 Page: 40.0	no
OAT 5	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=40 Page: 40.0	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=40 Page: 40 \| 144 \| 211	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=40 Page: 40 \| 144 \| 211	no
OCT 4	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=40 Page: 40.0	no
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=40 Page: 40.0	no
UGT1A1 479	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=141 Page: 141.0	no	5-hydroxyviloxazine 2
UGT1A3 470	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=141 Page: 141.0	no	5-hydroxyviloxazine 2
UGT1A6 343	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=141 Page: 141.0	no	5-hydroxyviloxazine 2
UGT2B7 456	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=141 Page: 141.0	no	5-hydroxyviloxazine 2
CYP1A2 1197	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=141 Page: 141.0	yes
CYP2B6 776	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=141 Page: 141.0	yes
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=40 Page: 40.0	yes
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=141 Page: 141.0	yes
UGT1A9 423	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=141 Page: 141.0	yes	5-hydroxyviloxazine 2
UGT2B15 236	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=141 Page: 141.0	yes	5-hydroxyviloxazine 2

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/211964Orig1s000IntegratedR.pdf#page=138 Page: 138.0

PubMed

Title	Date	PubMed
[Comparative evaluation of the therapeutic efficacy of the antidepressants adepren, linamiphen and emovit].	1986	3716711
[Apropos of atypical melancholia with Sustiva (efavirenz)].	2001 May-Jun	11488260
Stereochemistry and drug efficacy and development: relevance of chirality to antidepressant and antipsychotic drugs.	2002	12553493
Simultaneous determination of viloxazine, venlafaxine, imipramine, desipramine, sertraline, and amoxapine in whole blood: comparison of two extraction/cleanup procedures for capillary gas chromatography with nitrogen-phosphorus detection.	2002 Jul-Aug	12166817
Intravenous antidepressant treatment: focus on citalopram.	2002 Jun	12192466
Tricyclic and related drugs for nocturnal enuresis in children.	2003	12917922
A high-performance liquid chromatography method with photodiode-array UV detection for therapeutic drug monitoring of the nontricyclic antidepressant drugs.	2003 Oct	14508379
Contribution of sleep research to the development of new antidepressants.	2005	16416706
The AGNP-TDM Expert Group Consensus Guidelines: focus on therapeutic monitoring of antidepressants.	2005	16156382
Development of a solid phase extraction for 13 'new' generation antidepressants and their active metabolites for gas chromatographic-mass spectrometric analysis.	2005 Dec 9	16314157
Internet-based search of randomised trials relevant to mental health originating in the Arab world.	2005 Jul 26	16045805
Enhancing central noradrenergic function in depression: is there still a place for a new antidepressant?	2005 Mar	18568121
Gastrointestinal bleeding and massive liver damage in neuroleptic malignant syndrome.	2005 Sep	18360563
[Trazodone for the treatment of behavioral and psychological symptoms of dementia (BPSD) in Alzheimer's disease: a retrospective study focused on the aggression and negativism in caregiving situations].	2006 Jun	16856516
Quantitative determination of forty-eight antidepressants and antipsychotics in human serum by HPLC tandem mass spectrometry: a multi-level, single-sample approach.	2006 Oct 20	16798119
Comparison of electron and chemical ionization modes by validation of a quantitative gas chromatographic-mass spectrometric assay of new generation antidepressants and their active metabolites in plasma.	2007 Dec 28	18022628
Quantification of tricyclic antidepressants and monoamine oxidase inhibitors by high-performance liquid chromatography-tandem mass spectrometry in whole blood.	2007 May	17555643
Antidepressant drugs for narcolepsy.	2008 Jan 23	18254030
Narcolepsy: current treatment options and future approaches.	2008 Jun	18830438
A prognostic system applicable to patients with resectable liver metastasis from colorectal carcinoma staged by positron emission tomography with [18F]fluoro-2-deoxy-D-glucose: role of primary tumor variables.	2008 May	18471711
Adjustment Disorder: epidemiology, diagnosis and treatment.	2009 Jun 26	19558652
Determination of antidepressants in human postmortem blood, brain tissue, and hair using gas chromatography-mass spectrometry.	2009 Nov	18839201
Getting the balance right: Established and emerging therapies for major depressive disorders.	2010 Sep 7	20856599

Patents

Sample Use Guides

In Vivo Use Guide

Treatment of Attention Deficit Hyperactivity Disorder in adults: Recommended starting dosage is 200 mg once daily. May titrate in increments of 200 mg weekly, to maximum recommended dosage of 600 mg once daily.

Route of Administration: Oral

In Vitro Use Guide

Viloxazine exhibits an inhibitory effect on NE uptake, with an inhibitory constant (Ki) of 2300 nM in rat hypothalamic synaptosomes uptake assay.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:35:31 GMT 2025` Edited by `admin` on `Mon Mar 31 18:35:31 GMT 2025`
Record UNII	5I5Y2789ZF
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

VILOXAZINE

Official Name

English

(±)-2-(O-ETHOXYPHENOXYMETHYL)MORPHOLINE

Preferred Name

English

viloxazine [INN]

Common Name

English

Viloxazine [WHO-DD]

Common Name

English

VILOXAZINE [MI]

Common Name

English

MORPHOLINE, 2-((2-ETHOXYPHENOXY)METHYL)-

Systematic Name

English

VILOXAZIN

Common Name

English

VILOXAZINE [VANDF]

Common Name

English

Classification Tree Code System Code

WHO-ATC

N06AX09